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    TETRAHYDROQUINOXALINE UREA DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
    9.
    发明申请
    TETRAHYDROQUINOXALINE UREA DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF 有权

    公开(公告)号：US20120135958A1

    公开(公告)日：2012-05-31

    申请号：US13386827

    申请日：2010-07-23

    申请人： Claudie Namane ,  Eric Nicolai ,  Francois Pacquet ,  Cecile Pascal ,  Olivier Venier

    发明人： Claudie Namane ,  Eric Nicolai ,  Francois Pacquet ,  Cecile Pascal ,  Olivier Venier

    IPC分类号： A61K31/695 ,  A61K31/498 ,  C07D417/14 ,  C07F7/10 ,  C07D401/14 ,  C07D401/04 ,  A61P37/04 ,  A61P3/04 ,  A61P3/10 ,  A61P3/00 ,  A61P9/10 ,  A61P9/12 ,  A61P27/02 ,  A61P25/00 ,  A61P19/10 ,  A61P9/00 ,  A61P1/16 ,  A61P17/02 ,  A61P31/00 ,  A61K31/541

    CPC分类号： C07D401/10 ,  C07D401/12

    摘要： The invention relates to compounds of formula (I), where: A is a bond, an oxygen, or an —CH2— group; Ar1 is a phenyl or heteroaryl group; Ar2 is a phenyl, heteroaryl, or heterocycloalkyl group; R1a,b,c and R2a,b,c are hydrogen or halogen, or an alkyl, cycloalkyl, or lkyl-cycloalkyl group optionally, substituted by one or more halogen atoms, or a —OR5 (hydroxy or alkoxy), hydroxy-alkyl, alkoxy-alkyl, alkoxy-alkoxy, halogenoalkyl, —O-halogenoalkyl, oxo, —CO-alkyl, —CO-alkyl-NR6R7, —CO-halogenoalkyl, —COOR5, alkyl-COOR5, —O-alkyl-COOR5, —SO2-alkyl, —SO2-cycloalkyl, —SO2-alkyl-cycloalkyl, —SO2-alkyl-OR5, —SO2-alkyl-COOR5, —SO2-alkyl-NR6R7, —SO2-halogenoalkyl, alkyl-SO2-alkyl, —SO2—NR6R7, —SO2-alkyl-O-alkyl-OR5, —CONR6R7, -alkyl-CONR6R7, or -alkyl-NR6R7 group, or further R1a, R1b, and R1c are bonded to R2a, R2b, R2c, respectively, and to the carbon atom having same, and are -alkyl-O—; R3 is a hydrogen atom or an alkyl group; R4 is a hydrogen or halogen atom or a cyano, —OR5, hydroxyalkyl, —COOR5, —NR6R7, ONR6R7, —SO2-alkyl, SO2—NR6R7, —NR6—COOR5, —NR6—COR5, or —CO—NR6-alkyl-OR5 group; R5, R6, and R7 are a hydrogen, or an alkyl or alkyl-phenyl group; and R8 is an alkyl, alkyl-Si(alkyl)3, —SO2-alkyl-Si(alkyl)3, phenyl, alkoxy-imino group, or alkyl-cycloalkyl group optionally substituted by one or more halogen atoms or one or more hydroxyl or hydroxyl-alkyl groups; or R8 and R9, together with the carbon atoms to which they are bonded, form a cycloalkyl group optionally substituted by one or more halogen atoms or one or more carboxy groups; and R9 is a hydrogen atom or an alkyl group; with the proviso that, when R8 is an alkyl group, it is bonded onto the Ar2 silicon atom. The invention also relates to a method for preparing same and to the therapeutic use thereof.

    Tetrahydroquinoxaline urea derivatives as modulators of 11β-hydroxysteroid dehydrogenase type 1
    10.
    发明授权
    Tetrahydroquinoxaline urea derivatives as modulators of 11β-hydroxysteroid dehydrogenase type 1 有权
    四氢喹喔啉脲衍生物作为1型11β-羟基类固醇脱氢酶的调节剂

    公开(公告)号：US08530473B2

    公开(公告)日：2013-09-10

    申请号：US13386827

    申请日：2010-07-23

    申请人： Claudie Namane ,  Eric Nicolai ,  Francois Pacquet ,  Cecile Pascal ,  Olivier Venier

    发明人： Claudie Namane ,  Eric Nicolai ,  Francois Pacquet ,  Cecile Pascal ,  Olivier Venier

    IPC分类号： A61K31/495

    CPC分类号： C07D401/10 ,  C07D401/12

    摘要： The invention relates to a compound of the general formula (I), as defined herein which is useful in modulating the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are useful for treating pathologies in which such modulation is beneficial, as in the case of metabolic syndrome or of noninsulin-dependent type 2 diabetes. The invention also relates to pharmaceutical preparations containing such a compound, processes for preparing and intermediates useful in the preparation of a such a compound.

    摘要翻译： 本发明涉及如本文所定义的通式（I）化合物，其可用于调节1α-型11β-羟类固醇脱氢酶（11betaHSD1）的活性，并且可用于治疗其中这种调节有益的病态，如 代谢综合征或非胰岛素依赖型2型糖尿病的病例。 本发明还涉及含有这种化合物的药物制剂，制备方法和可用于制备这种化合物的中间体。