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![Substituted thieno[2,3-c]pyrazoles, process for preparing them, compositions containing them, and use thereof](/abs-image/US/2011/02/08/US07884123B2/abs.jpg.150x150.jpg)
1.发明授权Substituted thieno[2,3-c]pyrazoles, process for preparing them, compositions containing them, and use thereof 失效取代的噻吩并[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。
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![Hydrazinocarbonyl-thieno[2,3-C]pyrazoles, process for preparing them, compositions containing them and use thereof](/abs-image/US/2009/09/29/US07595320B2/abs.jpg.150x150.jpg)
2.发明授权Hydrazinocarbonyl-thieno[2,3-C]pyrazoles, process for preparing them, compositions containing them and use thereof 有权肼基 - 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：US07595320B2
公开(公告)日：2009-09-29
申请号：US11846669
申请日：2007-08-29
申请人： Claude Barberis , Jean-Christophe Carry , Gilles Doerflinger , Dominique Barbalat-Damour , Francois Clerc , Herve Minoux
发明人： Claude Barberis , Jean-Christophe Carry , Gilles Doerflinger , Dominique Barbalat-Damour , Francois Clerc , Herve Minoux
IPC分类号： A61K31/496 , A61K31/4162 , C07D231/54 , C07D409/14
CPC分类号： C07D495/04
摘要： The present invention concerns hydrazinocarbonyl-thieno[2,3-c]pyrazoles of formula (I): wherein R1, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions containing the same and their use for the treatment of pathological conditions, in particular as anticancer agents.
摘要翻译： 本发明涉及式（I）的肼基羰基 - 噻吩并[2,3-c]吡唑：其中R 1，R 3，R 4，R 5如本公开所定义; 其制备方法，含有该组合物的组合物及其用于治疗病理状况的用途，特别是作为抗癌剂。
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3.发明授权Derivatives of 3-(Guanidinocarbonyl) heterocycle, methods of preparation and intermediates thereof, their use as medicaments, and pharmaceutical compositions therefrom 失效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。
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4.发明申请Derivatives of 3-(guanidinocarbonyl) heterocycle, methods of preparation and intermediates thereof, their use as medicaments, and pharmaceutical compositions therefrom 失效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。
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5.发明授权Pyrazolyl derivatives, preparation process and intermediates of this process as medicinal products and pharmaceutical compositions containing them 失效吡唑基衍生物，该方法的制备方法和中间体作为药物产品和含有它们的药物组合物公开(公告)号：US07524838B2
公开(公告)日：2009-04-28
申请号：US10997736
申请日：2004-11-24
申请人： Arielle Genevois-Borella , Jean-Luc Malleron , Jean Bouquerel , Gilles Doerflinger , Andrees Bohme , Gaetan Touyer , Jean-Francois Sabuco , Corrine Terrier , Serge Mignani , Michel Evers , Youssef El-Ahmad
发明人： Arielle Genevois-Borella , Jean-Luc Malleron , Jean Bouquerel , Gilles Doerflinger , Andrees Bohme , Gaetan Touyer , Jean-Francois Sabuco , Corrine Terrier , Serge Mignani , Michel Evers , Youssef El-Ahmad
IPC分类号： A61K31/55 , A61K31/5377 , A61K31/454 , A61K31/4152 , A61K31/4155 , C07D403/06 , C07D231/18 , C07D401/06 , C07D453/02
CPC分类号： C07D231/12 , C07D231/14 , C07D231/20 , C07D401/04 , C07D401/06 , C07D403/06 , C07D409/04 , C07D453/02 , C07D453/06 , C07D487/08
摘要： The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl, to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.
摘要翻译： 本发明涉及式（I）的新衍生物，其中A是（C 1 -C 6）烷基，（C 3 -C 6）烯基，（C 3 -C 6）炔基，（C 3 （C 5 -C 7）氮杂双环烷基或（C 5 -C 9）氮杂双环链烯基;（C 1 -C 7）氮杂环烷基，（C 5 -C 9） A-R1使得R 1的氮和吡唑1位的氮必须分开至少两个碳原子，R3是H，卤素，OH，SH，NH2，ORc，SRc，SORa， SO 2 R a，NHCHO，NR a R b，NHC（O）R a，NHC（S）R a或NHSO 2 R a，R 4是芳基或杂芳基; 其中R 5为H，卤素，CF 3，CHF 2，CH 2 F，直链或支链（C 1 -C 6）烷基或（C 3 -C 7）环烷基，与其外消旋体，对映异构体和非对映异构体及其混合物，其互变异构体及其药学上可接受的 盐。
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6.发明申请Pyrazolyl derivatives, preparation process and intermediates of this process as medicinal products and pharmaceutical compositions containing them 失效吡唑基衍生物，该方法的制备方法和中间体作为药物产品和含有它们的药物组合物公开(公告)号：US20050165005A1
公开(公告)日：2005-07-28
申请号：US10997736
申请日：2004-11-24
申请人： Arielle Genevois-Borella , Jean-Luc Malleron , Jean Bouquerel , Gilles Doerflinger , Andrees Bohme , Gaetan Touyer , Jean-Francois Sabuco , Corrine Terrier , Serge Mignani , Michel Evers , Youssef El-Ahmad
发明人： Arielle Genevois-Borella , Jean-Luc Malleron , Jean Bouquerel , Gilles Doerflinger , Andrees Bohme , Gaetan Touyer , Jean-Francois Sabuco , Corrine Terrier , Serge Mignani , Michel Evers , Youssef El-Ahmad
IPC分类号： A61K31/41 , A61K31/416 , A61K31/435 , A61K31/454 , A61K31/55 , C07D231/12 , C07D231/14 , C07D231/20 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D409/04 , C07D453/02 , C07D453/06 , C07D487/08 , C07D43/02
CPC分类号： C07D231/12 , C07D231/14 , C07D231/20 , C07D401/04 , C07D401/06 , C07D403/06 , C07D409/04 , C07D453/02 , C07D453/06 , C07D487/08
摘要： The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.
摘要翻译： 本发明涉及式（I）的新衍生物，其中A是（C 1 -C 6）烷基，（C 3 -C 6）烯基，（C 3 -C 6）炔基，（C 3 （C 5 -C 7）氮杂双环烷基或（C 5 -C 9）氮杂双环链烯基;（C 5 -C 7）氮杂双环烷基或（C 5 -C 9） A-R1使得R 1的氮和吡唑的1位的氮必须分开至少两个碳原子，R 3是H，卤素，OH，SH，NH 2 >，ORc，SRc，SORa，SO 2 Ra，NHCHO，NRaRb，NHC（O）Ra，NHC（S）Ra或NHSO2Ra，R4是芳基 或杂芳基; 并且R 5是H，卤素，CF 3，CHF 2，CH 2 F，直链或支链（C 1 -C 6）烷基或（ C3-C7）环烷基与其外消旋体，对映异构体和非对映异构体及其混合物，它们的互变异构体及其药学上可接受的盐。
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7.发明授权Pyrazolyl derivatives, preparation process and intermediates of this process as medicinal products and pharmaceutical compositions containing them 失效吡唑基衍生物，该方法的制备方法和中间体作为药物产品和含有它们的药物组合物公开(公告)号：US08048893B2
公开(公告)日：2011-11-01
申请号：US12394589
申请日：2009-02-27
申请人： Arielle Genevois-Borella , Jean-Luc Malleron , Jean Bouquerel , Gilles Doerflinger , Andrees Bohme , Gaetan Touyer , Jean-Francois Sabuco , Corrine Terrier , Serge Mignani , Michel Evers , Youssef El-Ahmad
发明人： Arielle Genevois-Borella , Jean-Luc Malleron , Jean Bouquerel , Gilles Doerflinger , Andrees Bohme , Gaetan Touyer , Jean-Francois Sabuco , Corrine Terrier , Serge Mignani , Michel Evers , Youssef El-Ahmad
IPC分类号： A61K31/439 , A61K31/4155 , C07D231/20 , C07D453/02
CPC分类号： C07D231/12 , C07D231/14 , C07D231/20 , C07D401/04 , C07D401/06 , C07D403/06 , C07D409/04 , C07D453/02 , C07D453/06 , C07D487/08
摘要： The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl, to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.
摘要翻译： 本发明涉及式（I）的新衍生物，其中A是（C 1 -C 6）烷基，（C 3 -C 6）烯基，（C 3 -C 6）炔基，（C 3 （C 5 -C 7）氮杂双环烷基或（C 5 -C 9）氮杂双环链烯基;（C 1 -C 7）氮杂环烷基，（C 5 -C 9） A-R1使得R 1的氮和吡唑1位的氮必须分开至少两个碳原子，R3是H，卤素，OH，SH，NH2，ORc，SRc，SORa， SO 2 R a，NHCHO，NR a R b，NHC（O）R a，NHC（S）R a或NHSO 2 R a，R 4是芳基或杂芳基; 其中R 5为H，卤素，CF 3，CHF 2，CH 2 F，直链或支链（C 1 -C 6）烷基或（C 3 -C 7）环烷基，与其外消旋体，对映异构体和非对映异构体及其混合物，其互变异构体及其药学上可接受的 盐。
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8.发明授权Pyrimidine derivatives, preparation thereof, and pharmaceutical use thereof as akt(pkb) phosphorylation inhibitors 有权嘧啶衍生物，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：US09133168B2
公开(公告)日：2015-09-15
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 , Frank Halley , Karl Andreas Karlsson
发明人： Maurice Brollo , Jean-Christophe Carry , Victor Certal , Eric Didier , Gilles Doerflinger , Youssef El Ahmad , Frank Halley , Karl Andreas Karlsson
IPC分类号： C07D413/14 , C07D413/04 , C07D401/04 , C07D403/06 , C07D209/30 , C07D403/04 , C07D471/10 , 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。
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9.发明申请NOVEL PYRIMIDINE DERIVATIVES, PREPARATION THEREOF, AND PHARMACEUTICAL USE THEREOF AS AKT(PKB) PHOSPHORYLATION INHIBITORS 有权新型吡啶衍生物，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。
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![Pyrazolo[4,3-d]thiazole derivatives, and preparation and therapeutic application thereof](/abs-image/US/2010/08/10/US07772261B2/abs.jpg.150x150.jpg)
10.发明授权Pyrazolo[4,3-d]thiazole derivatives, and preparation and therapeutic application thereof 有权吡唑并[4,3-d]噻唑衍生物及其制备和治疗应用公开(公告)号：US07772261B2
公开(公告)日：2010-08-10
申请号：US12356740
申请日：2009-01-21
IPC分类号： C07D513/04 , A61K31/4162 , A61K31/429
CPC分类号： C07D513/04
摘要： The disclosure relates to a compound of formula (I): in which: R1, R2, R3 and R4 are as described in the specification, to compositions containing them and to their therapeutic use, especially as anticancer agents. The disclosure also relates to the process for preparing these compounds and to certain intermediate products.
摘要翻译： 本公开涉及式（I）的化合物：其中：R1，R2，R3和R4如本说明书所述，含有它们的组合物及其治疗用途，特别是作为抗癌剂。 本公开还涉及制备这些化合物和某些中间产物的方法。
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