Pharmaceutical compositions containing in combination two antagonists selective of arginine-vassopressin V receptors, even of V1 a and V2 receptors
    2.
    发明授权
    Pharmaceutical compositions containing in combination two antagonists selective of arginine-vassopressin V receptors, even of V1 a and V2 receptors 失效
    药物组合物包含组合两种选择性精氨酸 - 加压素V受体的拮抗剂,即使是V1a和V2受体

    公开(公告)号:US06627649B1

    公开(公告)日:2003-09-30

    申请号:US09622778

    申请日:2000-10-06

    IPC分类号: A61K3140

    摘要: The invention relates to pharmaceutical compositions containing (2S)-1-{(2R,3S)-5-chloro-3-(2-chlorophenyl)-1-(3,4-dimethoxybenzenesulfonyl)-3-hydroxy-2,3-dihydro-1H-indole-2-carbonyl}pyrrolidine-2-carboxamide, a selective V1a arginine vasopressin receptor antagonist, in combination with the equatorial isomer of 1-{4-(N-tert-butylcarbamoyl)-2-methoxybenzenesulfonyl}-5-ethoxy-3-spiro{4-(2-morpholinoethyloxy)cyclohexane}indol-2-one or one of its salts, a selective V2 arginine vasopressin receptor antagonist. The invention relates to the use of such compositions for the production of medicines designed to treat all diseases for which either arginine vasopressin or the V2 receptors are implicated or to treat all diseases related to a water overlead.

    摘要翻译: 本发明涉及含(2S)-1 - {(2R,3S)-5-氯-3-(2-氯苯基)-1-(3,4-二甲氧基苯磺酰基)-3-羟基-2,3- 二氢-1H-吲哚-2-羰基}吡咯烷-2-甲酰胺,选择性V1a精氨酸加压素受体拮抗剂,与1- {4-(N-叔丁基氨基甲酰基)-2-甲氧基苯磺酰基} -5 - 乙氧基-3-螺(4-(2-吗啉代乙氧基)环己烷]吲哚-2-酮或其一种盐,选择性V2精氨酸加压素受体拮抗剂。本发明涉及这种组合物在制备药物中的用途 治疗所有涉及精氨酸加压素或V2受体的疾病或治疗与水过度相关的所有疾病。

    Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
    8.
    发明授权
    Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof 有权
    哌嗪酰基哌啶衍生物,其制备和治疗用途

    公开(公告)号:US07294628B2

    公开(公告)日:2007-11-13

    申请号:US10516808

    申请日:2003-06-05

    CPC分类号: C07D417/14 C07D401/14

    摘要: The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4) alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents the aromatic group 1,3-thiazol-2-yl of formula: Preparation process and therapeutic application.

    摘要翻译: 本发明涉及通式(I)的取代的1-哌嗪基酰基哌啶衍生物,其中n为1或2; R 1表示卤素原子; 三氟甲基; (C 1 -C 4 -C 4)烷基; (C 1 -C 4 -C 4)烷氧基; 三氟甲氧基; R 2表示氢原子或卤素原子; R 3代表氢原子; 一个基团-OR 5; 基团-CH 2或OR 5; 基团-NR 6 R 7; 基团-NR 8 COR 9; 基团-NR 8 CONR 10 R 11; 基团-CH 2 NR 12 R 13; 基团-CH 2 NR 8 CONR 14 R 15 15; (C 1 -C 4 -C 4)烷氧基羰基; 基团-CONR 16 R 17 R 17; 或者R 3 3在其所连接的碳原子和哌啶环的相邻碳原子之间构成双键; R 4代表下式的芳族基团1,3-噻唑-2-基:制备方法和治疗应用。

    Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
    9.
    发明授权
    Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof 有权
    哌嗪酰基哌啶衍生物,其制备和治疗用途

    公开(公告)号:US07468368B2

    公开(公告)日:2008-12-23

    申请号:US10516704

    申请日:2003-06-05

    CPC分类号: C07D417/14 C07D401/14

    摘要: The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; p is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents an aromatic group selected from: the said aromatic groups being unsubstituted or being mono- or disubstituted by a substituent selected independently from a halogen atom; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethyl radical; Preparation process and therapeutic application.

    摘要翻译: 本发明涉及通式(I)的取代的1-哌嗪基酰基哌啶衍生物,其中n为1或2; p为1或2; R1表示卤素原子; 三氟甲基; (C1-C4)烷基; (C 1 -C 4)烷氧基; 三氟甲氧基; R2表示氢原子或卤素原子; R3表示氢原子; 一组-OR5; 基团-CH 2 OR 5; 基团-NR 6 R 7; 一个-NR8COR9基团; 一组-NR8CONR10R11; 基团-CH 2 NR 12 R 13; 基团-CH2NR8CONR14R15; (C1-C4)烷氧基羰基; 一组-CONR16R17; 或者R 3构成与其连接的碳原子和哌啶环的相邻碳原子之间的双键; R 4表示选自以下的芳族基团:所述芳族基团是未取代的或被独立地选自卤素原子的取代基单取代或二取代; (C1-C4)烷基; (C 1 -C 4)烷氧基; 三氟甲基; 制备工艺及治疗应用。