- 专利标题: Cyclic amine derivatives, processes for their preparation, and pharmaceutical compositions containing them
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申请号: US10554822申请日: 2004-05-07
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公开(公告)号: US20070073061A1公开(公告)日: 2007-03-29
- 发明人: Giuseppe Alvaro , Luca Arista , Francesca Cardullo , Lucilla D'Adamo , Aldo Feriani
- 申请人: Giuseppe Alvaro , Luca Arista , Francesca Cardullo , Lucilla D'Adamo , Aldo Feriani
- 申请人地址: GB Greenford, Middlesex UB6 0NN
- 专利权人: Glaxo Group Limited
- 当前专利权人: Glaxo Group Limited
- 当前专利权人地址: GB Greenford, Middlesex UB6 0NN
- 优先权: GB0310724.0 20030509
- 国际申请: PCT/EP04/05005 WO 20040507
- 主分类号: A61K31/452
- IPC分类号: A61K31/452 ; A61K31/445 ; C07D405/02 ; C07D211/26
摘要:
A compound of formula (I) wherein R is a radical selected from in which R7 is halogen, cyano, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy; p is an integer from 0 to 3; R1 is hydrogen, halogen, cyano, C2-4 alkenyl, C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy; R2 is hydrogen or C1-4 alkyl; R3 and R4 independently are hydrogen, C1-4 alkyl or R3 together with R4 is C3-7 cycloalkyl; R5 is phenyl substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl, naphthyl substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl, a 9 to 10 membered fused bicyclic heterocyclic group substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl or R5 is a 5 or 6 membered heteroaryl group substituted by 1 to 3 groups independently selected from trifluoromethyl, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethoxy, halogen or (SO)rC1-4 alkyl; R6 is hydrogen or (CH2)qR8; R8 is hydrogen, C3-7 cycloalkyl, C1-4 alkoxy, amine, C1-4 alkylamine, (C1-4 alkyl)2amine, OC(O)NR9R10 or C(O)NR9R10; R9 and R10 independently are hydrogen, C1-4 alkyl or C3-7 cycloalkyl; m is zero or 1; n is 1 or 2; q is an integer from 1 to 4; r is 1 or 2; or pharmaceutically acceptable salts and solvates thereof; processes for their preparation to pharmaceutical compositions containing them and their use in the treatment of conditions mediated by tachykinins and/or by selective inhibition of serotonin reuptake transporter protein.
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