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    PHARMACEUTICAL COMPOSITIONS COMPRISING NK1 RECEPTOR ANTAGONISTS AND SODIUM CHANNEL BLOCKERS
    6.
    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。

    Pharmaceutical compositions comprising 2-methoxy-5-(5-trifluoromethyl-tetrazol-1-yl-benzyl)-(2S-phenylpiperidin-3S-yl-)
    7.
    发明授权
    Pharmaceutical compositions comprising 2-methoxy-5-(5-trifluoromethyl-tetrazol-1-yl-benzyl)-(2S-phenylpiperidin-3S-yl-) 失效
    包含2-甲氧基-5-（5-三氟甲基 - 四唑-1-基 - 苄基） - （2S-苯基哌啶-3S-基） -

    公开(公告)号：US08093268B2

    公开(公告)日：2012-01-10

    申请号：US12524434

    申请日：2008-01-21

    申请人： Giuseppe Alvaro ,  Charles Large

    发明人： Giuseppe Alvaro ,  Charles Large

    IPC分类号： A61K31/454

    CPC分类号： A61K31/505 ,  A61K31/401 ,  A61K31/4015 ,  A61K31/4025 ,  A61K31/53 ,  A61K45/06 ,  A61K2300/00

    摘要： The present invention relates to pharmaceutical compositions comprising the NK1 receptor antagonist [2-Methoxy-5-(5-trifluoromethyl-tetrazol-1-yl)-benzyl]-(2S-phenyl-piperidin-3S-yl)-amine, or a pharmaceutically acceptable salt or solvate thereof, and a sodium channel blocker, as a combined preparation for simultaneous or sequential administration and to the use of such compositions in the treatment of certain disorders, including epilepsy, mood disorders and pain.

    摘要翻译： 本发明涉及包含NK1受体拮抗剂[2-甲氧基-5-（5-三氟甲基 - 四唑-1-基） - 苄基] - （2S-苯基 - 哌啶-3-基） - 胺的药物组合物，或 药物可接受的盐或溶剂合物，以及钠通道阻断剂，作为同时或连续施用的组合制剂，以及用于治疗某些疾病，包括癫痫，情绪障碍和疼痛的组合物。

    PHARMACEUTICAL COMPOSITIONS COMPRISING NK1 RECEPTOR ANTAGONISTS AND SODIUM CHANNEL BLOCKERS
    9.
    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：US20090318530A1

    公开(公告)日：2009-12-24

    申请号：US12524422

    申请日：2008-01-21

    申请人： Giuseppe Alvaro ,  Charles Large

    发明人： Giuseppe Alvaro ,  Charles Large

    IPC分类号： A61K31/401

    CPC分类号： A61K31/401 ,  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; q is 1 or 2; R3 and R4 are hydrogen; or when q is 1, R3 and R4, together with the interconnecting atoms, may form a cyclopropane ring; X is carbon or nitrogen; n is 0, 1 or 2, wherein when present each R5 is independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; and either R6 or R7 is —O—R8 or —OCH2R8, wherein the other R6 or R7 is hydrogen or R5; and wherein R8 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; q为1或2; R3和R4是氢; 或当q为1时，R3和R4与互连原子一起可形成环丙烷环; X是碳或氮; n为0,1或2，其中当存在时，每个R 5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; R6或R7是-O-R8或-OCH2R8，其中R6或R7是氢或R5; 并且其中R8是苯环或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。