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31. 发明授权

US07884123B2 Substituted thieno[2,3-c]pyrazoles, process for preparing them, compositions containing them, and use thereof 失效
标题翻译：取代的噻吩并[2,3-c]吡唑，其制备方法，含有它们的组合物及其用途
公开(公告)号：US07884123B2
公开(公告)日：2011-02-08
申请号：US11752612
申请日：2007-05-23
申请人： Jean-Christophe Carry , Gilles Doerflinger , Antony Bigot , Dominique Barbalat-Damour , François Clerc , Arielle Genevois-Borella , Baptiste Ronan , Hervé Minoux , Claude Barberis , Yves Janin
发明人： Jean-Christophe Carry , Gilles Doerflinger , Antony Bigot , Dominique Barbalat-Damour , François Clerc , Arielle Genevois-Borella , Baptiste Ronan , Hervé Minoux , Claude Barberis , Yves Janin
IPC分类号： A61K31/4162 , C07D487/04
CPC分类号： C07D495/04
摘要： Compounds of formula (I), wherein R1 and R3 have the meanings given in the description, said compounds being in all isomeric forms; and salts thereof; processes for the preparation of the compounds and intermediates; compositions containing them, and the use thereof as medicaments, particularly as anti-cancer agents.
摘要翻译：式（I）化合物，其中R1和R3具有本说明书中给出的含义，所述化合物为所有异构体形式; 及其盐; 制备化合物和中间体的方法; 含有它们的组合物及其作为药物的用途，特别是作为抗癌剂。

32. 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。

33. 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。

34. 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。

35. 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。

36. 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。

37. 发明授权

US08791255B2 (6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives, preparation thereof and pharmaceutical use thereof as AKT(PKB) phosphorylation inhibitors 有权
标题翻译：（6-氧代-1,6-二氢嘧啶-2-基）酰胺衍生物，其制备方法及其作为AKT（PKB）磷酸化抑制剂的药物用途
公开(公告)号：US08791255B2
公开(公告)日：2014-07-29
申请号：US13338011
申请日：2011-12-27
申请人： Jean-Christophe Carry , Victor Certal , Frank Halley , Karl Andreas Karlsson , Laurent Schio , Fabienne Thompson
发明人： Jean-Christophe Carry , Victor Certal , Frank Halley , Karl Andreas Karlsson , Laurent Schio , Fabienne Thompson
IPC分类号： C07D413/04
CPC分类号： C07D239/22 , C07D239/47 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/10 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D471/04
摘要： The invention relates to the novel materials of formula (I), wherein each of the substituents R, R1, R2, R3, R4 and R5 is as defined herein. The materials are useful as inhibitors of AKT(PKB) phosphorylation.
摘要翻译：本发明涉及式（I）的新型材料，其中取代基R 1，R 2，R 3，R 4和R 5中的每一个如本文所定义。该物质可用作AKT（PKB）磷酸化抑制剂。

38. 发明申请

US20130274253A1 NOVEL PYRIMIDINE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF AS AKT(PKB) PHOSPHORYLATION INHIBITORS 有权
标题翻译：新型吡啶衍生物，其制备方法及其作为AKT（PKB）磷酸化抑制剂的药物用途
公开(公告)号：US20130274253A1
公开(公告)日：2013-10-17
申请号：US13977396
申请日：2011-12-22
申请人： Maurice Brollo , Jean-Christophe Carry , Victor Certal , Eric Didier , Gilles Doerflinger , Youssef EL Ahmad , Bruno Filoche-Romme , Frank Halley , Karl Andreas Karlsson , Laurent Schio , Fabienne Thompson
发明人： Maurice Brollo , Jean-Christophe Carry , Victor Certal , Eric Didier , Gilles Doerflinger , Youssef EL Ahmad , Bruno Filoche-Romme , Frank Halley , Karl Andreas Karlsson , Laurent Schio , Fabienne Thompson
IPC分类号： C07D403/06 , C07D403/14
CPC分类号： C07D403/06 , C07D209/30 , C07D401/04 , C07D403/04 , C07D403/14 , C07D413/04 , C07D413/14 , C07D471/10
摘要： The present invention relates to novel chemical compounds derived from pyrimidines, to the method for preparing same, to the novel intermediates obtained, to the use thereof as drugs, to the pharmaceutical compositions containing same, and to the therapeutic use thereof as AKT inhibitors.
摘要翻译：本发明涉及衍生自嘧啶的新化合物，其制备方法，获得的新型中间体，作为药物的用途，含有其的药物组合物及其作为AKT抑制剂的治疗用途。

39. 发明申请

US20120220621A1 ANTI-CANCER COMPOUND AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME 有权
标题翻译：抗癌化合物和含有其的药物组合物
公开(公告)号：US20120220621A1
公开(公告)日：2012-08-30
申请号：US13320965
申请日：2010-05-17
申请人： Jean-Christophe Carry , Michel Cheve , Francois Clerc , Cecile Combeau , Sylvie Gontier , Alain Krick , Sylvette Lachaud , Laurent Schio
发明人： Jean-Christophe Carry , Michel Cheve , Francois Clerc , Cecile Combeau , Sylvie Gontier , Alain Krick , Sylvette Lachaud , Laurent Schio
IPC分类号： A61K31/4745 , C07D405/12 , A61P35/00 , C07D471/04
CPC分类号： C07D471/04 , C07D235/26
摘要： The invention relates to a compound of formula (I), more specifically in the levorotatory form (1a) thereof, in particular the form having a rotatory power [α]D=−38.6+0.7 at a concentration of 0.698 mg/ml in methanol. The compound may be in the form of a base or an acid addition salt, in particular a pharmaceutically acceptable acid. The compound is a selective Aurora A and B kinase inhibitor and can be used as an anticancer drug.
摘要翻译：本发明涉及式（I）化合物，更具体地说是其左旋形式（1a），特别是在甲醇中具有0.698mg / ml浓度的旋光度[α] D = -38.6 + 0.7的形式。化合物可以是碱或酸加成盐，特别是药学上可接受的酸的形式。该化合物是选择性的Aurora A和B激酶抑制剂，可用作抗癌药物。

40. 发明申请

US20120122947A1 SPIRO-OXINDOLE MDM2 ANTAGONISTS 有权
公开(公告)号：US20120122947A1
公开(公告)日：2012-05-17
申请号：US13294315
申请日：2011-11-11
申请人： Shaomeng Wang , Yujun Zhao , Wei Sun , Sanjeev Kumar , Lance Leopold , Laurent Debussche , Cedric Barriere , Jean-Christophe Carry , Kwame Amaning
发明人： Shaomeng Wang , Yujun Zhao , Wei Sun , Sanjeev Kumar , Lance Leopold , Laurent Debussche , Cedric Barriere , Jean-Christophe Carry , Kwame Amaning
IPC分类号： A61K31/407 , A61P35/00 , A61P35/02 , C07D487/10
CPC分类号： A61N5/10 , A61K31/407 , A61K45/06 , C07D487/10 , A61K2300/00
摘要： Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
摘要翻译：本文提供了药物化学领域中的化合物，组合物和方法。本文提供的化合物和组合物涉及用作p53和MDM2之间相互作用的拮抗剂的螺 - 羟基吲哚，以及它们作为治疗癌症和其它疾病的治疗剂的用途。

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