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    Acylaminothiazole derivatives, their preparation and their therapeutic use
    2.
    发明授权
    Acylaminothiazole derivatives, their preparation and their therapeutic use 失效
    酰氨基噻唑衍生物，其制备及其治疗用途

    公开(公告)号：US07563903B2

    公开(公告)日：2009-07-21

    申请号：US11186507

    申请日：2005-07-21

    申请人： Pierre Despeyroux ,  Daniel Frehel ,  Bruno Schoentjes ,  Viviane Van Dorsselaer

    发明人： Pierre Despeyroux ,  Daniel Frehel ,  Bruno Schoentjes ,  Viviane Van Dorsselaer

    IPC分类号： A61K31/426 ,  C07D277/46

    CPC分类号： C07D417/12 ,  C07D277/46

    摘要： Compound corresponding to the general formula (I): in which, X represents an oxygen or sulphur atom; R1 represents a C1-10 alkyl group optionally substituted, a C3-7 cycloalkyl, thienyl, pyridinyl or pyrimidinyl group; the thienyl groups being optionally substituted; the phenyl group being optionally substituted; R2 represents a C1-6 alkyl group optionally substituted, a C3-7 cycloalkyl, piperidinyl, phenyl or pyridinyl group; the C3-7 cycloalkyl and piperidinyl groups being optionally substituted; the phenyl and pyridinyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-6 alkyl group optionally substituted with a C3-7 cycloalkyl group; R4 represents a hydrogen atom or a C1-6 alkyl group; R5 and R5′ represent, independently of each other, a hydrogen or halogen atom, a hydroxyl or C1-3 alkyl group; or R5 and R5′ form together an oxo or oxime group such as: where R7 represents a hydrogen atom or a C1-3 alkyl; n represents an integer ranging from 0 to 3; and R6 represents, independently of each other when n=2 or 3, a hydrogen or halogen atom, a hydroxyl, C1-3 alkyl, C1-3 alkoxy, C1-3 fluoroalkyl or C1-3 fluoroalkoxy group; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. therapeutic application.

    摘要翻译： 对应于通式（I）的化合物：其中X表示氧或硫原子; R 1表示任选取代的C 1-10烷基，C 3-7环烷基，噻吩基，吡啶基或嘧啶基; 噻吩基任选被取代; 苯基任选被取代; R 2表示任选取代的C 1-6烷基，C 3-7环烷基，哌啶基，苯基或吡啶基; C3-7环烷基和哌啶基任选被取代; 苯基和吡啶基任选被取代; R3表示氢原子或任选被C 3-7环烷基取代的C 1-6烷基; R4表示氢原子或C1-6烷基; R5和R5'彼此独立地表示氢或卤素原子，羟基或C1-3烷基; 或R 5和R 5'一起形成氧基或肟基，例如：其中R 7表示氢原子或C 1-3烷基; n表示0〜3的整数， 当n = 2或3时，R 6表示独立地为氢或卤原子，羟基，C 1-3烷基，C 1-3烷氧基，C 1-3氟烷基或C 1-3氟烷氧基; 以碱的形式，与酸的加成盐，水合物或溶剂合物的治疗应用。

    Acylaminothiazole derivatives, their preparation and their therapeutic use
    3.
    发明申请
    Acylaminothiazole derivatives, their preparation and their therapeutic use 失效
    酰氨基噻唑衍生物，其制备及其治疗用途

    公开(公告)号：US20060052426A1

    公开(公告)日：2006-03-09

    申请号：US11186507

    申请日：2005-07-21

    申请人： Pierre Despeyroux ,  Daniel Frehel ,  Bruno Schoentjes ,  Viviane Van Dorsselaer

    发明人： Pierre Despeyroux ,  Daniel Frehel ,  Bruno Schoentjes ,  Viviane Van Dorsselaer

    IPC分类号： C07D277/18 ,  A61K31/426

    CPC分类号： C07D417/12 ,  C07D277/46

    摘要： Compound corresponding to the general formula (I): in which, X represents an oxygen or sulphur atom; R1 represents a C1-10 alkyl group optionally substituted, a C3-7 cycloalkyl, thienyl, pyridinyl or pyrimidinyl group; the thienyl groups being optionally substituted; the phenyl group being optionally substituted; R2 represents a C1-6 alkyl group optionally substituted, a C3-7 cycloalkyl, piperidinyl, phenyl or pyridinyl group; the C3-7 cycloalkyl and piperidinyl groups being optionally substituted; the phenyl and pyridinyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-6 alkyl group optionally substituted with a C3-7 cycloalkyl group; R4 represents a hydrogen atom or a C1-6 alkyl group; R5 and R5′ represent, independently of each other, a hydrogen or halogen atom, a hydroxyl or C1-3 alkyl group; or R5 and R5′ form together an oxo or oxime group such as: where R7 represents a hydrogen atom or a C1-3 alkyl; n represents an integer ranging from 0 to 3; and R6 represents, independently of each other when n=2 or 3, a hydrogen or halogen atom, a hydroxyl, C1-3 alkyl, C1-3 alkoxy, C1-3 fluoroalkyl or C1-3 fluoroalkoxy group; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. therapeutic application.

    摘要翻译： 对应于通式（I）的化合物：

    Antiinflammatory thieno [2,3-c]pyridine derivatives
    5.
    发明授权
    Antiinflammatory thieno [2,3-c]pyridine derivatives 失效
    抗炎噻吩并[2,3-c]吡啶衍生物

    公开(公告)号：US4496568A

    公开(公告)日：1985-01-29

    申请号：US487355

    申请日：1983-04-25

    申请人： Jean-Pierre Maffrand ,  Daniel Frehel

    发明人： Jean-Pierre Maffrand ,  Daniel Frehel

    IPC分类号： C07D513/02 ,  A61K31/435 ,  A61K31/4365 ,  A61P29/00 ,  C07D495/04 ,  A61K31/44

    CPC分类号： C07D495/04

    摘要： This invention relates to a process for the preparation of antiinflammatory thieno [2,3-c]- and [3,2-c]pyridines having respectively the following formulae: ##STR1## in which R.sub.1 and R.sub.2, which may be the same or different, represent each a hydrogen atom or an alkyl group, and their pharmaceutically acceptable acid addition salts, comprising:(a) condensing a compound of the following formulae (VII) or (VIII), respectively, ##STR2## with a sulfonyl chloride having the formula ClSO.sub.2 R.sub.3, in which R.sub.3 is a lower alkyl radical or a phenyl radical optionally substituted with a halogen atom or a lower alkyl group, within a two-phase solvent system and in the presence of sodium carbonate;(b) oxidizing in a solvent medium the resulting alcohols having respectively the following formula (V) or (VI): ##STR3## (c) treating the resulting ketones, having the following formula (III) or (IV): ##STR4## with a basic agent having the formula RO.sup.- M.sup.+ in which R is a branched- or straight-chain aliphatic alkyl radical and M.sup.+ is an alkali metal cation, within an alcohol solvent having the formula ROH, and at the reflux temperature of the reaction mixture, to give the compounds of the formula (I) or (II), respectively.

    摘要翻译： 本发明涉及分别具有以下分子式的抗炎噻吩并[2,3-c] - 和[3,2-c]吡啶的制备方法：其中R 1和R 2可以相同或不同， 不同的，各自表示氢原子或烷基，以及它们的药学上可接受的酸加成盐，其包括：（a）分别将下式（VII）或（VIII）的化合物与具有 其中R3是低级烷基或任选被卤素原子或低级烷基取代的苯基的式ClSO 2 R 3在两相溶剂体系内和在碳酸钠存在下; （b）在溶剂介质中氧化分别具有下式（Ⅴ）或（Ⅵ）的所得醇：（Ⅵ）（Ⅵ）（c）处理所得酮，具有下式（III ）或（IV）：其中R是支链或直链脂族烷基，M +是碱金属阳离子，具有式RO-M +的碱性试剂，（IV） 在具有式ROH的醇溶剂中，并在反应混合物的回流温度下分别得到式（I）或（II）的化合物。

    Thieno [2,3-c] and [3,2-c] pyridines
    6.
    发明授权
    Thieno [2,3-c] and [3,2-c] pyridines 失效
    噻吩并[b 2,3-c {9 {0和{8,2-c {9 {

    公开(公告)号：US4104390A

    公开(公告)日：1978-08-01

    申请号：US808694

    申请日：1977-06-21

    申请人： Gerard Ferrand ,  Daniel Frehel ,  Jean-Pierre Maffrand

    发明人： Gerard Ferrand ,  Daniel Frehel ,  Jean-Pierre Maffrand

    IPC分类号： A61K31/435 ,  A61K31/4365 ,  A61P7/02 ,  A61P29/00 ,  C07D333/20 ,  C07D333/36 ,  C07D495/04 ,  C07D513/04 ,  A61K31/38

    CPC分类号： C07D495/04 ,  C07D333/20

    摘要： This invention relates to pyridine derivatives of the formulae: ##STR1## in which R.sup.1 is hydrogen, lower alkyl, aralkyl optionally substituted on the aromatic nucleus with at least a halogen atom or a hydroxy, nitro, amino, cyano, carboxy, alkoxycarbonyl, lower alkyl, lower alkoxy or trifluoromethyl group; R.sup.2 is hydrogen or lower alkyl; and R.sup.3 is hydrogen or at least a substituent selected from a halogen atom, a hydroxy, lower alkyl and lower alkoxy group, and their pharmaceutically acceptable inorganic or organic acid addition salts.Said compounds have particularly an anti-inflammatory and blood-platelet aggregation inhibiting activity.

    摘要翻译： 本发明涉及以下结构式的吡啶衍生物：其中R 1为氢，低级烷基，任选在芳核上被至少具有卤素原子取代的芳烷基或羟基，硝基，氨基，氰基，羧基，烷氧基羰基，低级 烷基，低级烷氧基或三氟甲基; R2是氢或低级烷基; 和R3是氢或至少一个选自卤素原子，羟基，低级烷基和低级烷氧基的取代基，以及它们的药学上可接受的无机酸或有机酸加成盐。