Published June 21, 2005 | Version v2
Patent Open

Preparation of pyridazin-3(2H)-one derivatives as PDE4 inhibitors for the treatment of pathological diseases

Authors/Creators

  • 1. ROR icon Almirall (Spain)

Description

This patent describes pyridazin-3(2H)-one derivatives as new pharmaceutical entities, the processes for their preparation, as well as their corresponding pharmaceutical compositions.  These compounds are potent and selective inhibitors of the enzyme phosphodiesterase 4 (PDE4) and are therefore useful in the treatment, prevention or suppression of pathological conditions, diseases and disorders known to be susceptible to improvement following inhibition of this enzyme. These would include chronic and acute inflammatory diseases such as asthma, obstructive pulmonary disease, rheumatoid arthritis, atopic dermatitis, psoriasis or irritable bowel disease.

 

Other

The main objective of this patent is the synthesis of new potent and selective PDE4 inhibitors that may be an improvement over the PDE4 inhibitors in clinical development described so far. It is known that the clinical development in humans of early PDE4 inhibitors, such as rolipram, has been hampered by the occurrence of side effects such as nausea and vomiting at therapeutic plasma levels. The compounds described in this patent are hydrolysed at the systemic level, so this particular property gives the compounds high local activity and little or no systemic action, avoiding or reducing the risk of unwanted systemic side effects. Furthermore, the compounds of the present invention can also be used in combination with other drugs known to be effective in the treatment of these diseases. For example, they can be used in combination with steroids or immunosuppressive agents. In this case the administration of the compounds allows a reduction of the dose of the other drugs, thus avoiding the occurrence of the unwanted side effects associated with these other drugs.

 

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WO 2005123693A1 .pdf

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Additional details

Identifiers

Other
WO 2005/123693
Other
PCT/EP2005/006712