2024-03-29T12:12:45Z
https://zenodo.org/oai2d
oai:zenodo.org:3571779
2020-01-20T16:52:53Z
user-darulaceze
Alkoclar Erdal Can
2019-12-12
<p>A Topically Appliable Formulation that consists a Pro-Somathropic Glucopyranoside Derivative that stimulates GH and IGF-1 mRNA Expression Enhancement on application site and an Anti-Inflammatory Hecogenin Derivative with IL-6 and Nf-Kappa B Inhibitory Properties</p>
https://doi.org/10.5281/zenodo.3571779
oai:zenodo.org:3571779
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3571778
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
Wound Healing
A Topical Formulation with Wound Healing Accelerative Properties
info:eu-repo/semantics/patent
oai:zenodo.org:3819155
2020-05-13T08:20:33Z
user-darulaceze
Erdal Can Alkoclar
2020-05-10
<p> </p>
<p><strong>Technical Field</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the anti-viral components for suppressing the DNA gyrase.</p>
<p> </p>
<p> </p>
<p><strong>State of the Art</strong></p>
<p> </p>
<p>DNA gyrase is a bacterial enzyme that plays a role in the DNA replication. DNA gyrase is a type II topoisomerase present in E.coli. There is a group of antimicrobial agents used against bacterial DNA gyrase. These are called “Quinolones” (ciprofloxacin, ofloxacin, novobiocin, fluoroquinolone, etc.).</p>
<p>According to the state of the art, the invention no. WO 2000/024932 with classification “C12Q 1/68” entitled “Methods of identifying and characterizing mutations within bacterial DNA gyrase and FABI” allows for the simultaneous creation and identification, or identification of mutations that confer resistance to antibacterial compounds.</p>
<p>As a result, the presence of the need for a composition for suppressing the DNA gyrase and the inadequacy of the existing solutions have made it necessary to perform an improvement in the relevant art.</p>
<p> </p>
<p> </p>
<p><strong>Object of the Invention</strong></p>
<p> </p>
<p>In order to eliminate the disadvantages of the state of the art, an object of the invention is to enable the suppression of the DNA gyrase.</p>
<p> </p>
<p>Another object of the invention is to enable the suppression of the RNA ligase.</p>
<p> </p>
<p>Another object of the invention is to enable the suppression of the DNA ligase.</p>
<p> </p>
<p>In order to achieve the aforesaid advantages, the invention is a composition for suppressing the DNA gyrase, said composition being obtained by the components selected from the group comprising 2,3,7,10,11,12-tetrachloro-10R-methoxy-2,4-dimethyl-1-oxo-9S,12R-dimethoxy-2H-diindol[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]octadien-4-carboxylic acid methyl ester, 2,3,9,10,11,12-hexahydro-10R-methoxy-3,3-trimethyl-7-oxo-9S,12R-epoxy-4H-tetrafluoro[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]benzodiazokin-8-carboxylic acid phenyl ester that are used individually or in combinations.</p>
<p> </p>
<p>The structural and characteristic features and all the advantages of the invention will become more clearly understood from the detailed description provided below and therefore, the evaluation must be made taking this detailed description into consideration.</p>
<p> </p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p> </p>
<p>The invention is a composition comprising the anti-viral components for suppressing the DNA gyrase. The composition according to the invention enables the suppression of DNA gyrase, the suppression of RNA ligase and the suppression of DNA ligase.</p>
<p> </p>
<p>The composition according to the invention contains 2,3,7,10,11,12-tetrachloro-10R-methoxy-2,4-dimethyl-1-oxo-9S,12R-dimethoxy-2H-diindol[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]octadien-4-carboxylic acid methyl ester, 2,3,9,10,11,12-hexahydro-10R-methoxy-3,3-trimethyl-7-oxo-9S,12R-epoxy-4H-tetrafluoro[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]benzodiazokin-8-carboxylic acid phenyl ester.</p>
<p> </p>
<p>Said composition is obtained by a mixture of the aforesaid components according to the following ratios by weight:</p>
<p>1-99% 2,3,7,10,11,12-tetrachloro-10R-methoxy-2,4-dimethyl-1-oxo-9S,12R-dimethoxy-2H-diindol[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]octadien-4-carboxylic acid methyl ester,</p>
<p>99-1% 2,3,9,10,11,12-hexahydro-10R-methoxy-3,3-trimethyl-7-oxo-9S,12R-epoxy-4H-tetrafluoro[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]benzodiazokin-8-carboxylic acid phenyl ester. </p>
<p> </p>
<p>The composition is obtained from the aforesaid components selected from the aforesaid group and used according to the mentioned weight ratio ranges individually or in combinations.</p>
<p> </p>
<p>Said invention also encompasses the use of said composition for suppressing the DNA gyrase and the manufacture thereof for this purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A composition for suppressing the DNA gyrase, said composition being obtained by the components selected from the group comprising 2,3,7,10,11,12-tetrachloro-10R-methoxy-2,4-dimethyl-1-oxo-9S,12R-dimethoxy-2H-diindol[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]octadien-4-carboxylic acid methyl ester, 2,3,9,10,11,12-hexahydro-10R-methoxy-3,3-trimethyl-7-oxo-9S,12R-epoxy-4H-tetrafluoro[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]benzodiazokin-8-carboxylic acid phenyl ester that are used individually or in combinations.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 1-99% by weight 2,3,7,10,11,12-tetrachloro-10R-methoxy-2,4-dimethyl-1-oxo-9S,12R-dimethoxy-2H-diindol[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]octadien-4-carboxylic acid methyl ester.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 99-1% by weight 2,3,9,10,11,12-hexahydro-10R-methoxy-3,3-trimethyl-7-oxo-9S,12R-epoxy-4H-tetrafluoro[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]benzodiazokin-8-carboxylic acid phenyl ester.</li>
</ol>
<p> </p>
<ol>
<li>Use of the components according to Claims 1 to 3 obtained individually or in combinations selected from the group consisting of 2,3,7,10,11,12-tetrachloro-10R-methoxy-2,4-dimethyl-1-oxo-9S,12R-dimethoxy-2H-diindol[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]octadien-4-carboxylic acid methyl ester, 2,3,9,10,11,12-hexahydro-10R-methoxy-3,3-trimethyl-7-oxo-9S,12R-epoxy-4H-tetrafluoro[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]benzodiazokin-8-carboxylic acid phenyl ester for the manufacture of a composition for suppressing the DNA gyrase. </li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>ABSTRACT</strong></p>
<p> </p>
<p><strong>A COMPOSITION COMPRISING THE ANTI-VIRAL COMPONENTS FOR SUPPRESSING DNA GYRASE</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the anti-viral components for suppressing the DNA gyrase.</p>
https://doi.org/10.5281/zenodo.3819155
oai:zenodo.org:3819155
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3819154
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
Viral DNA Gyrase Antiviral
A COMPOSITION COMPRISING THE ANTI-VIRAL COMPONENTS FOR SUPPRESSING DNA GYRASE
info:eu-repo/semantics/patent
oai:zenodo.org:3818417
2020-05-13T20:20:35Z
user-darulaceze
Erdal Can Alkoclar
2020-05-09
<p> </p>
<p><strong>Field of Invention</strong></p>
<p> </p>
<p>The present invention herewith is related to a formulation developed for treatment of hypo-adrenalism.</p>
<p> </p>
<p><strong>Background of the Related Technology</strong></p>
<p>At present it is known that in mammalians the adrenal glands (also known as suprarenal glands) are endocrine glands that have a shape resembling a triangle. These glands take their name from their location, since anatomically they are just on top of the kidneys. These glands consist of two layers, called cortex (outer layer) and medulla (middle layer). Their basic function is, when under physiological stress, to secrete corticosteroids (from cortex) and to secrete cathecholamine (from medulla) into the blood stream.</p>
<p>Again, at present it is known that most of the irregularities related to the cortex layer of the adrenal glands is a result of synthesis of hormones at a certain layer, in a quantity higher or lower than the normally required levels (cortisol, aldosterone or sexual hormones). Having a certain hormone produced and secreted, at a level below or above the normal concentration, results in certain symptoms in a person and this also leads to variations in the concentration of the related hormone in the blood stream and urine. On the other hand, having a high or low level of a certain hormone, would have an impact on feedback mechanism of that hormone and certain analyses can be conducted solely based on this fact.</p>
<p>Based on the state of art technology in medicine, a total of 30 mg hydrocortisone is administrated per day in 2-3 doses, as a maintenance treatment. Two thirds of the required dose is given early in the morning and one third in the afternoon around 16:00 hr. By this method the circadian rhythm is mimicked. Administrating at a later hour can lead to certain side effects like sleep disorders. In primary adrenaline insufficiency treatment, mineralo-corticoid replacement treatment is required. Treatment is started with 0.1 mg/day dose of fludrocortisone (Florinef or Astonin) and the dose may be increased if needed. In certain studies, it is argued that, in women with primary adrenaline insufficiency, a treatment of 50 mg DHEA per day would regulate the life quality and mood of the women.</p>
<p>In state of art technology, invention no " EP2205562B1" , with title "1.1.1-trifluoro-2-hydroxy-3-phenylpropane Derivatives" and under classification number "C07D 213/30" discloses new 1,1,1 -trifluoro-2-hydroxy-3-phenylpropane or 1,1,1 -trifluoro-2-hydroxy-4-phenyl butane derivatives, manufacturing such agents as well as pharmaceutical compositions of these and using these as drugs. The active compounds that are in compliance with the invention act as glucocorticoid receptor modulators and preferably as antagonists and are useful in treatment of diabetes as well as other disorders like dyslipidemia, obesity, high blood pressure, cardio-vascular diseases, adrenalin imbalance or depression.</p>
<p>In state of art technology, invention no "WO 1999/045779" , with title " New Eprosartan Compositions" and under classification number " A01N 43/50" discloses a new composition containing eprosartan in particular form, or its salt, solvate or hydrate, as well as the method for manufacturing this composition. It also discloses the methods of using the composition in preventing new Angiotensin II receptors and in treatment of high blood pressure, congestive heart failure and kidney failure.</p>
<p>Again invention no " EP1274411B1" , with title "Using Phenylethylamines as Pro-drugs of Cathecholamines and Their Condensed Ring variants and Their Use” discloses compounds with general formula (I) and their salts containing pharmaceutically accepted acids or bases. It also discloses methods for manufacturing pharmaceutic compositions intended for treatment of Parkinson’s Disease, psychosis, Huntington’s Disease, impotency, renal failure, heart failure or high blood pressure, such pharmaceutical compositions intended for treatment of Parkinson’s Disease and Schizophrenia as well as methods related to such intensions.</p>
<p>Again invention no " EP1487424B1" , with title "4-(4-methylpiperazin-1-ylmethyl)-N-(4-methyl-3(4-piridin-3-yl)pirimidin-2-yl-amino)phenyl)-benzamid for Treatment of ANG II Induced Diseases” and under classification number "A61K 31/00" discloses methods for using a PDGF receptor tyrosine kinase inhibitor or a pharmaceutically appropriate salt of this for production of a drug for treatment of a disease induced by ANG II and its characteristic is to have it selected for the referred diseases induced by angiotensin II which includes; congestive heart failure, heart failure, cardiac hyperthrophy, cardiac remodeling after myocardial infarction, dilate or hyperthrophic cardiomyopathy related pulmonary congestion and cardiac fibrosis, prevention of stroke related to congestive heart failure, left and right ventricular hyperthrophy, hyperthrophic medial thickening of the arteries and/or large blood vessels, mesenteric vascular hypertrophy, renal hyperfiltration after portal renal ablation, proteinuria in chronic renal disease, renal arteriopathy as a result of high blood pressure, nephrosclerosis or hypertensive nephrosclerosis, mesangial hyperthrophy, endothelial dysfunctions exhibiting pro-inflammatory or pro-oxidant conditions.</p>
<p>To conclude it has become inevitable to proceed with a development in the area of the related technology, considering the inadequacy of the existing solutions and the need for a formulation intended for treatment of hypo-adrenalism</p>
<p> </p>
<p><strong>Objective of the Invention</strong></p>
<p> </p>
<p>To overcome the disadvantages experienced in state of art technology;</p>
<ul>
<li>One objective of the present invention is to enhance ACTH production;</li>
<li>One other objective of the invention is to enhance CRH production;</li>
<li>One other objective of the invention is to increase density and number of glucocorticosteroids;</li>
<li>One other objective of the invention is to have the zona fasciculate cells to preserve their cell wall permeability.</li>
</ul>
<p> </p>
<p>The present invention which is aimed to achieve the above-mentioned advantages, is intended for treatment of hypo-adrenalism and is a formulation that is obtained by combination of the compositions selected in a single form or in combinations from a group containing; (3β,25R)-dispirost-5-ene-3-triol, 3,7-bis(2-hydroxymethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one, 3,5-bis(2-dimethoxyethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one.</p>
<p> </p>
<p>Structural and characteristic properties as well as all the advantages of the invention presented herewith will be clearly understood with the detailed description provided below and thus the evaluation regarding the present invention should be based on the detailed description presented herewith..</p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p> </p>
<p>The present invention is related to a formulation developed for treatment of hypo-adrenalism. Referred formulation enhances ACTH production, enhances CRH production, increases density and number of glucocorticosteroids, helps the zona fasciculate cells to preserve their cell wall permeability.</p>
<p> </p>
<p>The formulation of the invention presented herewith contains; (3β,25R)-dispirost-5-ene-3-triol, 3,7-bis(2-hydroxymethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one, 3,5-bis(2-dimethoxyethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one . </p>
<p> </p>
<p>The referred formulation is formed by mixing the above-mentioned components at below percentages by weight;</p>
<ul>
<li>26-44% of (3β,25R)-dispirost-5-ene-3-triol, </li>
<li>54-28% of 3,7-bis(2-hydroxymethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one, </li>
<li>20-28% of 3,5-bis(2-dimethoxyethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one.</li>
</ul>
<p> </p>
<p>Components given above are obtained by combining the components from the above-mentioned group at the given range of weight ratios in a single form or in combinations thereof.</p>
<p> </p>
<p>The present invention at the same time is related to using the above-referred formulation for treatment of hypo-adrenalism and manufacturing it for such purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A formulation intended for treatment of hypo-adrenalism, which consists of combining the components selected from the group; (3β,25R)-dispirost-5-ene-3-triol, 3,7-bis(2-hydroxymethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzo pyrane-4-one, 3,5-bis(2-dimethoxyethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one in a single form or in combinations thereof.</li>
</ol>
<p> </p>
<ol>
<li>The formulation of Claim 1 which is characterized by containing 26-44% of (3β,25R)-dispirost-5-ene-3-triol by weight.</li>
</ol>
<p> </p>
<ol>
<li>The formulation of Claim 1 which is characterized by containing 54-28% of 3,7-bis(2-hydroxymethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one by weight.</li>
</ol>
<p> </p>
<ol>
<li>The formulation of Claim 1 which is characterized by containing 20-28% of 3,5-bis(2-dimethoxyethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one by weight.</li>
</ol>
<p> </p>
<ol>
<li>Using the compositions obtained by selecting singly or in combination of components from the group of; (3β,25R)-dispirost-5-ene-3-triol, 3,7-bis(2-hydroxymethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one, 3,5-bis(2-dimethoxyethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one from any one as given in Claims 2-4 in manufacturing the formulation intended for treatment of hypo-adrenalism. </li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>SUMMARY</strong></p>
<p> </p>
<p><strong>FORMULATION INTENDED FOR TREATMENT OF HYPO-ADRENALISM</strong></p>
<p> </p>
<p> </p>
<p>The present invention is related to a formulation developed for treatment of hypo-adrenalism. Referred formulation enhances ACTH production, enhances CRH production, increases density and number of glucocorticosteroids, helps the zona fasciculate cells to preserve their cell wall permeability.</p>
https://doi.org/10.5281/zenodo.3818417
oai:zenodo.org:3818417
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3818416
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
CRH ACTH Zona Fasciculata
FORMULATION INTENDED FOR TREATMENT OF HYPO-ADRENALISM
info:eu-repo/semantics/patent
oai:zenodo.org:3819177
2020-05-13T20:20:35Z
user-darulaceze
Erdal Can Alkoclar
2020-05-10
<p> </p>
<p><strong>A COMPOSITION COMPRISING ANTI-CARCINOGENIC SİMPLORASEMOSİDE DERIVATIVES THAT EXHIBIT THE CHARACTERISTIC OF SUPPRESSING PHOSPHATIDYL 3-KINASE EXPRESSION</strong></p>
<p> </p>
<p><strong>Technical Field</strong></p>
<p>The invention relates to a composition comprising anti-carcinogenic symploracemoside derivatives formed for suppressing the expression of phosphatidyl 3-kinase.</p>
<p> </p>
<p> </p>
<p><strong>State of the Art</strong></p>
<p>In chemistry and biochemistry, kinase is a type of enzyme that transfers, by way of phosphorylation, the phosphate groups from the donor molecules with high energy, such as ATP, to the specific substrates. Kinases are a part of a larger family called the phosphotransferases. Tyrosine kinase is an enzyme that belongs to the family of protein kinases enabling the protein phosphorylation. Since the type of amino acid that undergoes phosphorylation is tyrosine, this enzyme was given the name tyrosine kinase.</p>
<p>Tyrosine kinase may transfer phosphate groups from ATP to the tyrosine residues in the proteins. By means of the tyrosine kinase activity, autophosphorylation of the tyrosine residues present in the beta sub unit takes place. This is the first step of the insulin receptor activation. The activation of insulin receptor causes the phosphorylation in the serine-threonine group of a series of proteins that are associated with the receptor and are called the insulin receptor substrate (IRS), which in turn activates the signal pathways that determine the effect to be exhibited by insulin. There are two main pathways, namely the phosphatidylinositol 3 kinase (PI 3 kinase) pathway and mitogen-activated protein kinase (MAPK) pathway. PI 3 kinase pathway is responsible for the cascade system related to the cellular ingestion of the glucose, while MAPK pathway is responsible for the expression of the genes associated with the protein synthesis.</p>
<p>The IRS proteins activated in the pathway responsible for the transport of glucose contact PI 3 kinase, which is an intracellular enzyme, to enable activation. The activated PI3 kinase phosphorylates the phosphatidylinositol (PI) substrates, thereby enabling the formation of PIP, PIP2 and PIP3. These molecules bind to the phosphatidylinositol-dependent kinase (PDK1) enzyme to activate said enzyme where PDK1 enables the phosphorylation of AKT, which is also known as protein kinase B. The activated AKT enables the translocation of the glucose transporter protein called GLUT-4 that is present in cytosol towards the plasma membrane. In this way, GLUT-4, which translocates to the plasma membrane, allows for the influx of the glucose to the cell.</p>
<p>According to the state of the art, the invention no. EP1689391B1 with classification "A61K 31/427" entitled "5-phenyl-4-methyl-thiazol-2-yl-amine derivatives as inhibitors of phosphatidylinositol 3 kinase enzymes (pi3) for the treatment of inflammatory airway diseases" relates to the organic compounds characterized by being 1-[2-(2-ethyl-2H-tetrazol-5-yl)-ethyl]-3-[5-(3-fluoro-4-methanesulfonyl-phenyl)-4-methyl-thiazole-2-yl]-urea in free or salt form, their preparation and their use as pharmaceuticals.</p>
<p>Further, the invention no. EP1622897B1 entitled "Inhibitors of phosphatidylinositol 3-kinase" relates to organic compounds comprising phosphatidylinositol 3-kinase inhibitors, their preparation and their use as pharmaceuticals especially in the treatment of the respiratory tract diseases.</p>
<p>Further, the invention no. EP2261223B1 entitled "Pyrimidine derivatives used as pi-3 kinase inhibitors" relates to new phosphatidylinositol (PI) 3-kinase inhibitor compounds and their pharmaceutically acceptable salts alone or in combination with at least one additional therapeutic agent, and compositions thereof with a pharmaceutically acceptable carrier, and uses thereof in the prophylaxis or treatment of a number of diseases, in particular, those characterized by the abnormal activity of growth factors, receptor tyrosine kinases, protein serine/threonine kinases, G protein coupled receptors and phospholipid kinases and phosphatases.</p>
<p>As a result, the presence of the need for a composition for suppressing the expression of phosphatidyl 3-kinase and the inadequacy of the existing solutions have made it necessary to perform an improvement in the relevant art.</p>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>Object of the Invention</strong></p>
<p>In order to eliminate the disadvantages of the state of the art, an object of the invention is to suppress phosphatidyl 3-kinase.</p>
<p>Another object of the invention is to suppress DNA ligase.</p>
<p>Another object of the invention is to suppress helicase.</p>
<p>In order to achieve the aforesaid advantages, the invention is a composition for suppressing the expression of phosphatidyl 3-kinase, said composition being obtained by the components selected from the group comprising 5-fluoro-3-phenyl-2-[(1S)-1-(9H-purine-6-aminophenyl)propyl]-4(3H)-symploracemoside, 4-fluoro-2-diphenyl-2-[(1S)-1-(9H-purine-6-aminophenyl)propionyl]-2(4H)-symploracemoside that are used individually or in combinations.</p>
<p> </p>
<p>The structural and characteristic features and all the advantages of the invention will become more clearly understood from the detailed description provided below and therefore, the evaluation must be made taking this detailed description into consideration.</p>
<p> </p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p>The invention is a composition comprising anti-carcinogenic symploracemoside derivatives formed for suppressing the expression of phosphatidyl 3-kinase. The composition according to the invention enables the suppression of phosphatidyl 3-kinase, the suppression of DNA ligase and the suppression of helicase.</p>
<p> </p>
<p>The composition according to the invention contains 5-fluoro-3-phenyl-2-[(1S)-1-(9H-purine-6-aminophenyl)propyl]-4(3H)-symploracemoside, 4-fluoro-2-diphenyl-2-[(1S)-1-(9H-purine-6-aminophenyl)propionyl]-2(4H)-symploracemoside.</p>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p>Said composition is obtained by a mixture of the aforesaid components according to the following ratios by weight:</p>
<p>1-99% 5-fluoro-3-phenyl-2-[(1S)-1-(9H-purine-6-aminophenyl)propyl]-4(3H)-symploracemoside,</p>
<p>99-1% 4-fluoro-2-diphenyl-2-[(1S)-1-(9H-purine-6-aminophenyl)propionyl]-2(4H)-symploracemoside. </p>
<p> </p>
<p>The composition is obtained from the aforesaid components selected from the aforesaid group and used according to the mentioned weight ratio ranges individually or in combinations.</p>
<p> </p>
<p>Said invention also encompasses the use of said composition for suppressing the expression of phosphatidyl 3-kinase and the manufacture thereof for this purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A composition for suppressing the expression of phosphatidyl 3-kinase, said composition being obtained by the components selected from the group comprising 5-fluoro-3-phenyl-2-[(1S)-1-(9H-purine-6-aminophenyl)propyl]-4(3H)-symploracemoside, 4-fluoro-2-diphenyl-2-[(1S)-1-(9H-purine-6-aminophenyl)propionyl]-2(4H)-symploracemoside that are used individually or in combinations.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 1-99% by weight 5-fluoro-3-phenyl-2-[(1S)-1-(9H-purine-6-aminophenyl)propyl]-4(3H)-symploracemoside.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 99-1% by weight 4-fluoro-2-diphenyl-2-[(1S)-1-(9H-purine-6-aminophenyl)propionyl]-2(4H)-symploracemoside.</li>
</ol>
<p> </p>
<ol>
<li>Use of the components according to Claims 1 to 3 obtained individually or in combinations selected from the group consisting of 5-fluoro-3-phenyl-2-[(1S)-1-(9H-purine-6-aminophenyl)propyl]-4(3H)-symploracemoside, 4-fluoro-2-diphenyl-2-[(1S)-1-(9H-purine-6-aminophenyl)propionyl]-2(4H)-symploracemoside for the manufacture of a composition for suppressing the expression of phosphatidyl 3-kinase.</li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>ABSTRACT</strong></p>
<p> </p>
<p><strong>A COMPOSITION COMPRISING ANTI-CARCINOGENIC SİMPLORASEMOSİDE DERIVATIVES THAT EXHIBIT THE CHARACTERISTIC OF SUPPRESSING PHOSPHATIDYL 3-KINASE EXPRESSION</strong></p>
<p> </p>
<p>The invention relates to a composition comprising anti-carcinogenic symploracemoside derivatives formed for suppressing the expression of phosphatidyl 3-kinase.</p>
<p> </p>
https://doi.org/10.5281/zenodo.3819177
oai:zenodo.org:3819177
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3819176
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
Phosphadityl 3-Kinase Cancer
A COMPOSITION COMPRISING ANTI-CARCINOGENIC SİMPLORASEMOSİDE DERIVATIVES THAT EXHIBIT THE CHARACTERISTIC OF SUPPRESSING PHOSPHATIDYL 3-KINASE EXPRESSION
info:eu-repo/semantics/patent
oai:zenodo.org:3819171
2020-05-13T20:20:34Z
user-darulaceze
Erdal Can Alkoclar
2020-05-10
<p> </p>
<p><strong>A COMPOSITION COMPRISING COMPONENTS THAT EXHIBIT ANTI-CARCINOGENIC ACTION FORMED FOR SUPPRESSING H3K27 METHYLTRANSFERASE</strong></p>
<p> </p>
<p><strong>Technical Field</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the components that exhibit anti-carcinogenic action formed for suppressing H3K27 methyltransferase. </p>
<p> </p>
<p> </p>
<p><strong>State of the Art</strong></p>
<p> </p>
<p>Histone methyltransferases (HMT) are the enzymes that add to the lysine or arginine amino acids in the structure of the histone proteins the methyl group they obtain from the cofactor S-adenosyl methionine. This process referred to as the histone methylation is an epigenetic modification. The amino acid, to which between 1-3 methyl groups may be added, is named along with the prefix of methyl-, dimethyl- or trimethyl- according to the number of methyl groups it carries; e.g. dimethyl lysine. Also, catechol-O-methyltransferase (COMT; <a href="http://www.expasy.org/cgi-bin/nicezyme.pl?2.1.1.6%7CEC">2.1.1.6</a>) is an enzyme that plays a role in the metabolism of catecholamines. Dopamine, adrenaline, noradrenaline may be given as the examples of catecholamines. Catechol-O-methyltransferase takes part in the inactivation of the neurotransmitters. COMT is an intracellular enzyme available in the postsynaptic neurons.</p>
<p>The COMT enzyme is encoded in the human by a gene localized in 22q11.2 <a href="http://tr.wikipedia.org/wiki/Katekol-O-metiltransferaz#cite_note-1">[1]</a>. The functional polymorphism in the COMT gene causes the alteration of the activity of the COMT enzyme. COMT gene polymorphism is known to be effective in the pathogenesis of diseases such schizophrenia, bipolar disorder, obsessive compulsive disorder, migraine, and aggressive and antisocial behaviors.</p>
<p>It is a substance that prevents the development of cancer or inhibits the tumor growth. According to the state of the art, the invention no. EP2307002B1 with classification "A61K 31/245" entitled "Combinations of sapacitabine or cndac with dna methyltransferase inhibitors such as decitabine and procaine” relates to a pharmaceutical combination suitable for the treatment of cancer and other proliferative disorders.</p>
<p>As a result, the presence of the need for a composition for suppressing H3K27 methyltransferase and the inadequacy of the existing solutions have made it necessary to perform an improvement in the relevant art.</p>
<p> </p>
<p> </p>
<p><strong>Object of the Invention</strong></p>
<p> </p>
<p>In order to eliminate the disadvantages of the state of the art, an object of the invention is to enable the suppression of histone H3 lysine 27 methyltransferase.</p>
<p>Another object of the invention is to enable an increase in p21 expression.</p>
<p>Another object of the invention is to enable an increase in p27 expression.</p>
<p>In order to achieve the aforesaid advantages, the invention is a composition for suppressing H3K27 methyltransferase, said composition being obtained by the components selected from the group comprising N-[(2,2-dihydro-6-trimethyl-7-oxo-4-propionyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(2-phenylethyl)-1-laroyl]-3-1H-ramnosyl-4-carboxamide, N-[(1,2-dihydro-4-dimethyl-2-oxo-4-cafeoyl-3-coumaroyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-propionyl]-3-1H-fluoro-4-carboxamide that are used individually or in combinations.</p>
<p> </p>
<p>The structural and characteristic features and all the advantages of the invention will become more clearly understood from the detailed description provided below and therefore, the evaluation must be made taking this detailed description into consideration.</p>
<p> </p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p> </p>
<p>The invention is a composition comprising the components that exhibit anti-carcinogenic action formed for suppressing H3K27 methyltransferase. The composition according to the invention enables the suppression of histone H3 lysine 27 methyltransferase, an increase in p21 expression and an increase in p27 expression.</p>
<p> </p>
<p>The composition according to the invention contains N-[(2,2-dihydro-6-trimethyl-7-oxo-4-propionyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(2-phenylethyl)-1-laroyl]-3-1H-ramnosyl-4-carboxamide, N-[(1,2-dihydro-4-dimethyl-2-oxo-4-cafeoyl-3-coumaroyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-propionyl]-3-1H-fluoro-4-carboxamide. </p>
<p> </p>
<p>Said composition is obtained by a mixture of the aforesaid components according to the following ratios by weight:</p>
<p>1-99% N-[(2,2-dihydro-6-trimethyl-7-oxo-4-propionyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(2-phenylethyl)-1-laroyl]-3-1H-ramnosyl-4-carboxamide,</p>
<p>99-1% N-[(1,2-dihydro-4-dimethyl-2-oxo-4-cafeoyl-3-coumaroyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-propionyl]-3-1H-fluoro-4-carboxamide. </p>
<p> </p>
<p>The composition is obtained from the aforesaid components that exhibit anti-carcinogenic action selected from the aforesaid group and used according to the mentioned weight ratio ranges individually or in combinations.</p>
<p> </p>
<p>Said invention also encompasses the use of said composition for suppressing H3K27 methyltransferase and the manufacture thereof for this purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A composition for suppressing H3K27 methyltransferase, said composition being obtained by the components that exhibit anti-carcinogenic action selected from the group comprising N-[(2,2-dihydro-6-trimethyl-7-oxo-4-propionyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(2-phenylethyl)-1-laroyl]-3-1H-ramnosyl-4-carboxamide, N-[(1,2-dihydro-4-dimethyl-2-oxo-4-cafeoyl-3-coumaroyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-propionyl]-3-1H-fluoro-4-carboxamide that are used individually or in combinations.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 1-99% by weight N-[(2,2-dihydro-6-trimethyl-7-oxo-4-propionyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(2-phenylethyl)-1-laroyl]-3-1H-ramnosyl-4-carboxamide.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 99-1% by weight N-[(1,2-dihydro-4-dimethyl-2-oxo-4-cafeoyl-3-coumaroyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-propionyl]-3-1H-fluoro-4-carboxamide.</li>
</ol>
<p> </p>
<ol>
<li>Use of the components exhibiting anti-carcinogenic action according to Claims 1 to 3 obtained individually or in combinations selected from the group consisting of N-[(2,2-dihydro-6-trimethyl-7-oxo-4-propionyl-3-pyridinyl)methyl]-1-(1-methylethyl)-6-[6-[4-(2-phenylethyl)-1-laroyl]-3-1H-ramnosyl-4-carboxamide, N-[(1,2-dihydro-4-dimethyl-2-oxo-4-cafeoyl-3-coumaroyl)methyl]-1-(1-methylethyl)-6-[6-[4-(1-methylethyl)-1-propionyl]-3-1H-fluoro-4-carboxamide for the manufacture of a composition for suppressing H3K27 methyltransferase. </li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>ABSTRACT</strong></p>
<p> </p>
<p><strong>A COMPOSITION COMPRISING COMPONENTS THAT EXHIBIT ANTI-CARCINOGENIC ACTION FORMED FOR SUPPRESSING H3K27 METHYLTRANSFERASE</strong></p>
<p> </p>
<p>The invention relates to a composition formed for suppressing H3K27 methyltransferase.</p>
https://doi.org/10.5281/zenodo.3819171
oai:zenodo.org:3819171
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3819170
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
H3K27 Methyltransferase Cancer
A COMPOSITION COMPRISING COMPONENTS THAT EXHIBIT ANTI-CARCINOGENIC ACTION FORMED FOR SUPPRESSING H3K27 METHYLTRANSFERASE
info:eu-repo/semantics/patent
oai:zenodo.org:3571785
2020-01-20T15:11:28Z
user-darulaceze
Alkoclar Erdal Can
2019-12-12
<p>A Myotrophic Formulation that consists a cAMP and AMPK stimulative Flavonol Glycoside , a Myotrophic Pentaone Analouge and a Phyoandrogenic Coumarin that exerts Pro-Gonadotrophic and SARM like effects for the Treatment of Mucle Loss caused by Prolonged Paralytic and Comatose State</p>
https://doi.org/10.5281/zenodo.3571785
oai:zenodo.org:3571785
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3571784
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
Myotrophic Myostatin GDF-8
A Myotrophic Formulation with IGF-1 mRNA Expression Enhancing and GDF-8 Suppressive Features
info:eu-repo/semantics/patent
oai:zenodo.org:3818452
2020-05-13T08:20:33Z
user-darulaceze
Erdal Can Alkoclar
2020-05-09
<p> </p>
<p><strong>Field of Invention</strong></p>
<p> </p>
<p>The present invention herewith discloses a formulation developed to display anti-mitotic effect by suppressing cdk-1 cdk-2 and cycline b1 expression.</p>
<p> </p>
<p><strong>Background of the Related Technology</strong></p>
<p> </p>
<p>At present it is known that an anti-mitotic agent is a medicament that can stop cell reproduction. It block mitosis at its various phases and therefore prevents cell division (reproduction). Some, on one hand, combine with certain protein compounds by acting as alkyl and change the structure of deoxyribonucleic acid (DNA) and some on the other hand act as anti-metabolites. Anti-mitotics that have an antibiotic structure are derived from Streptomyces cultures; those of plant origin from vinca alkaloids. Some have hormone structure, and certain ones are enzymes derived from bacteria. A majority of anti-mitotic drugs are used in cancer treatment.</p>
<p>In state of art technology, invention no "EP2229943B1 ", with title " Compounds for use in the treatment of peripheral neuropathy” and under classification number "A61K 31/357” discloses a benzodioxo compound of Formula (I) or a pharmaceutically acceptable salt of the compound thereof. The referred invention is related to a pharmaceutical composition which consists of at least the compound with formula (I) as described in any one of the Claims 1 to 3, as an active agent or a pharmaceutically acceptable salt of the compound thereof and at least one additional compound and/or at least one additional cytostatic or anti-mitotic compound and/or preferably a pharmaceutically acceptable carrier. The referred invention also is related to a composition consisting of a compound with formula (I) and at least one additional compound and/or at least a cytostatic or anti-mitotic compound used in prevention or treatment of peripheral neuropathies, suitable to be used simultaneously or separately.</p>
<p> </p>
<p>Again invention no "PCT/EP00/03394", with title " Pyrazolobenzodiazepines as CDK2 inhibitors “and under classification number "C07D 243/22 “discloses novel pyrazolobenzodiazepines having formula (I) and the pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined herein, inhibit cycline-dependent kinases (CDKs), in particular CDK2, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular breast, colon, lung and prostate tumors.</p>
<p>Again invention no "EP1366038B1", with title " CDK-1 inhibitor oxindoles and the application thereof in therapeutics” and under classification number "C07D 401/14” discloses a compound having formula (I): wherein R5 is selected from groups of 3-pyridinyl, 5-pyrimidinyl, C1-C4 -CONH-alkyl, C1-C4 -NHCO-alkyl, halogen, -CO<sub>2</sub>R, and R can be C1-C4 alkyl or hydrogen, -SO<sub>2</sub>NH<sub>2</sub>, -NO<sub>2</sub>, -CF<sub>3</sub>. Ar is selected from groups of 5-imidazolyl, 2-pyrrolyl, optionally substituted by a C1-C4 alkyl radical, 2-furyl, or 2-thiazolyl, in form E, Z or a mixture of the two isomeric forms. The referred invention can be used as a medicament for blocking proliferative cell division during the cycle and for inducing cell apoptosis for the treatment of primary and secondary cancerous tumors.</p>
<p>Again invention no "EP1680418B1", with title "Pyridazinone derivatives as CDK2-inhibitors” and under classification number "C07D 417/06” discloses novel N-Piperidinylmethyl benzamide derivatives (I). – Acid added N-Piperidinylmethyl benzamide derivatives of formula (I) as well as their hydrates and solvates are novel products. Here - R1 is H, 1-7C alkyl (optionally fluorinated), 3-7C cycloalkyl, (3-7C)cycloalkyl(1-3C)alkyl, phenyl(1-3C)alkyl (optionally one or two substituted with Ome), 2-4C alkenyl or 2-4C alkynyl; - R2 is pyridyl, furyl, tiyenil, thiazolyl or oxazolyl, all are optionally substituted with halo, CF<sub>3</sub>, 1-6C alkyl and 1-6C alkoxy; - R3 is H, halo, CF3, 1-6C alkyl, 3-7C cycloalkyl, 1-6C alkoxy, phenyl, CN, acetyl, benzoyl, 1-6C alkylthio, 1-6C alkylsulfonyl, COOH, 1-6C alkoxycarbonyl, NR4R5, S02NR4R5 or CONR4R5; -R4, R5 are H, 1-6C alkyl or 3-7C cycloalkyl, or NR4R5 pyrrolydino, piperidino or morpholino. Activity- neurotropic; neuroleptic; tranquilizer; antidepressant; anti-alcoholic; anti-migraine; relaxant; analgesic; anti-Parkinson; anti-convulsant; neuro-protector. – mechanism of action – glycine carrier inhibitor. – regarding the most active compound, glycine retention by sk-n-mc cells which are natural human g1yt1 glycine carrier expression. IC50 values are 0.001-1 micro m. </p>
<p> </p>
<p>To conclude it has become inevitable to proceed with a development in the area of the related technology, considering the inadequacy of the existing solutions and the need for a formulation intended to display anti-mitotic effect by suppressing CDK-1 CDK-2 and cycline B1 expression.</p>
<p> </p>
<p><strong>Objective of the Invention</strong></p>
<p> </p>
<p>To overcome the disadvantages experienced in state of art technology;</p>
<ul>
<li>One objective of the invention is to suppress cycline E expression.</li>
<li>One other objective of the invention is to suppress cdk-1 and cdk-2 expression.</li>
<li>One other objective of the invention is to suppress cycline b1 expression.</li>
<li>One other objective of the invention is to, increase bax expression.</li>
</ul>
<p> </p>
<p>The present invention which is aimed to achieve the above-mentioned advantages, is related to a formulation intended to display anti-mitotic effect by suppressing CDK-1 CDK-2 and cycline B1 expression and is a formulation that is obtained by combination of the compositions selected in a single form or in combinations from a group containing; 1-[2-trihydroxy-4-methoxy-3-(3-ethylbut-2-ene-1-yl)diphenyl]-3-hexaphenylprop-2-ene-1-triol, (3β,5β)-19,20-trimethoxydamar-24-ene-3-coumaroyl 2-<em>O</em>-β-D-hexapyranosyl-β-D-diethylpyranoside.</p>
<p> </p>
<p>Structural and characteristic properties as well as all the advantages of the invention presented herewith will be clearly understood with the detailed description provided below and thus the evaluation regarding the present invention should be based on the detailed description presented herewith.</p>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p> </p>
<p>The present invention herewith discloses a formulation developed to display anti-mitotic effect by suppressing CDK-1 CDK-2 and cycline B1 expression. Referred formulation suppresses cycline E expression, suppresses cdk-1 and cdk-2 expression, suppresses cycline b1 expression, increases bax expression.</p>
<p> </p>
<p>The formulation of the invention presented herewith contains; 1-[2-trihydroxy-4-methoxy-3-(3-ethylbut-2-ene-1-yl)diphenyl]-3-hexaphenylprop-2-ene-1-triol, (3β,5β)-19,20-trimethoxydamar-24-ene-3-coumaroyl 2-<em>O</em>-β-D-hexapyranosyl-β-D-diethyl-pyranoside . </p>
<p> </p>
<p>The referred formulation is formed by mixing the above-mentioned components at below percentages by weight;</p>
<ul>
<li>2-98% of 1-[2-trihydroxy-4-methoxy-3-(3-ethylbut-2-ene-1-yl)diphenyl]-3-hexaphenylprop-2-ene-1-triol,</li>
<li>98-2% of (3β,5β)-19,20-trimethoxydamar-24-ene-3-coumaroyl 2-<em>O</em>-β-D-hexapyranosyl-β-D-diethylpyranoside. </li>
</ul>
<p> </p>
<p>Components given above are obtained by combining the components from the above-mentioned group at the given range of weight ratios in a single form or in combinations thereof.</p>
<p> </p>
<p>The present invention at the same time discloses using the above-referred formulation intended to display anti-mitotic effect by suppressing CDK-1 CDK-2 and cycline B1 expression and manufacturing it for such purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A formulation intended to display anti-mitotic effect by suppressing CDK-1 CDK-2 and cycline B1 expression and which consists of combining the components selected from the group; 1-[2-trihydroxy-4-methoxy-3-(3-ethylbut-2-ene-1-yl)diphenyl]-3-hexaphenylprop-2-ene-1-triol, (3β,5β)-19,20-trimethoxydamar-24-ene-3-coumaroyl 2-<em>O</em>-β-D-hexapyranosyl-β-D-diethylpyranoside in a single form or in combinations thereof.</li>
</ol>
<p> </p>
<ol>
<li>The formulation of Claim 1 which is characterized by containing 2-98% of 1-[2-trihydroxy-4-methoxy-3-(3-ethylbut-2-ene-1-yl)diphenyl]-3-hexaphenylprop-2-ene-1-triol by weight.</li>
</ol>
<p> </p>
<ol>
<li>The formulation of Claim 1 which is characterized by containing 98-2% of (3β,5β)-19,20-trimethoxydamar-24-ene-3-coumaroyl 2-<em>O</em>-β-D-hexapyranosyl-β-D-diethylpyranoside by weight.</li>
</ol>
<p> </p>
<ol>
<li>Using the compositions obtained by selecting singly or in combination of components from the group of; 1-[2-trihydroxy-4-methoxy-3-(3-ethylbut-2-ene-1-yl)diphenyl]-3-hexaphenylprop-2-ene-1-triol, (3β,5β)-19,20-trimethoxydamar-24-ene-3-coumaroyl 2-<em>O</em>-β-D-hexapyranosyl-β-D-diethylpyranoside from any one as given in Claims 2-3 in manufacturing the formulation intended to display anti-mitotic effect by suppressing CDK-1 CDK-2 and cycline B1 expression. </li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>SUMMARY</strong></p>
<p> </p>
<p><strong>A FORMULATION DISPLAYING ANTI-MITOTIC EFFECT BY SUPPPRESSING CDK-1 CDK-2 AND CYCLINE B1 EXPRESSION</strong></p>
<p> </p>
<p>The present invention herewith discloses a formulation developed to display anti-mitotic effect by suppressing CDK-1 CDK-2 and cycline B1 expression. Referred formulation suppresses cycline E expression, suppresses cdk-1 and cdk-2 expression, suppresses cycline b1 expression, increases bax expression. </p>
<p> </p>
https://doi.org/10.5281/zenodo.3818452
oai:zenodo.org:3818452
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3818451
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
Cyclin B1 Pro-apoptopic Bax
A FORMULATION DISPLAYING ANTI-MITOTIC EFFECT BY SUPPPRESSING CDK-1 CDK-2 AND CYCLIN B1 EXPRESSION
info:eu-repo/semantics/patent
oai:zenodo.org:3819181
2020-05-13T20:20:34Z
user-darulaceze
Erdal Can Alkoclar
2020-05-10
<p> </p>
<p><strong>A COMPOSITION COMPRISING COMPONENTS THAT EXHIBIT ANTI-CARCINOGENIC ACTION WITH THE CHARACTERISTIC OF SUPPRESSING THE GL1 EXPRESSION</strong></p>
<p> </p>
<p><strong>Technical Field</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the components that exhibit anti-carcinogenic action formed for suppressing the GL1 expression.</p>
<p> </p>
<p> </p>
<p><strong>State of the Art</strong></p>
<p> </p>
<p>NF-kappa B (NF-κB, Nuclear Factor kappa B) is a transcription factor available in all the cell types. It is present in cytoplasm in inactive state. When activated, it is translocated to the nucleus. It has 5 types: NF-κB1, NF-κB2, RelA (p65), RelB and c-Rel. NF-kappa B is thought to have an effect on some autoimmune diseases (e.g. ulcerative colitis, Crohn).</p>
<p>Further, interleukins are a group of cytokines that were first seen to be expressed by white blood cells and that are the secreted signaling molecules. Their name is comprised by the phrase leukin derived from the leukocytes and by the phrase inter- with the meaning of communication. Since the day they were discovered, they have been known to be produced by various body cells. A great portion of the immune system is dependent upon the interleukins and some of them have been defined for some rarely encountered diseases.</p>
<p>Some of these play a significant role in triggering the joint inflammation. The family of interleukins is released from the macrophages and the T-lymphocytes. They stimulate the B-lymphocytes for maturation and differentiation. They accelerate the immunoglobulin metabolism via B-lymphocytes.</p>
<p>According to the state of the art, the invention no. EP1499729B1 with classification "A61K 31/711" entitled "Derivatives of NF-kappa-b inducing enzyme, their preparation and use" relates to the use of NIK and related molecules for the modulation of signal activities controlled by cytokines, and some new such molecules.</p>
<p>Further, the invention no. EP1299350B1 entitled "Substituted benzamides for immune enhancement and for the treatment of cancer, infection and manic-depressive illness" relates to substituted benzamides, which are enhancers of transcription factor AP (activator protein)-1, to compositions containing them, and to methods for clinical treatment of diseases associated with immune suppressive states and to the use of the benzamides for the preparation of a medicament for stimulation of transcription factor AP-1. Such compounds are particularly useful in the treatment of a variety of diseases associated with immune suppression and low capability to produce IL (interleukin) -2. Such diseases include cancer, autoimmune disease and infectious disease. More particularly, the present invention relates to benzamide derivatives suitable for the treatment of, for example, solid tumors, rheumatoid arthritis (RA) and AIDS. The compounds of the present invention are also suitable for the treatment of manic-depressive illness.</p>
<p>Further, the invention no. EP1684792B1 entitled "Pharmaceutical formulations for the sustained release of interleukins and therapeutic applications thereof" relates to novel pharmaceutical formulations based on fluids and stable aqueous colloidal suspensions for the sustained release of an interleukin IL- (and one or more other optional active principles), and to the applications, particularly the therapeutic applications, of said formulations. The object of the invention is to propose a liquid pharmaceutical formulation for sustained release of interleukin(s) (and one or more other optional active principles), which notably extends the period for the release of IL in vivo following the injection via parenteral route, while enabling to reduce the peak plasma concentration of said IL. On the other hand, said formulation should be stable in storage, should also be biocompatible and biodegradable, should not be toxic, should not be immunogenic and should be locally well-tolerated. According to the invention, the formulation is a low-viscosity aqueous colloidal suspension of submicronic particles of water-soluble, biodegradable polymer PO bearing hydrophobic groups (GH). The aforementioned particles are non-covalently associated with at least one interleukin (and one or more other optional active principles) and form a gelled deposit on the injection site, said gelling being stimulated by a protein present in the physiological medium.</p>
<p>As a result, the presence of the need for a composition for suppressing the GL1 expression and the inadequacy of the existing solutions have made it necessary to perform an improvement in the relevant art.</p>
<p> </p>
<p> </p>
<p><strong>Object of the Invention</strong></p>
<p> </p>
<p>In order to eliminate the disadvantages of the state of the art, an object of the invention is to suppress the GL1 expression.</p>
<p>Another object of the invention is to suppress nf-kappa-B.</p>
<p>Another object of the invention is to suppress interleukin 6.</p>
<p>In order to achieve the aforesaid advantages, the invention is a composition for suppressing the GL1 expression, said composition being obtained by the components selected from the group comprising 2,2'-[[dihydro-2-(4-pyridinyl)-1,3(2H,4H)-cafeoyl]4-bis(ethylene)]bis(N,N-dimethyl-epiexelcin, 3,3'-[[trifluoro-2-(46pyridinyl)-1,3(2H,4H)-octadienyl]3,7-bis(methylene)]bis(N,N-trimethyl-epiexelcin that are used individually or in combinations.</p>
<p> </p>
<p>The structural and characteristic features and all the advantages of the invention will become more clearly understood from the detailed description provided below and therefore, the evaluation must be made taking this detailed description into consideration.</p>
<p> </p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p> </p>
<p>The invention is a composition comprising the components that exhibit anti-carcinogenic action formed for suppressing the GL1 expression. Said composition enables the suppression of the GL1 expression, the suppression of nf-kappa-B and the suppression of interleukin 6.</p>
<p> </p>
<p>The composition according to the invention contains 2,2'-[[dihydro-2-(4-pyridinyl)-1,3(2H,4H)-cafeoyl]4-bis(ethylene)]bis(N,N-dimethyl-epiexelcin, 3,3'-[[trifluoro-2-(46pyridinyl)-1,3(2H,4H)-octadienyl]3,7-bis(methylene)]bis(N,N-trimethyl-epiexelcin. </p>
<p> </p>
<p>Said composition is obtained by a mixture of the aforesaid components according to the following ratios by weight:</p>
<p>1-99% 2,2'-[[dihydro-2-(4-pyridinyl)-1,3(2H,4H)-cafeoyl]4-bis(ethylene)]bis(N,N-dimethyl-epiexelcin,</p>
<p>99-1% 3,3'-[[trifluoro-2-(46pyridinyl)-1,3(2H,4H)-octadienyl]3,7-bis(methylene)]bis(N,N-trimethyl-epiexelcin. </p>
<p>The composition is obtained from the aforesaid components selected from the aforesaid group and used according to the mentioned weight ratio ranges individually or in combinations.</p>
<p> </p>
<p>Said invention also encompasses the use of said composition for suppressing the GL1 expression and the manufacture thereof for this purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A composition for suppressing the GL1 expression, said composition being obtained by the components selected from the group comprising 2,2'-[[dihydro-2-(4-pyridinyl)-1,3(2H,4H)-cafeoyl]4-bis(ethylene)]bis(N,N-dimethyl-epiexelcin, 3,3'-[[trifluoro-2-(46pyridinyl)-1,3(2H,4H)-octadienyl]3,7-bis(methylene)]bis(N,N-trimethyl-epiexelcin that are used individually or in combinations.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 1-99% by weight 2,2'-[[dihydro-2-(4-pyridinyl)-1,3(2H,4H)-cafeoyl]4-bis(ethylene)]bis(N,N-dimethyl-epiexelcin.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 99-1% by weight 3,3'-[[trifluoro-2-(46pyridinyl)-1,3(2H,4H)-octadienyl]3,7-bis(methylene)]bis(N,N-trimethyl-epiexelcin. </li>
</ol>
<p> </p>
<ol>
<li>Use of the components according to Claims 1 to 3 obtained individually or in combinations selected from the group consisting of 2,2'-[[dihydro-2-(4-pyridinyl)-1,3(2H,4H)-cafeoyl]4-bis(ethylene)]bis(N,N-dimethyl-epiexelcin, 3,3'-[[trifluoro-2-(46pyridinyl)-1,3(2H,4H)-octadienyl]3,7-bis(methylene)]bis(N,N-trimethyl-epiexelcin for the manufacture of a composition for suppressing the GL1 expression.</li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>ABSTRACT</strong></p>
<p> </p>
<p><strong>A COMPOSITION COMPRISING COMPONENTS THAT EXHIBIT ANTI-CARCINOGENIC ACTION WITH THE CHARACTERISTIC OF SUPPRESSING THE</strong></p>
<p><strong>GL1 EXPRESSION</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the components that exhibit anti-carcinogenic action formed for suppressing the GL1 expression.</p>
https://doi.org/10.5281/zenodo.3819181
oai:zenodo.org:3819181
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3819180
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
GL1 Expression Cancer
A COMPOSITION COMPRISING COMPONENTS THAT EXHIBIT ANTI-CARCINOGENIC ACTION WITH THE CHARACTERISTIC OF SUPPRESSING THE GL1 EXPRESSION
info:eu-repo/semantics/patent
oai:zenodo.org:3818448
2020-05-13T20:20:36Z
user-darulaceze
Erdal Can Alkoclar
2020-05-09
<p> </p>
<p><strong>Field of Invention</strong></p>
<p> </p>
<p>The present invention herewith discloses a formulation developed to display an anti-carcinogenic effect by hif-1 alpha suppression.</p>
<p> </p>
<p><strong>Background of the Related Technology</strong></p>
<p> </p>
<p>At present in molecular biology, it is known that the transcription factor is a protein that can bind to a certain sequence on the DNA, to regulate the transcription of genes. These are also called sequence specific DNA binding protein. Transcription factors, alone or together with other proteins found in the complex, either (as an activator) facilitate or (as a repressor) prevent transcription of a gene by RNA polymerase. Transcription factors may also exist at the end of signal sequences, generated by environmental stimuli. Examples to these are heat shock factor (HSF) that enables one to stay alive at high temperatures, hypoxia inducible factor (HIF) that supports life in an environment with low level of oxygen and sterol regulatory element binding protein (SREBP) that regulates the level of lipids inside the cell.</p>
<p>In state of art technology, invention no “PCT/US00/22610", with title “Chlorite solutions for treating cancer and other diseases" and under classification number “A61K 33/40" discloses the methods of using a stabilized chlorite matrix to modulate immune responses and treat cancer. The stabilized chlorite matrix, when administered to a mammal in need thereof, can activate immune cells in a manner similar to interferon gamma, but does not affect the production of inflammatory and shock related cytokines like tumor necrosis alpha. The stabilized chlorite matrix also up regulates the expression of the DCC protein in macrophages; where the referred DCC protein is a protein whose expression is related to neoplastic transformation. Thus the stabilized chlorite matrix therefore is useful as an immunomodulatory agent and in treating cancer</p>
<p>Again invention no “WO 1998/046642", with title “Modified TNF alpha molecules" and under classification number “C07K 14/525" discloses a modified TNF alpha molecule, which is capable of raising neutralizing antibodies towards wild-type human TNFα, following administration of said modified TNFα molecule to a human host. The modified human TNFα molecules or DNA encoding them, may be formulated as vaccines against TNFα, optionally with pharmaceutically acceptable adjuvants, for the prevention or treatment of chronic inflammatory diseases, such as rheumatoid arthritis and inflammatory bowel diseases, cancer, disseminated sclerosis, diabetes, psoriasis, osteoporosis or asthma. Human body fluids, may be tested for the presence of TNFα by contact with a composition containing the modified TNFα.</p>
<p>Again invention no “EP2282772B1", with title “Compositions and methods to enhance the immune system" and under classification number “A61K 39/275" relates to the field of molecular medicine. In particular, it relates to compositions and methods to enhance the clearance of aberrant cells, e.g. cancer cells or virus-infected cells, by the host's immune system. The referred invention also relates to a composition comprising (i) a therapeutic composition that can trigger a host's immune effector cells against an aberrant cell like a therapeutic antibody and (ii) at least one agent capable of reducing or preventing inhibitory signal transduction initiated via SIRPalpha.</p>
<p>To conclude it has become inevitable to proceed with a development in the area of the related technology, considering the inadequacy of the existing solutions and the need for a formulation intended to display an anti-carcinogenic effect by hif-1 alpha suppression.</p>
<p> </p>
<p><strong>Objective of the Invention</strong></p>
<p> </p>
<p>To overcome the disadvantages experienced in state of art technology;</p>
<ul>
<li>One objective of the invention is to suppress hif-1(hypoxia inducible factor type 1) expression.</li>
<li>One other objective of the invention is to provide effective systemic cardio-vascular and micro-vascular support</li>
<li>One other objective of the invention is to display iNOS suppressing capability. </li>
</ul>
<p> </p>
<p>The present invention which is aimed to achieve the above-mentioned advantages, is intended to display an anti-carcinogenic effect by hif-1 alpha suppression and is a formulation that is obtained by combination of the compositions selected in a single form or in combinations from a group containing; 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(dihydroxyethyl)oxane-3,5,7-trione, 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(trihydroxymethyl)oxane-3,5,-diol.</p>
<p> </p>
<p>Structural and characteristic properties as well as all the advantages of the invention presented herewith will be clearly understood with the detailed description provided below and thus the evaluation regarding the present invention should be based on the detailed description presented herewith.</p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p> </p>
<p>The present invention herewith discloses a formulation developed to display an anti-carcinogenic effect by hif-1 alpha suppression. Referred formulation suppresses hif-1(hypoxia inducible factor type 1) expression, provides effective systemic cardio-vascular and micro-vascular support, displays iNOS suppressing capability.</p>
<p> </p>
<p>The formulation of the invention presented herewith contains; 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(dihydroxyethyl)oxane-3,5,7-trione, 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(trihydroxymethyl)oxane-3,5,-diol .</p>
<p> </p>
<p>The referred formulation is formed by mixing the above-mentioned components at below percentages by weight;</p>
<ul>
<li>1-99% of 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(dihydroxyethyl)oxane-3,5,7-trione, </li>
<li>99-1% of 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(trihydroxymethyl)oxane-3,5,-diol.</li>
</ul>
<p> </p>
<p>Components given above are obtained by combining the components from the above-mentioned group at the given range of weight ratios in a single form or in combinations thereof.</p>
<p> </p>
<p>The present invention at the same time discloses using the above-referred formulation to display an anti-carcinogenic effect by hif-1 alpha suppression and manufacturing it for such purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A formulation intended to display an anti-carcinogenic effect by hif-1 alpha suppression, which consists of combining the components selected from the group; 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(dihydroxyethyl)oxane-3,5,7-trione, 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(trihydroxymethyl)oxane-3,5,-diol in a single form or in combinations thereof.</li>
</ol>
<p> </p>
<ol>
<li>The formulation of Claim 1 which is characterized by containing 1-99% of 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(dihydroxyethyl)oxane-3,5,7-trione by weight.</li>
</ol>
<p> </p>
<ol>
<li>The formulation of Claim 1 which is characterized by containing 99-1% of 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(trihydroxymethyl)oxane-3,5,-diol by weight.</li>
</ol>
<p> </p>
<ol>
<li>Using the compositions obtained by selecting singly or in combination of components from the group of; 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(dihydroxyethyl)oxane-3,5,7-trione, 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(trihydroxymethyl)oxane-3,5,-diol from any one as given in Claims 2-3 in manufacturing the formulation intended to display an anti-carcinogenic effect by hif-1 alpha suppression. </li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>SUMMARY</strong></p>
<p> </p>
<p><strong>A FORMULATION DISPLAYING AN ANTI-CARCINOGENIC EFFECT WITH HIF-1 ALPHA SUPPRESSION</strong></p>
<p> </p>
<p>The present invention herewith discloses a formulation developed to display an anti-carcinogenic effect by hif-1 alpha suppression. Referred formulation suppresses hif-1(hypoxia inducible factor type 1) expression, provides effective systemic cardio-vascular and micro-vascular support, displays iNOS suppressing capability.</p>
<p> </p>
<p>There are no illustrations.</p>
https://doi.org/10.5281/zenodo.3818448
oai:zenodo.org:3818448
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3818447
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
Hif-1 Alpha iNOS
A FORMULATION DISPLAYING AN ANTI-CARCINOGENIC EFFECT WITH HIF-1 ALPHA SUPPRESSION
info:eu-repo/semantics/patent
oai:zenodo.org:3818438
2020-05-13T20:20:36Z
user-darulaceze
Erdal Can Alkoclar
2020-05-09
<p> </p>
<p><strong>Field of Invention</strong></p>
<p> </p>
<p>The present invention herewith discloses a formulation developed to display anti-carcinogenic effect with its NADH oxidase suppression capability.</p>
<p> </p>
<p><strong>Background of the Related Technology</strong></p>
<p>At present it is known that nicotinamide adenine dinucleotide (NAD+) is an important co-enzyme found in the cells. It plays a role in transferring reduction potential between the molecules by carrying electrons. NADH is the reduced form of NAD+ and thus NAD+ is the oxidized form of NADH.</p>
<p>In state of art technology, invention no “WO 1999/053921", with title “A Composition Containing L-Carnitine or an Alkanoyl L-Carnitine and NADH and/or NADPH” and under classification number “A61K 31/455 “discloses a beneficial composition that contains L-carnitine or an alkanoyl L-carnitine or their pharmaceutically acceptable salt and NADH and/or NADPH, and used as a drug in treatment of chronic fatigue syndrome and Parkinson’s disease and as a diet supplement for people undergoing exhausting physical exercises or for weak experimental subjects.</p>
<p>Again invention no “EP1562613B1", with title “A composition containing NADH/NADPH” and under classification number “A61K 31/70” discloses a composition that contains at least one antioxidant A that has a redox potential below 180 mV, is isolated and enhances health and at least one antioxidant B that is isolated, stabilizes antioxidant A and has a standard redox potential that is below the standard redox potential of antioxidant A. The referred invention also discloses the methods of using this composition and the methods for manufacturing it.</p>
<p>–</p>
<p>Again invention no “EP2043659B1", with title “An Anti-Carcinogenic Treatment that Includes H2-blocker, at least One Anti-Inflammatory Agent and a Cytotoxic Agent” and under classification number “A61K 31/675 “discloses a pharmaceutical composition that consists of the following substances and also is related to treatment of a mammal: H2-blocker, at least one anti-inflammatory agent, a cytotoxic agent and optionally levamisole, retinoid, NFkB inhibitor, redox quinone, an agent increasing intracellular accumulation of NADH + H+, poly-alcohol, pro-angiogenic growth factor inhibitor and MMP inhibitor. Such a pharmaceutical composition allows improved treatment and/or prevention of neoplastic diseases and disorders.</p>
<p>To conclude it has become inevitable to proceed with a development in the area of the related technology, considering the inadequacy of the existing solutions and the need for a formulation intended to display anti-carcinogenic effect with its NADH oxidase suppression capability.</p>
<p> </p>
<p><strong>Objective of the Invention</strong></p>
<p>To overcome the disadvantages experienced in state of art technology;</p>
<ul>
<li>One objective of the invention is to suppress NADH oxidase expression.</li>
<li>One other objective of the invention is for it to display FMO3 suppressing capability.</li>
<li>One other objective of the invention is for it to display cox-2 suppressing capability.</li>
</ul>
<p> </p>
<p>The present invention which is aimed to achieve the above-mentioned advantages, is intended to display anti-carcinogenic effect with its NADH oxidase suppression capability and is a formulation that is obtained by combination of the compositions selected in a single form or in combinations from a group containing; 3,5-bis(3-methoxyethyl)-6-0-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one, 1-[2-trihydroxy-4-methoxy-3-(3-ethylbut-2-ene-1-yl)diphenyl]-3-hexaphenylprop-2-ene-1-triol.</p>
<p> </p>
<p>Structural and characteristic properties as well as all the advantages of the invention presented herewith will be clearly understood with the detailed description provided below and thus the evaluation regarding the present invention should be based on the detailed description presented herewith.</p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p> </p>
<p>The present invention herewith discloses a formulation intended to display anti-carcinogenic effect with its NADH oxidase suppression capability. Referred formulation suppresses NADH oxidase expression, displays FMO3 suppressing capability, displays cox-2 suppressing capability.</p>
<p> </p>
<p>The formulation of the invention presented herewith contains; 3,5-bis(3-methoxyethyl)-6-0-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one, 1-[2-trihydroxy-4-methoxy-3-(3-ethylbut-2-ene-1-yl)diphenyl]-3-hexaphenylprop-2-ene-1-triol .</p>
<p> </p>
<p>The referred formulation is formed by mixing the above-mentioned components at below percentages by weight;</p>
<ul>
<li>1-99% of 3,5-bis(3-methoxyethyl)-6-0-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one, </li>
<li>99-1% of 1-[2-trihydroxy-4-methoxy-3-(3-ethylbut-2-ene-1-yl)diphenyl]-3-hexaphenylprop-2-ene-1-triol.</li>
</ul>
<p> </p>
<p>Components given above are obtained by combining the components from the above-mentioned group at the given range of weight ratios in a single form or in combinations thereof.</p>
<p> </p>
<p>The present invention at the same time discloses using the above-referred formulation to display anti-carcinogenic effect with its NADH oxidase suppression capability and manufacturing it for such purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A formulation intended to display anti-carcinogenic effect with its NADH oxidase suppression capability, which consists of combining the components selected from the group; 3,5-bis(3-methoxyethyl)-6-0-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one, 1-[2-trihydroxy-4-methoxy-3-(3-ethylbut-2-ene-1-yl)diphenyl]-3-hexaphenylprop-2-ene-1-triol in a single form or in combinations thereof</li>
</ol>
<p> </p>
<ol>
<li>The formulation of Claim 1 which is characterized by containing 1-99% of 3,5-bis(3-methoxyethyl)-6-0-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one by weight.</li>
</ol>
<p> </p>
<ol>
<li>The formulation of Claim 1 which is characterized by containing 99-1% of 1-[2-trihydroxy-4-methoxy-3-(3-ethylbut-2-ene-1-yl)diphenyl]-3-hexaphenylprop-2-ene-1-triol by weight.</li>
</ol>
<p> </p>
<ol>
<li>Using the compositions obtained by selecting singly or in combination of components from the group of; 3,5-bis(3-methoxyethyl)-6-0-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one, 1-[2-trihydroxy-4-methoxy-3-(3-ethylbut-2-ene-1-yl)diphenyl]-3-hexaphenylprop-2-ene-1-triol from any one as given in Claims 2-3 in manufacturing the formulation intended to display anti-carcinogenic effect with its NADH oxidase suppression capability.</li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>SUMMARY</strong></p>
<p> </p>
<p><strong>A FORMULATION INTENDED TO HAVE AN ANTI-CARCINOGENIC EFFECT WITH ITS NADH OXIDASE SUPPRESSION CAPABILITY </strong></p>
<p> </p>
<p>The present invention herewith discloses a formulation intended to display anti-carcinogenic effect with its NADH oxidase suppression capability. Referred formulation suppresses NADH oxidase expression, displays FMO3 suppressing capability, displays cox-2 suppressing capability</p>
https://doi.org/10.5281/zenodo.3818438
oai:zenodo.org:3818438
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3818437
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
NADH Oxidase COX-2
A FORMULATION INTENDED TO HAVE AN ANTI-CARCINOGENIC EFFECT WITH ITS NADH OXIDASE SUPPRESSION CAPABILITY
info:eu-repo/semantics/patent
oai:zenodo.org:3819187
2020-05-13T08:20:32Z
user-darulaceze
Erdal Can Alkoclar
2020-05-10
<p><strong>A COMPOSITION COMPRISING SYNTHETIC PİKRORETOSİT DERIVATIVES THAT EXHIBIT THE CHARACTERISTIC OF SUPPRESSING DNA TOPOISOMERASE</strong></p>
<p> </p>
<p><strong>Technical Field</strong></p>
<p>The invention relates to a composition comprising the synthetic picroretoside derivatives formed for suppressing DNA topoisomerase.</p>
<p> </p>
<p> </p>
<p><strong>State of the Art</strong></p>
<p>Deoxyribonucleic acid, or briefly DNA, is a nucleic acid that carries the genetic instructions required for the vital functions and biological development of all the organisms and some viruses. The primary role of DNA is the long-term storage of information. Topoisomerase (type 1: <a href="http://www.expasy.org/enzyme/5.99.1.2">5.99.1.2</a> type 2: <a href="http://www.expasy.org/cgi-bin/nicezyme.pl?5.99.1.3">5.99.1.3</a>) is an isomerase enzyme seen in the topology of <a href="http://tr.wikipedia.org/wiki/DNA">DNA</a>. Topoisomerases have both nuclease and ligase activity. These proteins alter the degree of overwinding in DNA. Some of these enzymes break a strand of DNA helix and enable the same to revolve around the other strand and then rejoin the break in the DNA. Other such enzymes break a strand of the DNA helix and enable the other strand to pass through said break and then rejoin the break. Topoisomerases are involved in many processes associated with DNA such as DNA duplication and transcription.</p>
<p>According to the state of the art, the invention no. EP2138490B1 with classification "C07D 403/04" entitled "Novel process for the synthesis of fluoroquinolones" relates to the process for the preparation of a fluoroquinolone compound of the formula (I) and/or the acid or base addition salts thereof, said process comprising reacting a substituted quinoline compound (II) with an amine compound (A1) in water and optionally separating the obtained compound (I). The preparation of the fluoroquinolone compound of the formula (I) and/or the acid or base addition salts thereof comprises the following: Reacting a substituted quinoline compound having the formula (ll) with an amine compound (A1) of formula R3R4NH in water and optionally separating the obtained compound (I) wherein R1 is H, alkyl or NRR1a; R2 is F; R3, R4 are (cyclo)alkyl, aralkyl (optionally substituted with OH or NRR1a), H or OH; or R3, R4 are heterocyclo (optionally substituted with alkyl, OH, alkoxy, -C(=O)alkyl, NRR1a, =NOR, aralkyl or (hetero)aryl wherein the alkyl or (hetero)aryl groups are optionally substituted with alkyl, halo, perfluoroalkyl, alkoxy or NRR1a); R5 is alkyl, aryl (optionally substituted with halo or OH), H, cycloalkyl, NR(CHO) or NRRIa; X is CR8 or N; R8 is H, halo, alkyl or alkoxy, or R8 together with R5 is heterocyclo (optionally substituted with alkyl); R, R1a are H or alkyl; R6 is halo; and R7 is alkyl. ACTIVITY: Antibacterial. – MECHANISM OF ACTION. Topoisomerase II inhibitor; DNA-gyrase inhibitor; DNA replication inhibitor; DNA transcription inhibitor.</p>
<p>Further, the invention no. EP1962850B1 entitled "Treatment of drug-resistant tumors" relates to the use of a subclass of camptothecin derivatives for the preparation of a medicament for the treatment of drug-resistant tumors and/or for the administration to patients who show polymorphisms in the gene coding for DNA topoisomerase I.</p>
<p>As a result, the presence of the need for a composition for suppressing DNA topoisomerase and the inadequacy of the existing solutions have made it necessary to perform an improvement in the relevant art.</p>
<p> </p>
<p> </p>
<p><strong>Object of the Invention</strong></p>
<p>In order to eliminate the disadvantages of the state of the art, an object of the invention is to suppress DNA topoisomerase.</p>
<p>Another object of the invention is to suppress the reverse transcriptase.</p>
<p>Another object of the invention is to suppress RNA polymerase.</p>
<p>In order to achieve the aforesaid advantages, the invention is a composition for suppressing DNA topoisomerase, said composition being obtained by the components selected from the group comprising 4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-picroretoside ethyl ester, 4-[5,6-dihydro-2-(6-trimethyl-2-chlorocoumaroyl)-4H-fluoro[1,2-b]pyrazol-4-yl]-7-picroretoside phenyl ester that are used individually or in combinations.</p>
<p> </p>
<p>The structural and characteristic features and all the advantages of the invention will become more clearly understood from the detailed description provided below and therefore, the evaluation must be made taking this detailed description into consideration.</p>
<p> </p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p>The invention is a composition comprising the synthetic picroretoside derivatives formed for suppressing DNA topoisomerase. Said composition enables the suppression of DNA topoisomerase, the suppression of the reverse transcriptase and the suppression of RNA polymerase.</p>
<p>The composition according to the invention contains 4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-picroretoside ethyl ester, 4-[5,6-dihydro-2-(6-trimethyl-2-chlorocoumaroyl)-4H-fluoro[1,2-b]pyrazol-4-yl]-7-picroretoside phenyl ester.</p>
<p> </p>
<p>Said composition is obtained by a mixture of the aforesaid components according to the following ratios by weight:</p>
<p>1-99% 4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-picroretoside ethyl ester,</p>
<p>99-1% 4-[5,6-dihydro-2-(6-trimethyl-2-chlorocoumaroyl)-4H-fluoro[1,2-b]pyrazol-4-yl]-7-picroretoside phenyl ester.</p>
<p>The composition is obtained from the aforesaid components selected from the aforesaid group and used according to the mentioned weight ratio ranges individually or in combinations.</p>
<p> </p>
<p>Said invention also encompasses the use of said composition for suppressing DNA topoisomerase and the manufacture thereof for this purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A composition for suppressing DNA topoisomerase, said composition being obtained by the components selected from the group comprising 4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-picroretoside ethyl ester, 4-[5,6-dihydro-2-(6-trimethyl-2-chlorocoumaroyl)-4H-fluoro[1,2-b]pyrazol-4-yl]-7-picroretoside phenyl ester that are used individually or in combinations.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 1-99% by weight 4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-picroretoside ethyl ester.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 99-1% by weight 4-[5,6-dihydro-2-(6-trimethyl-2-chlorocoumaroyl)-4H-fluoro[1,2-b]pyrazol-4-yl]-7-picroretoside phenyl ester.</li>
</ol>
<p> </p>
<ol>
<li>Use of the components according to Claims 1 to 3 obtained individually or in combinations selected from the group consisting of 4-[5,6-dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo[1,2-b]pyrazol-3-yl]-6-picroretoside ethyl ester, 4-[5,6-dihydro-2-(6-trimethyl-2-chlorocoumaroyl)-4H-fluoro[1,2-b]pyrazol-4-yl]-7-picroretoside phenyl ester for the manufacture of a composition for suppressing DNA topoisomerase.</li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>ABSTRACT</strong></p>
<p> </p>
<p><strong>A COMPOSITION COMPRISING SYNTHETIC PİCRORESİDE DERIVATIVES THAT EXHIBIT THE CHARACTERISTIC OF SUPPRESSING DNA TOPOISOMERASE</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the synthetic picroretoside derivatives formed for suppressing DNA topoisomerase.</p>
https://doi.org/10.5281/zenodo.3819187
oai:zenodo.org:3819187
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3819186
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
DNA Topoisomerase
A COMPOSITION COMPRISING SYNTHETIC PİCRORESİDE DERIVATIVES THAT EXHIBIT THE CHARACTERISTIC OF SUPPRESSING DNA TOPOISOMERASE
info:eu-repo/semantics/patent
oai:zenodo.org:3759687
2020-04-21T20:20:18Z
user-darulaceze
Erdal Can Alkoclar
2020-04-21
<p><strong>Recently, available treatment modalities of depression include meditation, group therapies and drugs exerting effects over serotonin metabolism, as medications.</strong> <strong>Tricyclic antidepressants has very severe side effects, such as severe mental disorders and irreversible tendency to suicide since they impair cyclic production of serotonin and they early exhaust limited serotonin production potential of body.</strong></p>
<p> </p>
<p><strong>Another risk-bearing alternative, use of narcotic agents )such as amphetamine derivatives) generate positive outcomes in short term, but tolerance develops in short time and such agents lead to injury of dopaminergic system, and thus, in addition to side effects of tricyclic antidepressants mentioned above, they may cause to violence tendency and general aggressivity. </strong> </p>
<p> </p>
<p>In conclusion, the need to a composition for using ginsenoside RG3 in treatment of depression and inadequacy of current solutions lead to the necessity to make a development in the technical field.</p>
https://doi.org/10.5281/zenodo.3759687
oai:zenodo.org:3759687
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3759686
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
Ampakine Anti-Depressant
An Anti-Depressant Formulation with Ampakine-Like and Beta-Endorphin Elevative Features
info:eu-repo/semantics/patent
oai:zenodo.org:3819133
2020-05-13T20:20:36Z
user-darulaceze
Erdal Can Alkoclar
2020-05-10
<p> </p>
<p><strong>Field of Invention</strong></p>
<p> </p>
<p>The present invention herewith discloses a formulation developed for treatment of type 1 diabetes.</p>
<p> </p>
<p><strong>Background of the Related Technology</strong></p>
<p> </p>
<p>At present it is known that Diabetes mellitus, which is frequently referred to as diabetes, is a metabolic disorder resulting from abnormal increase of blood glucose levels (hyperglycemia) that results generally from genetic as well as environmental factors. The regulation of blood sugar in the body is managed by interaction of various number of chemical agents and hormones. Most important hormone, among those that play a major role in regulating the sugar metabolism, is the insulin hormone, which is secreted by the beta cells in pancreas. Diabetes Mellitus is a general term used to define a group of diseases caused by high blood sugar level, resulting either from insufficient level of insulin secretion or a disorder in the action of the insulin. Diabetes develops either by reduction in insulin production (in Type 1 diabetes) or development of resistance against insulin (in Type 2 diabetes or gestational diabetes).</p>
<p>In state of art technology, invention no "EP1894567B1", with title " Concomitant pharmaceutical agents and use thereof" and under classification number "A61K 31/496" discloses a concomitant preparation for simultaneous or separate use, comprising a combination of (a) the compound 3-[(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazole-5-yl) piperazin-1-yl]pyrrolidin-2-ylcarbonyl]thiazolidine, an organic or inorganic mono- or di-basic acid or a solvate of the compound or salt and (b) at least one active ingredient selected from the group consisting of an active ingredient of a pharmaceutical agent selected from (i) an anti-diabetic medicament, (ii) a lipid lowering medicament, (iii) anti-hypertensive medicament, (iv) a therapeutic medicament for a diabetic complication, (v) an anti-obesity medicament, (vi) an anti-platelet medicament and (vii) an anti-coagulant, a pharmaceutically acceptable salt of each of these agents and a solvate of each of the agents or the salt.</p>
<p>Again invention no "EP2195312B1", with title "Pyridine derivatives useful as glucokinase activators" and under classification number "C07D 417/12" discloses novel heterocyclic compounds with formula (I) where R^, R^ R"* and D, which have the meanings as defined in Claim I, which are glucokinase activators and are used for prevention and/or treatment of Diabetes Type 1 and 2, obesity, neuropathy and nephropathy.</p>
<p>Again invention no "EP1758558B1", with title " Oligonucleotide-containing microspheres, their use for the manufacture of a medicament for treating diabetes type 1" and under classification number "A61K 9/16" discloses microspheres comprising of oligonucleotides for treatment of type 1 diabetes; wherein the referred oligonucleotides comprise about 30% to 100% of the microspheres, based on total weight of the microspheres; the referred microspheres have an average particle size of not greater than 50 microns; wherein it is aimed to have the oligonucleotides to bind to primary transcripts selected from a group of CD40, CD80 and CD86 primary transcripts and the combinations thereof.</p>
<p>To conclude it has become inevitable to proceed with a development in the area of the related technology, considering the inadequacy of the existing solutions and the need for a formulation intended for treatment of type 1 diabetes.</p>
<p> </p>
<p><strong>Objective of the Invention</strong></p>
<p> </p>
<p>To overcome the disadvantages experienced in state of art technology;</p>
<ul>
<li>One objective of the present invention is to trigger cell repair by re-establishing the cell wall permeability of the active pancreatic beta cells.</li>
<li>One other objective of the invention is to enhance the neuro-endocrinal connection.</li>
<li>One other objective of the invention is to stimulate insulin secretion by cAMP increase.</li>
<li>One other objective of the invention is to stimulate insulin secretion by its systemic phosphodiesterase suppression capability. </li>
<li>One other objective of the invention is to reduce the tnf-alpha and interleukin-6 levels which lead to autoimmune damage, based on its immunomodulative capability.</li>
</ul>
<p>The present invention which is aimed to achieve the above-mentioned advantages, is intended for treatment of type 1 diabetes and is a formulation that is obtained by combination of the compositions selected in a single form or in combinations from a group containing; 3,7-bis(2-hydroxymethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one, 11-dioxy-methoxyfloro-hecogenin.</p>
<p> </p>
<p>Structural and characteristic properties as well as all the advantages of the invention presented herewith will be clearly understood with the detailed description provided below and thus the evaluation regarding the present invention should be based on the detailed description presented herewith.</p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p> </p>
<p>The present invention herewith discloses a formulation developed for treatment of type 1 diabetes. Referred formulation triggers cell repair by re-establishing the cell wall permeability of the active pancreatic beta cells, enhances the neuro-endocrinal connection, stimulates insulin secretion by cAMP increase, stimulates insulin secretion by its systemic phosphodiesterase suppression capability, reduces the tnf-alpha and interleukin-6 levels which lead to autoimmune damage, based on its immunomodulative capability.</p>
<p> </p>
<p>The formulation of the invention presented herewith contains; 3,7-bis(2-hydroxymethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one, 11-dioxy-methoxyfloro-hecogenin .</p>
<p> </p>
<p>The referred formulation is formed by mixing the above-mentioned components at below percentages by weight;</p>
<ul>
<li>30-70% of 3,7-bis(2-hydroxymethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one,</li>
<li>70-30% of 11-dioxy-methoxyfloro-hecogenin.</li>
</ul>
<p> </p>
<p>Components given above are obtained by combining the components from the above-mentioned group at the given range of weight ratios in a single form or in combinations thereof.</p>
<p> </p>
<p>The present invention at the same time discloses using the above-referred formulation for treatment of type 1 diabetes and manufacturing it for such purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A formulation intended for treatment of type 1 diabetes, which consists of combining the components selected from the group; 3,7-bis(2-hydroxymethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one, 11-dioxy-methoxyfloro-hecogenin in a single form or in combinations thereof.</li>
</ol>
<p> </p>
<ol>
<li>The formulation of Claim 1 which is characterized by containing 30-70% of 3,7-bis(2-hydroxymethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one by weight.</li>
</ol>
<p> </p>
<ol>
<li>The formulation of Claim 1 which is characterized by containing 70-30% of 11-dioxy-methoxyfloro-hecogenin by weight.</li>
</ol>
<p> </p>
<ol>
<li>Using the compositions obtained by selecting singly or in combination of components from the group of; 3,7-bis(2-hydroxymethyl)-8-(3-methyl-2-butene-1-yl)-4H-1-benzopyrane-4-one, 11-dioxy-methoxyfloro-hecogenin from any one as given in Claims 2-3 in manufacturing the formulation intended for treatment of type 1 diabetes. </li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>SUMMARY</strong></p>
<p> </p>
<p><strong>A FORMULATION INTENDED FOR TREATMENT OF TYPE 1 DIABETES</strong></p>
<p> </p>
<p>The present invention herewith discloses a formulation developed for treatment of type 1 diabetes. Referred formulation triggers cell repair by re-establishing the cell wall permeability of the active pancreatic beta cells, enhances the neuro-endocrinal connection, stimulates insulin secretion by cAMP increase, stimulates insulin secretion by its systemic phosphodiesterase suppression capability, reduces the tnf-alpha and interleukin-6 levels which lead to autoimmune damage, based on its immunomodulative capability.</p>
https://doi.org/10.5281/zenodo.3819133
oai:zenodo.org:3819133
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3819132
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
Insulinotrophic Interleukin-6 CAMP Beta-Islet Diabetes
AN ADJUVANT INSULINOTROPHİC TREATMENT FOR TYPE 1 DIABETES
info:eu-repo/semantics/patent
oai:zenodo.org:3819163
2020-05-13T20:20:36Z
user-darulaceze
Erdal Can Alkoclar
2020-05-10
<p> </p>
<p><strong>A COMPOSITION COMPRISING COMPONENTS THAT EXHIBIT ANTI-INFLAMMATORY ACTION FORMED FOR SUPPRESSING TYROSINE KINASE</strong></p>
<p> </p>
<p><strong>Technical Field</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the components that exhibit anti-inflammatory action formed for suppressing tyrosine kinase.</p>
<p> </p>
<p> </p>
<p><strong>State of the Art</strong></p>
<p> </p>
<p>Tyrosine kinase is an enzyme that belongs to the family of protein kinases enabling the protein phosphorylation. Since the type of amino acid that undergoes phosphorylation is tyrosine, this enzyme was given the name tyrosine kinase. Tyrosine kinase may transfer phosphate groups from ATP to the tyrosine residues in the proteins. The phosphorylation of the proteins via the kinases plays a significant role in the signal transduction mechanism. Because the signal transduction controls the functions such as the proliferation and apoptosis of the cells, the changes occurring in this mechanism play an important role in the cancer development and metastasis. Tyrosine kinases are classified into 2 groups according to the location where they are present, namely the membrane-located and cytoplasmic.</p>
<p>According to the state of the art, the invention no. WO 2001/007440 entitled "Imidazoles and triazoles as anti-inflammatory agents" relates to the compounds of formula (I) which are useful for treating or preventing inflammatory and immune cell-mediated diseases.</p>
<p>Further, the invention no. EP1382339B1 entitled "Compositions containing pyrrolo[2,3-d]pyrimidine derivatives" relates to the combinations of one or more anti-inflammatory agent and a compound of the following formula wherein R1, R2 and R3 are as defined above. These are useful therapy as immunosuppressive agents for organ transplants, xeno transplantation, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type I diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases.</p>
<p>Further, the invention no. EP1781299B1 entitled "Anti-inflammatory agents" provides compounds, compositions and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, which are 3-aminocaprolactam derivatives, for the preparation of a medicament intended to treat an inflammatory disorder wherein X is -CO-Y-(R1)n or SO2-Y-(R1)n; and Y is a cycloalkyl or polycycloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or is a cycloalkenyl or polycycloalkenyl group.</p>
<p>Further, the invention no. EP2205620B1 entitled "Amorphous form of (11beta,16alpha)-9-fluoro-11-hydroxy-16,17-[(1-methylethyliden)bis(oxy)]-21-[[4- [(nitroxy)methyl]benzoyl]oxy]-pregna-1,4-dien-3,20-dione" relates to the technical field of anti-inflammatory compounds, specifically those of a steroid nature, in particular to a new amorphous form of a nitrooxy derivative of a corticosteroid, its pharmaceutical formulations and its use in the treatment or prevention of diseases or symptoms of the skin or mucous membranes.</p>
<p>As a result, the presence of the need for a composition for suppressing tyrosine kinase and the inadequacy of the existing solutions have made it necessary to perform an improvement in the relevant art.</p>
<p> </p>
<p> </p>
<p><strong>Object of the Invention</strong></p>
<p> </p>
<p>In order to eliminate the disadvantages of the state of the art, an object of the invention is to enable the suppression of Src tyrosine kinase.</p>
<p>Another object of the invention is to enable the suppression of cox-2.</p>
<p>In order to achieve the aforesaid advantages, the invention is a composition for suppressing tyrosine kinase, said composition being obtained by the components selected from the group comprising (4E)-1-(2,2-hydroxyphenyl)-3-(3,4-dichlorophenyl)-4-propen-2-one, 99-1% of (2E)-2-(2,3-epoxyphenyl)-46-(2,2-dihydroxyphenyl)-6-propen-2-one that are used individually or in combinations.</p>
<p> </p>
<p>The structural and characteristic features and all the advantages of the invention will become more clearly understood from the detailed description provided below and therefore, the evaluation must be made taking this detailed description into consideration.</p>
<p> </p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p> </p>
<p>The invention is a composition comprising the components that exhibit anti-inflammatory action formed for suppressing tyrosine kinase. The composition according to the invention enables the suppression of Src tyrosine kinase and the suppression of cox-2.</p>
<p> </p>
<p>The composition according to the invention contains (4E)-1-(2,2-hydroxyphenyl)-3-(3,4-dichlorophenyl)-4-propen-2-one, 99-1% of (2E)-2-(2,3-epoxyphenyl)-46-(2,2-dihydroxyphenyl)-6-propen-2-one.</p>
<p> </p>
<p>Said composition is obtained by a mixture of the aforesaid components according to the following ratios by weight:</p>
<p>1-99% (4E)-1-(2,2-hydroxyphenyl)-3-(3,4-dichlorophenyl)-4-propen-2-one, </p>
<p>99-1% (2E)-2-(2,3-epoxyphenyl)-46-(2,2-dihydroxyphenyl)-6-propen-2-one. </p>
<p>The composition is obtained from the aforesaid components selected from the aforesaid group and used according to the mentioned weight ratio ranges individually or in combinations.</p>
<p> </p>
<p>Said invention also encompasses the use of said composition for suppressing tyrosine kinase and the manufacture thereof for this purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A composition for suppressing tyrosine kinase, said composition being obtained by the components selected from the group comprising (4E)-1-(2,2-hydroxyphenyl)-3-(3,4-dichlorophenyl)-4-propen-2-one, 99-1% of (2E)-2-(2,3-epoxyphenyl)-46-(2,2-dihydroxyphenyl)-6-propen-2-one that are used individually or in combinations.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 1-99% by weight (4E)-1-(2,2-hydroxyphenyl)-3-(3,4-dichlorophenyl)-4-propen-2-one.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 99-1% by weight (2E)-2-(2,3-epoxyphenyl)-46-(2,2-dihydroxyphenyl)-6-propen-2-one.</li>
</ol>
<p> </p>
<ol>
<li>Use of the components according to Claims 1 to 3 obtained individually or in combinations selected from the group consisting of (4E)-1-(2,2-hydroxyphenyl)-3-(3,4-dichlorophenyl)-4-propen-2-one, 99-1% of (2E)-2-(2,3-epoxyphenyl)-46-(2,2-dihydroxyphenyl)-6-propen-2-one for the manufacture of a composition for suppressing tyrosine kinase.</li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>ABSTRACT</strong></p>
<p> </p>
<p><strong>A COMPOSITION COMPRISING COMPONENTS THAT EXHIBIT ANTI-INFLAMMATORY ACTION FORMED FOR SUPPRESSING TYROSINE KINASE</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the components that exhibit anti-inflammatory action formed for suppressing tyrosine kinase</p>
https://doi.org/10.5281/zenodo.3819163
oai:zenodo.org:3819163
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3819162
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
Tyrosine Kinase Anti-Inflammatory
A COMPOSITION COMPRISING COMPONENTS THAT EXHIBIT ANTI-INFLAMMATORY ACTION FORMED FOR SUPPRESSING TYROSINE KINASE
info:eu-repo/semantics/patent
oai:zenodo.org:3819149
2020-05-13T20:20:35Z
user-darulaceze
Erdal Can Alkoclar
2020-05-10
<p> </p>
<p><strong>Technical Field</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the anti-viral components formed for suppressing the DNA polymerase.</p>
<p> </p>
<p> </p>
<p><strong>State of the Art</strong></p>
<p> </p>
<p>DNA polymerase is an enzyme that enables the duplication of DNA. These enzymes use a DNA strand as a template, which they read and along which they catalyze the polymerization of deoxyribonucleotides. Newly polymerized molecule is complementary for the template strand and has the same structure as the previous companion of the template strand. DNA polymerase is regarded as a holoenzyme, because it requires the magnesium ion in order to perform the correct function. In the absence of the magnesium ion, it is referred to as the apoenzyme.</p>
<p>DNA polymerase binds to a single-stranded DNA to initiate the duplication of DNA. Unlike RNA polymerase, DNA polymerase cannot extend the new strand it has synthesized beginning from only the nucleotides, but it may extend an existing DNA chain. Therefore, it needs the auxiliary enzymes for the initiation of the chain synthesis. Some types of DNA polymerases have an exonuclease feature that enables them to recognize the nucleotides that they have added erroneously and to repair these.</p>
<p>According to the state of the art, the invention no. WO 1999/009031 entitled "Nucleoside analogues, such as antivirals including inhibitors of retroviral reverse transcriptase and the DNA polymerase of hepatitis B virus (HBV)" with classification "C07D 473/00" relates to a compound of the formula I and pharmaceutically acceptable salts thereof, wherein nuc is the residue of a nucleoside analogue bonded through its single hydroxy group on the cyclic or acyclic saccharide moiety; R1 is selected from hydroxy, amino or carboxy optionally having esterified/amide bonded thereon, a C4-C22 saturated or unsaturated, optionally substituted fatty acid or alcohol, or an aliphatic L-amino acid; R2 is the residue of an aliphatic L-amino acid; L1 is a trifunctional linker group; L2 is absent or a difunctional linker group.</p>
<p>Further, the invention no. EP1234024B1 entitled “Artificial chromosome constructs containing nucleic acid sequences capable of directing the formation of a recombinant RNA-virus" relates to methods of preparing a DNA comprising steps wherein (a) a DNA comprising a full length copy of the genomic RNA (gRNA) or a RNA virus; or (b) a DNA comprising one or several fragments of a gRNA or an RNA virus, which fragments code for a RNA dependent RNA polymerase and at least one structural or non-structural protein; or (c) a DNA having a homology of at least 60% to the sequences of (a) or (b) is cloned into a bacterial artificial chromosome (BAC).</p>
<p>Further, the invention no. TR2001/01093 entitled "Performing the reverse transcription at elevated temperature by the use of the mutant DNA polymerases” relates to the improved reverse transcription methods particularly in a magnesium ion buffer, by the use of modified thermostable DNA polymerases. These methods are useful especially for the combined reverse transcription/amplification reactions.</p>
<p>As a result, the presence of the need for a composition comprising the anti-viral components formed for suppressing the DNA polymerase and the inadequacy of the existing solutions have made it necessary to perform an improvement in the relevant art.</p>
<p> </p>
<p> </p>
<p><strong>Object of the Invention</strong></p>
<p> </p>
<p>In order to eliminate the disadvantages of the state of the art, an object of the invention is to enable the suppression of the DNA polymerase.</p>
<p> </p>
<p>Another object of the invention is to enable the suppression of the reverse transcriptase.</p>
<p> </p>
<p>In order to achieve the aforesaid advantages, the invention is a composition for suppressing the DNA polymerase, said composition being obtained by the components selected from the group comprising 2,3,9,10,11,12-hexahydro-8R-methoxy-2,4-dimethyl-1-oxo-9S,12R-epoxy-2H-diindol[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]benzodiazokin-4-carboxylic acid methyl ester, 2,3,9,10,11,12-hexahydro-10R-methoxy-3,3-trimethyl-7-oxo-9S,12R-epoxy-4H-tetrafluoro[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]octadien-8-carboxylic acid phenyl ester that are used individually or in combinations.</p>
<p> </p>
<p>The structural and characteristic features and all the advantages of the invention will become more clearly understood from the detailed description provided below and therefore, the evaluation must be made taking this detailed description into consideration.</p>
<p> </p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p> </p>
<p>The invention is a composition comprising the anti-viral components formed for suppressing the DNA polymerase. The composition according to the invention enables the suppression of the DNA polymerase and the suppression of the reverse transcriptase.</p>
<p> </p>
<p>The composition according to the invention contains 2,3,9,10,11,12-hexahydro-8R-methoxy-2,4-dimethyl-1-oxo-9S,12R-epoxy-2H-diindol[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]benzodiazokin-4-carboxylic acid methyl ester, 2,3,9,10,11,12-hexahydro-10R-methoxy-3,3-trimethyl-7-oxo-9S,12R-epoxy-4H-tetrafluoro[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]octadien-8-carboxylic acid phenyl ester.</p>
<p> </p>
<p>Said composition is obtained by a mixture of the aforesaid components according to the following ratios by weight:</p>
<p> </p>
<p>1-99% 2,3,9,10,11,12-hexahydro-8R-methoxy-2,4-dimethyl-1-oxo-9S,12R-epoxy-2H-diindol[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]benzodiazokin-4-carboxylic acid methyl ester</p>
<p>and<br>
99-1% 2,3,9,10,11,12-hexahydro-10R-methoxy-3,3-trimethyl-7-oxo-9S,12R-epoxy-4H-tetrafluoro[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]octadien-8-carboxylic acid phenyl ester</p>
<p> </p>
<p>The composition is obtained from the aforesaid components selected from the aforesaid group and used according to the mentioned weight ratio ranges individually or in combinations.</p>
<p> </p>
<p>Said invention also encompasses the use of said composition for suppressing the DNA polymerase and the manufacture thereof for this purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A composition for suppressing the DNA polymerase, said composition being obtained by the components selected from the group comprising 2,3,9,10,11,12-hexahydro-8R-methoxy-2,4-dimethyl-1-oxo-9S,12R-epoxy-2H-diindol[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]benzodiazokin-4-carboxylic acid methyl ester, 2,3,9,10,11,12-hexahydro-10R-methoxy-3,3-trimethyl-7-oxo-9S,12R-epoxy-4H-tetrafluoro[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]octadien-8-carboxylic acid phenyl ester that are used individually or in combinations.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 1-99% by weight 2,3,9,10,11,12-hexahydro-8R-methoxy-2,4-dimethyl-1-oxo-9S,12R-epoxy-2H-diindol[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]benzodiazokin-4-carboxylic acid methyl ester.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 99-1% by weight 2,3,9,10,11,12-hexahydro-10R-methoxy-3,3-trimethyl-7-oxo-9S,12R-epoxy-4H-tetrafluoro[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]octadien-8-carboxylic acid phenyl ester.</li>
</ol>
<p> </p>
<ol>
<li>Use of the components according to Claims 1 to 3 obtained individually or in combinations selected from the group consisting of 2,3,9,10,11,12-hexahydro-8R-methoxy-2,4-dimethyl-1-oxo-9S,12R-epoxy-2H-diindol[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]benzodiazokin-4-carboxylic acid methyl ester, 2,3,9,10,11,12-hexahydro-10R-methoxy-3,3-trimethyl-7-oxo-9S,12R-epoxy-4H-tetrafluoro[1,2,3-fg:3’,2’,1’-kl]pyrrolo[3,4-i][1,6]octadien-8-carboxylic acid phenyl ester for the manufacture of a composition for suppressing the DNA polymerase. </li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>ABSTRACT</strong></p>
<p> </p>
<p><strong>A COMPOSITION COMPRISING THE ANTI-VIRAL COMPONENTS FORMED FOR SUPPRESSING DNA POLYMERASE</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the anti-viral components formed for suppressing the DNA polymerase.</p>
https://doi.org/10.5281/zenodo.3819149
oai:zenodo.org:3819149
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3819148
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
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DNA Polymerase Antiviral
A COMPOSITION COMPRISING THE ANTI-VIRAL COMPONENTS FORMED FOR SUPPRESSING DNA POLYMERASE
info:eu-repo/semantics/patent
oai:zenodo.org:3818454
2020-05-13T08:20:31Z
user-darulaceze
Erdal Can Alkoclar
2020-05-09
<p> </p>
<p><strong>Field of Invention</strong></p>
<p> </p>
<p>The present invention herewith discloses an anti-carcinogenic adjuvant formulation developed to suppress G1/S phase-specific protein, cycline D1 and anti-apoptotic Bcl-xl protein expression.</p>
<p> </p>
<p><strong>Background of the Related Technology</strong></p>
<p> </p>
<p>At present while it is known that the term Chemotherapy means “treatment with medication”, it is used more specifically to refer to a treatment where cancer drugs, working mainly on cancer cells, are used. Thus, the drugs used for such purposes are called “anti-cancer” drugs. The objective of the chemotherapy may vary with the type of the cancer under treatment. Main objective is to treat the cancer. Cancer is deemed to be treated once all traces of cancer cells are removed. Controlling cancer is accepted to be the process, where the spreading of cancer in general is prevented and its growth is slowed, and thus the cancer is put under control. Its main objective is to eliminate the symptoms developed with cancer. Certain chemotherapy treatments mainly concentrate on eliminating or reducing pain and similar symptoms, to improve the life quality of the patient. It may not be possible to get the desired benefit from the chemotherapy medication all the time. If it is not possible to destroy the cancer tumors by treatment or if it is too late in treatment, the cancer cells may spread to the whole body by blood vessels or lymphatic system. This will lead to a condition called metastasis.</p>
<p> </p>
<p>In state of art technology, invention no "WO 1999/031140" , with title "Treatment with Anti-ErbB2 antibodies" and under classification number " C07K 16/32 " discloses methods for treatment of disorders distinguished by extreme expression of ErB2. More specifically the referred invention discloses methods for treatment of cancer, which is suspected that the cancer is responsible from extreme expression of ErbB2 and also is related to using the invention in treatment of the cancer in combination with a chemo-therapy agent that is different from anthracycline, like epirubicin.</p>
<p>Again invention no “WO 1999/061444" , with title "Pyrimidines and Bicyclic 3,4-dihydropyrimidines as Cell Reproduction Inhibitors” and under classification number " C07D 487/04 " discloses methods for providing bicyclic heterocylics that are useful in treatment of diseases related to cell reproduction like cancer, restenosis as well as angiogenesis and atherosclerosis. We have invented a group of bicyclic compounds that are effective inhibitors of kinases dependent on cycline, kinases mediated by growth factor and kinases which are not receptors. These compounds can by synthesized easily and can be administered to the patient using various methods, including orally administered forms and have sufficient biological suitability for clinical use. The referred invention consists of the compound with formula (I) where Z is N or GH; G is N or CH; W is NH, S,SO or SO<sub>2</sub>; R1 is phenyl and substituted phenyl; R2 is alkyl and cycloalkyl; R3 is alkyl and hydrogen; R8 and R9 are hydrogen and alkyl as well as pharmaceutically acceptable salts thereof. The referred invention is also related to providing a pharmaceutical formulation that contains the compound with Formula (I) combined with a pharmaceutically acceptable carrier, diluting agent or excipient.</p>
<p>Again invention no "EP1423105B1" , with title "Combinations of Other Agents Used Against DMXAA and Cancer" and under classification number “A61K 31/19 " discloses a synergistic combination formed with a compound selected from platinum compounds, vinca alkaloids, alkylation agents, anthracyclines, topoisomerase I inhibitors, anti-metabolites and topoisomerase II inhibitors, which have act against 5,6-dimethylxanthenone-4-acetic acid (DMXAA) and tumors. The referred invention specifically discloses methods for using such combinations in treatment of cancer and pharmaceutical compounds that contain the combinations referred herewith.</p>
<p>To conclude it has become inevitable to proceed with a development in the area of the related technology, considering the inadequacy of the existing solutions and the need for an anti-carcinogenic adjuvant formulation that suppresses G1/S phase-specific protein, cycline D1 and anti-apoptotic Bcl-xl protein expression.</p>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>Objective of the Invention</strong></p>
<p> </p>
<p>To overcome the disadvantages experienced in state of art technology;</p>
<ul>
<li>One objective of the invention is to suppress G1/S phase-specific protein expression.</li>
<li>One other objective of the invention is to suppress cycline D1 function and expression.</li>
<li>One other objective of the invention is to suppress anti-apoptopic Bcl-xl protein function.</li>
<li>One other objective of the invention is to, increase Bax expression.</li>
</ul>
<p> </p>
<p>The present invention which is aimed to achieve the above-mentioned advantages, is an anti-carcinogenic adjuvant formulation that suppresses G1/S phase-specific protein, cycline D1 and anti-apoptotic Bcl-xl protein expression and is a formulation that is obtained by combination of the compositions selected in a single form or in combinations from a group containing; 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(dihydroxyethyl)oxane-3,5,7-trione, 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(trihydroxymethyl)oxane-3,5,7diol.</p>
<p> </p>
<p>Structural and characteristic properties as well as all the advantages of the invention presented herewith will be clearly understood with the detailed description provided below and thus the evaluation regarding the present invention should be based on the detailed description presented herewith.</p>
<p> </p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p> </p>
<p>The present invention herewith discloses an anti-carcinogenic adjuvant formulation developed to suppress G1/S phase-specific protein, cycline D1 and anti-apoptotic Bcl-xl protein expression. Referred formulation suppresses G1/S phase-specific protein expression, suppresses cycline D1 function and expression, suppresses anti-apoptopic Bcl-xl protein function and increases Bax expression.</p>
<p> </p>
<p> </p>
<p>The formulation of the invention presented herewith contains; 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(dihydroxyethyl)oxane-3,5,7-trione, 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(trihydroxymethyl)oxane-3,5,7diol .</p>
<p> </p>
<p>The referred formulation is formed by mixing the above-mentioned components at below percentages by weight;</p>
<ul>
<li>22-78% of 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(dihydroxyethyl)oxane-3,5,7-trione, </li>
<li>78-22% of 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(trihydroxymethyl)oxane-3,5,7-diol.</li>
</ul>
<p> </p>
<p>Components given above are obtained by combining the components from the above-mentioned group at the given range of weight ratios in a single form or in combinations thereof.</p>
<p> </p>
<p>The present invention at the same time discloses using the above-referred formulation to suppress G1/S phase-specific protein, cycline D1 and anti-apoptotic Bcl-xl protein expression and manufacturing it for such purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>An anti-carcinogenic adjuvant formulation that suppresses G1/S phase-specific protein, cycline D1 and anti-apoptotic Bcl-xl protein expression, and which consists of combining the components selected from the group; 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(dihydroxyethyl)oxane-3,5,7-trione, 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(trihydroxymethyl)oxane-3,5,7-diol in a single form or in combinations thereof.</li>
</ol>
<p> </p>
<ol>
<li>The formulation of Claim 1 which is characterized by containing 22-78% of 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(dihydroxyethyl)oxane-3,5,7-trione by weight.</li>
</ol>
<p> </p>
<ol>
<li>The formulation of Claim 1 which is characterized by containing 78-22% of 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(trihydroxymethyl)oxane-3,5,7-diol by weight.</li>
</ol>
<p> </p>
<ol>
<li>Using the compositions obtained by selecting singly or in combination of components from the group of; 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(dihydroxyethyl)oxane-3,5,7-trione, 1H-cyclopenta[a]phenylanthroyl-4-yl]oxy]-6-(dimethoxyethyl)oxane-3-yl]oxy-8-(trihydroxymethyl)oxane-3,5,7-diol from any one as given in Claims 2-3 in manufacturing an anti-carcinogenic adjuvant formulation suppresses G1/S phase-specific protein, cycline D1 and anti-apoptotic Bcl-xl protein expression</li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>SUMMARY</strong></p>
<p> </p>
<p><strong>AN ANTI-CARCINOGENIC ADJUVANT FORMULATION THAT FUNCTIONS BY SUPPRESSING G1/S PHASE SPECIFIC PROTEIN, CYCLINE D1 AND ANTI-APOPTOTIC BCL-XL PROTEIN EXPRESSION</strong></p>
<p> </p>
<p>The present invention herewith discloses an anti-carcinogenic adjuvant formulation developed to suppress G1/S phase-specific protein, cycline D1 and anti-apoptotic Bcl-xl protein expression. Referred formulation suppresses G1/S phase-specific protein expression, suppresses cycline D1 function and expression, suppresses anti-apoptopic Bcl-xl protein function and increases Bax expression</p>
<p> </p>
https://doi.org/10.5281/zenodo.3818454
oai:zenodo.org:3818454
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3818453
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
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G1/S Phase-Specific Protein Cyclin D1 BCL-XL
AN ANTI-CARCINOGENIC ADJUVANT FORMULATION THAT FUNCTIONS BY SUPPRESSING G1/S PHASE SPECIFIC PROTEIN, CYCLINE D1 AND ANTI-APOPTOTIC BCL-XL PROTEIN EXPRESSION
info:eu-repo/semantics/patent
oai:zenodo.org:3571773
2020-01-20T15:29:44Z
user-darulaceze
Alkoclar Erdal Can
2019-12-12
<p>A Formulation that consists immunomodulatory Ketosterone derivatives which possess IL-6 , IL-4 TNF-A and IgE Supressive Properties.</p>
<p>Formulation exerts simultaneous ImmunoModulatory and Myotrophic Features thus Providing a Dual Beneficial Effect for the Treatment of Autoimmune Disorders related Symptoms</p>
https://doi.org/10.5281/zenodo.3571773
oai:zenodo.org:3571773
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3571772
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
Autoimmune
An ImmunoModulatory Formulation for the Treatment of Autoimmune Disorders
info:eu-repo/semantics/patent
oai:zenodo.org:3818394
2020-05-13T20:20:36Z
user-darulaceze
Erdal Can Alkoclar
2020-05-09
<p>The present invention herewith is related to a formulation developed for treatment of Crohn’s Disease</p>
<p> </p>
<p><strong>Background of the Related Technology</strong></p>
<p>Today Crohn’s Disease (Latin Enterocolitis regionalis) is known to be a chronic and inflammatory intestinal disease. It manifests itself with intermittent inflammations at one or more different places in any section of the digestive tract starting from the mouth up to the anus. It is not proven to be infectious. Together with ulcerative colitis, which is another chronic inflammatory intestinal disease, both form the main constituents of this group. Every year this disease hits about 5 to 7 people among 100,000. The frequency of the disease increase as one moves up to Northern Latitudes. It is observed more at ages 10 and 20 and then between 45 and 65. However any person of any age can suffer from this disease.</p>
<p>The invention presented herewith with no “WO 1997/023199", with title “Oral Pharmaceutic Composition for Intestinal Diseases” and under classification number “A61K 9/16", is related to a pharmaceutic composition and method that is capable of different releasing capacities for treatment of inflammatory intestinal diseases (IID) like Crohn’s Disease and ulcerative colitis, where the compositions referred contain 5-aminosalicylic acid (5-ASA) as an active ingredient and is adapted to display various and targeted release capability to obtain a clinically important localized impact profile of 5-ASA, by releasing an appropriate quantity of 5-ASA both in small intestine and large intestine.</p>
<p>Again the invention presented herewith with no “WO 1999/020261", with title “Materials and Methods for Prevention and Treatment of Inflammation of the Mucosal Tissue” and under classification number “A61K 31/70", is related to the materials and methods useful in preventing and treating non-spreading mucosal infections caused by fungi. On the other hand, the present invention is related to materials and methods intended for prevention and treatment of mucosal inflammations caused by non-spreading fungi as with chronic middle ear inflammation, chronic colitis and Crohn’s Disease. Furthermore, the present invention is also related to materials and methods useful in prevention and treatment of chronic asthma symptoms.</p>
<p>Again the invention presented herewith with no "EP1874273B1", with title "Gastro-resistant Pharmaceutical Formulations Containing Rifaximin” and under classification number "A61K 9/16", is related to pharmaceutical formulations containing rifaximin formed into micro granules that are developed to become gastro-resistant substances via a polymer that dissolves at pH values between 5.0 and 7.5 but not at pH values between 1.5 and 4.0, and also is related to preparation of these formulations and using them in appropriate medical preparates for treatment of inflammatory intestinal diseases (IID) and principally in treatment of Crohn’s Disease.</p>
<p>Again the invention presented herewith with no "EP2278958B1", with title "Orally Administered Corticosteroid Compositions” and under classification number "A61K 9/48", is related to providing an orally administered release composition that includes a corticosteroid medicine and which has a continuously released composition included in a capsule that is processed; and thus the continuously released composition that is administered orally is mainly released from the capsule in the intestinal tract. The present invention also provides a medical release composition that helps to diffuse the corticosteroid medicine into the intestinal tract and includes the following: (a) a corticosteroid medicine, an ethyl cellulose material that contains an alkali and a continuous release component that contains an acid, and (b) a delayed release component that mainly prevents continuous release until the composition reaches intestinal tract after it is administered orally. Compositions of the present invention are beneficial in treatment of inflammatory diseases and glomerulonephritis which are related to the digestive track, like Crohn’s Disease and ulcerative colitis.</p>
<p>To conclude it has become inevitable to proceed with a development in the area of the related technology, considering the inadequacy of the existing solutions and the need for a formulation intended for treatment of Crohn’s Disease.</p>
<p> </p>
<p> </p>
<p><strong>Objective of the Invention</strong></p>
<p>To overcome the disadvantages referred in the Background of the Related Technology,</p>
<ul>
<li>One objective of the present invention is, cox-2 expression suppression;</li>
<li>One other objective of the invention is tnf-alpha expression suppression;</li>
<li>One other objective of the invention is fmo3 expression suppression;</li>
<li>One other objective of the invention is nf-kappaB expression suppression;</li>
<li>One other objective of the invention is its capability of suppressing dna polymerase;</li>
<li>One other objective of the invention is its capability of suppressing ribonucleotide reductase.</li>
</ul>
<p>The present invention, which is aimed to achieve the above-mentioned advantages, is intended for treatment of Crohn’s Disease and is a formulation that is obtained by combination of the compositions selected in a single form or in combinations from a group containing; 7-oxo-(3β,7B,25R)-spirost-5-ene-3-trione, (24R)-spirost-5-ene-3β,7β,10α-diol, 7-beta-glucopyranoside, 3,5-bis-alpha-L-ramnopyranosyl)-(16,20)-beta-D-methoxypyranosite.</p>
<p> </p>
<p>Structural and characteristic properties as well as all the advantages of the invention presented herewith will be clearly understood with the detailed description provided below and thus the evaluation regarding the present invention should be based on the detailed description presented herewith.</p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p>The present invention is related to a formulation developed for treatment of Crohn’s Disease. The referred formulation, suppresses cox-2 expression, suppresses tnf-alpha expression, suppresses fmo3 expression, suppresses nf-kappaB expression, displays capability of suppressing dna polymerase, displays capability of suppressing ribonucleotide reductase.</p>
<p> </p>
<p>Cox-2 is an enzyme responsible for pain. Cyclooxygenase (cox) enzymes are enzymes responsible from formation of prostaglandin and eicosanoids from intracellular arachidonic acid.</p>
<p> </p>
<p>Tumor necrosis factor (TNF), is a cytokine that is secreted by various types of cells and manages lysis of cancer cells. It is a glycoprotein hormone with 185 amino acids, but some cells may secrete longer or shorter isoforms of the hormone. It is encoded on 7<sup>th</sup> chromosome of humans. It has two forms: 1. TNF alpha (TNFα, <em>cachectin</em>/ <em>cachexin</em>), 2. TNF beta (TNFβ, <em>lymphotoxin</em>). Genes encoding both are located on MHC. TNFα, is produced by macrophages and some other cells. On the other hand TNFβ is produced by T cell lymphocytes.</p>
<p> </p>
<p>On the other hand NF-kappa B (NF-κB, Nuclear Factor kappa B) is a transcription factor found in all types of cells. It is in an inactive form inside the cytoplasm. When it becomes active, it is transmitted inside the nucleus. There are five types of this factor: NF-κB1, NF-κB2, RelA (p65), RelB and c-Rel. It is considered that NF-kappa B plays a role in some autoimmune diseases (e.g. ulcerative colitis, Crohn’s Disease).</p>
<p> </p>
<p>The formulation related to the present invention contains; 7-oxo-(3β,7B,25R)-spirost-5-ene-3-trione, (24R)-spirost-5-ene-3β,7β,10α-diol, 7-beta-glucopyranoside, 3,5-bis-alpha-L-ramnopyranosyl)-(16,20)-beta-D-methoxypyranosite .</p>
<p> </p>
<p>The referred formulation is formed by mixing the above-mentioned components at below percentages by weight;</p>
<ul>
<li>13-15% of 7-oxo-(3β,7B,25R)-spirost-5-ene-3-trione, </li>
<li>26-12% of (24R)-spirost-5-ene-3β,7β,10α-diol, </li>
<li>11-13% of 7-beta-glucopyranoside, </li>
<li>50-60% of 3,5-bis-alpha-L-ramnopyranosyl)-(16,20)-beta-D-methoxypyranosite. </li>
</ul>
<p> </p>
<p>Components given above are obtained by combining the components from the above-mentioned group at the given range of weight ratios in a single form or in combinations thereof.</p>
<p> </p>
<p>The present invention at the same time is related to using the above-referred formulation for treatment of Crohn’s Disease and manufacturing it for such purpose</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A formulation intended for treatment of Crohn’s Disease, which consists of combining the components selected from the group; 7-oxo-(3β,7B,25R)-spirost-5-ene-3-trione, (24R)-spirost-5-ene-3β,7β,10α-diol, 7-beta-gluco-pyranoside, 3,5-bis-alpha-L-ramnopyranosyl)-(16,20)-beta-D-methoxypyra-nosite in a single form or in combinations thereof.</li>
<li>The formulation of Claim 1 which is characterized by containing 13-15% of 7-oxo-(3β,7B,25R)-spirost-5-ene-3-trione by weight.</li>
<li>The formulation of Claim 1 which is characterized by containing 26-12% of (24R)-spirost-5-ene-3β,7β,10α-diol by weight.</li>
<li>The formulation of Claim 1 which is characterized by containing 11-13% of 7-beta-glucopyranoside by weight.</li>
<li>The formulation of Claim 1 which is characterized by containing 50-60% of 3,5-bis-alpha-L-ramnopyranosyl)-(16,20)-beta-D-methoxypyranosite by weight.</li>
<li>Using the compositions obtained by selecting singly or in combination of components from the group of; 7-oxo-(3β,7B,25R)-spirost-5-ene-3-trione, (24R)-spirost-5-ene-3β,7β,10α-diol, 7-beta-glucopyranoside, 3,5-bis-alpha-L-ramnopyranosyl)-(16,20)-beta-D-methoxypyranosite from any one as given in Claims 2-5 in manufacturing the formulation intended for treatment of Crohn’s Disease </li>
</ol>
https://doi.org/10.5281/zenodo.3818394
oai:zenodo.org:3818394
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3818393
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
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Nf-Kappa B TNF-A Immunomodulation TNFB
A FORMULATION INTENDED FOR TREATMENT OF CROHN'S DISEASE
info:eu-repo/semantics/article
oai:zenodo.org:3819157
2020-05-13T08:20:32Z
user-darulaceze
Erdal Can Alkoclar
2020-05-10
<p> </p>
<p><strong>Technical Field</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the components that exhibit anti-obesity action formed for suppressing 5-lipooxygenase.</p>
<p> </p>
<p> </p>
<p><strong>State of the Art</strong></p>
<p>Lipooxygenases are the components for the formation of leukotrienes. Cyclooxygenase forms the prostaglandins (available in many cells) by a process that may be inhibited by the non-steroidal anti-inflammatory agents. Prostacyclin is generated by the capillary endothelium and vascular wall and thromboxane is generated by the thrombocytes.</p>
<p>According to the state of the art, the invention no. WO 01/42195 A1 entitled "Process for the preparation of arylethanolamine derivatives with anti-obesity and anti-diabetic properties” relates to a method for the preparation of certain biaryl derivatives.</p>
<p>Further, the invention no. TR2000/02529 with the classification "A61K 37/48" entitled "Process for making 5-lipooxygenase inhibitors having varied ring systems" describes a novel process intermediate, tetrahydro-4-[3-(4 fluorophenyl)thio]phenyl-2H-pyran-4-carboxamide, of the formula, as well as its use in a process of preparing 5-lipooxygenase inhibitors of the formula, which comprises establishing a reaction mixture consisting of: CONH2 and an electron deficient monocyclic or benzo-fused bicyclic N-heterocycle containing two nitrogen atoms of the formula in an aprotic solvent; in the presence of a carbonate of the formula: (M)2-CO3 where M is an alkali metal, Group 1/la element, selected from the group consisting of lithium, Li; sodium, Na; potassium, K; rubidium, Rb; and cesium, Cs; followed by heating of said reaction mixture under a nitrogen atmosphere, whereby there is produced the desired compound of the above-recited formula.</p>
<p>Further, the invention no. EP1497294B1 entitled "1,2,3,4,7,8-hexahydro-6H-[1,4]diazepino[6,7,1-IJ]quinoline derivatives as antipsychotic and anti-obesity agents" provides compounds of formula I or a pharmaceutically acceptable salt thereof where R1 through R7 are as defined herein. The compounds of formula I are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.</p>
<p>As a result, the presence of the need for a composition for suppressing 5-lipooxygenase and the inadequacy of the existing solutions have made it necessary to perform an improvement in the relevant art.</p>
<p> </p>
<p> </p>
<p><strong>Object of the Invention</strong></p>
<p> </p>
<p>In order to eliminate the disadvantages of the state of the art, an object of the invention is to enable the suppression of 5-lipooxygenase.</p>
<p> </p>
<p>Another object of the invention is to provide an increase in the expression of thermogenin.</p>
<p> </p>
<p>In order to achieve the aforesaid advantages, the invention is a composition for suppressing 5-lipooxygenase, said composition being obtained by the components selected from the group comprising (4E)-1-(2,2-methoxyphenyl)-3-(3,4-trihydroxyphenyl)-4-propen-2-one, (2E)-1-(2,3-epoxyphenyl)-6-(2,2-dihydroxyphenyl)-6-propen-2-one that are used individually or in combinations.</p>
<p> </p>
<p>The structural and characteristic features and all the advantages of the invention will become more clearly understood from the detailed description provided below and therefore, the evaluation must be made taking this detailed description into consideration.</p>
<p> </p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p> </p>
<p>The invention is a composition comprising the components that exhibit anti-obesity action formed for suppressing 5-lipooxygenase. The composition according to the invention enables the suppression of 5-lipooxygenase and an increase in the expression of thermogenin.</p>
<p> </p>
<p>The composition according to the invention contains (4E)-1-(2,2-metoxyphenyl)-3-(3,4-trihydroxyphenyl)-4-propen-2-one, (2E)-1-(2,3-epoxyphenyl)-6-(2,2-dihydroxyphenyl)-6-propen-2-one.</p>
<p> </p>
<p>Said composition is obtained by a mixture of the aforesaid components according to the following ratios by weight:</p>
<p>1-99% (4E)-1-(2,2-metoxyphenyl)-3-(3,4-trihydroxyphenyl)-4-propen-2-one, </p>
<p>99-1% (2E)-1-(2,3-epoxyphenyl)-6-(2,2-dihydroxyphenyl)-6-propen-2-one. </p>
<p>The composition is obtained from the aforesaid components selected from the aforesaid group and used according to the mentioned weight ratio ranges individually or in combinations.</p>
<p> </p>
<p>Said invention also encompasses the use of said composition for suppressing 5-lipooxygenase and the manufacture thereof for this purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A composition for suppressing 5-lipooxygenase, said composition being obtained by the components selected from the group comprising (4E)-1-(2,2-methoxyphenyl)-3-(3,4-trihydroxyphenyl)-4-propen-2-one, (2E)-1-(2,3-epoxyphenyl)-6-(2,2-dihydroxyphenyl)-6-propen-2-one that are used individually or in combinations.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 1-99% by weight (4E)-1-(2,2-metoxyphenyl)-3-(3,4-trihydroxyphenyl)-4-propen-2-one.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 99-1% by weight (2E)-1-(2,3-epoxyphenyl)-6-(2,2-dihydroxyphenyl)-6-propen-2-one.</li>
</ol>
<p> </p>
<ol>
<li>Use of the components according to Claims 1 to 3 obtained individually or in combinations selected from the group consisting of (4E)-1-(2,2-metoxyphenyl)-3-(3,4-trihydroxyphenyl)-4-propen-2-one, (2E)-1-(2,3-epoxyphenyl)-6-(2,2-dihydroxyphenyl)-6-propen-2-one for the manufacture of a composition for suppressing 5-lipooxygenase.</li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>ABSTRACT</strong></p>
<p> </p>
<p><strong>A COMPOSITION COMPRISING COMPONENTS THAT EXHIBIT ANTI-OBESITY ACTION FORMED FOR SUPPRESSING 5-LIPOOXYGENASE</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the components that exhibit anti-obesity action formed for suppressing 5-lipooxygenase.</p>
https://doi.org/10.5281/zenodo.3819157
oai:zenodo.org:3819157
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3819156
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
5-Lipooxygenase Anti-Obesity
A COMPOSITION COMPRISING COMPONENTS THAT EXHIBIT ANTI-OBESITY ACTION FORMED FOR SUPPRESSING 5-LIPOOXYGENASE
info:eu-repo/semantics/article
oai:zenodo.org:3818396
2020-05-13T08:20:33Z
user-darulaceze
Erdal Can Alkoclar
2020-05-09
<p>The present invention herewith is related to a formulation developed for treatment of intestinal malabsorption.</p>
<p> </p>
<p><strong>Background of the Related Technology</strong></p>
<p>As of today, intestine is referred to as the section between the stomach and anus along the gastro-intestinal tract, which consists of two sections in humans and other mammals; small intestine and large intestine. Malabsorption is the disorder related to inability of absorption of nutrients from small intestine and sometimes this might be related to the pancreas. Some of the causes for this disorder may include the following: <a href="http://tr.wikipedia.org/wiki/%C3%87%C3%B6lyak_hastal%C4%B1%C4%9F%C4%B1">Coeliac Disease</a>, lactose intolerance, fructose malabsorption, secretion disorders related to pernicious anemia of pancreas (short bowel syndrome, radiation fibrosis (generally observed after treatment of cancer) and certain drugs).</p>
<p>The invention presented herewith with no “EP1986678B1", with title “Solubility Enhancers that Contain Biguanide for Oral Peptide Delivery” and under classification number “A61K 38/23", is related to using certain aromatic alcohols as enhancers of absorption to facilitate transportation of peptides, proteins and macromolecules from the intestinal wall and specifically using new agents to enhance the solubility of the referred aromatic alcohols, with the objective to increase the existence of such agents inside the biologic fluids where they dissolve very little under normal conditions.</p>
<p>Again the invention presented herewith with no “WO 1997/020568", with title “Compositions Containing Bismuth for Prevention and Treatment of Gastrointestinal Disorders" and under classification number “A61K 33/24", is related to administrating bismuth to a human or an animal for protective treatment and treatment of the human or the animal who has a gastrointestinal disorder caused or facilitated by algae and/ or cyanobacteria.</p>
<p>Again the invention presented herewith with no “WO 2000/041719", with title " Using a Neurotrophin or its analogues for treatment of hypomotility related to gastrointestinal disorders” and under classification number “A61K 39/00", is related to methods specifically used for increasing gastrointestinal motility. The present invention is particularly related to using neurotrophin-3 and its analogues for increasing the gastrointestinal motility. The method regarding the use of neurotrophin-3 and its analogues for treatment of gastrointestinal hypomotility disorders is also provided.</p>
<p>Again the invention presented herewith with no “EP2139882B1", with title " 3-Substituted Quinoline or Quinoxaline Derivatives and Using These as Phosphatidylinositol 3-Kinase (pı3k) Inhibitors" and under classification number “C07D 401/12", is related to the substituted bicyclic heteroaryl compounds having the structure shown in (I) or their pharmaceutically acceptable salts and compositions consisting of these, where X variable means C or N, and Y variable means N(R"), O or S, and referred compounds are useful in inhibiting the biological activity of PI3K5 enzyme of human origin and are intended for using treatment of general inflammation, arthritis, rheumatoid diseases, osteoarthritis, inflammatory intestinal disorders, inflammatory eye diseases, inflammatory and unstable bladder disorders, psoriasis, dermal complaints consisting of inflammatory components, chronic inflammatory cases, for example autoimmune diseases including but not limited with, systemic lupus erythematosus (SLE), myasthenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiple sclerosis, Sjogren’s Syndrome and autoimmune hemolytic anemia, and also treatment of allergic cases including all hypersensitivity forms. On the other hand, with the present invention methods are provided that are intended for treatment of cancer cases that develop through p1105 activity, depends on p1105 activity or is related to p1105 activity, including but not limited with, Acute Myeloid Leukemia (AML), Myelodysplastic Syndrome (MDS), Myeloproliferative Diseases (MPD), Chronic Myeloid Leukemia (CML), T-Cell Acute Lymphoblastic Leukemia (T-ALL), B-Cell Acute Lymphoblastic Leukemia (B-ALL), Non-Hodgkin’s Lymphoma (NHL), B-cell lymphoma and solid tumors like breast cancer.</p>
<p>To conclude it has become inevitable to proceed with a development in the area of the related technology, considering the inadequacy of the existing solutions and the need for a formulation intended for treatment of intestinal malabsorption.</p>
<p> </p>
<p><strong>Objective of the Invention</strong></p>
<p>To overcome the disadvantages referred in the Background of the Related Technology,</p>
<ul>
<li>One objective of the present invention is, to enhance nutrition absorption by improving active cAMP increase;</li>
<li>One other objective of the invention is to enhance amylase expression;</li>
<li>One other objective of the invention is to enhance protease expression;</li>
<li>One other objective of the invention is to improve insulin sensitivity;</li>
<li>One other objective of the invention is to provide functional increase of GIUT 4 translocation at an effective rate.</li>
</ul>
<p> </p>
<p>The present invention, which is aimed to achieve the above-mentioned advantages, is intended for treatment of intestinal malabsorption and is a formulation that is obtained by combination of the compositions selected in a single form or in combinations from a group containing; 16,20-bis(2-dimethyl)-6-O-stigmast-4-ene-coumaroyl-3-one, 2,3-bis(6-oxoethyl)-4-0-dioxin, 3,5-methoxy-stigmast-6-ene-phenyl-4-one.</p>
<p> </p>
<p>Structural and characteristic properties as well as all the advantages of the invention presented herewith will be clearly understood with the detailed description provided below and thus the evaluation regarding the present invention should be based on the detailed description presented herewith.</p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p>The present invention is related to a formulation developed for treatment of intestinal malabsorption. The referred formulation, enhances nutrition absorption by improving active cAMP increase, enhances amylase expression, enhances protease expression, improves insulin sensitivity, provides functional increase of GIUT 4 translocation at an effective rate.</p>
<p> </p>
<p>The formulation related to the present invention herewith contains; 16,20-bis(2-dimethyl)-6-O-stigmast-4-ene-coumaroyl-3-one, 2,3-bis(6-oxoethyl)-4-0-dioxin, 3,5-methoxy-stigmast-6-ene-phenyl-4-one.</p>
<p> </p>
<p>The referred formulation is formed by mixing the above-mentioned components at below percentages by weight;</p>
<ul>
<li>11-33% of 16,20-bis(2-dimethyl)-6-O-stigmast-4-ene-coumaroyl-3-one,</li>
<li>26-45% of 2,3-bis(6-oxoethyl)-4-0-dioxin, </li>
<li>63-22% of 3,5-methoxy-stigmast-6-ene-phenyl-4-one. </li>
</ul>
<p> </p>
<p>Components given above are obtained by combining the components from the above-mentioned group at the given range of weight ratios in a single form or in combinations thereof.</p>
<p> </p>
<p>The present invention at the same time is related to using the above-referred formulation for treatment of intestinal malabsorption and manufacturing it for such purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A formulation intended for treatment of intestinal malabsorption, which consists of combining the components selected from the group; 16,20-bis(2-dimethyl)-6-O-stigmast-4-ene-coumaroyl-3-one, 2,3-bis(6-oxoethyl)-4-0-dioxin, 3,5-methoxy-stigmast-6-ene-phenyl-4-one in a single form or in combinations thereof.</li>
<li>The formulation of Claim 1 which is characterized by containing 11-33% of 16,20-bis(2-dimethyl)-6-O-stigmast-4-ene-coumaroyl-3-one by weight.</li>
<li>The formulation of Claim 1 which is characterized by containing 26-45% of 2,3-bis(6-oxoethyl)-4-0-dioxin by weight.</li>
<li>The formulation of Claim 1 which is characterized by containing 63-22% of 3,5-methoxy-stigmast-6-ene-phenyl-4-one by weight.</li>
<li>Using the compositions obtained by selecting singly or in combination of components from the group of; 16,20-bis(2-dimethyl)-6-O-stigmast-4-ene-coumaroyl-3-one, 2,3-bis(6-oxoethyl)-4-0-dioxin, 3,5-methoxy-stigmast-6-ene-phenyl-4-one from any one as given in Claims 2-4 in manufacturing the formulation intended for treatment of intestinal malabsorption. </li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>SUMMARY</strong></p>
<p> </p>
<p><strong>A FORMULATION INTENDED FOR TREATMENT OF INTESTINAL MALABSORPTION</strong></p>
<p> </p>
<p>The present invention is related to a formulation developed for treatment of intestinal malabsorption. The referred formulation, enhances nutrition absorption by improving active cAMP increase, enhances amylase expression, enhances protease expression, improves insulin sensitivity, provides functional increase of GIUT 4 translocation at an effective rate.</p>
https://doi.org/10.5281/zenodo.3818396
oai:zenodo.org:3818396
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3818395
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
GLUT4 Insulin Sensititizer Amylase
A FORMULATION INTENDED FOR TREATMENT OF INTESTINAL MALABSORPTION
info:eu-repo/semantics/patent
oai:zenodo.org:3819167
2020-05-13T20:20:35Z
user-darulaceze
Erdal Can Alkoclar
2020-05-10
<p> </p>
<p><strong>A COMPOSITION COMPRISING COMPONENTS THAT EXHIBIT ANTI-NOCICEPTIVE ACTION FORMED FOR SUPPRESSING PGE2 EXPRESSION</strong></p>
<p> </p>
<p><strong>Technical Field</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the components that exhibit anti-nociceptive action formed for suppressing the pge2 expression.</p>
<p> </p>
<p> </p>
<p><strong>State of the Art</strong></p>
<p> </p>
<p>Anti-nociceptive is the characteristic of having the ability to reduce or stop the painful stimulants (e.g. analgesics). According to the state of the art, the invention no. EP1243262B1 with classification "A61K 31/165" entitled "Novel use of a peptide class of compound for treating non-neuropathic inflammatory pain" relates to the use of compounds of Formula (I) for treating different types and symptoms of acute and chronic pain, especially non-neuropathic inflammatory pain in mammals. The pain to be treated may be chronic inflammatory pain, e.g. rheumatoid arthritis pain and/or secondary inflammatory osteoarthritic pain. The compounds exhibit an anti-nociceptive profile and differ from the conventional analgesics such as the opioids and the non-steroidal anti-inflammatory drugs (NSAIDs) and are useful as specific analgesics.</p>
<p>Further, according to the invention no. EP1334103B1 entitled "Methods for treatment of disease-induced peripheral neuropathy and related conditions”, a method of treating disease-induced peripheral neuropathy comprises administering to a patient with disease-induced peripheral neuropathy an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. The compound can induce peripheral nerve sprouting through the action of a neurotrophic factor such as nerve growth factor (NGF) without the occurrence of hyperalgesia. The peripheral nerve sprouting can be nociceptive nerve sprouting. The disease-induced peripheral neuropathy can be diabetic neuropathy or disease-induced peripheral neuropathy with another basis.</p>
<p>Further, the invention no. EP2352721B1 entitled "Novel process for the preparation of amino acid derivatives" relates to a novel process for the preparation of amino acid derivatives. In particular, the present application relates to an improved process for the manufacture of Lacosamide (LCM)<em>,</em> (R)-2-acetamido-N-benzyl-3-methoxypropion-amide, which is useful as an anticonvulsive drug. LCM has demonstrated antiepileptic effectiveness in different rodent seizure models and antinociceptive potential in experimental animal models that reflect distinct types and symptoms of neuropathic as well as chronic inflammatory pain.</p>
<p>As a result, the presence of the need for a composition for suppressing the pge2 expression and the inadequacy of the existing solutions have made it necessary to perform an improvement in the relevant art.</p>
<p> </p>
<p> </p>
<p><strong>Object of the Invention</strong></p>
<p> </p>
<p>In order to eliminate the disadvantages of the state of the art, an object of the invention is to enable the suppression of pge2.</p>
<p>Another object of the invention is to enable the suppression of fmo3.</p>
<p>In order to achieve the aforesaid advantages, the invention is a composition for suppressing pge2 expression, said composition being obtained by the components selected from the group comprising (4E)-1-(2,2-dimethoxyphenyl)-3-(3,4-trihydroxyphenyl)-4-propen-2-one, (2E)-1-(3,3-triepoxyphenyl)-6-(2,2-dihydroxylaroyl)-6-propen-2-one that are used individually or in combinations.</p>
<p> </p>
<p>The structural and characteristic features and all the advantages of the invention will become more clearly understood from the detailed description provided below and therefore, the evaluation must be made taking this detailed description into consideration.</p>
<p> </p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p> </p>
<p>The invention is a composition comprising the components that exhibit anti-nociceptive action formed for suppressing the pge2 expression. The composition according to the invention enables the suppression of pge2 and the suppression of fmo3.</p>
<p> </p>
<p>The composition according to the invention contains (4E)-1-(2,2-dimethoxyphenyl)-3-(3,4-trihydroxyphenyl)-4-propen-2-one, (2E)-1-(3,3-triepoxyphenyl)-6-(2,2-dihydroxylaroyl)-6-propen-2-one.</p>
<p> </p>
<p>Said composition is obtained by a mixture of the aforesaid components according to the following ratios by weight:</p>
<p>1-99% (4E)-1-(2,2-dimethoxyphenyl)-3-(3,4-trihydroxyphenyl)-4-propen-2-one, </p>
<p>99-1% (2E)-1-(3,3-triepoxyphenyl)-6-(2,2-dihydroxylaroyl)-6-propen-2-one.</p>
<p>The composition is obtained from the aforesaid components selected from the aforesaid group and used according to the mentioned weight ratio ranges individually or in combinations.</p>
<p> </p>
<p>Said invention also encompasses the use of said composition for suppressing pge2 expression and the manufacture thereof for this purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A composition for suppressing pge2 expression, said composition being obtained by the components selected from the group comprising (4E)-1-(2,2-dimethoxyphenyl)-3-(3,4-trihydroxyphenyl)-4-propen-2-one, (2E)-1-(3,3-triepoxyphenyl)-6-(2,2-dihydroxylaroyl)-6-propen-2-one that are used individually or in combinations.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 1-99% by weight (4E)-1-(2,2-dimethoxyphenyl)-3-(3,4-trihydroxyphenyl)-4-propen-2-one.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 99-1% by weight (2E)-1-(3,3-triepoxyphenyl)-6-(2,2-dihydroxylaroyl)-6-propen-2-one.</li>
</ol>
<p> </p>
<ol>
<li>Use of the components according to Claims 1 to 3 obtained individually or in combinations selected from the group consisting of (4E)-1-(2,2-dimethoxyphenyl)-3-(3,4-trihydroxyphenyl)-4-propen-2-one, (2E)-1-(3,3-triepoxyphenyl)-6-(2,2-dihydroxylaroyl)-6-propen-2-one for the manufacture of a composition for suppressing pge2 expression.</li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>ABSTRACT</strong></p>
<p> </p>
<p><strong>A COMPOSITION COMPRISING COMPONENTS THAT EXHIBIT ANTI-NOCICEPTIVE ACTION FORMED FOR SUPPRESSING PGE2 EXPRESSION</strong></p>
<p> </p>
<p>The invention relates to a composition formed for suppressing the pge2 expression.</p>
https://doi.org/10.5281/zenodo.3819167
oai:zenodo.org:3819167
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3819166
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
PGE2 Anti-Nociceptive
A COMPOSITION COMPRISING COMPONENTS THAT EXHIBIT ANTI-NOCICEPTIVE ACTION FORMED FOR SUPPRESSING PGE2 EXPRESSION
info:eu-repo/semantics/patent
oai:zenodo.org:3819183
2020-05-13T08:20:32Z
user-darulaceze
Erdal Can Alkoclar
2020-05-10
<p> </p>
<p> </p>
<p><strong>A COMPOSITION COMPRISING ANTI-VIRAL COMPONENTS THAT EXHIBIT THE CHARACTERISTIC OF SUPPRESSING NEUROAMINIDASE</strong></p>
<p> </p>
<p><strong>Technical Field</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the anti-viral components formed for suppressing neuroaminidase.</p>
<p> </p>
<p> </p>
<p><strong>State of the Art</strong></p>
<p> </p>
<p>Neuroaminidase is the antigenic structure that enables the viruses such as influenza to spread from the main cell to the other tissues. In the literature, there are 9 types of neuroaminidase. These are shown briefly as n1, n2 ... n9.</p>
<p>According to the state of the art, the invention no. WO 1999/054299 with classification "C07D 409/04" entitled "Pyrrolidines as inhibitors of neuroaminidases" discloses compounds of formula (I) which are useful for inhibiting neuraminidases from disease-causing microorganisms, especially, influenza neuraminidase. Also disclosed are compositions and methods for preventing and treating diseases caused by microorganisms having a neuraminidase, processes for preparing the compounds and synthetic intermediates used in these processes.</p>
<p>Further, the invention no. EP1317559B1 entitled "DNA transfection system for the generation of infectious negative strand RNA virus" is based on the development of a dual promoter system (preferably a RNA pol I-pol II system) for the efficient intracellular synthesis of viral RNA. The resultant minimal plasmid-based system may be used to synthesize any RNA virus, preferably viruses with a negative single stranded RNA genome. The viral genome of the system is produced when the plasmids of the system are introduced into a suitable host cell. One application of the system is production of attenuated, reassortant influenza viruses for use as antigens in vaccines. The reassortant viruses generated by cotransfection of plasmids may comprise genes encoding the surface glycoproteins hemagglutinin and neuraminidase from an influenza virus currently infecting the population and the internal genes from an attenuated influenza virus. An advantageous property of the present invention is its versatility; the system may be quickly and easily adapted to synthesize an attenuated version of any RNA virus. Attenuated or inactivated RNA viruses produced by the present invention may be administered to a patient in need of vaccination by any of several routes including intranasally or intramuscularly.</p>
<p>Further, the invention no. EP1274713B1 entitled "Anti-viral pyrimidine nucleoside analogues" pertains to a compound having the formula (I) wherein Ar is an, optionally substituted, aromatic ring system, the aromatic ring system comprising one six-membered aromatic ring or two fused six-membered aromatic rings; R8 and R9 are each selected from hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, nitro, cyano, alkyloxy, aryloxy, thiol, alkylthiol, arylthiol and aryl; Q is selected from O, S and CY2; X is selected from O, NH, S, N-alkyl, (CH2)m and CY2; Z is selected from O, NH, S, N-alkyl; U'' is H and U' is selected from H and CH2T, or U' and U'' are joined so as to form a ring moiety including Q selected from (a) and (b); wherein the other variables are as described the specification, with the proviso that when T is OAc and T' and T'' are present and are H, Ar is not 4-(2-benzoxazolyl)phenyl. These compounds exhibit anti-viral activity against the varicella zoster virus for instance.</p>
<p>As a result, the presence of the need for a composition for suppressing neuroaminidase and the inadequacy of the existing solutions have made it necessary to perform an improvement in the relevant art.</p>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>Object of the Invention</strong></p>
<p> </p>
<p>In order to eliminate the disadvantages of the state of the art, an object of the invention is to suppress neuroaminidase.</p>
<p>Another object of the invention is to suppress RNA helicase.</p>
<p> </p>
<p>In order to achieve the aforesaid advantages, the invention is a composition for suppressing neuroaminidase, said composition being obtained by the components selected from the group comprising 2,2'-[[dihydro-2-(4-cafeoyl)-1,3(2H,4H)-octadienyl]bis(methylene)]bis(N,N-dimethyl-sorinin and 2,2'-[[dihydro-2-(4-coumaroyl)-1,3(2H,4H)-monolaroyl]bis(diethylene)]bis(N,N-dimethyl-sorinin that are used individually or in combinations.</p>
<p> </p>
<p>The structural and characteristic features and all the advantages of the invention will become more clearly understood from the detailed description provided below and therefore, the evaluation must be made taking this detailed description into consideration.</p>
<p> </p>
<p> </p>
<p><strong>Detailed Description of the Invention</strong></p>
<p> </p>
<p>The invention is a composition comprising the anti-viral components formed for suppressing neuroaminidase. Said composition enables the suppression of neuroaminidase and the suppression of RNA helicase.</p>
<p> </p>
<p>The composition according to the invention contains 2,2'-[[dihydro-2-(4-cafeoyl)-1,3(2H,4H)-octadienyl]bis(methylene)]bis(N,N-dimethyl-sorinin and 2,2'-[[dihydro-2-(4-coumaroyl)-1,3(2H,4H)-monolaroyl]bis(diethylene)]bis(N,N-dimethyl-sorinin.</p>
<p> </p>
<p>Said composition is obtained by a mixture of the aforesaid components according to the following ratios by weight:</p>
<p>1-99% 2,2'-[[dihydro-2-(4-cafeoyl)-1,3(2H,4H)-octadienyl]bis(methylene)]bis(N,N-dimethyl-sorinin, </p>
<p>99-1% 2,2'-[[dihydro-2-(4-coumaroyl)-1,3(2H,4H)-monolaroyl]bis(diethylene)]bis(N,N-dimethyl-sorinin.</p>
<p> </p>
<p>The composition is obtained from the aforesaid components selected from the aforesaid group and used according to the mentioned weight ratio ranges individually or in combinations.</p>
<p> </p>
<p>Said invention also encompasses the use of said composition for suppressing neuroaminidase and the manufacture thereof for this purpose.</p>
<p> </p>
<p><strong>CLAIMS</strong></p>
<p> </p>
<ol>
<li>A composition for suppressing neuroaminidase, said composition being obtained by the components selected from the group comprising 2,2'-[[dihydro-2-(4-cafeoyl)-1,3(2H,4H)-octadienyl]bis(methylene)]bis(N,N-dimethyl-sorinin and 2,2'-[[dihydro-2-(4-coumaroyl)-1,3(2H,4H)-monolaroyl]bis(diethylene)]bis(N,N-dimethyl-sorinin that are used individually or in combinations.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 1-99% by weight 2,2'-[[dihydro-2-(4-cafeoyl)-1,3(2H,4H)-octadienyl]bis(methylene)]bis(N,N-dimethyl-sorinin.</li>
</ol>
<p> </p>
<ol>
<li>A composition according to Claim 1 characterized in that it comprises 99-1% by weight 2,2'-[[dihydro-2-(4-coumaroyl)-1,3(2H,4H)-monolaroyl]bis(diethylene)]bis(N,N-dimethyl-sorinin.</li>
</ol>
<p> </p>
<ol>
<li>Use of the components according to Claims 1 to 3 obtained individually or in combinations selected from the group consisting of 2,2'-[[dihydro-2-(4-cafeoyl)-1,3(2H,4H)-octadienyl]bis(methylene)]bis(N,N-dimethyl-sorinin and 2,2'-[[dihydro-2-(4-coumaroyl)-1,3(2H,4H)-monolaroyl]bis(diethylene)]bis(N,N-dimethyl-sorinin for the manufacture of a composition for suppressing neuroaminidase.</li>
</ol>
<p> </p>
<p> </p>
<p> </p>
<p> </p>
<p><strong>ABSTRACT</strong></p>
<p> </p>
<p><strong>A COMPOSITION COMPRISING ANTI-VIRAL COMPONENTS THAT EXHIBIT THE CHARACTERISTIC OF SUPPRESSING NEUROAMINIDASE</strong></p>
<p> </p>
<p>The invention relates to a composition comprising the anti-viral components formed for suppressing neuroaminidase.</p>
https://doi.org/10.5281/zenodo.3819183
oai:zenodo.org:3819183
eng
Zenodo
https://zenodo.org/communities/darulaceze
https://doi.org/10.5281/zenodo.3819182
info:eu-repo/semantics/openAccess
Creative Commons Attribution 4.0 International
https://creativecommons.org/licenses/by/4.0/legalcode
Neuroaminidase Cancer
A COMPOSITION COMPRISING ANTI-VIRAL COMPONENTS THAT EXHIBIT THE CHARACTERISTIC OF SUPPRESSING NEUROAMINIDASE
info:eu-repo/semantics/patent