发明授权
- 专利标题: Substituted 2-quinolyl-oxazoles useful as PDE4 inhibitors
- 专利标题(中): 用作PDE4抑制剂的取代的2-喹啉基 - 恶唑
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申请号: US11130359申请日: 2005-05-16
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公开(公告)号: US07511062B2公开(公告)日: 2009-03-31
- 发明人: Rongze Kuang , David Blythin , Neng-Yang Shih , Ho-Jane Shue , Xiao Chen , Jianhua Cao , Danlin Gu , Ying Huang , John H. Schwerdt , Pauline C. Ting , Shing-Chun Wong , Li Xiao
- 申请人: Rongze Kuang , David Blythin , Neng-Yang Shih , Ho-Jane Shue , Xiao Chen , Jianhua Cao , Danlin Gu , Ying Huang , John H. Schwerdt , Pauline C. Ting , Shing-Chun Wong , Li Xiao
- 申请人地址: US NJ Kenilworth
- 专利权人: Schering Corporation
- 当前专利权人: Schering Corporation
- 当前专利权人地址: US NJ Kenilworth
- 代理商 Anita W. Magatti; Serena I. Farquharson-Torres; Gerard E. Reinhardt
- 主分类号: C07D215/38
- IPC分类号: C07D215/38 ; A61K31/44
摘要:
The invention claims compounds of the formula wherein is a 5-membered heteroaryl; X is S or O; R1 is H, alkyl, cycloalkyl, cylcoalkylalkyl-, —CH2F, —CHF2, —CF3, —C(O)alkyl or —C(O)NR18R19; R3 and R4 H, alkyl, hydroxyalkyl or —C(O)Oalkyl; R5 and R6 are H, alkyl, hydroxyalkyl, alkoxyalkyl, mercaptoalkyl, —CH2F, —CHF2, —CF3, —C(O)OH or —C(O)Oalkyl; R7 is H, alkyl, alkenyl, hydroxyalkyl, cycloalkyl, alkoxyalkyl, aminoalkyl, (R17-phenyl)alkyl or —CH2—C(O)—O-alkyl; and R8 comprises alkyl, heteroaryl, phenyl or cycloalkyl, or heterocycloalkyl, all optionally substituted, or a cycloalkyl- or heterocycloalkyl-substituted amide; or R7 and R8 and the nitrogen to which they are attached together form an optionally substituted ring; and the remaining variables are as defined in the specification. Also claimed are pharmaceutical compositions, the use of the compounds as PDE4 inhibitors, and combinations with other actives.
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