Pyrazolo[3,4-b]pyridine compounds, and their use as phosphodiesterase inhibitors

• Main Authors: COOK, CAROLINE MARY, JOHNSON, MARTIN REDPATH, COOPER, ANTHONY WILLIAM JAMES, ALLEN, DAVID GEORGE, MITCHELL, CHARLOTTE JANE, HAMBLIN, JULIE NICOLE, REDGRAVE, ALISON JUDITH, EDLIN, CHRISTOPHER DAVID, COE, DIANE MARY, LINDVALL, MIKA KRISTIAN, DOWLE, MICHAEL DENNIS, JONES, PAUL SPENCER
• Format: Patent
• Language: English
• Published: 13.09.2012
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

Abstract The invention relates to a compound of formula (I) or a salt thereof: Formula (I) wherein: R1 is C .4alkyl, C1.3fluoroalkyl or -(CH 2)20H; R2 is a hydrogen atom (H), methyl or Cifluoroalkyl; R3a is a hydrogen atom (H) or C1.3alkyl; R3 is optionally substituted 5 branched C3 .6 alkyl, optionally substituted C3.scycloalkyl, optionally substituted mono unsaturated-C 5.7cycloalkenyl, optionally substituted phenyl, or an optionally substituted heterocyclic group of sub-formula (aa), or (bb) or (cc) in which nI and n2 independently are I or 2; and Y is 0, S, SO 2 , or NR4, and wherein Het is of sub-formula (i), or (ii), or (iii), or (iv) or (v). The compounds are phosphodiesterase (PDE) inhibitors, in particular 10 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.