发明公开
EP0810991A1 1-ARYL-2-ACYLAMINO-ETHANE COMPOUNDS AND THEIR USE AS NEUROKININ ESPECIALLY NEUROKININ 1 ANTAGONISTS
失效
1-ARYL-2-ACYLAMINO-ETHAN-VERBINDUNGEN UND IHRE VERWENDUNG ALS NEUROKININ- INSBESONDERE ALS NEUROKININ-1-ANTAGONISTEN
- 专利标题: 1-ARYL-2-ACYLAMINO-ETHANE COMPOUNDS AND THEIR USE AS NEUROKININ ESPECIALLY NEUROKININ 1 ANTAGONISTS
- 专利标题(中): 1-ARYL-2-ACYLAMINO-ETHAN-VERBINDUNGEN UND IHRE VERWENDUNG ALS NEUROKININ- INSBESONDERE ALS NEUROKININ-1-ANTAGONISTEN
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申请号: EP96901800.0申请日: 1996-02-09
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公开(公告)号: EP0810991A1公开(公告)日: 1997-12-10
- 发明人: GERSPACHER, Marc , VON SPRECHER, Andreas , ROGGO, Silvio , MAH, Robert , OFNER, Silvio , VEENSTRA, Siem, Jacob , BETSCHART, Claudia , AUBERSON, Yves , SCHILLING, Walter
- 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: Roth, Bernhard M., et al
- 优先权: EP19950810117 19950222
- 国际公布: WO1996026183 19960829
- 主分类号: C07D249
- IPC分类号: C07D249 ; A61K31 ; A61P1 ; A61P9 ; A61P11 ; A61P25 ; A61P29 ; A61P37 ; A61P43 ; C07C231 ; C07C237 ; C07C255 ; C07C311 ; C07D207 ; C07D209 ; C07D211 ; C07D213 ; C07D215 ; C07D223 ; C07D231 ; C07D233 ; C07D235 ; C07D239 ; C07D241 ; C07D295 ; C07D401 ; C07D403 ; C07D405 ; C07D417 ; C07D471 ; C07D521
摘要:
1-Aryl-2-acylamino-ethane compounds of formula (I), wherein R1 is aryl or heteroaryl; R2 is hydrogen, lower alkyl or aryl-lower alkyl; R3 is hydrogen, lower alkyl, aryl or heteroaryl; R4 is aryl or heteroaryl; X is C1-C7alkylene, C2-C7 alkenyline or C4-C7 alkanedienylene, and Am is an unsubstituted or mono- or di-substituted amino group, a disubstituted amino group being understood as including also an amino group in which the amino nitrogen is bonded into a ring, or a salt thereof, have valuable pharmaceutical properties and are especially effective as NK1 antagonists. They are prepared in a manner known per se.
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