发明名称 PYRAZOLO [3,4-B] PYRIDINE COMPOUNDS, AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS
摘要 The invention provides a compound of formula (I) or a salt thereof: wherein Ar has the sub-formula (x) or (z): and wherein R<SUP>3 </SUP>is optionally substituted C<SUB>3-8</SUB>cycloalkyl, optionally substituted C<SUB>5-7</SUB>cycloalkenyl, an optionally substituted heterocyclic group (aa), (bb) or (cc), or a bicyclic group (ee); and wherein R<SUP>4 </SUP>is H, C<SUB>1-3</SUB>alkyl, C<SUB>1-2</SUB>fluoroalkyl, cyclopropyl, -CH<SUB>2</SUB>OR<SUP>4a</SUP>, -CH(Me)OR<SUP>4a</SUP>, or -CH<SUB>2</SUB>CH<SUB>2</SUB>OR<SUP>4a</SUP>; and R<SUP>5 </SUP>is inter alia H, C<SUB>1-8</SUB>alkyl, C<SUB>1-3</SUB>fluoroalkyl, C<SUB>3-8</SUB>cycloalkyl, certain substituted alkyl groups, -(CH<SUB>2</SUB>)<SUB>n</SUB><SUP>13</SUP>-Het, or optionally substituted phenyl or -CH<SUB>2</SUB>-Ph; or R<SUP>4 </SUP>and R<SUP>5 </SUP>taken together are -(CH<SUB>2</SUB>)<SUB>p</SUB><SUP>1</SUP>- or -(CH<SUB>2</SUB>)<SUB>p</SUB><SUP>3</SUP>-X<SUP>5</SUP>-(CH<SUB>2</SUB>)<SUB>p</SUB><SUP>4</SUP>-; provided that at least one of R<SUP>4 </SUP>and R<SUP>5 </SUP>is not a hydrogen atom (H). The invention also provides the use of the compounds as inhibitors of phosphodiesterase type IV (PDE4) and/or for the treatment and/or prophylaxis of inflammatory and/or allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, allergic rhinitis or atopic dermatitis.
申请公布号 CA2557004(A1) 申请公布日期 2005.06.30
申请号 CA20042557004 申请日期 2004.12.17
申请人 GLAXO GROUP LIMITED 发明人 DOWLE, MICHAEL DENNIS;EDLIN, CHRISTOPHER DAVID;TRIVEDI, NAIMISHA;ROBINSON, JOHN EDWARD;JONES, PAUL SPENCER;COE, DIANE MARY;ALLEN, DAVID GEORGE;LINDVALL, MIKA KRISTIAN;HAMBLIN, JULIE NICOLE;MITCHELL, CHARLOTTE JANE;JOHNSON, MARTIN REDPATH;REDGRAVE, ALISON JUDITH;COOK, CAROLINE MARY
分类号 C07D471/04;A61K31/437;A61P11/00;A61P29/00;C07D221/00;C07D231/00 主分类号 C07D471/04
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