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    DERIVES DE N-(AMINO-HETEROARYL)-1H-PYRROLOPYRIDINE-2-CARBOXAMIDES, LEUR PRÉPARATION ET LEUR APPLICATION EN THERAPEUTIQUE
    1.
    发明公开
    DERIVES DE N-(AMINO-HETEROARYL)-1H-PYRROLOPYRIDINE-2-CARBOXAMIDES, LEUR PRÉPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 有权
    N-（氨基 - 杂芳基）-1H-吡咯并吡啶-2-甲酰胺衍生物，它们的制备和治疗用途

    公开(公告)号：EP2125811A2

    公开(公告)日：2009-12-02

    申请号：EP07872409.3

    申请日：2007-12-20

    申请人： Sanofi-Aventis

    发明人： DUBOIS, Laurent ,  EVANNO, Yannick ,  GILLE, Catherine ,  MACHNIK, David ,  MALANDA, André

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04 ,  C07D213/74 ,  C07D241/20

    摘要： The invention relates to compounds of the general formula (I) in which: the pyrrolopyridine node is optionally substituted at the 4, 5, 6 and / or 7 carbonated position by one or more identical or different X substituents selected from a hydrogen or halogen atom or a C1C6-alkyl, C3-C7- cycloalkyl, C3-C7cycloalkyl-C1C6-alkylene, C1C6-fluoroalkyl, C1C6-alkoxyl, C3-C7- cycloalkoxyl, C3-C7-cycloalkyl-C1C6-alkylene-O-, C1C6-fluoroalkoxyl, cyano, C1-C6- thioalkyl, -S(O)-C1C6-alkyl, -S(O)-C2-C6-alkyl, SF5, C(O)NR1R2, SO2NR1R2, nitro, NR1R2, OCONR1R2, NR3COR4, NR3CONR1R2, NR3SO2R5, NR3SO2NR1R2, aryl-C1C6- alkylene, heteroaryl-C1C6-alkylene, aryl or heteroaryl group, the aryl and heteroaryl being optionally substituted; Z1, Z2, Z3, Z4 independently represent a nitrogen atom or a C(R6) group, one of which at least corresponds to a nitrogen atom and one of which at least corresponds to a C(R6) group; Z in a cyclic amine bound by the nitrogen atom or cyclic amine bound by the nitrogen and of the formula NraRb; wherein the compounds can be in the base state or in the state of an addition salt for an acid, or in a hydrate or solvate state. The invention also relates to a method for making the same and to the use thereof in therapy.

    DERIVES DE N- (AMINO-HETEROARYL) - 1H-INDOLE-2 -CARBOXAMIDES COMME ANTAGONISTES DES RECEPTEURS DE TYPE TRPV1 OU VR1
    2.
    发明公开
    DERIVES DE N- (AMINO-HETEROARYL) - 1H-INDOLE-2 -CARBOXAMIDES COMME ANTAGONISTES DES RECEPTEURS DE TYPE TRPV1 OU VR1 有权
    N-（氨基杂芳基）-1H-吲哚-2-甲酰胺衍生物及其制备和治疗用途

    公开(公告)号：EP2046775A1

    公开(公告)日：2009-04-15

    申请号：EP07823311.1

    申请日：2007-07-20

    申请人： Sanofi-Aventis

    发明人： DUBOIS, Laurent ,  EVANNO, Yannick ,  MALANDA, André

    IPC分类号： C07D401/12 ,  A61K31/435 ,  A61P25/00 ,  A61P29/00 ,  A61P17/00 ,  A61P3/00 ,  A61P15/00 ,  A61P13/00 ,  A61P31/00 ,  A61P11/00

    CPC分类号： C07D401/12

    摘要： The invention relates to compounds of general formula (I): in which X1 is a hydrogen or halogen atom or a (C1-C6)-alkyl, (C3-C7)-cycloalkyl, (C3-C7)-cycloalkyl-(C1-C3)-alkylene, (C1-C6)-fluoroalkyl, cyano, C(O)NR1R2, nitro, (C1-C6)-thioalkyl, -S(O)-(C1-C6)-alkyl, -S(O)2-(C1-C6)-alkyl, SO2NR1R2, aryl-(C1-C6)-alkylene, aryl or heteroaryl group, the aryl and the heteroaryl being optionally substituted; X2 is a hydrogen or halogen atom or a (C1-C6)-alkyl, (C3-C7)-cycloalkyl, (C3-C7)-cycloalkyl-(C1-C3)-alkylene, (C1-C6)-fluoroalkyl, (C1-C6)-alkoxyl, (C3-C7)-cycloalkyl-(C1-C6)-alkylene-O-, (C1-C6)-fluoroalkoxyl, cyano, C(O)NR1R2, (C1-C6)-thioalkyl, -S(O)-(C1-C6)-alkyl, -S(O)2-(C1-C6)-alkyl, SO2NR1R2, aryl-(C1-C6)-alkylene, aryl or heteroaryl group, the aryl and the heteroaryl being optionally substituted; X3 and X4 are, independently of one another, a hydrogen or halogen atom or a (C1-C6)-alkyl, (C3-C7)-cycloalkyl, (C3-C7)-cycloalkyl-(C1-C3)-alkylene, (C1-C6)-fluoroalkyl, (C1-C6)-alkoxyl, (C3-C7)-cycloalkyl-(C1-C6)-alkylene-O-, (C1-C6)-fluoroalkoxyl, cyano, C(O)NR1R2, nitro, NR1R2, (C1-C6)-thioalkyl, -S(O)-(C1-C6)-alkyl, -S(O)2-(C1-C6)-alkyl, SO2NR1R2, NR3COR4, NR3SO2R5, aryl-(C1-C6)-alkylene, aryl or heteroaryl group, the aryl and the heteroaryl being optionally substituted; Z1, Z2, Z3 and Z4 are, independently of one another, a nitrogen atom or a C(R6) group; n is equal to 0, 1, 2 or 3; Y is an optionally substituted aryl or heteroaryl; Ra and Rb are, independently of one another, a hydrogen atom or a (C1-C6)-alkyl, (C3-C7)-cycloalkyl, (C3-C7)-cycloalkyl-(C1-C3)-alkylene, (C1-C6)-fluoroalkyl, hydroxyl, (C1-C6)-alkoxyl, (C3-C7)-cycloalkyl-(C1-C6)-alkylene-O-, (C1-C6)-fluoroalkoxyl, aryl or heteroaryl group, wherein Ra and Rb may be optionally substituted; in the form of a base or an addition salt with an acid, and also in the form of a hydrate or of a solvate. Process for the preparation thereof and therapeutic use.

    DERIVES DE N-(1 H-INDOLYL)-I H-IND0LE-2-CARB0XAMIDES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE
    3.
    发明公开
    DERIVES DE N-(1 H-INDOLYL)-I H-IND0LE-2-CARB0XAMIDES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 有权
    N-（1 H-吲哚基）-1 H-吲哚-2-甲酰胺衍生物，它们的制备和SO治疗用途

    公开(公告)号：EP1776340A1

    公开(公告)日：2007-04-25

    申请号：EP05793766.6

    申请日：2005-08-02

    申请人： Sanofi-Aventis

    发明人： DUBOIS, Laurent ,  EVANNO, Yannick ,  EVEN, Luc

    IPC分类号： C07D209/42 ,  A61K31/404 ,  A61P29/00

    CPC分类号： C07D209/42

    摘要： The invention concerns compounds of general formula (I), wherein: X1, X2, X3, X4, Z1, Z2, Z3, Z4 and Z5 represent, independently of one another, a hydrogen or halogen atom, or a C1-C6-alkyl, C3-C7-cycloalkyl, C1-C6-fluoroalkyl, C1-C6-alkoxy, C1-C6-fluoroalkoxy, cyano, C(O)NR1R2, nitro, NR1R2, C1-C6-thioalkyl, -S(O)-C1-C6-alkyl, -S(O)2-C1-C6-alkyl, SO2NR1R2, NR3COR4, NR3SO2R5, or aryl group; X5 represents a hydrogen or halogen atom or a C1-C6-alkyl, C1-C6-fluoroalkyl group; R represents a 4-, 5-, 6- or 7-indolyl group optionally substituted; Y represents a hydrogen atom or a C1-C6-alkyl group; n is equal to 0, 1, 2 or 3; R1 and R2, represent, independently of each other a hydrogen atom or a C1-C6-alkyl, C3-C7-cycloalkyl, C3-C7-cycloalkyl-C1-C3-alkyl, or aryl group; or R1 and R2 together with the nitrogen atom bearing them form a azetidine, pyrrolidine, piperidine, azepine, morpholine, thiomorpholine, piperazine, homopiperazine group, said group being optionally substituted by C1-C6-alkyl, C3-C7-cycloalkyl, C3-C7-cycloalkyl-C1-C3-alkyl or aryl group; R3 and R4 represent, independently of each other, a hydrogen atom or a C1-C6-alkyl or aryl group; R5 represents a C1-C6-alkyl or aryl group; in base or acid addition salt, hydrate or solvate form. The invention also concerns a method for preparing said compounds and their therapeutic use.