发明申请
- 专利标题: VLA-4 INTEGRIN ANTAGONISTS
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申请号: PCT/EP0012226申请日: 2000-12-05
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公开(公告)号: WO0142192A3公开(公告)日: 2002-01-10
- 发明人: WATTANASIN SOMPONG , WEIDMANN BEAT
- 申请人: NOVARTIS AG , NOVARTIS ERFIND VERWALT GMBH , WATTANASIN SOMPONG , WEIDMANN BEAT
- 专利权人: NOVARTIS AG,NOVARTIS ERFIND VERWALT GMBH,WATTANASIN SOMPONG,WEIDMANN BEAT
- 当前专利权人: NOVARTIS AG,NOVARTIS ERFIND VERWALT GMBH,WATTANASIN SOMPONG,WEIDMANN BEAT
- 优先权: US45567099 1999-12-07
- 主分类号: C07D295/12
- IPC分类号: C07D295/12 ; A61K31/197 ; A61K31/5375 ; A61K31/5377 ; A61P11/00 ; A61P19/02 ; A61P27/02 ; A61P37/06 ; A61P43/00 ; C07C273/18 ; C07C275/42 ; C07C279/28 ; C07D295/13 ; C07D295/18 ; C07D295/185 ; C07C275/38 ; A61K31/17
摘要:
Compounds of formula (I) wherein Ar is carbocyclic or heterocyclic aryl, or biaryl; Q is O, S or N-CN; 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.