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    • 3. 发明申请
    • NOVEL PHARMACEUTICAL COMPOSITIONS
    • 新型药物组合物
    • WO2008090116A1
    • 2008-07-31
    • PCT/EP2008/050623
    • 2008-01-21
    • GLAXO GROUP LIMITEDALVARO, GiuseppeLARGE, Charles
    • ALVARO, GiuseppeLARGE, Charles
    • A61K31/401A61P25/08
    • A61K31/401A61K2300/00
    • The present invention relates to pharmaceutical compositions comprising an NK1 receptor antagonist and a sodium channel blocker compound of formula (I) wherein R 1 and R 2 are independently hydrogen, C 1-6 alkyl or C 3-6 cycloalkyl 1-6 galkyl; or R 1 and R 2 , 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; R 3 and R 4 are hydrogen; or when q is 1, R 3 and R 4 , 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 R 5 is independently selected from the list consisting of C 1-3 alkyl, halogen, cyano, haloC 1-3 alkyl, hydroxy, C 1-3 alkoxy and C 1-3 haloalkoxy; and either R 6 or R 7 is -O-R 8 or -OCH 2 R 8 , wherein the other R 6 or R 7 is hydrogen or R 5 ; and wherein R 8 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 C 1-3 alkyl, halogen, cyano, haloC 1-3 alkyl, hydroxy, C 1-3 alkoxy and C 1-3 haloalkoxy; 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.
    • 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 ,其中R 6或R 7是氢或R 5; 并且其中R 8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),其中苯环或杂环是 任选地被一个或多个独立地选自C 1-3烷基,卤素,氰基,卤代C 1-3烷基,羟基,C 1 -C 4烷基, 1-3个烷氧基和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。
    • 5. 发明申请
    • PHARMACEUTICAL COMPOSITIONS COMPRISING NK1 RECEPTOR ANTAGONISTS AND SODIUM CHANNEL BLOCKERS
    • 包含NK1受体拮抗剂和钠通道阻断剂的药物组合物
    • WO2008090115A1
    • 2008-07-31
    • PCT/EP2008/050622
    • 2008-01-21
    • GLAXO GROUP LIMITEDALVARO, GiuseppeLARGE, Charles
    • ALVARO, GiuseppeLARGE, Charles
    • A61K31/704A61K31/4015A61K31/401A61P25/08
    • A61K31/4015A61K31/401A61K31/407A61K2300/00
    • The present invention relates to pharmaceutical compositions comprising an NK1 receptor antagonist and a sodium channel blocker compound of formula (I) wherein R 1 and R 2 are independently hydrogen, C 1-6 alkyl or C 3-6 cycloalkylC 1-6 alkyl; or R 1 and R 2 , together with the nitrogen to which they are attached, may form an unsubstitued 3-, 4-, 5- or 6-membered saturated ring; R 3 is C 1-6 alkyl, C 1-6 haloalkyl, C 1-3 alkoxyC 1-3 alkyl or C 1-3 haloalkoxyC 1-3 alkyl; or R 1 and R 3 , 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 R 4 is independently selected from the list consisting of C 1-3 alkyl, halogen, cyano, haloC 1-3 alkyl, hydroxy, C 1-3 alkoxy and C 1-3 haloalkoxy; q is 1 or 2; either R 5 or R 6 is -O-R 7 or -OCH 2 R 7 , wherein the other R 5 or R 6 is hydrogen or R 4 ; and wherein R 7 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 C 1-3 alkyl, halogen, cyano, haloC 1-3 alkyl, hydroxy, C 1-3 alkoxy and C 1-3 haloalkoxy; 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.
    • 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 ,其中R 5或R 6是氢或R 4; 并且其中R 7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),其中苯环或杂环是 任选地被一个或多个独立地选自C 1-3烷基,卤素,氰基,卤代C 1-3烷基,羟基,C 1 -C 4烷基, 1-3个烷氧基和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。
    • 10. 发明授权
    • PHARMACEUTICAL COMPOSITIONS COMPRISING NK1 RECEPTOR ANTAGONISTS AND SODIUM CHANNEL BLOCKERS
    • 药物制剂含NK1受体拮抗剂和钠通道阻滞化合物
    • EP2117535B1
    • 2011-10-26
    • EP08708027.1
    • 2008-01-21
    • Glaxo Group Limited
    • ALVARO, GiuseppeLARGE, Charles
    • A61K31/401A61P25/08
    • A61K31/401A61K2300/00
    • 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 C3-6cycloalkyl1-6galkyl; 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.