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 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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