公开(公告)号：US08372864B2

公开(公告)日：2013-02-12

申请号：US12693597

申请日：2010-01-26

申请人： Bernard Baudoin ,  Michel Evers ,  Arielle Genevois-Borella ,  Andreas Karlsson ,  Jean-Luc Malleron ,  Magali Mathieu

发明人： Bernard Baudoin ,  Michel Evers ,  Arielle Genevois-Borella ,  Andreas Karlsson ,  Jean-Luc Malleron ,  Magali Mathieu

IPC分类号： A61K31/4035 ,  A61K31/47 ,  C07D209/44 ,  C07D217/24

CPC分类号： C07D209/46 ,  C07D217/24 ,  C07D413/12

摘要： The present invention relates to derivatives of 1-oxo-isoindoline-4-carboxamides and of 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamides, to the preparation thereof and to the therapeutic use thereof.

摘要翻译： 本发明涉及1-氧代 - 异吲哚啉-4-甲酰胺和1-氧代-1,2,3,4-四氢异喹啉-5-甲酰胺的衍生物及其制备方法及其治疗用途。

公开(公告)号：US08030320B2

公开(公告)日：2011-10-04

申请号：US12693598

申请日：2010-01-26

申请人： Michel Evers ,  Arielle Genevois-Borella ,  Andreas Karlsson ,  Jean-Luc Malleron

发明人： Michel Evers ,  Arielle Genevois-Borella ,  Andreas Karlsson ,  Jean-Luc Malleron

IPC分类号： A61K31/517

CPC分类号： C07D217/24 ,  C07D239/88

摘要： The present invention relates to compounds of formula I, to the preparation thereof and to the therapeutic use thereof.

摘要翻译： 本发明涉及式I化合物及其制备及其治疗用途。

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。

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。

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。

公开(公告)号：US06566362B2

公开(公告)日：2003-05-20

申请号：US10029950

申请日：2001-12-31

申请人： Jean-François Desconclois ,  Arielle Genevois-Borella ,  Philippe Girard ,  Michel Kryvenko ,  Marc Pierre Lavergne ,  Jean-Luc Malleron ,  Guy Picaut ,  Michel Tabart ,  Sylvie Wentzler

发明人： Jean-François Desconclois ,  Arielle Genevois-Borella ,  Philippe Girard ,  Michel Kryvenko ,  Marc Pierre Lavergne ,  Jean-Luc Malleron ,  Guy Picaut ,  Michel Tabart ,  Sylvie Wentzler

IPC分类号： A61K314375

CPC分类号： C07D215/38 ,  C07D471/04

摘要： Benzo[f]naphthyridine derivatives of formula (I): benzo[f]naphthyridine derivatives and benzo[f]naphthyridine esters of formula (IVa): aminoquinoline derivatives of formula (X): processes for preparing such compounds; and compositions comprising them.

摘要翻译： 式（I）的苯并[f]萘啶衍生物：苯并[f]萘啶衍生物和式（IVa）的苯并[f]萘啶酯：式（X）的氨基喹啉衍生物：制备此类化合物的方法; 和包含它们的组合物。

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。

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。

公开(公告)号：US08063068B2

公开(公告)日：2011-11-22

申请号：US12348605

申请日：2009-01-05

申请人： Jeffrey Daniel Schmitt ,  Gary Maurice Dull ,  Craig Harrison Miller ,  Arielle Genevois-Borella ,  Marc Capet ,  Michel Cheve

发明人： Jeffrey Daniel Schmitt ,  Gary Maurice Dull ,  Craig Harrison Miller ,  Arielle Genevois-Borella ,  Marc Capet ,  Michel Cheve

IPC分类号： C07D401/02 ,  A61K31/351

CPC分类号： A61K31/506 ,  C07D405/14

摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.

摘要翻译： 公开了式（I）的新型乙烯基氮杂环烷化合物。 这些化合物是各种nAChR的配体。 化合物及其药学上可接受的盐可用于制备旨在预防或治疗与nAChR功能障碍相关的疾病，特别是在中枢神经系统或胃肠系统内的药物组合物和/或药物。 可以治疗的疾病类型的实例包括神经变性疾病，包括中枢神经系统疾病如阿尔茨海默病，认知障碍，运动障碍如帕金森病，药物成瘾，行为障碍和胃肠系统内的炎性疾病。 化合物也可用作治疗急性，慢性或复发性疼痛的镇痛药。

公开(公告)号：US20100010042A1

公开(公告)日：2010-01-14

申请号：US12348605

申请日：2009-01-05

申请人： Jeffrey Daniel Schmitt ,  Gary Maurice Dull ,  Craig Harrison Miller ,  Arielle Genevois-Borella ,  Marc Capet ,  Michel Cheve

发明人： Jeffrey Daniel Schmitt ,  Gary Maurice Dull ,  Craig Harrison Miller ,  Arielle Genevois-Borella ,  Marc Capet ,  Michel Cheve

IPC分类号： A61K31/454 ,  A61K31/4545 ,  C07D401/02 ,  A61P25/00 ,  A61P1/00

CPC分类号： A61K31/506 ,  C07D405/14

摘要： Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.