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1.发明授权Streptogramin derivatives, their preparation and compositions containing them 有权链球菌素衍生物，它们的制备和含有它们的组合物公开(公告)号：US06541451B1
公开(公告)日：2003-04-01
申请号：US09627791
申请日：2000-07-27
IPC分类号： A61K3708
CPC分类号： C07D498/14 , C07K11/02
摘要： B-Group streptogramin compounds of formula (I): are useful as antimicrobial agents, optionally combined with at least one A-group streptogramin compound.
摘要翻译： 式（I）的B-组链霉素化合物：可用作抗微生物剂，任选地与至少一种A组链霉素化合物组合。
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2.发明授权Streptogramin derivatives, preparation method and compositions containing same 有权链球菌素衍生物，制备方法和含有它们的组合物公开(公告)号：US07019110B2
公开(公告)日：2006-03-28
申请号：US10790260
申请日：2004-03-02
申请人： Pascal Desmazeau , Gilles Doerflinger , Yves Ribeill , Eric Bacque , Jean-Claude Barriere , Gilles Dutruc-Rosset , Gérard Puchault
发明人： Pascal Desmazeau , Gilles Doerflinger , Yves Ribeill , Eric Bacque , Jean-Claude Barriere , Gilles Dutruc-Rosset , Gérard Puchault
IPC分类号： C07K7/50
摘要： Group B streptogramin derivatives of general formula (I) are disclosed: wherein Ra, Rb, Rc, Rd, R1, R2 and Y are as defined in the description, including preparation methods and compositions containing the same. Such derivatives are particularly useful as antimicrobial agents, optionally combined with at least one group A streptogramin derivative.
摘要翻译： 公开了通式（I）的B组链霉素衍生物：其中R a，R b，R c，R d，R 1，R 2和Y如说明书中所定义， 包括制备方法和含有它们的组合物。 这样的衍生物特别可用作抗微生物剂，任选地与至少一种A链烷togram啉衍生物组合。
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3.发明授权Streptogramin derivatives, preparation method and compositions containing same 有权链球菌素衍生物，制备方法和含有它们的组合物公开(公告)号：US06958383B2
公开(公告)日：2005-10-25
申请号：US10161804
申请日：2002-06-05
申请人： Pascal Desmazeau , Gilles Doerflinger , Yves Ribeill , Eric Bacque , Jean-Claude Barriere , Gilles Dutruc-Rosset , Gérard Puchault
发明人： Pascal Desmazeau , Gilles Doerflinger , Yves Ribeill , Eric Bacque , Jean-Claude Barriere , Gilles Dutruc-Rosset , Gérard Puchault
摘要： Group B streptogramin derivatives of general formula (I): wherein Ra, Rb, Rc, Rd, R1, R2 and Y are as defined in the description, including preparation methods and compositions containing same. Such derivatives are particularly useful as antimicrobial agents, optionally combined with at least one group A streptogramin derivative.
摘要翻译： 通式（I）的B组链霉素衍生物：其中Ra，Rb，Rc，Rd，R 1，R 2和Y如说明书中所定义，包括制备 含有其的方法和组合物。 这样的衍生物特别可用作抗微生物剂，任选地与至少一种A链烷togram啉衍生物组合。
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![Substituted 1H-pyrrolo[2,3-c]pyridine-2-carboxamides and related analogs as inhibitors of casein kinase Iε](/abs-image/US/2009/12/01/US07626027B2/abs.jpg.150x150.jpg)
4.发明授权Substituted 1H-pyrrolo[2,3-c]pyridine-2-carboxamides and related analogs as inhibitors of casein kinase Iε 有权取代的1H-吡咯并[2,3-c]吡啶-2-甲酰胺和相关类似物作为酪蛋白激酶Iepsilon的抑制剂公开(公告)号：US07626027B2
公开(公告)日：2009-12-01
申请号：US12106681
申请日：2008-04-21
申请人： William A. Metz, Jr. , Frank Halley , Gilles Dutruc-Rosset , Yong Mi Choi-Sledeski , Gregory Bernard Poli , David Marc Fink , Gilles Doerflinger , Bao-Guo Huang , Ann Marie Gelormini , Juan Anotonio Gamboa , Andrew Giovanni , Joachim E. Roehr , Joseph T. Tsay , Fernando Camacho , William Joseph Hurst , Stephen Wayne Harnish , Yulin Chiang
发明人： William A. Metz, Jr. , Frank Halley , Gilles Dutruc-Rosset , Yong Mi Choi-Sledeski , Gregory Bernard Poli , David Marc Fink , Gilles Doerflinger , Bao-Guo Huang , Ann Marie Gelormini , Juan Anotonio Gamboa , Andrew Giovanni , Joachim E. Roehr , Joseph T. Tsay , Fernando Camacho , William Joseph Hurst , Stephen Wayne Harnish , Yulin Chiang
IPC分类号： C07D471/02
CPC分类号： C07D471/04
摘要： The present invention discloses and claims compounds of formula (I) wherein M is N, and K and L are each C with the remaining substituents further defined herein. These compounds are effective as inhibitors of human casein kinase Iε, and as such are useful in the treatment of central nervous system diseases and disorders including mood disorders and sleep disorders. Pharmaceutical compositions comprising compounds of formula (I) and methods for the preparation of compounds of formula (I) are also disclosed and claimed.
摘要翻译： 本发明公开并要求其中M为N的式（I）化合物，并且K和L各自为C，其余取代基进一步定义。 这些化合物作为人酪氨酸激酶Iepsilon的抑制剂是有效的，因此可用于治疗中枢神经系统疾病和病症，包括情绪障碍和睡眠障碍。 还公开并要求保护包含式（I）化合物和制备式（I）化合物的方法的药物组合物。
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![Substituted 1H-pyrrolo[3,2-b, 3,2-c, and 2,3-c]pyridine-2-carboxamides and related analogs as inhibitors of casein kinase lepsilon](/abs-image/US/2008/07/22/US07402672B2/abs.jpg.150x150.jpg)
5.发明授权Substituted 1H-pyrrolo[3,2-b, 3,2-c, and 2,3-c]pyridine-2-carboxamides and related analogs as inhibitors of casein kinase lepsilon 有权取代的1H-吡咯并[3,2-b，3,2-c和2,3-c]吡啶-2-甲酰胺和相关类似物作为酪蛋白激酶lepsilon的抑制剂公开(公告)号：US07402672B2
公开(公告)日：2008-07-22
申请号：US11001533
申请日：2004-12-01
申请人： William A. Metz, Jr. , Frank Halley , Gilles Dutruc-Rosset , Yong Mi Choi-Sledeski , Gregory Bernard Poli , David Marc Fink , Gilles Doerflinger , Bao-Guo Huang , Ann Marie Gelormini , Juan Antonio Gamboa , Andrew Giovanni , Joachim E. Roehr , Joseph T. Tsay , Fernando Camacho , William Joseph Hurst , Stephen Wayne Harnish , Yulin Chiang
发明人： William A. Metz, Jr. , Frank Halley , Gilles Dutruc-Rosset , Yong Mi Choi-Sledeski , Gregory Bernard Poli , David Marc Fink , Gilles Doerflinger , Bao-Guo Huang , Ann Marie Gelormini , Juan Antonio Gamboa , Andrew Giovanni , Joachim E. Roehr , Joseph T. Tsay , Fernando Camacho , William Joseph Hurst , Stephen Wayne Harnish , Yulin Chiang
IPC分类号： C07D471/00
CPC分类号： C07D471/04
摘要： The present invention discloses and claims compounds of formula (I) as inhibitors of human casein kinase IF, and methods of using said compounds of formula (I) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. Pharmaceutical compositions comprising compounds of formula (I) and methods for the preparation of compounds of formula (I) are also disclosed and claimed.
摘要翻译： 本发明公开并要求作为人酪蛋白激酶IF抑制剂的式（I）化合物，以及使用所述式（I）化合物治疗中枢神经系统疾病和病症（包括情绪障碍和睡眠障碍）的方法。 还公开并要求保护包含式（I）化合物和制备式（I）化合物的方法的药物组合物。
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![Substituted 1H-pyrrolo[3,2-b, 3,2-c, and 2,3-c]pyridine-2-carboxamides and related analogs as inhibitors of casein kinase lepsilon](/abs-image/US/2005/06/16/US20050131012A1/abs.jpg.150x150.jpg)
6.发明申请Substituted 1H-pyrrolo[3,2-b, 3,2-c, and 2,3-c]pyridine-2-carboxamides and related analogs as inhibitors of casein kinase lepsilon 有权取代的1H-吡咯并[3,2-b，3,2-c和2,3-c]吡啶-2-甲酰胺和相关类似物作为酪蛋白激酶lepsilon的抑制剂公开(公告)号：US20050131012A1
公开(公告)日：2005-06-16
申请号：US11001533
申请日：2004-12-01
申请人： William Metz , Frank Halley , Gilles Dutruc-Rosset , Yong Choi-Sledeski , Gregory Bernard Poli , David Fink , Gilles Doerflinger , Bao-Guo Huang , Ann Gelormini , Juan Gamboa , Andrew Giovanni , Joachim Roehr , Joseph Tsay , Fernando Camacho , William Hurst , Stephen Harnish , Yulin Chiang
发明人： William Metz , Frank Halley , Gilles Dutruc-Rosset , Yong Choi-Sledeski , Gregory Bernard Poli , David Fink , Gilles Doerflinger , Bao-Guo Huang , Ann Gelormini , Juan Gamboa , Andrew Giovanni , Joachim Roehr , Joseph Tsay , Fernando Camacho , William Hurst , Stephen Harnish , Yulin Chiang
IPC分类号： A61K31/437 , C07D471/04 , C07D471/02 , A61K31/4745
CPC分类号： C07D471/04
摘要： The present invention discloses and claims compounds of formula (I) as inhibitors of human casein kinase IF, and methods of using said compounds of formula (I) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. Pharmaceutical compositions comprising compounds of formula (I) and methods for the preparation of compounds of formula (I) are also disclosed and claimed.
摘要翻译： 本发明公开并要求作为人酪蛋白激酶IF抑制剂的式（I）化合物，以及使用所述式（I）化合物治疗中枢神经系统疾病和病症（包括情绪障碍和睡眠障碍）的方法。 还公开并要求保护包含式（I）化合物和制备式（I）化合物的方法的药物组合物。
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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：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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公开(公告)号：US20050070571A1
公开(公告)日：2005-03-31
申请号：US10993637
申请日：2004-11-19
申请人： Patrick Mailliet , Abdekazize Laoui , Jean-Francois Riou , Gilles Doerflinger , Jean-Louis Mergny , Francois Hamy , Thomas Caulfield
发明人： Patrick Mailliet , Abdekazize Laoui , Jean-Francois Riou , Gilles Doerflinger , Jean-Louis Mergny , Francois Hamy , Thomas Caulfield
IPC分类号： A61K31/53 , C07D401/12 , C07D401/14 , C07D405/14 , C07D453/02 , A61K31/4709 , C07D41/14
CPC分类号： C07D401/14 , A61K31/53 , C07D401/12 , C07D405/14 , C07D453/02
摘要： The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which is quite specific. It also relates to novel chemical compounds as well as their therapeutic application in humans.
摘要翻译： 本发明涉及癌症治疗和具有非常特异性的作用机制的新型抗癌剂。 它还涉及新型化合物以及它们在人体中的治疗应用。
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公开(公告)号：US07179816B2
公开(公告)日：2007-02-20
申请号：US10954808
申请日：2004-09-30
申请人： Patrick Mailliet , Jean-Francois Riou , Marcel Alasia , Thomas Caulfield , Gilles Doerflinger , Jean-Louis Mergny , Abdelazize Laoui , Odile Petitgenet , Emmanuelle Renou
发明人： Patrick Mailliet , Jean-Francois Riou , Marcel Alasia , Thomas Caulfield , Gilles Doerflinger , Jean-Louis Mergny , Abdelazize Laoui , Odile Petitgenet , Emmanuelle Renou
IPC分类号： C07D239/50 , C07D213/02 , C07D215/38 , A61K31/505 , A61K31/506 , A61P35/00
CPC分类号： C07D401/12 , A61K31/53 , C07D401/14 , C07D453/02
摘要： The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which inhibits telomerase. It also relates to novel chemical compounds as well as their therapeutic application in humans.
摘要翻译： 本发明涉及癌症治疗和具有抑制端粒酶的作用机制的新型抗癌剂。 它还涉及新型化合物以及它们在人体中的治疗应用。
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![Substituted thieno [2,3-c] pyrazoles and their use as medicinal products](/abs-image/US/2005/02/03/US20050026984A1/abs.jpg.150x150.jpg)
10.发明申请Substituted thieno [2,3-c] pyrazoles and their use as medicinal products 审中-公开取代噻吩并[2,3-c]吡唑及其用作药用产品公开(公告)号：US20050026984A1
公开(公告)日：2005-02-03
申请号：US10900549
申请日：2004-07-28
IPC分类号： C07D495/04 , A61K31/4162 , C07D498/02
CPC分类号： C07D495/04
摘要： The present invention relates in particular to novel chemical compounds, particularly novel substituted thieno[2,3-c]pyrazoles, to the compositions containing them and to their use as medicinal products for treating cancers and also neurodegenerative diseases.
摘要翻译： 本发明特别涉及含有它们的组合物的新型化合物，特别是新型取代的噻吩并[2,3-c]吡唑，以及它们作为用于治疗癌症和神经变性疾病的药物的用途。
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