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公开(公告)号：US20070259892A1
公开(公告)日：2007-11-08
申请号：US11779585
申请日：2007-07-18
IPC分类号： A61K31/506 , A61K31/426 , C07D277/62 , C07D401/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/64 , C07D417/06 , C07D417/14
摘要： The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstituted or substituted C1-C6 alkyl; G is an unsubstituted or substituted pyrimidinyl group.
摘要翻译： 本发明涉及特别用作药物活性化合物的苯并唑衍生物以及含有这种苯并唑衍生物的药物制剂。 所述的苯并唑衍生物是JNK途径的有效调节剂，它们特别是JNK2和/或3的有效和选择性抑制剂。本发明还涉及新的苯并唑衍生物及其制备方法。 X是O，S或NR 0，其中R 0是H或未取代或取代的C 1 -C 6 - 烷基; G是未取代或取代的嘧啶基。
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公开(公告)号：US07470686B2
公开(公告)日：2008-12-30
申请号：US11779585
申请日：2007-07-18
IPC分类号： A61K31/506 , C07D417/06
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D277/64 , C07D417/06 , C07D417/14
摘要： The present invention is related to benzazole derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such benzazole derivatives. Said benzazole derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK2 and/or 3. The present invention is furthermore related to novel benzazole derivatives as well as to methods of their preparation. X is O, S or NR0, with R0 being H or an unsubstantiated or substituted C1-C6 alkyl; G is an unsubstantiated or substituted pyrimidinyl group.
摘要翻译： 本发明涉及特别用作药物活性化合物的苯并唑衍生物以及含有这种苯并唑衍生物的药物制剂。 所述的苯并唑衍生物是JNK途径的有效调节剂，它们特别是JNK2和/或3的有效和选择性抑制剂。本发明还涉及新的苯并唑衍生物及其制备方法。 X为O，S或NRO，其中R 0为H或未经取代或取代的C 1 -C 6烷基; G是未经证实或取代的嘧啶基。
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公开(公告)号：US08410110B2
公开(公告)日：2013-04-02
申请号：US13225760
申请日：2011-09-06
申请人： Serge Halazy , Dennis Church , Bruno Antonsson , Agnes Bombrun , Patrick Gerber , Jean-Claude Martinou
发明人： Serge Halazy , Dennis Church , Bruno Antonsson , Agnes Bombrun , Patrick Gerber , Jean-Claude Martinou
IPC分类号： A61K31/497
CPC分类号： C07D209/88 , C07D209/86
摘要： Piperazine compounds for use as pharmaceutically active compounds and in pharmaceutical formulations that are useful for the treatment of disorders associated with apoptosis, including neurodegenerative disorders, diseases associated with polyglutamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders, renal hypoxia, hepatitis and AIDS, where the piperazine compounds are represented by formula (I) and the terms R0, R1, R2, R3, k, l, m, n, and X are defined herein:
摘要翻译： 用作药物活性化合物的哌嗪化合物和可用于治疗与凋亡相关的疾病的药物制剂中的哌嗪化合物，包括神经变性疾病，与多聚谷氨酰胺束相关的疾病，癫痫，缺血，不育症，心血管疾病，肾脏缺氧，肝炎和AIDS， 其中哌嗪化合物由式（I）表示，术语R 0，R 1，R 2，R 3，k，l，m，n和X定义如下：
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公开(公告)号：US06770656B2
公开(公告)日：2004-08-03
申请号：US10182745
申请日：2002-12-26
申请人： Serge Halazy , Matthias Schwarz , Bruno Antonsson , Agnes Bombrun , Jean-Claude Martinou , Dennis Church
发明人： Serge Halazy , Matthias Schwarz , Bruno Antonsson , Agnes Bombrun , Jean-Claude Martinou , Dennis Church
IPC分类号： C07D21304
CPC分类号： C07D217/26 , C07B2200/07 , C07C237/22 , C07C2601/14 , C07D207/16 , C07D211/60 , C07D277/06
摘要： The present invention is related to substituted amine derivatives notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such amine derivatives of formula (I). Said substituted amine derivatives are efficient modulators, in particular inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel substituted amine derivatives as well as methods of their preparation.
摘要翻译： 本发明涉及特别用作药物活性化合物的取代胺衍生物，以及含有式（I）胺衍生物的药物制剂。 所述取代的胺衍生物是Bax功能和/或活化的有效调节剂，特别是抑制剂。 本发明还涉及新型取代的胺衍生物及其制备方法。
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公开(公告)号：US08053436B1
公开(公告)日：2011-11-08
申请号：US10110199
申请日：2000-10-18
申请人： Serge Halazy , Dennis Church , Bruno Antonsson , Agnes Bombrun , Patrick Gerber , Jean-Claude Martinou
发明人： Serge Halazy , Dennis Church , Bruno Antonsson , Agnes Bombrun , Patrick Gerber , Jean-Claude Martinou
IPC分类号： A61K31/497 , C07D403/06 , C07D413/14
CPC分类号： C07D209/88 , C07D209/86
摘要： The present invention is related to piperazine derivatives of carbazole of formula (I) notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such piperazine derivatives of carbazole. Said piperazine derivatives of carbazole are efficient modulators, in particular efficient inhibitors, of the Bax function and/or activation. The present invention is furthermore related to novel piperazine derivatives of carbazole as well as methods of their preparation.
摘要翻译： 本发明涉及特别用作药物活性化合物的式（I）咔唑的哌嗪衍生物，以及含有咔唑类哌嗪衍生物的药物制剂。 所述咔唑的哌嗪衍生物是Bax功能和/或活化的有效调节剂，特别是有效的抑制剂。 本发明还涉及咔唑的新型哌嗪衍生物及其制备方法。
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16.发明申请公开(公告)号：US20120040933A1
公开(公告)日：2012-02-16
申请号：US13225760
申请日：2011-09-06
申请人： Serge HALAZY , Dennis Church , Bruno Antonsson , Agnes Bombrun , Patrick Gerber , Jean-Claude Martinou
发明人： Serge HALAZY , Dennis Church , Bruno Antonsson , Agnes Bombrun , Patrick Gerber , Jean-Claude Martinou
IPC分类号： A61K31/496 , C07D417/14 , C07D401/14 , C07D413/14 , A61K31/5377 , C07F5/02 , A61K31/69 , A61P25/08 , A61P25/28 , A61P25/14 , A61P25/16 , A61P27/02 , A61P25/00 , A61P1/00 , A61P37/00 , A61P29/00 , A61P11/06 , A61P37/06 , A61P9/10 , A61P9/00 , A61P9/04 , A61P13/12 , A61P31/14 , A61P15/08 , C07D403/06
CPC分类号： C07D209/88 , C07D209/86
摘要： piperazine compounds for use as pharmaceutically active compounds and in pharmaceutical formulations that are useful for the treatment of disorders associated with apoptosis, including neurodegenerative disorders, diseases associated with polyglutamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders, renal hypoxia, hepatitis and AIDS, where the piperazine compounds are represented by formula (I) and the terms R0, R1, R2, R3, k, l, m, n, and X are defined herein:
摘要翻译： 用作药物活性化合物的哌嗪化合物和可用于治疗与凋亡相关的病症的药物制剂，包括神经变性疾病，与多聚谷氨酰胺束相关的疾病，癫痫，缺血，不育症，心血管疾病，肾脏缺氧，肝炎和艾滋病， 其中哌嗪化合物由式（I）表示，术语R 0，R 1，R 2，R 3，k，l，m，n和X定义如下：
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公开(公告)号：US20060122176A1
公开(公告)日：2006-06-08
申请号：US10520621
申请日：2003-07-10
IPC分类号： A61K31/538 , A61K31/517 , A61K31/498 , A61K31/4709 , A61K31/427 , A61K31/426 , C07D417/02
CPC分类号： C07D277/20 , A61K31/426 , A61K31/427 , A61K31/4709 , A61K31/498 , A61K31/517 , A61K31/538 , C07D417/06 , C07D417/14
摘要： The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R1, R2 and n are as described in the description.
摘要翻译： 本发明涉及用于治疗和/或预防自身免疫性疾病和/或炎性疾病，心血管疾病，神经变性疾病，细菌或病毒感染，肾脏疾病，血小板聚集的式（I）的唑烷二酮 - 乙烯基稠合 - 苯衍生物 ，癌症，移植排斥或肺部损伤。 式（I）其中A，X，Y，Z，R 1，R 2和n如说明书所述。
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公开(公告)号：US08071597B2
公开(公告)日：2011-12-06
申请号：US12064284
申请日：2006-08-25
申请人： Pascale Gaillard , Anna Quattropani , Vincent Pomel , Thomas Rueckle , Jasna Klicic , Dennis Church
发明人： Pascale Gaillard , Anna Quattropani , Vincent Pomel , Thomas Rueckle , Jasna Klicic , Dennis Church
IPC分类号： A61K31/50 , A61K31/495 , A01N43/58 , A01N43/60 , C07D241/36
CPC分类号： C07D241/44 , C07D401/12 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention is related to pyrazine derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
摘要翻译： 本发明涉及式（I）的吡嗪衍生物，特别是用于治疗和/或预防自身免疫疾病和/或炎性疾病，心血管疾病，神经变性疾病，细菌或病毒感染，肾脏疾病，血小板聚集，癌症， 移植，移植排斥或肺部损伤。
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公开(公告)号：US07846925B2
公开(公告)日：2010-12-07
申请号：US10520621
申请日：2003-07-10
IPC分类号： A61K31/536 , A61K31/53 , A61K31/498 , A61K31/517 , A61K31/4709 , A61K31/427 , A61K31/423 , A61K31/4184 , A61K31/343 , A61K31/352 , C07D265/36 , C07D253/08 , C07D417/02 , C07D241/36 , C07D215/38 , C07D277/32 , C07D261/20 , C07D235/04 , C07D319/16 , C07D317/46 , C07D307/78
CPC分类号： C07D277/20 , A61K31/426 , A61K31/427 , A61K31/4709 , A61K31/498 , A61K31/517 , A61K31/538 , C07D417/06 , C07D417/14
摘要： The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R1, R2 and n are as described in the description.
摘要翻译： 本发明涉及用于治疗和/或预防自身免疫性疾病和/或炎性疾病，心血管疾病，神经变性疾病，细菌或病毒感染，肾脏疾病，血小板聚集的式（I）的唑烷二酮 - 乙烯基稠合 - 苯衍生物 ，癌症，移植排斥或肺部损伤。 式（I）其中A，X，Y，Z，R 1，R 2和n如说明书所述。
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20.发明授权2-imino-4-(thio) oxo-5-polycyclovinylazolines for use as PI3 kinase inhibitors 失效用于PI3激酶抑制剂的2-亚氨基-4-（硫代）氧代-5-聚环乙烯基恶唑啉公开(公告)号：US08106214B2
公开(公告)日：2012-01-31
申请号：US10565976
申请日：2004-07-27
申请人： Thomas Rueckle , Jeffrey Shaw , Dennis Church , David Covini
发明人： Thomas Rueckle , Jeffrey Shaw , Dennis Church , David Covini
IPC分类号： C07D277/04 , A61K31/425
CPC分类号： C07D417/06 , C07D417/14
摘要： The present invention is related to 2-imino-azolinone-vinyl fused-benzene derivatives of Formula (1) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
摘要翻译： 本发明涉及式（1）的2-亚氨基 - 唑啉酮 - 乙烯基稠合 - 苯衍生物，特别是用于治疗和/或预防自身免疫性疾病和/或炎性疾病，心血管疾病，神经变性疾病，肾脏疾病，血小板 聚集，癌症，移植，移植排斥或肺部损伤。
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