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    DÉRIVÉS D'URÉE DE TETRAHYDROQUINOXALINE, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE J
    1.
    发明公开
    DÉRIVÉS D'URÉE DE TETRAHYDROQUINOXALINE, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE J 有权
    四氢脲衍生物，其制备和治疗应用

    公开(公告)号：EP2238126A2

    公开(公告)日：2010-10-13

    申请号：EP09720707.0

    申请日：2009-01-27

    申请人： Sanofi-Aventis

    发明人： BRAUN, Alain ,  CRESPIN, Olivier ,  NAMANE, Claudie ,  NICOLAI, Eric ,  PACQUET, François ,  PASCAL, Cécile ,  PHILIPPO, Christophe ,  VENIER, Olivier

    IPC分类号： C07D401/12 ,  C07D401/10 ,  C07D417/04 ,  A61K31/495 ,  A61K31/506 ,  A61P3/00 ,  A61P9/12 ,  A61P25/28 ,  A61P27/06

    CPC分类号： C07D239/26 ,  C07D241/44 ,  C07D401/10 ,  C07D401/12

    摘要： The invention relates to compounds of the formula (I) in which: A is a bond, an oxygen atom, or a -0-CH
    2 - group; Ar
    1 is a phenyl or heteroaryl group; Ar
    2 is a phenyl, heteroaryl or heterocycloalkyl group; R
    1a,b,c and R
    2a,b,c are a hydrogen or halogen atom or an alkyl, cycloalkyl, -alkyl-cycloalkyl group optionally substituted by one or more halogen atoms, -OR
    5 (hydroxy ou alkoxy), hydroxy- alkyl, alkoxy-alkyl, alkoxy-alkoxy, halogenoalkyl, -O-halogenoalkyl, oxo, -CO- alkyl, -CO-alkyl-NR6R7, -CO-halogenoalkyl, -COOR5, alkyl-COOR5, -O-alkyl- COOR
    5, -SO
    2 -alkyl, -SO
    2 -cycloalkyl, -SO
    2 -alkyl-cycloalkyl, -SO
    2 -alkyl-OR
    5 , -SO
    2 - alkyl-COOR
    5, -SO
    2 -alkyl-NR
    6 R
    7 -S0
    2 -halogenoalkyl, alkyl-S0
    2 -alkyl, -SO
    2 -NR
    6 R
    7, - SO
    2 -alkyl-O-alkyl-OR
    5 , -CONR
    6 R
    7 , -alkyl-CONR
    6 R
    7 or -O-alkyl-NR
    6 R
    7 , or R
    1a R
    1b , R
    1c are respectively bonded to R
    2a, R
    2b, R
    2c and to the carbon atom bearing them and represent -O-alkyl-0-; R
    3 is a hydrogen atom or an alkyl group; R
    4 is a hydrogen or halogen atom or a cyano group, -OR
    5, hydroxy-alkyl, -COOR
    5 , -NR
    6 R
    7 , -CONR
    6 R
    7, -SO
    2 -alkyl or -SO
    2 -NR
    6 R
    7 , -NR
    6 - COOR
    5 , -NR
    6 -COR
    5, -CO-NR
    6 -alkyl-OR
    5 ;; R
    5 , R
    6 and R
    7 are a hydrogen atom, an alkyl or –alkyl-phenyl group; and R
    8 is a hydrogen atom, a -SO
    2 -alkyl group or a group of the formula –B-Het in which B can be absent or represents a bond, an oxygen atom or a -CO- ou -SO
    2 - (CH
    2 )n group with n equal to 0, 1 or 2, and Het is a heteroaryl or heterocycloalkyl optionally substituted by alkyl, -SO
    2 -alkyl and - COOR
    5 groups. The invention also relates to a method for making the same and to the therapeutic application thereof.

    INDAZOLES SUBSTITUES, LEUR PREPARATION ET LEUR UTILISATION EN THERAPEUTIQUE
    3.
    发明公开
    INDAZOLES SUBSTITUES, LEUR PREPARATION ET LEUR UTILISATION EN THERAPEUTIQUE 审中-公开
    新的取代的吲唑和其生产和使用治疗剂

    公开(公告)号：EP2170865A2

    公开(公告)日：2010-04-07

    申请号：EP08826411.4

    申请日：2008-06-18

    申请人： Sanofi-Aventis

    发明人： ALETRU, Michel ,  DAMOUR, Dominique ,  MONSEAU, Catherine ,  MOUGENOT, Patrick ,  NAMANE, Claudie ,  NARDI, Frederico ,  NEMECEK, Patrick ,  PHILIPPO, Christophe

    IPC分类号： C07D401/12 ,  C07D401/14 ,  A61K31/416

    CPC分类号： C07D401/14 ,  C07D401/12

    摘要： The invention relates to compounds of formula (I) wherein: E is a grouping (i) of formula -NT-CO-O- or -NT-CX-NT'- wherein X is =O or =S and T and T', that can be identical or different and selected independently, from H or an alkyl group, or (ii) forming a five-membered or six-membered ring bound in position 5 or 6 of the indazole nucleus by -NT- or by the nitrogen atom N1; R1 is at least one substituent selected independently when there are several, and being a halogen atom, an alkyl, alkenyl, alkynyl, halogenoalkyl, halogenoalcoxy, aryl, heteroaryl, heterocycloalkyl, cycloalkyl, CN, NRR', OR, NO2, COOR, CONRR', or NRCOR' group; R2 is a hydrogen atom, or an alkyl, alkenyl or alkynyl group; R3 is at least one substituent selected independently when there are several, and being a hydrogen atom, an alkyl, alkenyl, alkynyl, halogenoalcoxy, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, CN, NRR', CF3, OR, NO2, COOR, CONRR', or NRCOR' group; R4 is a hydrogen atom or a halogen atom, an alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycloalkyl, -NR-CO-R', COOR, NRR', CHO, or CONR(OR') group; R and R' are identical or different and are independently a hydrogen atom, or an alkyl, aryl, heterocycloalkyl, cycloalkyl or heteroaryl group; and n1 is a whole number between 0 and 5, and n3 is a whole number between 0 and 3.