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    TETRAHYDROQUINOXALINE UREA DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
    4.
    发明申请
    TETRAHYDROQUINOXALINE UREA DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF 有权

    公开(公告)号：US20120165337A1

    公开(公告)日：2012-06-28

    申请号：US13386830

    申请日：2010-07-23

    申请人： Olivier Crespin ,  Eric Nicolai ,  Olivier Venier

    发明人： Olivier Crespin ,  Eric Nicolai ,  Olivier Venier

    IPC分类号： A61K31/498 ,  A61P3/04 ,  A61P3/10 ,  A61P7/00 ,  A61P5/48 ,  A61P3/00 ,  A61P9/12 ,  A61P9/10 ,  A61P25/28 ,  A61P27/06 ,  A61P19/10 ,  A61P9/00 ,  A61P9/04 ,  A61P1/16 ,  A61P31/00 ,  A61P17/02 ,  C07D401/14

    CPC分类号： C07D401/12 ,  C07D401/10

    摘要： The invention relates to compounds of formula (I), where: A is a bond, an oxygen atom, 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 a hydrogen or halogen atom, or an alkyl, cycloalkyl, or lkyl-cycloalkyl group optionally substituted by one or more halogen atoms, or an —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, as well as to the carbon atom having same, and are -alkyl-O—; R3 is a hydrogen atom or an alkyl group; R4 is a ONR6R7 group, a hydroxyalkyl group substituted by a halogenoalkyl group, or an lkyl-NH—SO2-alkyl, NH—SO2-alkyl, —O—SO2—NR6R7, -alkyl-CO—NR6R7, —O-alkyl-CO—NR6R7, -alkyl-NR6R7, —O—CO—NR6R7, -alkyl-heteroaryl, a heteroaryl group optionally substituted by an alkyl, alkoxy-imino, or —NH—NH—CO-alkyl group, with the proviso that R4 is in the cis position when it is the ONR6R7 group and that R6 and R7 are each hydrogen, or an lkyl or lkyl-phenyl group; R5 is hydrogen, an lkyl group, or lkyl-phenyl; R6 and R7, identical or different, are each a hydrogen atom, an alkyl group, alkoxy, or an alkyl-phenyl group; and R8 is a hydrogen atom or an O2-alkyl group, or a group of formula -Het, where B can be absent or be a bond, an oxygen atom, or a O— or O2—(CH2)n group, with n being equal to 0, 1, or 2, and where Het is a heteroaryl or heterocycloaryl optionally substituted by the alkyl, —SO2-alkyl, and —COOR5 groups. The invention also relates to a method for preparing same to the therapeutic use thereof.

    Tetrahydroquinoxaline urea derivatives as modulators of 11β-hydroxysteroid dehydrogenase type 1
    9.
    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。