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

    TETRAHYDROQUINOXALINE UREA DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
    5.
    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.

    Oxophenyl-Cyclohexyl-Propanolamine Derivatives, Production And Use Thereof In Therapeutics
    7.
    发明申请
    Oxophenyl-Cyclohexyl-Propanolamine Derivatives, Production And Use Thereof In Therapeutics 审中-公开
    氧苯基 - 环己基 - 丙醇胺衍生物，其生产和使用

    公开(公告)号：US20100075986A1

    公开(公告)日：2010-03-25

    申请号：US12627536

    申请日：2009-11-30

    申请人： Philippe R. BOVY ,  Roberto CECCHI ,  Tiziano CROCI ,  Olivier VENIER

    发明人： Philippe R. BOVY ,  Roberto CECCHI ,  Tiziano CROCI ,  Olivier VENIER

    IPC分类号： A61K31/4965 ,  C07D211/06 ,  C07D241/04 ,  C07D401/04 ,  A61K31/438 ,  A61K31/4453 ,  A61P1/00 ,  A61P1/06

    CPC分类号： C07D221/20 ,  C07D207/16 ,  C07D209/44 ,  C07D211/16 ,  C07D211/22 ,  C07D211/58 ,  C07D211/62 ,  C07D295/192

    摘要： The invention relates to the compounds of general formula (I) where R1 represents H, a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl being optionally substituted, R2 represents H, a halogen atom, an —S(O)zR3, —NHSO2R3, —NHSO2-phenyl or —NHSO2—(C1-C4)alkylphenyl group where z is equal to 0, 1 or 2 and where R3 represents a (C1-C4)alkyl group, said phenyl being optionally substituted; A is chosen from where n is equal to 0, 1 or 2, R4 and R5 represent H, a (C1-C4)alkyl, hydroxyl, cyano, phenyl, benzyl, piperidyl, —CONH2, —CO-phenyl, —COOR3, —CH(phenyl) (OH) and —C(phenyl)2(OH) group, or R4 and R5 form together an optionally substituted 6-membered aromatic ring, R6 represents H, a (C1-C4)alkyl, phenyl or benzyl group, and B represents a 5- or 6-membered nitrogen-containing heterocycle or homocycle optionally fused with a phenyl group or optionally substituted; their addition salts; their method of preparation and their therapeutic application.

    摘要翻译： 本发明涉及通式（I）的化合物，其中R1表示H，（C1-C4）烷基，-CO（C1-C4）烷基，（C1-C4）烷基苯基或-CO-苯基， 任选取代，R 2表示H，卤素原子，-S（O）z R 3，-NHSO 2 R 3，-NHSO 2 - 苯基或-NHSO 2 - （C 1 -C 4）烷基苯基，其中z等于0,1或2，其中R 3 表示（C1-C4）烷基，所述苯基任选被取代; A选自其中n等于0,1或2，R 4和R 5表示H，a（C 1 -C 4）烷基，羟基，氰基，苯基，苄基，哌啶基，-CONH 2，-CO-苯基，-COOR 3， -CH（苯基）（OH）和-C（苯基）2（OH）基团，或R 4和R 5一起形成任选取代的6元芳环，R 6表示H，（C 1 -C 4）烷基，苯基或苄基 并且B表示任选地与苯基稠合的5-或6-元含氮杂环或任选取代的杂环; 它们的加成盐; 其制备方法及其治疗应用。

    Phenylcyclohexylpropanolamine derivatives, preparation and therapeutic application thereof
    8.
    发明授权
    Phenylcyclohexylpropanolamine derivatives, preparation and therapeutic application thereof 失效

    公开(公告)号：US07453010B2

    公开(公告)日：2008-11-18

    申请号：US10515145

    申请日：2003-05-26

    申请人： Philippe R. Bovy ,  Roberto Cecchi ,  Tiziano Croci ,  Olivier Venier

    发明人： Philippe R. Bovy ,  Roberto Cecchi ,  Tiziano Croci ,  Olivier Venier

    IPC分类号： C07C311/00 ,  A61K31/18

    CPC分类号： C07D317/58 ,  C07C311/08 ,  C07C311/21 ,  C07C317/22 ,  C07C2601/14 ,  C07C2603/18

    摘要： The invention relates to compounds of general formula (I): where R1 represents H or a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl optionally being substituted; R2 represents H, a halogen atom, an —S(O)z(C1-C4)alkyl group, where z is equal to 0, 1 or 2, an —NHSO2(C1-C4)alkyl group, an —NHSO2-phenyl group or an —NHSO2—(C1-C4)alkylphenyl group, said phenyl optionally being substituted; R3 represents an —X—R4 group—in which X represents a bond, an oxygen atom or a —CH2— group and R4 represents H or a —CR5R6—COOR7 group, where R5, R6 and R7 independently represent H or a (C1-C4)alkyl group—a phenyl group optionally substituted or fused with a dioxolane group, a —CO—NR8R9 group—where R8 represents H, a (C1-C4)alkyl group or a (C1-C4)alkyl(C1-C4)alkoxy group and R9 represents a (C1-C4)alkyl(C1-C4)alkoxy group, a —(CH2)n-A group, where n is equal to 0, 1, 2, 3 or 4 and where A represents an indolyl group, a fluorenyl group or a phenyl group which is substituted, an optionally substituted —NH-phenyl group or a —CH(R10)—(CH2)n—COOR11 group, where n is 0, 1, 2 or 3 and where R11 represents H or a (C1-C4)alkyl group and R10 represents H, a (C1-C4)alkyl group or a —CH2-phenyl group, said phenyl optionally being substituted, or a —COOR12 group, where R12 represents H or a (C1-C4)alkyl group; their process of preparation and their therapeutic application.