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1. 发明授权

US07396958B2 Sulphonamide derivatives, their preparation and their therapeutic application 失效
标题翻译：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。

2. 发明授权

US07968534B2 Sulfonamide derivatives, preparation thereof and use thereof as antagonists of orexin 2 receptors 失效
标题翻译：磺酰胺衍生物，其制备及其作为食欲素2受体的拮抗剂的用途
公开(公告)号：US07968534B2
公开(公告)日：2011-06-28
申请号：US12176753
申请日：2008-07-21
申请人： Pierre Despeyroux , Evelyne Fontaine , Gilles Courtemanche , Pierrick Rochard , Claudine Serradeil-Le Gal
发明人： Pierre Despeyroux , Evelyne Fontaine , Gilles Courtemanche , Pierrick Rochard , Claudine Serradeil-Le Gal
IPC分类号： A61K31/135 , A61K31/397 , A61K31/40 , A61K31/445 , C07D295/027 , C07D205/04 , C07D211/56 , C07C311/21
CPC分类号： C07D403/12 , C07C311/29 , C07C2601/08 , C07D205/04 , C07D207/14 , C07D211/58 , C07D401/14
摘要： The present invention is directed to a compound of formula (I): wherein Ar1, Ar2, Ar3, R1 and T are as defined herein, its preparation, pharmaceutical composition and uses as orexin 2 receptor antagonist.
摘要翻译：本发明涉及式（I）化合物：其中Ar1，Ar2，Ar3，R1和T如本文所定义，其制备，药物组合物和用作食欲肽2受体拮抗剂。

3. 发明申请

US20080058380A1 ACYLAMINOTHIAZOLE DERIVATIVES, THEIR PREPARATION AND THEIR THERAPEUTIC USE 审中-公开
标题翻译：丙酰胺唑衍生物，其制备及其治疗用途
公开(公告)号：US20080058380A1
公开(公告)日：2008-03-06
申请号：US11858454
申请日：2007-09-20
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： C07D277/20 , A61K31/426 , A61K31/454 , C07D401/02 , A61P25/00
CPC分类号： C07D417/12 , C07D277/40 , C07D277/42 , C07D277/46
摘要： The invention relates to a compound corresponding to the general formula (I): wherein, X, R1, R2, R3, R4, R5, R5′ and R6 are as defined herein. More specifically, this invention relates to intermediates to prepare a compound of formula (I) as well as its utility in treating a variety of diseases including Alzheimer's disease and Parkinson's disease.
摘要翻译：本发明涉及对应于通式（I）的化合物：其中X，R 1，R 2，R 3，R R 5，R 5，R 5'和R 6如本文所定义。更具体地，本发明涉及制备式（I）化合物的中间体以及其在治疗各种疾病（包括阿尔茨海默氏病和帕金森病）中的用途。

4. 发明授权

US5731340A Glycinamide derivatives, processes for their preparation and medicines containing them 失效
标题翻译：甘氨酰胺衍生物，其制备方法和含有它们的药物
公开(公告)号：US5731340A
公开(公告)日：1998-03-24
申请号：US515640
申请日：1995-08-16
申请人： Jean-Pierre Bras , Paul de Cointet , Pierre Despeyroux , Daniel Frehel , Danielle Gully , Jean-Pierre Maffrand , Eric Bignon
发明人： Jean-Pierre Bras , Paul de Cointet , Pierre Despeyroux , Daniel Frehel , Danielle Gully , Jean-Pierre Maffrand , Eric Bignon
IPC分类号： C07C237/12 , A61K31/16 , A61K31/165 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/47 , A61K31/472 , A61K38/00 , A61P1/00 , A61P1/14 , A61P3/04 , A61P25/00 , A61P25/18 , A61P43/00 , C07C209/08 , C07C211/16 , C07C211/40 , C07C211/44 , C07C231/02 , C07C237/04 , C07C237/14 , C07C237/20 , C07C237/22 , C07C271/22 , C07C309/04 , C07C323/60 , C07D209/42 , C07D215/48 , C07D215/54 , C07D217/26 , C07D405/04 , C07D471/06 , A61K31/445 , A61K31/535
CPC分类号： C07D405/04 , C07C237/04 , C07C237/14 , C07C237/20 , C07C237/22 , C07C271/22 , C07C323/60 , C07D209/42 , C07D215/48 , C07D215/54 , C07D217/26 , C07D471/06 , C07C2101/02 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要： The present invention relates to compounds of formula: ##STR1## which are agonists of cholecystokinin receptors and pharmaceutical compositions containing them.
摘要翻译：本发明涉及作为胆囊收缩素受体的激动剂和含有它们的药物组合物的下式的化合物。

5. 发明授权

US07563903B2 Acylaminothiazole derivatives, their preparation and their therapeutic use 失效
标题翻译：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。

6. 发明授权

US5798353A Polysubstituted 3-acylamino-5-phenyl-1,4-benzodiazepin-2-one derivatives, process for their preparation and the pharmaceutical compositions containing them 失效
标题翻译：多取代的3-酰基氨基-5-苯基-1,4-苯并二氮杂-2-酮衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5798353A
公开(公告)日：1998-08-25
申请号：US975003
申请日：1997-11-20
申请人： Alain Badorc , Pierre Despeyroux , Daniele Gully , Paul De Cointet , Daniel Frehel , Jean-Pierre Maffrand
发明人： Alain Badorc , Pierre Despeyroux , Daniele Gully , Paul De Cointet , Daniel Frehel , Jean-Pierre Maffrand
IPC分类号： C12N9/99 , A61K31/55 , A61K31/551 , A61P1/00 , A61P3/04 , A61P25/18 , A61P25/28 , A61P43/00 , C07D243/24 , C07D243/30 , C07D401/12 , C07D403/12 , C07K5/068 , C07K14/575 , C07K14/655 , C07K14/705
CPC分类号： C07D403/12 , C07D243/24
摘要： The invention relates to the compounds of formula (I) ##STR1## in which R.sub.I, R.sub.II, X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are as defined in claim 1.
摘要翻译：本发明涉及其中RI，RII，X1，X2，X3和X4如权利要求1中所定义的式（I）化合物。

7. 发明申请

US20060052426A1 Acylaminothiazole derivatives, their preparation and their therapeutic use 失效
标题翻译：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：

8. 发明授权

US5534530A 5-acylamino-1,2,4-thiadiazoles, their preparation and pharmaceutical compositions containing them 失效
标题翻译： 5-酰基氨基-1,2,4-噻二唑，其制备方法和含有它们的药物组合物
公开(公告)号：US5534530A
公开(公告)日：1996-07-09
申请号：US226862
申请日：1994-04-13
申请人： Daniel Frehel , Danielle Gully , Robert Boigegrain , Alain Badorc , Jean-Pierre Bras , Pierre Despeyroux
发明人： Daniel Frehel , Danielle Gully , Robert Boigegrain , Alain Badorc , Jean-Pierre Bras , Pierre Despeyroux
IPC分类号： A61K31/41 , A61K31/415 , A61K31/433 , A61K31/47 , A61K31/4725 , A61K31/475 , A61P1/00 , A61P1/04 , A61P1/14 , A61P1/16 , A61P3/04 , A61P25/00 , A61P25/04 , A61P25/20 , A61P43/00 , C07D285/08 , C07D417/12 , C07D417/14 , C07D471/06 , C07D285/12
CPC分类号： C07D285/08 , C07D417/12 , C07D417/14 , C07D471/06 , Y02P20/55
摘要： The invention relates to thiadiazole derivatives corresponding to the general formula ##STR1## in which Ar represents a nitrogen-containing aromatic heterocycle, in particular indolyl which is substituted or unsubstituted on the nitrogen atom with CO--(C.sub.1 -C.sub.4)alkyl; with (CH.sub.2).sub.n COR in which n represents 1 or 2 and R represents OR.sub.1 or NR.sub.1 R.sub.2 with R.sub.1 and R.sub.2, which may be identical or different, representing H or (C.sub.1 -C.sub.4)alkyl; with (C.sub.1 -C.sub.4) hydroxyalkyl; with (C.sub.2 -C.sub.6) alkoxyalkyl; tetrahydropyranyl; or with a --(CH.sub.2).sub.3 -- chain, the last carbon of which is attached to the phenyl ring of the indole to form a 6-membered ring;Z represents(a) the group ##STR2## where A and B, independently of each other, represent C, CH or N; and X.sub.1, X.sub.2, X.sub.3 and X.sub.4, which may be identical or different, represent H, (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, Cl, Br or trifluoromethyl, or alternatively(b) an optionally substituted naphthyl group, as well as their pharmaceutically acceptable salts.
摘要翻译：本发明涉及对应于通式为I的噻二唑衍生物，其中Ar表示含氮芳族杂环，特别是在氮原子上具有取代或未取代的具有CO-（C 1 -C 4）烷基的吲哚基; 其中n表示1或2，R表示OR 1或NR 1 R 2，R 1和R 2可以相同或不同，表示H或（C 1 -C 4）烷基; 与（C 1 -C 4）羟烷基; 与（C 2 -C 6）烷氧基烷基; 四氢吡喃基; 或与 - （CH 2）3 - 链结合，最后一个碳与吲哚的苯环连接形成6-元环; Z表示（a）组，其中A和B彼此独立地表示C，CH或N; 可以相同或不同的X 1，X 2，X 3和X 4表示H，（C 1 -C 3）烷基，（C 1 -C 3）烷氧基，Cl，Br或三氟甲基，或者（b）任选取代的萘基，以及它们的药学上可接受的盐。

9. 发明授权

US07288659B2 Acylaminothiazole derivatives, their preparation and therapeutic use 有权
标题翻译：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

10. 发明授权

US5719143A Polysubstituted 3-acylamino-5-phenyl-1, 4-benzodiazepin-2-one derivatives, process for their preparation and the pharmaceutical compositions containing them 失效
标题翻译：多取代的3-酰基氨基-5-苯基-1,4-苯并二氮杂-2-酮衍生物，其制备方法和含有它们的药物组合物
公开(公告)号：US5719143A
公开(公告)日：1998-02-17
申请号：US390770
申请日：1995-02-14
申请人： Alain Badorc , Pierre Despeyroux , Daniele Gully , Paul de Cointet , Daniel Frehel , Jean-Pierre Maffrand
发明人： Alain Badorc , Pierre Despeyroux , Daniele Gully , Paul de Cointet , Daniel Frehel , Jean-Pierre Maffrand
IPC分类号： C12N9/99 , A61K31/55 , A61K31/551 , A61P1/00 , A61P3/04 , A61P25/18 , A61P25/28 , A61P43/00 , C07D243/24 , C07D243/30 , C07D401/12 , C07D403/12 , C07K5/068 , C07K14/575 , C07K14/655 , C07K14/705 , A61K31/395
CPC分类号： C07D403/12 , C07D243/24
摘要： The invention relates to the compounds of formula (I) ##STR1## in which R.sub.I, R.sub.II, X.sub.1, X.sub.2, X.sub.3 and X.sub.4 are as defined in claim 1.
摘要翻译：本发明涉及其中RI，RII，X1，X2，X3和X4如权利要求1中所定义的式（I）化合物。

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