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    Cyclic Amine Derivatives, Processes For Their Preparation, And Pharmaceutical Compositions Containing Them
    6.
    发明申请
    Cyclic Amine Derivatives, Processes For Their Preparation, And Pharmaceutical Compositions Containing Them 审中-公开
    环胺衍生物，其制备方法以及含有它们的药物组合物

    公开(公告)号：US20090192194A1

    公开(公告)日：2009-07-30

    申请号：US11869945

    申请日：2007-10-10

    申请人： Giuseppe Alvaro ,  Luca Arista ,  Francesca Cardullo ,  Lucilla D'Adamo ,  Aldo Feriani ,  Riccardo Giovannini ,  Catia Seri

    发明人： Giuseppe Alvaro ,  Luca Arista ,  Francesca Cardullo ,  Lucilla D'Adamo ,  Aldo Feriani ,  Riccardo Giovannini ,  Catia Seri

    IPC分类号： A61K31/445 ,  C07D401/02 ,  C07D211/22 ,  A61P25/22

    CPC分类号： C07D405/04 ,  C07D211/34 ,  C07D405/12

    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.

    摘要翻译： 式（I）化合物，其中R为选自其中R 7为卤素，氰基，C 1-4烷基，C 1-4烷氧基，三氟甲基或三氟甲氧基的基团; p是0至3的整数; R 1是氢，卤素，氰基，C 2-4链烯基，任选地被卤素，氰基或C 1-4烷氧基取代的C 1-4烷基; R2是氢或C1-4烷基; R3和R4独立地是氢，C1-4烷基或R3与R4一起是C3-7环烷基; R5是被1-3个独立地选自三氟甲基，C1-4烷基，氰基，C1-4烷氧基，三氟甲氧基，卤素或（SO）rC1-4烷基取代的苯基，被1至3个独立地选自三氟甲基， C 1-4烷基，氰基，C 1-4烷氧基，三氟甲氧基，卤素或（SO）r C 1-4烷基，被1至3个独立地选自三氟甲基，C 1-4烷基，氰基的1-3元基团取代的9至10元稠合双环杂环基 ，C 1-4烷氧基，三氟甲氧基，卤素或（SO）rC 1-4烷基或R 5是被1-3个独立地选自三氟甲基，C 1-4烷基，氰基，C 1-4烷氧基， 三氟甲氧基，卤素或（SO）rC 1-4烷基; R6是氢或（CH2）qR8; R 8为氢，C 3-7环烷基，C 1-4烷氧基，胺，C 1-4烷基胺，（C 1-4烷基）2胺，OC（O）NR 9 R 10或C（O）NR 9 R 10; R9和R10独立地是氢，C1-4烷基或C3-7环烷基; m为零或1; n为1或2; q是1至4的整数; r为1或2; 或其药学上可接受的盐和溶剂化物; 其制备方法用于含有它们的药物组合物及其用于治疗由速激肽介导的病症和/或通过选择性抑制5-羟色胺再摄取转运蛋白。