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71. 发明授权

US5026717A 2-imino-6-polyfluoroalkoxybenzothiazole derivatives, and pharmaceutical compositions containing them 失效
标题翻译： 2-亚氨基-6-多氟烷氧基苯并噻唑衍生物和含有它们的药物组合物
公开(公告)号：US5026717A
公开(公告)日：1991-06-25
申请号：US543418
申请日：1990-06-26
申请人： Francois Audiau , Claude Gueremy , Patrick Jimonet , Serge Mignani
发明人： Francois Audiau , Claude Gueremy , Patrick Jimonet , Serge Mignani
IPC分类号： A61K31/425 , A61K31/428 , A61K31/44 , A61K31/505 , A61P25/00 , A61P25/08 , A61P25/18 , A61P25/28 , C07D277/82 , C07D417/12
CPC分类号： C07D417/12 , C07D277/82
摘要： Compounds of formula: ##STR1## and their salts, in which R.sub.1 represents polyfluoroalkoxy, and R.sub.2 represents alkyl, alkenyl (3-6 C), [cycloalkyl (3-6 C)]-alkyl, carbamoylalkyl, dialkylcarbamoylalkyl, acylaminoalkyl, phenylthioalkyl, hydroxyalkyl, cyanoalkyl, sulphamoylethyl, N-alkylsulphamoylethyl, pyridylthioalkyl, pyridiylalkylthioalkyl, pyridylsulphinylalkyl, alkynyl (3-6 C), phenylsulphinylalkyl, halophenylthioalkyl, (2,2,2-trifluoroethylthio)alkyl, 2-dialkylaminopropyl, pyrimidinylsulphinylalkyl, pyridylalkylsulphinylalkyl, halophenylsulphinylalkyl or (2,2,2-trifluoroethylsulphinyl)alkyl are useful in the treatment of medical conditions associated with the effects of glutamate.

72. 发明授权

US07230007B2 Derivatives of 3-(Guanidinocarbonyl) heterocycle, methods of preparation and intermediates thereof, their use as medicaments, and pharmaceutical compositions therefrom 失效
标题翻译： 3-（胍基羰基）杂环的衍生物，其制备方法及其中间体，其作为药物的用途及其药物组合物
公开(公告)号：US07230007B2
公开(公告)日：2007-06-12
申请号：US10865454
申请日：2004-06-10
申请人： Jean-Christophe Carry , Gilles Doerflinger , Arielle Genevois-Borella , Michel Evers , Alain Le Brun , Jean-Paul Martin , Pascal Desmazeau , Serge Mignani , Heinz-Werner Kleemann
发明人： Jean-Christophe Carry , Gilles Doerflinger , Arielle Genevois-Borella , Michel Evers , Alain Le Brun , Jean-Paul Martin , Pascal Desmazeau , Serge Mignani , Heinz-Werner Kleemann
IPC分类号： A61K31/44 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention discloses and claims compounds of formula I and their pharmaceutically acceptable salts, and methods of using said compounds of formula I, either alone or in combination with other medicaments, as antiarrhythmic medicaments with a cardioprotective component for prophylaxis or treatment of infarction, for the treatment of angina pectoris, and as inhibitors of pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure. Pharmaceutical compositions comprising compounds of formula I or compounds of formula I in combination with one or more other medicaments and processes for the preparation of compounds of formula I are also disclosed and claimed.
摘要翻译：本发明公开并要求式I化合物及其药学上可接受的盐，以及使用所述式I化合物单独或与其它药物组合的抗心律失常药物与预防或治疗梗死的心脏保护组分的方法，用于心绞痛的治疗以及与局部缺血诱导的损伤发展相关的病理生理过程的抑制剂，特别是引发缺血诱导的心律失常和心力衰竭。包含式I化合物或式I化合物与一种或多种其它药物组合的药物组合物和式I化合物的制备方法也被公开并要求保护。

73. 发明申请

US20060148880A1 Isoindolone derivatives, preparation process and intermediates of this process, their use as medicaments, and pharmaceutical compositions comprising them 有权
公开(公告)号：US20060148880A1
公开(公告)日：2006-07-06
申请号：US11365319
申请日：2006-03-01
申请人： Heinz-Werner Kleemann , Armin Hofmeister , Jean-Christophe Carry , Baptiste Ronan , Serge Mignani , Antony Bigot
发明人： Heinz-Werner Kleemann , Armin Hofmeister , Jean-Christophe Carry , Baptiste Ronan , Serge Mignani , Antony Bigot
IPC分类号： A61K31/4035 , C07D403/02 , C07D209/46
CPC分类号： C07D209/46
摘要： The present invention relates to the novel isoindolone derivatives of the formula I in which R1 to R6 have the meanings stated in the claims. The inventive compounds are suitable as antiarrhythmic medicaments with a cardioprotective component for infarction prophylaxis and infarction treatment and for the treatment of angina pectoris. They also inhibit in a preventive manner the pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure.

74. 发明申请

US20050014758A1 Derivatives of 3-(guanidinocarbonyl) heterocycle, methods of preparation and intermediates thereof, their use as medicaments, and pharmaceutical compositions therefrom 失效
标题翻译： 3-（胍基羰基）杂环的衍生物，其制备方法及其中间体，它们作为药物的用途及其药物组合物
公开(公告)号：US20050014758A1
公开(公告)日：2005-01-20
申请号：US10865454
申请日：2004-06-10
申请人： Jean-Christophe Carry , Gilles Doerflinger , Arielle Genevois-Borella , Michel Evers , Alain Le Brun , Jean-Paul Martin , Pascal Desmazeau , Serge Mignani , Heinz-Werner Kleemann
发明人： Jean-Christophe Carry , Gilles Doerflinger , Arielle Genevois-Borella , Michel Evers , Alain Le Brun , Jean-Paul Martin , Pascal Desmazeau , Serge Mignani , Heinz-Werner Kleemann
IPC分类号： C07D471/04 , C07D471/02 , A61K31/4745 , A61K31/503 , A61K31/519 , C07D487/02
CPC分类号： C07D471/04
摘要： The present invention discloses and claims compounds of formula I and their pharmaceutically acceptable salts, and methods of using said compounds of formula I, either alone or in combination with other medicaments, as antiarrhythmic medicaments with a cardioprotective component for prophylaxis or treatment of infarction, for the treatment of angina pectoris, and as inhibitors of pathophysiological processes associated with the development of ischemia-induced damage, in particular in the triggering of ischemia-induced cardiac arrhythmias and of heart failure. Pharmaceutical compositions comprising compounds of formula I or compounds of formula I in combination with one or more other medicaments and processes for the preparation of compounds of formula I are also disclosed and claimed.
摘要翻译：本发明公开并要求式I化合物及其药学上可接受的盐，以及使用所述式I化合物单独或与其它药物组合的抗心律失常药物与预防或治疗梗死的心脏保护组分的方法，用于心绞痛的治疗以及与局部缺血诱导的损伤发展相关的病理生理过程的抑制剂，特别是引发缺血诱导的心律失常和心力衰竭。包含式I化合物或式I化合物与一种或多种其它药物组合的药物组合物和式I化合物的制备方法也被公开并要求保护。

75. 发明授权

US06420566B2 Pharmaceutical compositions containing a 4, 5-dihydro-1, 3-thiazol-2-ylamine derivative, novel derivatives and preparation thereof 失效
标题翻译：含有4,5,5-二氢-1,3-噻唑-2-基胺衍生物的药物组合物及其制备方法
公开(公告)号：US06420566B2
公开(公告)日：2002-07-16
申请号：US09878045
申请日：2001-06-08
申请人： Jean-Christophe Carry , Dominique Damour , Claude Guyon , Serge Mignani , Eric Bacque , Antony Bigot
发明人： Jean-Christophe Carry , Dominique Damour , Claude Guyon , Serge Mignani , Eric Bacque , Antony Bigot
IPC分类号： C07D27708
CPC分类号： C07D277/18
摘要： The present invention relates to pharmaceutical compositions containing, as active principle, a 4,5-dihydro-1,3-thiazol-2-ylamine derivative of formula (I): in which R represents an -alk-S-alk-Ar radical, a phenyl radical or a phenyl radical substituted with alkoxy or halogen, or to one of the pharmaceutically acceptable salts thereof, to the novel derivatives of formula (I) and to their preparation.
摘要翻译：本发明涉及含有式（I）的4,5-二氢-1,3-噻唑-2-基胺衍生物作为活性成分的药物组合物：其中R表示-alk-S-alk-Ar基团，苯基或被烷氧基或卤素取代的苯基或其一种药学上可接受的盐与式（I）的新衍生物及其制备方法。

76. 发明授权

US06362185B1 Polyhydroxyalkylpyrazine derivatives, their preparation and the medicaments comprising them 有权
标题翻译：聚羟基烷基吡嗪衍生物，其制备方法和包含它们的药物
公开(公告)号：US06362185B1
公开(公告)日：2002-03-26
申请号：US09483939
申请日：2000-01-14
申请人： Georges Bashiardes , Jean-Christophe Carry , Michel Evers , Bruno Filoche , Serge Mignani
发明人： Georges Bashiardes , Jean-Christophe Carry , Michel Evers , Bruno Filoche , Serge Mignani
IPC分类号： A61K314965
CPC分类号： A61K31/495 , C07D241/12
摘要： The present invention relates to medicaments comprising at least one compound of formula: wherein either R1 represents a —CH(Ra)—CHOH—CHOH—CH2OH chain and R2 represents a —CH2—CHOH—CHOH—CH2OH chain, or R1 represents a —CHOH—CHF—CHOH—CH2OH chain and R2 represents a —CH2—CHF—CHOH—CH2OH chain, or R1 represents a —CHOH—CHOH—CHOH—Rb chain and R2 represents a —CH2—CHOH—CHOH—Rb chain, or R1 represents a —CH2—CHOH—CHOH—CH2OH chain and R2 represents a —CH2—CHOH—CHOH—CH2OH chain, or R1 and R2 are identical and each represent a —(CHOH)n—CH2OH chain in which n is equal to 1, 2, 3 or 4, Ra represents an alkoxy radical (1-6 C in a straight or branched chain) or a fluorine atom, and Rb represents a carboxyl, —CO—NH2 or —CH2—NH2 radical, or one of their stereoisomers or their salts with an inorganic or organic acid, to novel compounds of formula (I) and to their preparation.
摘要翻译：本发明涉及包含至少一种下式的化合物的药物：其中R1表示-CH（Ra）-CHOH-CHOH-CH2OH链，R2表示-CH2-CHOH-CHOH-CH2OH链，或R1表示-CHOH- CHF-CHOH-CH2OH链，R2表示-CH2-CHF-CHOH-CH2OH链，或R1表示-CHOH-CHOH-CHOH-Rb链，R2表示-CH2-CHOH-CHOH-Rb链，或R1表示 -CH 2 -CHOH-CHOH-CH 2 OH链，R 2表示-CH 2 -CHOH-CHOH-CH 2 OH链，或R 1和R 2相同，各自表示其中n等于1的 - （CHOH）n -CH 2 OH链， 2,3或4中，Ra表示烷氧基（直链或支链中1-6C）或氟原子，Rb表示羧基，-CO-NH2或-CH2-NH2基，或其立体异构体或它们与无机或有机酸的盐，与式（I）的新型化合物及其制备。

77. 发明授权

US5965527A Cyclosporin compounds, their preparation and the pharmaceutical compositions which contain them 失效
标题翻译：环孢菌素化合物，它们的制备和含有它们的药物组合物
公开(公告)号：US5965527A
公开(公告)日：1999-10-12
申请号：US996699
申请日：1997-12-23
申请人： Jean-Claude Barriere , Georges Bashiardes , Jean-Christophe Carry , Michel Evers , Bruno Filoche , Jean-Pierre Leconte , Serge Mignani
发明人： Jean-Claude Barriere , Georges Bashiardes , Jean-Christophe Carry , Michel Evers , Bruno Filoche , Jean-Pierre Leconte , Serge Mignani
IPC分类号： A61K38/00 , A61P31/14 , C07K7/64 , A61K37/02 , C07K5/12
CPC分类号： C07K7/645 , A61K38/00
摘要： A cyclosporin compound of the formula (I): ##STR1## wherein Alk and R are as defined herein, or a pharmaceutically acceptable salt thereof, which derivatives are is useful in the treatment and/or prophylaxis of retrovirus infections.
摘要翻译：式（I）的环孢菌素化合物：其中Alk和R如本文所定义，或其药学上可接受的盐，该衍生物可用于治疗和/或预防逆转录病毒感染。

78. 发明授权

US5948755A Cyclosporin compound, its preparation and the pharmaceutical compositions which contain it 失效
标题翻译：环孢菌素化合物，其制剂和含有它的药物组合物
公开(公告)号：US5948755A
公开(公告)日：1999-09-07
申请号：US997613
申请日：1997-12-23
申请人： Jean-Claude Barriere , Georges Bashiardes , Jean-Christophe Carry , Michel Evers , Bruno Filoche , Serge Mignani
发明人： Jean-Claude Barriere , Georges Bashiardes , Jean-Christophe Carry , Michel Evers , Bruno Filoche , Serge Mignani
IPC分类号： A61K38/00 , A61P31/14 , C07K7/64 , A61K37/02
CPC分类号： C07K7/645 , A61K38/00
摘要： The cyclosporin compound of formula (I) is particularly useful in the treatment and/or prophylaxis of retrovirus infections. ##STR1##
摘要翻译：式（I）的环孢菌素化合物特别可用于治疗和/或预防逆转录病毒感染。

79. 发明授权

US5795903A 6-polyfluoroalkoxy-and 6-polyfluoroalkyl-2-aminobenzothiazole derivatives 失效
标题翻译： 6-多氟烷氧基和6-多氟烷基-2-氨基苯并噻唑衍生物
公开(公告)号：US5795903A
公开(公告)日：1998-08-18
申请号：US817744
申请日：1997-04-24
申请人： Philip Chapelle , Claude Gaillard , Patrick Jimonet , Erik Louvel , Michel Martinet , Serge Mignani , Gerard Sanderink
发明人： Philip Chapelle , Claude Gaillard , Patrick Jimonet , Erik Louvel , Michel Martinet , Serge Mignani , Gerard Sanderink
IPC分类号： C07D277/68 , A61K31/425 , A61K31/428 , A61P7/00 , A61P9/08 , A61P9/10 , A61P21/00 , A61P25/00 , A61P25/08 , A61P25/20 , A61P25/28 , A61P43/00 , C07D277/82
CPC分类号： C07D277/82
摘要： Compounds of formula (I): ##STR1## wherein R is a polyfluoroalkoxy or polyfluoroalkyl radical and R.sub.1 is a hydrogen atom and R.sub.2 is a hydroxyl radical, or R.sub.1 is a hydroxyl radical and R.sub.2 is a hydrogen atom, salts thereof, the preparation of said compounds, and drugs containing same.
摘要翻译： PCT No.PCT / FR95 / 01392 Sec。 371日期1997年04月24日 102（e）日期1997年4月24日PCT提交1995年10月23日PCT公布。出版物WO96 / 13492 日期：1996年5月9日，式（I）化合物：其中R为多氟烷氧基或多氟烷基，R 1为氢原子，R 2为羟基，或R 1为羟基，R 2为氢原子，其盐，所述化合物的制备和含有它们的药物。

80. 发明授权

US5789406A Indeno�1,2-E!pyrazine-4-ones, their preparation and the medicaments containing them 失效
标题翻译：茚并[1,2-E]吡嗪-4-酮，它们的制备方法和含有它们的药物
公开(公告)号：US5789406A
公开(公告)日：1998-08-04
申请号：US714163
申请日：1996-09-27
申请人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Patrick Jimonet , Serge Mignani , Yves Ribeill
发明人： Jean-Claude Aloup , Fran.cedilla.ois Audiau , Michel Barreau , Dominique Damour , Arielle Genevois-Borella , Patrick Jimonet , Serge Mignani , Yves Ribeill
IPC分类号： A61K31/495 , A61P1/08 , A61P1/16 , A61P3/04 , A61P9/00 , A61P9/08 , A61P9/10 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/12 , A61P37/04 , A61P39/02 , C07D405/04 , C07D409/04 , C07D487/04 , C07D487/14 , C07D491/147 , C07D495/14 , C02D487/04
CPC分类号： C07D487/04
摘要： The compounds of formula (I) ##STR1## wherein R, R.sub.1 and R.sub.2 are defined in the disclosure, and salts thereof. The compounds of formula (I) are non-competitive N-methyl-D-asparate (NMDA) receptor antagonists, particularly NMDA receptor glycine modulation site ligands, and are alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists, this receptor is also known as the quisqualate receptor.
摘要翻译： PCT No.PCT / FR95 / 00357 Sec。 371日期1996年9月27日第 102（e）1996年9月27日PCT 1995年3月23日PCT公布。公开号WO95 / 26349 日期1995年10月5日本公开内容中定义R 1，R 2和R 2的式（I）化合物（Ⅰ）及其盐。式（I）化合物是非竞争性的N-甲基-D-天冬氨酸（NMDA）受体拮抗剂，特别是NMDA受体甘氨酸调节位点配体，是α-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体拮抗剂，该受体也称为quisqualate受体。

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