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    DERIVATIVES OF TRIAZINES AND URACILS, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPEUTICS
    2.
    发明申请
    DERIVATIVES OF TRIAZINES AND URACILS, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPEUTICS 失效
    TRIAZINES和URACILS的衍生物，其制备及其在人类治疗中的应用

    公开(公告)号：US20110118266A1

    公开(公告)日：2011-05-19

    申请号：US13054293

    申请日：2009-07-07

    申请人： Isabelle Leroy ,  Elisabeth Dupont-Passelaigue ,  Karine Valeille ,  Yves Rival ,  Didier Junquero

    发明人： Isabelle Leroy ,  Elisabeth Dupont-Passelaigue ,  Karine Valeille ,  Yves Rival ,  Didier Junquero

    IPC分类号： A61K31/53 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  A61K31/513 ,  A61P3/00 ,  A61P17/00

    CPC分类号： C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D409/14

    摘要： The present invention relates to derivatives of general formula I wherein: —W represents nitrogen, —R1 represents: •a hydrogen or a linear or branched C1-C5 alkyl radical or, •a C1-C3 alkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C1-C3 alcoxy, C3-C6 alkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C1-C3 N-alkylcarbamoyl groups or, •a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C1-C4 alkyl, linear or branched C1-C3 alkoxy groups, •a C6 2-oxocycloalkyl radical—R2 represents a methyl or heptyl, —m, n are equal to 1, —V represents CH2, —X—Y represents —N— (C═O)—, —CH—O—, —Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C1-C4 alkyl groups.

    摘要翻译： 本发明涉及通式I的衍生物，其中：-W表示氮，-R1表示：●氢或直链或支链C1-C5烷基，或●被基团取代的C1-C3烷基，例如三氟甲基， 腈，羟基，C 1 -C 3烷氧基，C 3 -C 6烷氧基烷氧基，吲哚基，噻吩基，氧代噻吩基，C 1 -C 3 N-烷基氨基甲酰基，或者 - 任选被一个或多个基团取代的苯基或吡啶基或​​萘基， 原子，硝基，腈，三氟甲基，乙烯基，甲基硫烷基，直链支链C 1 -C 4烷基，直链或支链C 1 -C 3烷氧基，C 6 2-氧代环烷基-R 2表示甲基或庚基，-m，n等于 1，-V表示CH 2，-X-Y表示-N-（C = O） - ， - CH-O-，-Z表示被一个或多个三氟甲基取代的苯基，卤素原子或直链C 1 -C 4烷基 团体

    Derivatives of triazines and uracils, their preparation and their application in human therapeutics
    3.
    发明授权
    Derivatives of triazines and uracils, their preparation and their application in human therapeutics 失效
    三嗪和尿嘧啶的衍生物，其制备及其在人类治疗中的应用

    公开(公告)号：US08618287B2

    公开(公告)日：2013-12-31

    申请号：US13054293

    申请日：2009-07-07

    申请人： Isabelle Leroy ,  Elisabeth Dupont-Passelaigue ,  Karine Valeille ,  Yves Rival ,  Didier Junquero

    发明人： Isabelle Leroy ,  Elisabeth Dupont-Passelaigue ,  Karine Valeille ,  Yves Rival ,  Didier Junquero

    IPC分类号： C07D403/04 ,  C07D403/14 ,  C07D401/14 ,  C07D253/075 ,  A61K31/4523 ,  A61K31/496 ,  A61P3/04 ,  A61P3/10

    CPC分类号： C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D409/14

    摘要： The present invention relates to derivatives of general formula I wherein: —W represents nitrogen, —R1 represents: •a hydrogen or a linear or branched C1-C5 alkyl radical or, •a C1-C3 alkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C1-C3 alcoxy, C3-C6 alkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C1-C3 N-alkylcarbamoyl groups or, •a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C1-C4 alkyl, linear or branched C1-C3 alkoxy groups, •a C6 2-oxocycloalkyl radical—R2 represents a methyl or heptyl, -m, n are equal to 1, —V represents CH2, —X—Y represents —N— (C═O)—, —CH—O—, —Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C1-C4 alkyl groups.

    摘要翻译： 本发明涉及通式I的衍生物，其中：-W表示氮，-R1表示：氢或直链或支链C1-C5烷基，或.1,1,3-三氟甲基， 腈，羟基，C 1 -C 3烷氧基，C 3 -C 6烷氧基烷氧基，吲哚基，噻吩基，氧代噻吩基，C 1 -C 3 N-烷基氨基甲酰基，或苯基或吡啶基或​​萘基，或任选被一个或多个基团取代的噻吩基，例如卤素 原子，硝基，腈，三氟甲基，乙烯基，甲基硫烷基，直链支链C 1 -C 4烷基，直链或支链C 1 -C 3烷氧基，a C 2 2-氧代环烷基基团-R 2表示甲基或庚基，-m，n等于 1，-V表示CH 2，-XY表示-N-（C = O） - ， - CH-O-，-Z表示被一个或多个三氟甲基，卤素原子或直链C 1 -C 4烷基取代的苯基。

    1,2,4-Triazine Derivatives, Preparation and Use Thereof in Human Therapy
    4.
    发明申请
    1,2,4-Triazine Derivatives, Preparation and Use Thereof in Human Therapy 有权

    公开(公告)号：US20080167313A1

    公开(公告)日：2008-07-10

    申请号：US11885630

    申请日：2006-03-02

    申请人： Elisabeth Dupont-Passelaigue ,  Isabelle Leroy ,  Jean-Francois Patoiseau ,  Didier Junquero ,  Yves Rival ,  Andre Delhon

    发明人： Elisabeth Dupont-Passelaigue ,  Isabelle Leroy ,  Jean-Francois Patoiseau ,  Didier Junquero ,  Yves Rival ,  Andre Delhon

    IPC分类号： A61K31/53 ,  C07D253/06 ,  A61P3/06 ,  A61P3/04 ,  A61P3/10 ,  A61P17/00

    CPC分类号： C07D253/075

    摘要： The invention concerns 3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives of general formula (I), wherein: R1 and R2, identical or different, represent a branched or linear C1-C7 alkyl or alkenyl radical, a C1-C6 alkyl radical substituted by groups such as trifluoromethyl, C5-C6 cycloalkyl, nitrile, C1-C4 alkoxycarbonylvinyl, hydroxycarbonylvinyl, C1-C4 alkoxycarbonyl, carboxylate, benzyloxy or phenyl (for which the phenyl ring is optionally substituted by one or more groups such as C1-C4 alkoyl, C1-C4 alkoxy, nitro, halogen, trifluoromethyl); YR3 represents oxygen or NR3 for which R3 represents hydrogen, a linear or branched C1-C7 alkyl or alkenyl radical, a C1-C6 alkyl radical substituted by groups such as trifluoromethyl or phenyl (for which the phenyl ring is optionally substituted by one or more groups such as C1-C4 alkoyl, C1-C4 alkoxy, nitro, halogen, trifluoromethyl); Z represents an oxygen atom or a carbon atom capable of being bound to the ortho, meta or para positions of the phenyl group of formula I; n can be 0 to 5 when Z=C or 2 to 4 when Z=O; X represents oxygen or sulphur; R4, R5, R6, R7 and R8 represent hydrogen or fluorine; R9, R10 and R11 represent hydrogen or a linear or branched C1-C5 alkyl group as well as the pharmaceutically acceptable base addition salts, and the various enantiomers of compounds having asymmetric carbons, and their mixtures in all proportions including in particular the racemic mixtures.

    Cyclohexane derivatives difunctionalised in 1,4 as ligands of 5T H1A receptors
    7.
    发明授权
    Cyclohexane derivatives difunctionalised in 1,4 as ligands of 5T H1A receptors 有权
    环己烷衍生物在1,4中作为5T H1A受体的配体双功能化

    公开(公告)号：US06191130B1

    公开(公告)日：2001-02-20

    申请号：US09529783

    申请日：2000-04-14

    申请人： Jean-François Patoiseau ,  Elisabeth Dupont-Passelaigue ,  Wouter Koek

    发明人： Jean-François Patoiseau ,  Elisabeth Dupont-Passelaigue ,  Wouter Koek

    IPC分类号： C07D25306

    CPC分类号： C07D253/075 ,  C07D403/12 ,  C07D405/12

    摘要： The invention concerns novel cyclohexane derivatives difunctionalised in 1.4 of general formula (1) in which A represents a group such as (IIa) in which Ar itself represents an aromatic structure such as phenyl or pyrimidinyl optionally substituted by one or several groups such as C1-C3 alkyl, C1-C3 alkoxy, trifluoromethyl or halogen (IIb); B represents a heterocyclic group such as: 3,5-dioxo-(2H,4H)-1,2,4 triazine substituted in position 2 (IIIa); 3-oxo-(2H)-1,2,4 triazine substituted in position 5 (IIIb); 3,5-dioxo-6-amino-(2H,4H)-1,2,4-triazine (IIIc) in which R represents a C1-C3 alkyl group. The invention also concerns the salts of compounds of general formula I with pharmaceutically acceptable acids. It also concerns the various “cis” and “trans” isomers and the various enantiomers with asymmetric carbons.

    摘要翻译： 本发明涉及在1.4通式（1）中双官能化的新型环己烷衍生物，其中A代表其中Ar本身表示芳族结构的基团，例如苯基或嘧啶基，其任选被一个或多个基团取代，如C1- C3烷基，C1-C3烷氧基，三氟甲基或卤素（IIb）; B表示杂环基，例如：位置2（IIIa）取代的3,5-二氧代 - （2H，4H）-1,2,4-三嗪; 在位置5（IIIb）取代的3-氧代 - （2H）-1,2,4-三嗪; 3,5-二氧代-6-氨基 - （2H，4H）-1,2,4-三嗪（IIIc），其中R表示C1-C3烷基。 本发明还涉及通式I的化合物与药学上可接受的酸的盐。 它还涉及各种“顺式”和“反式”异构体和具有不对称碳的各种对映异构体。

    Derivatives of 2H pyridazin-3-ones, their preparation and their use as SCD-1 inhibitors
    9.
    发明授权
    Derivatives of 2H pyridazin-3-ones, their preparation and their use as SCD-1 inhibitors 有权
    2H哒嗪-3-酮的衍生物，其制备及其作为SCD-1抑制剂的用途

    公开(公告)号：US08946225B2

    公开(公告)日：2015-02-03

    申请号：US13388884

    申请日：2010-08-05

    申请人： Elisabeth Dupont-Passelaigue ,  Samuel Mialhe ,  Jean-Pierre Rieu ,  Didier Junquero ,  Karine Valeille

    发明人： Elisabeth Dupont-Passelaigue ,  Samuel Mialhe ,  Jean-Pierre Rieu ,  Didier Junquero ,  Karine Valeille

    IPC分类号： A61K31/50 ,  A61K31/501 ,  C07D237/02

    CPC分类号： C07D237/22 ,  C07D401/12 ,  C07D403/12

    摘要： The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: —R1 represents one or more groups such as: trifluoromethyl, halogen such as F, Cl, —when n=m=1, W represents CH then Y represents oxygen, —U represents: •either —(C═O)CH2NH— and is branched at position 4 of pyridazinone, then R2 represents H, •or —(C═O)NH— and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, —R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enzyme inhibitors for the treatment of obesity, type-2 diabetes and lipid disorders.

    摘要翻译： 本发明涉及通式（I）的化合物，其特征在于（式1）其中特别地：-R 1表示一个或多个基团，例如三氟甲基，卤素如F，Cl， - 当n = m = 1时， W表示CH，Y表示氧，-U表示：• - （C = O）CH2NH-，并且在哒嗪酮的第4位分支，则R2表示H，•或 - （C = O）NH-，U为支链 在哒嗪酮的位置（4），（5）或（6）中，R 2表示H，-R 3表示氢或甲基，加成盐与药学上可接受的碱和酸和不同的异构体， 用作SCD-1酶抑制剂用于治疗肥胖，2型糖尿病和脂质疾病。