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1. 发明授权

US4496568A Antiinflammatory thieno [2,3-c]pyridine derivatives 失效
标题翻译：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。

2. 发明授权

US4104390A Thieno [2,3-c] and [3,2-c] pyridines 失效
标题翻译：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。

3. 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。

4. 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。

5. 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。

6. 发明授权

US4740510A Derivatives of alpha-(2-oxo 2,4,5,6,7,7a-hexahydro thieno[3,2-c]5-pyridyl) phenyl acetic acid, and their use as platelet and thrombotic aggregation inhibitors 失效
标题翻译： α-（2-氧代2,4,5,6,7,7a-六氢噻吩并[3,2-c] -5-吡啶基）苯基乙酸的衍生物及其作为血小板和血栓聚集抑制剂的用途
公开(公告)号：US4740510A
公开(公告)日：1988-04-26
申请号：US825068
申请日：1986-01-31
申请人： Alain Badorc , Daniel Frehel , Jean-Pierre Maffrand , Eric Vallee
发明人： Alain Badorc , Daniel Frehel , Jean-Pierre Maffrand , Eric Vallee
IPC分类号： A61K31/435 , A61K31/4365 , A61P7/02 , C07D495/04 , C07D471/04
CPC分类号： C07D495/04
摘要： The present invention relates to novel derivatives of alpha-(2-oxo 2,4,5,6,7,7a-hexahydro thieno [3,2-c] 5-pyridyl) phenyl acetic acid corresponding to the following general formula: ##STR1## their addition salts with pharmaceutically-acceptable inorganic or organic acids as well as isomers and their mixtures.The invention also relates to their process of preparation and to medicaments containing these compounds which are of therapeutic use as inhibitors of platelet- and thrombotic-aggregation.
摘要翻译：本发明涉及对应于以下通式的α-（2-氧代2,4,5,6,7,7a-六氢噻吩并[3,2-c] -5-吡啶基）苯基乙酸的新衍生物：它们与药学上可接受的无机酸或有机酸的加成盐以及异构体及其混合物。本发明还涉及它们的制备方法和含有这些化合物的药物，其作为血小板聚集和血栓形成聚集的抑制剂具有治疗用途。

7. 发明授权

US5576328A Method for the secondary prevention of ischemic events 失效
标题翻译：二次预防缺血事件的方法
公开(公告)号：US5576328A
公开(公告)日：1996-11-19
申请号：US190332
申请日：1994-01-31
申请人： Jean-Marc Herbert , Daniel Frehel , Andr e Bernat , Alain Badorc , Pierre Savi , Denis Delebass ee , Gilles Kieffer , Ghislain Defreyn , Jean-Pierre Maffrand
发明人： Jean-Marc Herbert , Daniel Frehel , Andr e Bernat , Alain Badorc , Pierre Savi , Denis Delebass ee , Gilles Kieffer , Ghislain Defreyn , Jean-Pierre Maffrand
IPC分类号： A61K31/4365 , A61K31/44
CPC分类号： A61K31/4365
摘要： The invention relates to a new method for the secondary prevention of ischemic events comprising administering to a man in need thereof a therapeutically effective amount of a compound selected from clopidogrel and its pharmaceutically acceptable acid addition salts in association with a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及一种用于二次预防缺血事件的新方法，包括向有需要的人施用治疗有效量的与药学上可接受的载体结合的选自氯吡格雷及其药学上可接受的酸加成盐的化合物。

8. 发明授权

US4523013A 4-Acyl-2,6-dioxo-1-phenethyl piperozines 失效
标题翻译： 4-酰基-2,6-二氧代-1-苯乙基哌嗪
公开(公告)号：US4523013A
公开(公告)日：1985-06-11
申请号：US462397
申请日：1983-01-31
申请人： Daniel Frehel , Jean-Pierre Maffrand
发明人： Daniel Frehel , Jean-Pierre Maffrand
IPC分类号： C07D241/06 , C07D241/08 , C07D471/04
CPC分类号： C07D241/06 , C07C255/00 , C07D241/08 , C07D471/04
摘要： 2-Acyl-1,3,4,6,7,11b-hexahydro-2H-pyrazino-[2,1-a]-4-isoquinoleinones having anthelmintic activity of the formula ##STR1## are prepared from 4-acyl-2,6-dioxopierazines by reaction with a phenethyl halide, selective reduction of one of the oxo groups and cyclization, by the novel intermediates of formula ##STR2## in which Y represents O or H, OH.
摘要翻译：具有式“IMAGE”的具有驱虫活性的2-酰基-1,3,4,6,7,11b-六氢-2H-吡嗪并[2,1-a] -4-异喹啉酮由4-酰基-2 通过与苯乙基卤化物反应，选择性还原一个氧代基和环化，通过其中Y代表O或H，OH的式“IMAGE”的新型中间体，6-二氧杂吡咯嗪。

9. 发明授权

US4500534A Thieno-pyridinone derivatives, process for its preparation, and anti-blood-platelet and anti-thrombotic applications thereof 失效
标题翻译：噻吩并吡啶酮衍生物，其制备方法，抗血小板和抗血栓形成应用
公开(公告)号：US4500534A
公开(公告)日：1985-02-19
申请号：US504524
申请日：1983-06-15
申请人： Daniel Frehel , Jean-Pierre Maffrand , Eric Vallee
发明人： Daniel Frehel , Jean-Pierre Maffrand , Eric Vallee
IPC分类号： C07D495/00 , A61K31/381 , A61K31/435 , A61K31/4535 , A61P7/02 , C07D495/04
CPC分类号： C07D495/04
摘要： This invention relates to a new thieno-pyridinone derivative of the formula: ##STR1## and its pharmaceutically acceptable inorganic or organic acid addition salts.This invention relates also to a process for the preparation of said compound and to its therapeutic application as blood-platelet anti-aggregation agent and anti-thrombosis agent.
摘要翻译：本发明涉及下式的新的噻吩并吡啶酮衍生物及其药学上可接受的无机酸或有机酸加成盐。本发明还涉及制备所述化合物及其治疗应用的血小板抗凝集剂和抗血栓形成剂的方法。

10. 发明授权

US4136186A Thieno[3,2-c]pyridine derivatives 失效
标题翻译：噻吩（3,2-C）吡啶衍生物
公开(公告)号：US4136186A
公开(公告)日：1979-01-23
申请号：US763876
申请日：1977-01-13
申请人： Daniel Frehel , Jean-Pierre Maffrand
发明人： Daniel Frehel , Jean-Pierre Maffrand
IPC分类号： A61K31/435 , A61K31/4365 , A61P7/02 , A61P25/20 , A61P29/00 , C07D211/78 , C07D495/04 , C07D513/04 , A61K31/44
CPC分类号： C07D495/04 , C07D211/78
摘要： This invention relates to thieno[3,2-c]pyridine derivatives having the formula: ##STR1## in which: R.sub.1 represents an alkyl radical having 1-6 carbon atoms;R.sub.2 represents a radical selected from hydrogen and an acyl group;R.sub.3 represents a radical selected from hydrogen; an acyl group; an alkoxycarbonyl group; a phenyl group; a phenyl group substituted with at least a substitutent selected with at least a substituent selected from halogen, hydroxy, nitro, amino, cyano, carboxy, alkoxycarbonyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy; a phenoxy group; a phenoxy group substituted with at least a substituent selected from halogen, hydroxy, nitro, amino, cyano, carboxy, alkoxycarbonyl, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; and a trifluoromethyl group;R.sub.4 represents hydrogen, an acyl group, an alkoxy carbonyl group, or a phenyl or phenoxy group optionally substituted with at least a halogen atom or a hydroxy, nitro, amino, cyano, carboxy, alkoxycarbonyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy group, or a trifluoromethyl group, andN is an integer from 0 to 15; and their pharmaceutically acceptable acid addition salts.Said derivatives have an inhibiting activity on blood-platelet aggregation, and anti-inflammator and sedative activities.

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