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    Diarylpyridazinone derivatives, preparation thereof, and use thereof for the treatment of humans
    1.
    发明授权
    Diarylpyridazinone derivatives, preparation thereof, and use thereof for the treatment of humans 有权
    二芳基哒嗪酮衍生物，其制备方法及其用于治疗人的用途

    公开(公告)号：US08993569B2

    公开(公告)日：2015-03-31

    申请号：US13823671

    申请日：2011-12-20

    申请人： Elisabeth Dupont-Passelaigue ,  Isabelle Le Roy ,  Samuel Mialhe ,  Christophe Pignier

    发明人： Elisabeth Dupont-Passelaigue ,  Isabelle Le Roy ,  Samuel Mialhe ,  Christophe Pignier

    IPC分类号： A01N43/58 ,  A61K31/50 ,  C07D237/00 ,  C07D237/02 ,  C07D237/14 ,  C07D231/20

    CPC分类号： C07D237/14 ,  C07D231/20

    摘要： The present invention relates to diarylpyridazinone derivatives that block the potassium Kv channels (specifically the Kv1.5, Kv4.3, and Kv11.1 channels) and to the use thereof for the treatment of humans. Said compounds have the general formula (I), where R1 and R2 are simultaneously or independently one or more groupings such as: halogen, such as F, Br, Cl, a straight or branched C1-C4 alkyl, hydroxy, a straight or branched C1-C4 alkoxy, arylsulfonamido, in which the aryl is optionally replaced with a straight or branched C1-C4 alkyl, or nitrile, as well as the various enantiomers and the mixtures thereof in any proportion, and the pharmaceutically acceptable salts thereof.

    摘要翻译： 本发明涉及阻断Kv通道（特别是Kv1.5，Kv4.3和K​​v11.1通道）的二芳基哒嗪酮衍生物及其用于治疗人的用途。 所述化合物具有通式（I），其中R 1和R 2同时或独立地是一个或多个基团，例如：卤素如F，Br，Cl，直链或支链C 1 -C 4烷基，羟基，直链或支链 其中芳基任选被直链或支链C 1 -C 4烷基或腈取代的芳基磺酰氨基，以及各种对映异构体及其任何比例的混合物及其药学上可接受的盐。

    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

    3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives as 5HT.sub.1A ligands
    4.
    发明授权
    3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives as 5HT.sub.1A ligands 失效
    3,5-二氧代 - （2H，4H）-1,2,4-三嗪衍生物作为5HT1A配体

    公开(公告)号：US5591743A

    公开(公告)日：1997-01-07

    申请号：US578522

    申请日：1996-03-26

    申请人： Jean-Francois Patoiseau ,  Francoise Couret ,  Christian Faure ,  Elisabeth Dupont-Passelaigue ,  Wouter Koek

    发明人： Jean-Francois Patoiseau ,  Francoise Couret ,  Christian Faure ,  Elisabeth Dupont-Passelaigue ,  Wouter Koek

    IPC分类号： C07D253/06 ,  A61K31/53 ,  A61P1/04 ,  A61P9/00 ,  A61P25/20 ,  C07D253/075 ,  C07D403/12 ,  C07D405/12 ,  A01N43/707

    CPC分类号： C07D253/075 ,  C07D405/12

    摘要： A 3,5-dioxo-(2H,4H)-1,2,4-triazine compounds of formula I ##STR1## in which: R.sub.1 and R.sub.2, which are identical or different, represent hydrogen or C.sub.1 -C.sub.6 alkyl, n is 2 to 6, inclusive,A represents aryl piperazino II ##STR2## the Ar grouping representing phenyl, naphthyl, pyrimidyl, or pyridyl, unsubstituted or substituted by C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, hydroxy, trifluoromethyl, or halogen, or III benzodioxanyl-methyl-amino or pyridodioxanyl-methyl-amino ##STR3## in which R represents hydrogen or C.sub.1 -C.sub.3 alkyl and X represents a nitrogen or carbon atom, therapeutically-acceptable salts and enantiomers thereof, pharmaceutical compositions thereof, and method for treatment of diseases requiring a 5HT.sub.1A receptor agonist therewith.

    摘要翻译： PCT No.PCT / FR94 / 00772 Sec。 371日期：1996年3月26日 102（e）1996年3月26日PCT 1994年6月27日PCT公布。 第WO95 / 01965号公报 日期：1995年1月19日A式Ⅰ的3,5-二氧代 - （2H，4H）-1,2,4-三嗪化合物其中：R1和R2相同或不同，表示氢或C1 C 1-6烷基，n为2至6，包括端值，A表示芳基哌嗪基II代表苯基，萘基，嘧啶基或吡啶基的Ar基团，未取代或被C 1 -C 3烷基，C 1 -C 3烷氧基，羟基， 三氟甲基或卤素，或III苯并二恶烷基 - 甲基 - 氨基或吡啶并二恶烷基 - 甲基 - 氨基，其中R表示氢或C1-C3烷基，X表示氮或碳原子，其治疗上可接受的盐和对映体，药物 其组合物，以及治疗需要5HT1A受体激动剂的疾病的方法。

    Derivatives of triazines and uracils, their preparation and their application in human therapeutics
    5.
    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。

    DERIVATIVES OF HETEROARYLSULFONAMIDES, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPY
    6.
    发明申请
    DERIVATIVES OF HETEROARYLSULFONAMIDES, THEIR PREPARATION AND THEIR APPLICATION IN HUMAN THERAPY 有权
    异氟醚的衍生物，其制备及其在人类治疗中的应用

    公开(公告)号：US20130172326A1

    公开(公告)日：2013-07-04

    申请号：US13822406

    申请日：2011-11-23

    申请人： Elisabeth Dupont-Passelaigue ,  Isabelle Le Roy ,  Christophe Pignier

    发明人： Elisabeth Dupont-Passelaigue ,  Isabelle Le Roy ,  Christophe Pignier

    IPC分类号： C07D417/14 ,  C07D413/14

    CPC分类号： C07D417/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

    摘要： The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C1-C4 alkyl, or linear or branched C1-C4 alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents —C(═O)—, or B represents CH when n=0 and D represents —CH2O— or when n=1 and D represents —O—, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C1-C4 alkyl, a linear or branched C1-C4 alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.

    摘要翻译： 本发明涉及杂芳基磺酰胺的衍生物，特别是作为Kv钾通道的阻断剂，更特别地是通道Kv1.5，Kv4.3或Kv11.1，其在临床治疗中的应用及其制备方法。 这些化合物对应于以下通式（I）：其中R 1表示苯基核心X的一个或多个取代基，例如：氢，卤素，三氟甲基，三氟甲氧基，直链或支链C 1 -C 4烷基，或直链或支链C 1 -C 4 烷氧基，A表示氧或硫，当n = 1或2时，B表示氮，D表示-C（= O） - ，或B表示CH，当n = 0时，D表示-CH2O-，或当n = 1时，D表示 -O-，R 2表示氢，甲基，氟或氯原子或甲氧基，HetAr表示可被基团例如直链或支链C1-C4烷基取代的吡啶基或喹啉基，直链或支链C1 -C4烷氧基，卤素或三氟甲基，以及它们的药学上可接受的盐。

    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。

    Derivatives of heteroarylsulfonamides, their preparation and their application in human therapy
    10.
    发明授权
    Derivatives of heteroarylsulfonamides, their preparation and their application in human therapy 有权
    杂芳基磺酰胺的衍生物，其制备及其在人类治疗中的应用

    公开(公告)号：US08846930B2

    公开(公告)日：2014-09-30

    申请号：US13822406

    申请日：2011-11-23

    申请人： Elisabeth Dupont-Passelaigue ,  Isabelle Le Roy ,  Christophe Pignier

    发明人： Elisabeth Dupont-Passelaigue ,  Isabelle Le Roy ,  Christophe Pignier

    IPC分类号： C07D261/20 ,  C07D417/00 ,  C07D413/00 ,  C07D419/00 ,  A61K31/497 ,  A61K31/445 ,  A01N43/40 ,  C07D417/14 ,  C07D413/14 ,  C07D417/12 ,  C07D413/12

    CPC分类号： C07D417/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12

    摘要： The present invention concerns derivatives of heteroarylsulfonamides, notably as blockers of Kv potassium channels, and more particularly of channels Kv1.5, Kv4.3 or Kv11.1, their application in clinical therapy and their preparation methods. These compounds correspond to the following general formula (I): where R1 represents one or more substituents of the phenyl core X such as: hydrogen, halogen, trifluoromethyl, trifluoromethoxy, linear or branched C1-C4 alkyl, or linear or branched C1-C4 alkoxy, A represents oxygen or sulphur, B represents nitrogen when n=1 or 2 and D represents —C(═O)—, or B represents CH when n=0 and D represents —CH2O— or when n=1 and D represents —O—, R2 represents a hydrogen, a methyl, a fluorine or chlorine atom or a methoxy, HetAr represents a pyridyl or quinolyl group, possibly substituted by a group such as a linear or branched C1-C4 alkyl, a linear or branched C1-C4 alkoxy, a halogen, or a trifluoromethyl, and to their pharmaceutically acceptable salts.

    摘要翻译： 本发明涉及杂芳基磺酰胺的衍生物，特别是作为Kv钾通道的阻断剂，更特别地是通道Kv1.5，Kv4.3或Kv11.1，其在临床治疗中的应用及其制备方法。 这些化合物对应于以下通式（I）：其中R 1表示苯基核心X的一个或多个取代基，例如：氢，卤素，三氟甲基，三氟甲氧基，直链或支链C 1 -C 4烷基，或直链或支链C 1 -C 4 烷氧基，A表示氧或硫，当n = 1或2时，B表示氮，D表示-C（= O） - ，或B表示CH，当n = 0且D表示-CH2O-时，或当n = 1时，D表示 -O-，R 2表示氢，甲基，氟或氯原子或甲氧基，HetAr表示可被基团例如直链或支链C1-C4烷基取代的吡啶基或喹啉基，直链或支链C1 -C4烷氧基，卤素或三氟甲基，以及它们的药学上可接受的盐。