发明申请
US20080132536A1 PYRAZOLO [3,4-B] PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS
审中-公开
吡咯并[3,4-B]吡啶化合物及其用作PDE4抑制剂
![PYRAZOLO [3,4-B] PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS](/docs/US/2008-06-05/US20080132536A1/abs.jpg.600x600.jpg)
- 专利标题： PYRAZOLO [3,4-B] PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS
- 专利标题（中）： 吡咯并[3,4-B]吡啶化合物及其用作PDE4抑制剂
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申请号： US12022372申请日： 2008-01-30
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公开(公告)号： US20080132536A1公开(公告)日： 2008-06-05
- 发明人: David George Allen , Diane Mary Coe , Caroline Mary Cook , Michael Dennis Dowle , Christopher David Edlin , Julie Nicole Hamblin , Martin Redpath Johnson , Paul Spencer Jones , Mika Kristian Lindvall , Charlotte Jane Mitchell , Alison Judith Redgrave , John Edward Robinson , Naimisha Trivedi
- 申请人： David George Allen , Diane Mary Coe , Caroline Mary Cook , Michael Dennis Dowle , Christopher David Edlin , Julie Nicole Hamblin , Martin Redpath Johnson , Paul Spencer Jones , Mika Kristian Lindvall , Charlotte Jane Mitchell , Alison Judith Redgrave , John Edward Robinson , Naimisha Trivedi
- 专利权人： Glaxo Group Limited
- 当前专利权人： Glaxo Group Limited
- 优先权： EPPCT/EP2003/014867 20031219; GB0405899.6 20040316; GB0405936.6 20040316; GB0406754.2 20040325
- 主分类号： A61K31/437
- IPC分类号： A61K31/437 ; A61P11/00 ; A61P19/02 ; A61P37/08 ; A61P17/00 ; C07D471/04 ; A61K31/4545 ; C07D487/04
![PYRAZOLO [3,4-B] PYRIDINE COMPOUNDS, AND THEIR USE AS PDE4 INHIBITORS](/abs-image/US/2008/06/05/US20080132536A1/abs.jpg.150x150.jpg)
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 R3 is optionally substituted C3-8cycloalkyl, optionally substituted C5-7cycloalkenyl, an optionally substituted heterocyclic group (aa), (bb) or (cc), or a bicyclic group (ee); and wherein R4 is H, C1-3alkyl, C1-2fluoroalkyl, cyclopropyl, —CH2OR4a, —CH(Me)OR4a, or —CH2CH2OR4a; and R5 is inter alia H, C1-8alkyl, C1-3fluoroalkyl, C3-8cycloalkyl, certain substituted alkyl groups, —(CH2)n13-Het, or optionally substituted phenyl or —CH2-Ph; or R4 and R5 taken together are —(CH2)p1— or —(CH2)p3—X5—(CH2)p4—; provided that at least one of R4 and R5 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.