发明公开
- 专利标题: VLA-4 INTEGRIN ANTAGONISTS
- 专利标题(中): VLA-4整联蛋白拮抗剂
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申请号: EP00990650.4申请日: 2000-12-05
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公开(公告)号: EP1235793A2公开(公告)日: 2002-09-04
- 发明人: WATTANASIN, Sompong , WEIDMANN, Beat
- 申请人: Novartis AG , Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.
- 申请人地址: Lichtstrasse 35 4056 Basel CH
- 专利权人: Novartis AG,Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.
- 当前专利权人: Novartis AG,Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.
- 当前专利权人地址: Lichtstrasse 35 4056 Basel CH
- 优先权: US455670 19991207
- 国际公布: WO01042192 20010614
- 主分类号: C07C275/38
- IPC分类号: C07C275/38 ; C07D295/13 ; A61K31/5375 ; A61K31/17 ; A61P27/02
摘要:
Compounds of formula (I) wherein Ar is carbocyclic or heterocyclic aryl, or biaryl; Q is O, S or N-C N; X is arylene; V is NH, O, NHOH, CH2 or a direct bond; W is NH, O, NHOH, CH2 or a direct bond; Alk is C2-C7-alkylene or C2-C7-alkylene interrupted by O, S, SO, SO2 or NR3; Y is amino, acylamino, mono- or di- (lower alkyl, aryl or aralkyl)-amino, pyrrolidino, perhydroazepino or a group of the formula (II) in which M1 is N; and M2 is CH2, O, NR3, S, SO or SO2; R1, R2 and R3 are independently hydrogen, lower alkyl, lower alkenyl, cycloalkyl, aryl, cycloalkyl-lower alkyl, aryl-lower alkyl or aryl-lower alkenyl; Z is lower alkylene or lower alkylene substituted by one or more of lower alkyl, lower alkenyl, cycloalkyl, aryl, cycloalkyl-lower alkyl, aryl-lower alkyl or aryl-lower alkenyl; or Z is lower alkylene interrupted by O, S, SO, SO2 or NR3; pharmaceutically acceptable esters and amides thereof; and pharmaceutically acceptable salts thereof, which are useful as VLA-4 integrin antagonists.
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