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11 条记录 (耗时 0.017 秒)

    3,5-dioxo-(2H,4H)-1,2,4-triazine derivatives as 5HT.sub.1A ligands
    1.
    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。

    3-oxo-2(H)-1,2,4-triazine derivatives as ligands of 5 HT1A receptors
    2.
    发明授权
    3-oxo-2(H)-1,2,4-triazine derivatives as ligands of 5 HT1A receptors 有权
    3-羟基-2（H）-1,2,4-三嗪衍生物作为5个HT1A受体的配体

    公开(公告)号：US06303603B1

    公开(公告)日：2001-10-16

    申请号：US09529728

    申请日：2000-04-14

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

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

    IPC分类号： A61K3153

    CPC分类号： C07D253/075 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D471/04

    摘要： The invention concerns novel 3-oxo-(2H)-1,2,4-triazine derivatives of general formula (I) in which R1 represents: hydrogen, when A is an optionally substituted nitrogen atom; a linear or branched 1-C4 alkyl group; a C1-C4phenyl alkyl group, the phenyl ring being optionally substituted by one or several groups such as C1-C4 alkyl, C1-C3 alkoxy, halogen, trifluoromethyl. R2 represents: hydrogen; a linear or branched C1-C4 alkyl radical; a C1-C4 phenyl or phenylalkyl group, the phenyl ring being optionally substituted by one or several groups such as C1-C4 alkyl, C1-C3 alkoxy, halogen, trifluoromethyl. A represents an oxygen atom or a nitrogen atom optionally NR3 substituted. R3 represents hydrogen or a methyl group. B represents a group such as (IIa) in which Ar itself represents an aromatic structure such as phenyl, pyridyl or pyrimidyl, optionally substituted by one or several groups such as C1-C3 alkyl, C1-C3 alkoxy, hydroxy, trifluoromethyl or halogen and n can be whole numbers ranging between 3 and 5; (IIb) in which Ar is as defined in formula (IIa) and m can be a whole number ranging between 1 and 2; (IIc) in which R4 represents hydrogen or a C1-C3 alkyl group and n can be whole numbers ranging between 3 and 5.

    摘要翻译： 本发明涉及通式（I）的新的3-氧代 - （2H）-1,2,4-三嗪衍生物，其中当R1是任意取代的氮原子时，R 1表示：氢; 直链或支链的1-C4烷基; C1-C4苯基烷基，苯环任选被一个或多个基团取代，例如C 1 -C 4烷基，C 1 -C 3烷氧基，卤素，三氟甲基。 R2表示：氢; 直链或支链C 1 -C 4烷基; C 1 -C 4苯基或苯基烷基，苯环任选被一个或几个基团例如C 1 -C 4烷基，C 1 -C 3烷氧基，卤素，三氟甲基取代。 A表示氧原子或任选被NR 3取代的氮原子。 R3表示氢或甲基。 B表示其中Ar本身表示芳族结构的基团，例如苯基，吡啶基或嘧啶基，任选被一个或多个基团例如C 1 -C 3烷基，C 1 -C 3烷氧基，羟基，三氟甲基或卤素取代， n可以是3到5之间的整数; （IIb）其中Ar如式（IIa）中所定义，m可以是1和2之间的整数; （IIc）其中R4表示氢或C1-C3烷基，n可以是3至5的整数。

    1,2,4-Triazine Derivatives, Preparation and Use Thereof in Human Therapy
    3.
    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.

    Glycylanilide derivatives, their preparation and their application in therapy
    9.
    发明授权
    Glycylanilide derivatives, their preparation and their application in therapy 失效
    甘氨酰苯胺衍生物，其制备及其在治疗中的应用

    公开(公告)号：US5760087A

    公开(公告)日：1998-06-02

    申请号：US875191

    申请日：1997-07-17

    申请人： Jean-Francois Patoiseau ,  Jean-Marie Autin ,  Andre Delhon ,  Philippe Oms

    发明人： Jean-Francois Patoiseau ,  Jean-Marie Autin ,  Andre Delhon ,  Philippe Oms

    IPC分类号： A61K31/165 ,  A61P3/06 ,  A61P9/10 ,  A61P43/00 ,  C07C231/02 ,  C07C237/22 ,  C07C323/60 ,  A01N37/18

    CPC分类号： C07C237/22 ,  C07C323/60

    摘要： The invention relates to new derivatives of glycylanilides having general formula (I), wherein, particularly, R.sub.1, R.sub.3, R.sub.4, R.sub.8, R.sub.9 represent CH.sub.3 ; R.sub.2, R.sub.5, R.sub.6, R.sub.7 represent H; R.sub.10 represents C.sub.12 H.sub.25 and A is a sulfur atom. It also relates to the preparation process and the pharmaceutical compositions comprising as active principle at least one of said compounds, as well as the utilization of said derivatives for the fabrication of drugs intended to the treatment of hypercholesterolemy or atherosclerosis. ##STR1##

    摘要翻译： PCT No.PCT / FR96 / 00081 Sec。 371日期1997年7月17日 102（e）日期1997年7月17日PCT 1996年1月18日PCT PCT。 第WO96 / 22279号公报 日期：1996年7月25日本发明涉及具有通式（I）的脯氨酰苯胺的新衍生物，其中，特别地，R 1，R 3，R 4，R 8，R 9表示CH 3; R2，R5，R6，R7表示H; R 10表示C12H25，A为硫原子。 它还涉及制备方法和药物组合物，其包含作为至少一种所述化合物的活性成分，以及所述衍生物用于制备旨在治疗高胆固醇血症或动脉粥样硬化的药物的用途。 （一）