PYFLUP :New molecules for the treatment of respiratory diseases
Description
Type 4 Phosphodiesterases (PDE-4) are a major subfamilies of PDE enzymes present in inflammatory and immune cells, bronchial smooth muscle and brain. Inhibition of PDE4 activity results in the bronch by anti-inflammatory effects in combination with a relaxation of bronchial smooth muscle. A new family of pyridazinone-type molecules were synthesized, for selective inhibition of PDE4 compared to other isoforms.
Benefits :
- Obtained by synthesis of new fluorinated pyridazinones
- The methodology allows, according to a general formula, large number of pharmaco-modulations: structure-activity-selectivity developments
- The nature of the fluorinated pattern allows the modulation of the selectivity of molecules and limits the known side- effects
- Activity equal or greater than marketed molecule Roflumilast
- Selectivity for PDE-4B (bronchi) relative to isoforms (PDE-4D) and subtypes (PDE-1, PDE-7A, PDE-10A).
- Specific inhibition of subtype PDE-4B reduces the known side-effects related to a non specific inhibition such as headache, nausea, weight loss, depression...
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