发明公开
EP0942903A1 ARYL-SUBSTITUTED ACRYLAMIDES WITH LEUKOTRIENE B4 (LTB-4) RECEPTOR ANTAGONIST ACTIVITY
失效
具有ACRYLIC白三烯B4芳基 - 取代的胺(LTB-4)受体拮抗作用
- 专利标题: ARYL-SUBSTITUTED ACRYLAMIDES WITH LEUKOTRIENE B4 (LTB-4) RECEPTOR ANTAGONIST ACTIVITY
- 专利标题(中): 具有ACRYLIC白三烯B4芳基 - 取代的胺(LTB-4)受体拮抗作用
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申请号: EP97943901.0申请日: 1997-09-24
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公开(公告)号: EP0942903A1公开(公告)日: 1999-09-22
- 发明人: GREENSPAN, Paul, David , FUJIMOTO, Roger, Aki
- 申请人: Novartis AG
- 申请人地址: Schwarzwaldallee 215 4058 Basel CH
- 专利权人: Novartis AG
- 当前专利权人: Novartis AG
- 当前专利权人地址: Schwarzwaldallee 215 4058 Basel CH
- 代理机构: Becker, Konrad, et al
- 优先权: US19960027468P 19960926
- 国际公布: WO1998013347 19980402
- 主分类号: A61K31
- IPC分类号: A61K31 ; A61P29 ; A61P43 ; C07C235 ; C07C255 ; C07C317 ; C07C323 ; C07D213 ; C07D307 ; C07D333
摘要:
Disclosed are compounds of formula (I) wherein W is CH or N; R is (mono- or di-carbocyclic or heterocyclic aryl)-lower alkyl; R1 is hydrogen or lower alkyl; R?2 and R3¿ are hydrogen, lower alkyl, lower alkoxy-lower alkyl or aryl-lower alkyl; or R?2 and R3¿ joined together represent lower alkylene optionally interrupted by O, NH, N-lower alkyl or S so as to form a ring with the amide nitrogen; X is O, S, SO, SO¿2? or a direct bond; X?1¿ is O, S, SO, SO¿2? or a direct bond; Y is a direct bond, lower alkylene or lower alkylidene; and Z is carboxyl, 5-tetrazolyl, hydroxymethyl or carboxyl derivatized in the form of a pharmaceutically acceptable ester; and pharmaceutically acceptable salts thereof; which are useful as LTB-4 antagonists.
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