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6 条记录 (耗时 0.025 秒)

    Substitute 1-(piperidin-4-yl)-3-(aryl)-isothioureas, their preparation and therapeutic use
    1.
    发明授权
    Substitute 1-(piperidin-4-yl)-3-(aryl)-isothioureas, their preparation and therapeutic use 失效
    替代1-（哌啶-4-基）-3-（芳基） - 异硫脲，其制备和治疗用途

    公开(公告)号：US06583159B1

    公开(公告)日：2003-06-24

    申请号：US09889811

    申请日：2001-07-20

    申请人： Jean-François Patoiseau ,  Jean-Pierre Rieu ,  Gareth John ,  Bruno Legrand ,  Yvan Verscheure

    发明人： Jean-François Patoiseau ,  Jean-Pierre Rieu ,  Gareth John ,  Bruno Legrand ,  Yvan Verscheure

    IPC分类号： A61K31445

    CPC分类号： C07D211/58

    摘要： The invention concerns compounds of formula (I) wherein: R1 and R2, identical or different, represent a saturated or unsaturated alkyl radical, branched or not and containing 1 to 7 carbon atoms; R3 to R8, identical or different, represent a hydrogen, an alkyl branched or not and containing 1 to 5 carbon atoms, an acyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or alkoxy group containing 1 to 5 carbon atoms, a dialkylamino group containing 1 to 5 carbon atoms, a trifluoromethyl or trifluoro methoxyl group; Z represents an oxygen or sulphur atom or methylene; m represents an integer between 0 and 4 inclusively; n represents an integer between 2 and 7 inclusively; and their pure enantiomers and mixtures, the therapeutically acceptable mineral or organic salts of the compounds of formula (I) and their possible hydrates.

    摘要翻译： 本发明涉及式（I）的化合物，其中：R 1和R 2相同或不同，表示饱和或不饱和的烷基，分支或不具有1至7个碳原子; R3至R8相同或不同，表示氢，支链或不支链，含有1至5个碳原子的烷基，酰氧基，支链或不支化，含有1至5个碳原子，卤代，硝基，羟基，酰基或烷氧基 含有1至5个碳原子的二烷基氨基，含有1至5个碳原子的二烷基氨基，三氟甲基或三氟甲氧基; Z表示氧或硫原子或亚甲基; m表示0和4之间的整数; n表示2〜7的整数， 和它们的纯对映异构体和混合物，式（I）化合物的治疗上可接受的矿物或有机盐及其可能的水合物。

    Substituted 1-(4-piperidyl)-3-(aryl) isothioureas their preparation and their therapeutic application
    2.
    发明授权
    Substituted 1-(4-piperidyl)-3-(aryl) isothioureas their preparation and their therapeutic application 失效
    取代的1-（4-哌啶基）-3-（芳基）异硫脲的制备及其治疗应用

    公开(公告)号：US06531469B1

    公开(公告)日：2003-03-11

    申请号：US09889805

    申请日：2001-07-20

    申请人： Jean-Pierre Rieu ,  Jean-François Patoiseau ,  Gareth John ,  Bruno Legrand ,  Yvan Verscheure

    发明人： Jean-Pierre Rieu ,  Jean-François Patoiseau ,  Gareth John ,  Bruno Legrand ,  Yvan Verscheure

    IPC分类号： C07D41712

    CPC分类号： C07D413/12 ,  C07D417/12

    摘要： The invention concerns novel substituted N-benzo(thia/oxa)zines-2-yl-1-arylalkyloxyalkyl-4-piperidinamine, their preparation and their therapeutic use. The invention concerns compounds of formula (1) wherein: X represents an oxygen or sulphur atom; Y represents either an alkylene radical, branched or not and containing 2 to 6 carbon atoms or a CH2—CH(OH)—CH2— radical. R represents a hydrogen, an alkyl radical, branched or not and containing 1 to 7 carbon atoms; R1 to R6, identical or different, represent a hydrogen, a saturated or unsaturated alkyl, branched or not and containing 1 to 5 carbon atoms, a saturated or unsaturated alkyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or acyloxy group comprising 2 to 3 carbon atoms, an alkylamino group containing 1 to 5 carbon atoms, a trifluoro methyl or trifluoro methoxyl group; n is an integer ranging from 1 to 6 inclusively, and their pure, enantiomers or their mixtures, the therapeutically acceptable mineral and organic salts of the compounds of formula (1) and their possible hydrates.

    摘要翻译： 本发明涉及新型取代的N-苯并（噻唑/氧杂）嗪-2-基-1-芳基烷氧基烷基-4-哌啶胺及其制备及其治疗用途。 本发明涉及式（1）的化合物，其中：X表示氧或硫原子; Y表示亚烷基，支链或不支链，含有2-6个碳原子或CH2-CH（OH）-CH2-基。 R表示氢，烷基，支链或不支链，含有1至7个碳原子; R 1至R 6相同或不同，表示氢，饱和或不饱和的烷基，支链或不含并且含有1至5个碳原子，饱和或不饱和烷氧基，支链或不具有1至5个碳原子，卤代，硝基 ，含有2〜3个碳原子的羟基，酰基或酰氧基，含1至5个碳原子的烷基氨基，三氟甲基或三氟甲氧基; n是1至6的整数，以及它们的纯的对映体或它们的混合物，式（1）化合物的治疗上可接受的矿物和有机盐及其可能的水合物。

    Cyclohexane derivatives difunctionalised in 1,4 as ligands of 5T H1A receptors
    5.
    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。