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    PHARMACEUTICAL COMPOSITIONS COMPRISING NK1 RECEPTOR ANTAGONISTS AND SODIUM CHANNEL BLOCKERS
    58.
    发明申请
    PHARMACEUTICAL COMPOSITIONS COMPRISING NK1 RECEPTOR ANTAGONISTS AND SODIUM CHANNEL BLOCKERS 审中-公开
    包含NK1受体拮抗剂和钠通道阻断剂的药物组合物

    公开(公告)号：US20090326032A1

    公开(公告)日：2009-12-31

    申请号：US12524429

    申请日：2008-01-21

    申请人： Giuseppe Alvaro ,  Charles Large

    发明人： Giuseppe Alvaro ,  Charles Large

    IPC分类号： A61K31/407

    CPC分类号： A61K31/4015 ,  A61K31/401 ,  A61K31/407 ,  A61K2300/00

    摘要： The present invention relates to pharmaceutical compositions comprising an NK1 receptor antagonist and a sodium channel blocker compound of formula (I) wherein R1 and R2 are independently hydrogen, C1-6alkyl or C3-6cycloalkylC1-6alkyl; or R1 and R2, together with the nitrogen to which they are attached, may form an unsubstituted 3-, 4-, 5- or 6-membered saturated ring; R3 is C1-6alkyl, C1-6haloalkyl, C1-3alkoxyC1-3alkyl or C1-3haloalkoxyC1-3alkyl; or R1 and R3, together with the interconnecting atoms, form a saturated or unsaturated 4- to 6-membered ring; X is carbon or nitrogen; n is 0, 1 or 2, wherein when present each R4 is independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; q is 1 or 2; either R5 or R6 is —O—R7 or —OCH2R7, wherein the other R5 or R6 is hydrogen or R4; and wherein R7 is either a phenyl ring or a 5- or 6-membered aromatic heterocyclic ring (independently containing one or more nitrogen, sulphur or oxygen atoms) wherein either the phenyl ring or the heterocyclic ring is optionally substituted by one or more groups independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; or a pharmaceutically acceptable salt or solvate thereof; as a combined preparation for simultaneous or sequential administration, and to the use of such compositions in the treatment of certain disorders, including epilepsy and mood disorders.

    摘要翻译： 本发明涉及包含NK1受体拮抗剂和式（I）的钠通道阻断剂化合物的药物组合物，其中R 1和R 2独立地是氢，C 1-6烷基或C 3-6环烷基C 1-6烷基; 或R 1和R 2与它们所连接的氮一起可以形成未取代的3-，4-，5-或6-元饱和环; R 3是C 1-6烷基，C 1-6卤代烷基，C 1-3烷氧基C 1-3烷基或C 1-3卤代烷氧基C 1-3烷基; 或R 1和R 3与互连原子一起形成饱和或不饱和的4-至6-元环; X是碳或氮; n为0,1或2，其中当存在时，每个R 4独立地选自C 1-3烷基，卤素，氰基，卤代C 1-3烷基，羟基，C 1-3烷氧基和C 1-3卤代烷氧基; q为1或2; R5或R6是-O-R7或-OCH2R7，其中R5或R6是氢或R4; 并且其中R 7为苯环或5或6元芳族杂环（独立地含有一个或多个氮，硫或氧原子），其中苯环或杂环任选被一个或多个独立地基团取代 选自C 1-3烷基，卤素，氰基，卤代C 1-3烷基，羟基，C 1-3烷氧基和C 1-3卤代烷氧基; 或其药学上可接受的盐或溶剂化物; 作为同时或连续给药的组合制剂，以及这些组合物在治疗某些疾病（包括癫痫和情绪障碍）中的用途。

    Cyclic amine derivatives, processes for their preparation, and pharmaceutical compositions containing them
    59.
    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.

    Spiro (piperidine-4,2′-pyrrolidine)-1-(3,5-trifluoromethyl phenyl) methylcarboxamides as NK1 tachikynin receptor antagonists
    60.
    发明授权
    Spiro (piperidine-4,2′-pyrrolidine)-1-(3,5-trifluoromethyl phenyl) methylcarboxamides as NK1 tachikynin receptor antagonists 有权
    螺（哌啶-4,2'-吡咯烷）-1-（3,5-三氟甲基苯基）甲基甲酰胺作为N​​K1振动子受体拮抗剂

    公开(公告)号：US08367692B2

    公开(公告)日：2013-02-05

    申请号：US12989699

    申请日：2009-04-29

    申请人： Giuseppe Alvaro ,  Emiliano Castiglioni ,  Agostino Marasco

    发明人： Giuseppe Alvaro ,  Emiliano Castiglioni ,  Agostino Marasco

    IPC分类号： A61K31/438 ,  C07D401/04 ,  C07D471/10

    CPC分类号： C07D471/10 ,  C07D498/20

    摘要： Compounds of formula (I) or a pharmaceutically acceptable salt thereof. wherein R is hydrogen or C1-4 alkyl; R1 is hydrogen, C1-4 alkyl, C(O)OH, C(O)NH2 or (C1-4 alkylene)R10; R2 and R3 are independently hydrogen, C1-4 alkyl or R2 together with R3 and together with the carbon atom to which they are attached form a C3-8 cycloalkyl group; R4 is C1-4 alkyl, C1-4 alkoxy or halogen; R5 and R7 are independently hydrogen, hydroxy, halogen, C(O)NH2, C(O)OH or (C1-4 alkylene)R10; R6 and R8 are independently hydrogen or halogen; R9 is hydrogen, (C1-4 alkylene)R10, C(O)NH2, C(O)OH or R9 together with R form a 6 membered heterocyclic ring optionally containing a further heteroatom selected from oxygen, sulphur or nitrogen; R10 is hydrogen, halogen, hydroxy, C(O)NH2, C(O)NH(C1-4 alkyl), C(O)N(C1-4 alkyl)2 or C(O)OH; n is 0, 1 or 2. processes for their preparation, to compositions containing them and to their use in the treatment of diseases and conditions for which antagonism of NK1 is beneficial.

    摘要翻译： 式（I）化合物或其药学上可接受的盐。 其中R是氢或C 1-4烷基; R 1是氢，C 1-4烷基，C（O）OH，C（O）NH 2或（C 1-4亚烷基）R 10; R2和R3独立地为氢，C1-4烷基或R2与R3一起并与它们所连接的碳原子一起形成C 3-8环烷基; R4是C1-4烷基，C1-4烷氧基或卤素; R 5和R 7独立地是氢，羟基，卤素，C（O）NH 2，C（O）OH或（C 1-4亚烷基）R 10; R6和R8独立地是氢或卤素; R9是氢，（C1-4亚烷基）R10，C（O）NH2，C（O）OH或R9与R一起形成任选地含有另外选自氧，硫或氮的杂原子的6元杂环; R 10是氢，卤素，羟基，C（O）NH 2，C（O）NH（C 1-4烷基），C（O）N（C 1-4烷基）2或C（O） n为0,1或2.其制备方法，含有它们的组合物及其在治疗NK1拮抗作用有益的疾病和病症中的用途。