公开(公告)号：EP1289955A1

公开(公告)日：2003-03-12

申请号：EP01951591.5

申请日：2001-06-13

申请人： SMITHKLINE BEECHAM PLC

发明人： BRANCH, Clive, Leslie,c/o GlaxoSmithKline ,  JOHNSON, Christopher, Norbert,c/o GlaxoSmithKline ,  STEMP, Geoffrey,c/o GlaxoSmithKline ,  THEWLIS, Kevin,c/o GlaxoSmithKline

IPC分类号： C07D211/26 ,  C07D417/06 ,  C07D401/10 ,  C07D417/14 ,  C07D413/14 ,  C07D413/06 ,  C07D471/04 ,  C07D401/06 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  A61K31/501 ,  A61P3/04

CPC分类号： C07D401/06 ,  C07D211/26 ,  C07D401/10 ,  C07D405/06 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/06 ,  C07D417/14 ,  C07D471/04

摘要： Compounds of formula (I) wherein Y represents a group (CH2)n, wherein n represents 0, 1 or 2; R1 is phenyl, naphthyl, a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; or a group NR3R4 wherein one of R?3 and R4¿ is hydrogen or optionally substituted (C¿1-4?)alkyl and the other is phenyl, naphthyl or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S, or R?3 and R4¿ together with the N atom to which they are attached form a 5 to 7-membered cyclic amine which has an optionally fused phenyl ring; any of which R1 groups may be optionally substituted; R2 represents phenyl or a 5- or 6-membered hereroaryl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heteroaryl group is substituted by R5, and further optional substituents; or R2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R5 represents an optionally substituted (C¿1-4?)alkoxy, halo, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6-membered heterocyclic ring containing up to 3 heteroatoms selected from N, O and S; or pharmaceutically acceptable salts thereof.

公开(公告)号：EP1385845A1

公开(公告)日：2004-02-04

申请号：EP02722482.3

申请日：2002-05-02

申请人： SMITHKLINE BEECHAM PLC

发明人： BRANCH, Clive, Leslie,c/o GlaxoSmithKline ,  COULTON, Steven,c/o GlaxoSmithKline ,  JOHNS, Amanda,c/o GlaxoSmithKline ,  JOHNSON, Christopher, Norbert,c/o GlaxoSmithKlin ,  PORTER, Roderick, Alan,c/o GlaxoSmithKline ,  STEMP, Geoffrey,c/o GlaxoSmithKline ,  THEWLIS, Kevin,c/o GlaxoSmithKline

IPC分类号： C07D417/14 ,  A61K31/445 ,  C07D413/12 ,  C07D413/14 ,  C07D401/12 ,  A61K31/505 ,  C07D471/04 ,  A61K31/5377 ,  C07D401/14 ,  C07D498/04 ,  C07D403/14 ,  A61P25/20 ,  A61P9/10 ,  A61P3/04

CPC分类号： C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/14 ,  C07D409/14 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

摘要： This invention relates to N-aroyl cyclic amine derivatives and their use as orexin antagonists wherein: Y represents a bond, oxygen, or a group (CH2)n, wherein n represents 1, 2 or 3; m represents 1, 2, or 3; p represents O or 1; X is NR, wherein R is H or (C1-4)alkyl; Ar1 is aryl, or a mono or bicyclic heteroaryl group containing up to 3 heteroatoms selected from N, O and S; any of which may be optionally substituted; A2 represents phenyl or a 5- or 6-membered heterocyclyl group containing up to 3 heteroatoms selected from N, O and S, wherein the phenyl or heterocyclyl group is substituted by R1 and further optional substituents; or Ar2 represents an optionally substituted bicyclic aromatic or bicyclic heteroaromatic group containing up to 3 heteroatoms selected from N, O and S; R1 represents hydrogen, optionally substituted (C¿1-4?)alkoxy, halo, cyano, optionally substituted (C1-6)alkyl, optionally substituted phenyl, or an optionally substituted 5- or 6- membered heterocyclyl group containing up to 4 heteroatoms selected from N, O and S; when Ar?1¿ is aryl p is not 1; or a pharmaceutical acceptable salt thereof.