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    Cyclic Amine Derivatives, Processes For Their Preparation, And Pharmaceutical Compositions Containing Them
    1.
    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。

    Cyclic amine derivatives, processes for their preparation, and pharmaceutical compositions containing them
    2.
    发明申请
    Cyclic amine derivatives, processes for their preparation, and pharmaceutical compositions containing them 审中-公开

    公开(公告)号：US20070073061A1

    公开(公告)日：2007-03-29

    申请号：US10554822

    申请日：2004-05-07

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

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

    IPC分类号： A61K31/452 ,  A61K31/445 ,  C07D405/02 ,  C07D211/26

    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.

    N-benzyl-3-phenyl-3-heterocyclyl-propionamide compounds as tachykinin and/or serotonin reuptake inhibitors
    3.
    发明申请
    N-benzyl-3-phenyl-3-heterocyclyl-propionamide compounds as tachykinin and/or serotonin reuptake inhibitors 审中-公开
    N-苄基-3-苯基-3-杂环基 - 丙酰胺化合物作为速激肽和/或5-羟色胺再摄取抑制剂

    公开(公告)号：US20060058348A1

    公开(公告)日：2006-03-16

    申请号：US10521159

    申请日：2003-07-02

    申请人： Giuseppe Alvaro ,  Francesca Cardullo ,  Lucilla D'Adamo ,  Elisabeth Piga ,  Catia Seri

    发明人： Giuseppe Alvaro ,  Francesca Cardullo ,  Lucilla D'Adamo ,  Elisabeth Piga ,  Catia Seri

    IPC分类号： C07D211/26 ,  A61K31/445

    CPC分类号： C07D207/08 ,  A61K31/40 ,  A61K31/44 ,  A61K31/445 ,  A61K31/535 ,  C07D207/20 ,  C07D211/34 ,  C07D211/38 ,  C07D211/70 ,  C07D213/56 ,  C07D265/30

    摘要： The present invention relates to heterocyclic derivatives of formula (I) wherein R represents halogen, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy; R1 represents a 5 or 6 membered heteroaryl group, in which the 5-membered heteroaryl group contains at least one heteroatom selected from oxygen, sulphur or nitrogen and the 6-membered heteroaryl group contains from 1 to 3 nitrogen atoms, or R1 represents a 4, 5 or 6 membered heterocyclic group, wherein saids 5 or 6 membered heteroaryl or the 4, 5 or 6 membered heterocyclic group may optionally be substituted by one to three substituents, which may be the same or different, selected from (CH2)pR6, wherein p is zero or an integer from 1 to 4 and R6 is selected from: halogen, C1-4alkoxy, C1-4alkyl, C3-7cycloalkyl, C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy, hydroxy, cyano, nitro, trifluoromethyl, carboxy, NH(C1-4 alkyl), N(C1-4 alkyl)2 NH(C3-7 cycloalkyl), N(C1-4 alkyl)(C3-7 cycloalkyl); NH(C1-4alkylOC1-4alkoxy), OC(O)NR7R8, NR8C(O)R7 or C(O)NR7R8; R2 represents hydrogen, or C1-4 alkyl; R3 and R4 independently represent hydrogen, C1-4 alkyl or R3 together with R4 represents C3-7 cycloalkyl; R5 represents trifluoromethyl, S(O)qC1-4 alkyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy, halogen or cyano; R7 and R8 independently represent hydrogen, C1-4 alkyl or C3-7 cycloalkyl; L is a single or a double bond; n is an integer from 1 to 3; m is zero or an integer from 1 to 3; q is zero or an integer from 1 to 2; provided that a) when L is a double bond, R1 is not an optionally substituted 5 or 6 membered heteroaryl group, in which the 5-membered heteroaryl group contains at least one heteroatom selected from oxygen, sulphur or nitrogen and the 6-membered heteroaryl group contains from 1 to 3 nitrogen atoms; b) the group R1 is linked to the carbon atom shown as * via a carbon atom; and c) when the heteroatom contained in the group R1 is substituted, p is not zero; and pharmaceutically acceptable salts and solvates thereof; process for their preparation 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： 本发明涉及式（I）的杂环衍生物，

    Chemical compounds
    5.
    发明申请
    Chemical compounds 审中-公开

    公开(公告)号：US20060128752A1

    公开(公告)日：2006-06-15

    申请号：US10520143

    申请日：2003-07-02

    申请人： Giuseppe Alvaro ,  Francesca Cardullo ,  Romano Di Fabio ,  Riccardo Giovannini ,  Elisabeth Piga ,  Maria Tranquillini

    发明人： Giuseppe Alvaro ,  Francesca Cardullo ,  Romano Di Fabio ,  Riccardo Giovannini ,  Elisabeth Piga ,  Maria Tranquillini

    IPC分类号： A61K31/445 ,  C07D211/06

    CPC分类号： C07D211/34 ,  C07D211/64 ,  C07D223/04 ,  C07D223/06

    摘要： The present invention relates to cyclic amine derivatives of formula(l) wherein R represents halogen, C1-4 alkyl, cyano, C1-4 alkoxy, trifluoromethyl or trifluoromethoxy; R1 represents hydrogen, halogen, C3-7cycloalkyl, hydroxy, nitro, cyano or C1-4 alkyl optionally substituted by halogen, cyano or C1-4 alkoxy; R2 represents hydrogen or C1-4 alkyl; R3 and R4 independently represent hydrogen, cyano, C1-4 alkyl or R3 together with R4 represents C3-7 cycloalkyl; R5 represents trifluoromethyl, S(O)t C1-4 alkyl, C1-4 alkyl, C1-4 alkoxy, trifluoromethoxy, halogen or cyano; R6 represents hydrogen or (CH2)rR7; R7 represents hydrogen, C37 cycloalkyl, NH(C1-4alkylOC1-4alkoxy), NH(C1-4alkyl), N(C1-4alkyl)2, OC(O)NR9R8, NR8C(O)R9 or C(O)NR9R8; R9 and R8 independently represent hydrogen, C1-4 alkyl or C3-7 cycloalkyl; m represents zero or an integer from 1 to 4; n represents 1 or 2; p is zero or an integer from 1 to 3; q is an integer from 1 to 3; r is an integer from 1 to 4; t is 0, 1 or 2; provided that when m is 0, p is 2, q , r and n represent 1, R1, R2,R3, R4, R5 and R7 are hydrogen and R is chlorine, R5 is not iodine; and pharmaceutically acceptable salts and solvates thereof; process for their preparation and their use in the treatment of conditions mediated by tackykinins and/or by selective inhibition of serotonin reuptake transporter protein.