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    Acylaminothiazole derivatives, their preparation and therapeutic use
    2.
    发明授权
    Acylaminothiazole derivatives, their preparation and therapeutic use 有权
    酰氨基噻唑衍生物，其制备和治疗用途

    公开(公告)号：US07288659B2

    公开(公告)日：2007-10-30

    申请号：US10485837

    申请日：2002-08-05

    申请人： Paul De Cointet ,  Pierre Despeyroux ,  Daniel Frehel ,  Chantal Guenet ,  Corinne Heckel ,  Jean-Pierre Maffrand ,  Rebecca Pruss

    发明人： Paul De Cointet ,  Pierre Despeyroux ,  Daniel Frehel ,  Chantal Guenet ,  Corinne Heckel ,  Jean-Pierre Maffrand ,  Rebecca Pruss

    IPC分类号： C07D277/46

    CPC分类号： C07D417/12 ,  C07D277/40 ,  C07D277/42 ,  C07D277/46

    摘要： The invention concerns a compound of general formula (I), wherein: X represents an oxygen or sulphur atom; R1 represents, independently of each other when n=2 or 3, a halogen atom, a hydroxy, a C1-C3 alkyl, a C1-C3 alkoxy, a trifluoromethyl, a trifluoromethyloxy or a methylenedioxy; R2 represents a C1-C6 alkyl group optionally substituted, a C3-C7 cycloalkyl, piperidinyl or phenyl group, the C3-C7 cycloalkyl, piperidinyl or phenyl groups being optionally substituted; R3 represents a hydrogen atom or a C1-C6 alkyl group optionally substituted; R4 represents a hydrogen atom or a C1-C4 alkyl group; and R5 and R5′ represent, independently of each other, a hydrogen atom, a hydroxy, a halogen atom, a C1-C3 alkyl group, or R5 and R5′ form together an oxo group; R6 represents a hydrogen atom, a halogen atom, a C1-C3 alkyl, a C1-C3 alkoxy, a trifluoromethyl, or a trifluoromethoxy; in the form of a base, addition to an acid, hydrate or solvate. The invention is applicable in therapy

    摘要翻译： 本发明涉及通式（I）的化合物，其中：X表示氧或硫原子; R 1表示n = 2或3时彼此独立地表示卤素原子，羟基，C 1 -C 3烷基 C 1 -C 3烷氧基，三氟甲基，三氟甲氧基或亚甲二氧基; R 2表示任选取代的C 1 -C 6烷基，C 3 -C 6烷基， 7个环烷基，哌啶基或苯基，C 3 -C 7环烷基，哌啶基或苯基任选被取代; R 3表示任选取代的氢原子或C 1 -C 6 -C 6烷基; R 4表示氢原子或C 1 -C 4烷基; R 5和R 5'彼此独立地表示氢原子，羟基，卤素原子，C 1〜 C 3烷基或R 5和R 5'一起形成氧代基; R 6表示氢原子，卤素原子，C 1 -C 3烷基，C 1〜 -C 3烷氧基，三氟甲基或三氟甲氧基; 以碱的形式加入酸，水合物或溶剂化物。 本发明适用于治疗

    Acylaminothiazole derivatives, their preparation and their therapeutic use
    6.
    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
    7.
    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：

    Sulphonamide derivatives, their preparation and their therapeutic application
    9.
    发明授权
    Sulphonamide derivatives, their preparation and their therapeutic application 失效
    磺酰胺衍生物，其制备及其治疗应用

    公开(公告)号：US07396958B2

    公开(公告)日：2008-07-08

    申请号：US11670586

    申请日：2007-02-02

    申请人： Gilles Courtemanche ,  Pierre Despeyroux ,  Evelyne Fontaine ,  Pierrick Rochard ,  Claudine Serradeil-Le Gal

    发明人： Gilles Courtemanche ,  Pierre Despeyroux ,  Evelyne Fontaine ,  Pierrick Rochard ,  Claudine Serradeil-Le Gal

    IPC分类号： C07C303/00 ,  A01N41/06

    CPC分类号： C07D213/42 ,  C07C311/21 ,  C07C311/29 ,  C07C311/44 ,  C07D217/06 ,  C07D233/64 ,  C07D257/04 ,  C07D271/06 ,  C07D277/28 ,  C07D317/62 ,  C07D319/18 ,  C07D333/20

    摘要： Disclosed are compounds having the general formula (I) as defined herein, the preparation thereof, and the use thereof for the prophylaxis or treatment of any disease involving a dysfunction associated with the orexin 2 receptor such as obesity, appetite or taste disorders including cachexia, anorexia and bulimia, diabetes, metabolic syndromes, vomiting and nausea, depression and anxiety, addictions, mood and behaviour disorders, schizophrenia, sleep disorders, restless legs syndrome, memory learning disorders, sexual and psychosexual dysfunctions, pain, visceral or neuropathic pain, hyperalgesia, allodynia, digestive disorders, irritable bowel syndrome, neuronal degenerescence, ischaemic or haemorrhagic attacks, Cushing's disease, Guillain-Barré syndrome, myotonic dystrophy, urinary incontinence, hyperthyroidism, pituitary function disorders, hypertension or hypotension.

    摘要翻译： 公开了具有本文所定义的通式（I）的化合物，其制备方法及其用于预防或治疗涉及食欲肽2受体相关功能障碍的任何疾病，例如肥胖，食欲或味觉障碍，包括恶病质， 厌食和贪食症，糖尿病，代谢综合征，呕吐和恶心，抑郁和焦虑，瘾，情绪和行为障碍，精神分裂症，睡眠障碍，不宁腿综合征，记忆学习障碍，性和心理性功能障碍，疼痛，内脏或神经性疼痛，痛觉过敏 ，异常性疼痛，消化系统疾病，肠易激综合征，神经元脱色，缺血性或出血性发作，库欣氏病，吉兰巴利综合征，强直性营养不良，尿失禁，甲状腺机能亢进，垂体功能障碍，高血压或低血压。