公开(公告)号：EP0810991A1

公开(公告)日：1997-12-10

申请号：EP96901800.0

申请日：1996-02-09

申请人： Novartis AG

发明人： GERSPACHER, Marc ,  VON SPRECHER, Andreas ,  ROGGO, Silvio ,  MAH, Robert ,  OFNER, Silvio ,  VEENSTRA, Siem, Jacob ,  BETSCHART, Claudia ,  AUBERSON, Yves ,  SCHILLING, Walter

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

CPC分类号： C07D213/40 ,  C07C237/22 ,  C07C255/29 ,  C07C311/51 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07D209/08 ,  C07D209/12 ,  C07D209/20 ,  C07D211/22 ,  C07D211/44 ,  C07D211/48 ,  C07D211/58 ,  C07D213/70 ,  C07D215/46 ,  C07D223/12 ,  C07D231/12 ,  C07D231/38 ,  C07D233/56 ,  C07D235/16 ,  C07D235/28 ,  C07D239/42 ,  C07D241/20 ,  C07D249/08 ,  C07D295/13 ,  C07D295/135 ,  C07D295/185 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D471/10

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.

摘要翻译： PCT No.PCT / EP96 / 00555 Sec。 371日期：1997年8月21日 102（e）日期1997年8月21日PCT提交1996年2月9日PCT公布。 WO96 / 26183 PCT出版物 日期：1961年8月29日 - 其中R 1 -R 4，X和Am如说明书中所定义的式I的芳基-2-酰基氨基乙烷化合物具有有价值的药物性质，并且作为NK-1拮抗剂特别有效。

公开(公告)号：EP0810991B1

公开(公告)日：1999-04-14

申请号：EP96901800.1

申请日：1996-02-09

申请人： Novartis AG ,  Novartis-Erfindungen Verwaltungsgesellschaft m.b.H.

发明人： GERSPACHER, Marc ,  VON SPRECHER, Andreas ,  ROGGO, Silvio ,  MAH, Robert ,  OFNER, Silvio ,  VEENSTRA, Siem, Jacob ,  BETSCHART, Claudia ,  AUBERSON, Yves ,  SCHILLING, Walter

IPC分类号： C07C237/22 ,  A61K31/16 ,  C07D213/40 ,  C07D209/08 ,  C07D211/58 ,  C07C311/51 ,  C07D295/185 ,  C07D295/13 ,  C07D209/12 ,  C07D209/20

CPC分类号： C07D213/40 ,  C07C237/22 ,  C07C255/29 ,  C07C311/51 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07D209/08 ,  C07D209/12 ,  C07D209/20 ,  C07D211/22 ,  C07D211/44 ,  C07D211/48 ,  C07D211/58 ,  C07D213/70 ,  C07D215/46 ,  C07D223/12 ,  C07D231/12 ,  C07D231/38 ,  C07D233/56 ,  C07D235/16 ,  C07D235/28 ,  C07D239/42 ,  C07D241/20 ,  C07D249/08 ,  C07D295/13 ,  C07D295/135 ,  C07D295/185 ,  C07D401/12 ,  C07D403/12 ,  C07D417/12 ,  C07D471/10

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.

公开(公告)号：EP1194421B1

公开(公告)日：2005-10-12

申请号：EP00923603.5

申请日：2000-04-21

申请人： H. LUNDBECK A/S ,  Novartis AG

发明人： MARZABADI, Mohammad, R. ,  WONG, Wai, C. ,  NOBLE, Stewart, A. ,  BUHLMAYER, Peter ,  RUEGER, Heinrich ,  YAMAGUCHI, Yasuchika ,  SCHILLING, Walter

IPC分类号： C07D277/60 ,  A61K31/426 ,  A61K31/428 ,  C07D277/42 ,  C07D417/12 ,  C07D513/04 ,  A61K31/429

CPC分类号： C07D277/60 ,  C07D277/42 ,  C07D417/12 ,  C07D513/04

摘要： This invention is directed to bicyclic and tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. The invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.