发明名称 5-HT4 receptor antagonist
摘要 PCT No. PCT/EP94/01583 Sec. 371 Date Nov. 22, 1995 Sec. 102(e) Date Nov. 22, 1995 PCT Filed May 16, 1994 PCT Pub. No. WO94/27987 PCT Pub. Date Dec. 8, 1994Compounds of formula (I) and pharmaceutically acceptable salts thereof, and the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof: X-CO-CH2-Z(I) wherein X is a monocyclic or polycyclic aromatic group, Z is of sub-formula (h), (j) or (k): <IMAGE> (h) <IMAGE> (j) <IMAGE> (k) wherein n1 is 1, 2, 3 or 4; n2 is 0, 1, 2, 3 or 4; n3 is 2, 3, 4 or 5; q is 0, 1, 2 or 3; p is 0, 1 or 2; m is 0, 1 or 2; R5 is hydrogen, C1-12 alkyl, aralkyl or R5 is (CH2)z-R10 wherein z is 2 or 3 and R10 is selected from cyano, hydroxyl, C1-6 alkoxy, phenoxy, C(O)C1-6 alkyl, COC6H5, -CONR11R12, NR11COR12, SO2NR11R12 or NR11SO2R12 wherein R11 and R12 are hydrogen or C1-6 alkyl; or R5 is straight or branched chain alkylene of chain length 1-6 carbon atoms terminally substituted by aryl, 3 to 8 membered cycloalkyl, 3 to 8 membered heterocyclyl, 5 or 6 membered monocyclic heteroaryl or 9 or 10 membered fused bicyclic heteroaryl linked through carbon, C2-7 alkoxycarbonyl, or secondary or tertiary hydroxy substituted C1-6 alkyl; and R6, R7 and R8 are independently hydrogen or C1-6 alkyl; and R9 is hydrogen or C1-10 alkyl; and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorders are provided.
申请公布号 US5741801(A) 申请公布日期 1998.04.21
申请号 US19950553390 申请日期 1995.11.22
申请人 发明人
分类号 A61K31/44;A61K31/4427;A61K31/445;A61P9/06;A61P43/00;C07D401/06;C07D498/04;(IPC1-7):A61K31/445 主分类号 A61K31/44
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