PYRAZOLO [3,4-b] PYRIDINE COMPOUNDS, AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS

摘要

THE INVENTION RELATES TO A COMPOUND OF FORMULA (I) OR A SALT THEREOF: WHEREIN: R1 IS C1-4ALKYL, C1-3FLUOROALKYL, -CH2CH2OH OR -CH2CH2CO2C1-2A1KYL; R2 IS A HYDROGEN ATOM (H), METHYL OR C1 FLUOROALKYL; R3 IS OPTIONALLY SUBSTITUTED C3-8CYCLOALKYL OR OPTIONALLY SUBSTITUTED MONO-UNSATURATED-C5-7CYCLOALKENYL OR AN OPTIONALLY SUBSTITUTED HETEROCYCLIC GROUP OF SUB-FORMULA (AA), (BB) OR (CC); IN WHICH N1 AND N2 INDEPENDENTLY ARE 1 OR 2; AND IN WHICH Y IS O, S, SO2, OR NR10; OR R3 IS A BICYCLIC GROUP (DD) OR (EE): AND WHEREIN X IS NR4R5 OR OR5A.THE COMPOUNDS ARE PHOSPHODIESTERASE (PDE) INHIBITORS, IN PARTICULAR PDE4 INHIBITORS.ALSO PROVIDED IS THE USE OF A COMPOUND OF FORMULA (I), OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF,IN THE MANUFACTURE OF A MEDICAMENT FOR THE TREATMENT AND/OR PROPHYLAXIS OF AN INFLAMMATORY AND/OR ALLERGIC DISEASE IN A MAMMAL SUCH AS A HUMAN, FOR EXAMPLE CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), ASTHMA, OR ALLERGIC RHINITIS.