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1. 发明授权

US07470686B2 Method of inhibiting the expression and/or the activity of JNK 有权
标题翻译：抑制JNK表达和/或活性的方法
公开(公告)号：US07470686B2
公开(公告)日：2008-12-30
申请号：US11779585
申请日：2007-07-18
申请人： Serge Halazy , Dennis Church , Monstserrat Camps , Pascale Gaillard , Jean-Pierre Gotteland
发明人： Serge Halazy , Dennis Church , Monstserrat Camps , Pascale Gaillard , Jean-Pierre Gotteland
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。

2. 发明申请

US20070259892A1 METHOD OF INHIBITING THE EXPRESSION AND/OR THE ACTIVITY OF JNK 有权
标题翻译：抑制JNK的表达和/或活性的方法
公开(公告)号：US20070259892A1
公开(公告)日：2007-11-08
申请号：US11779585
申请日：2007-07-18
申请人： Serge Halazy , Dennis Church , Monstserrat Camps , Pascale Gaillard , Jean-Pierre Gotteland
发明人： Serge Halazy , Dennis Church , Monstserrat Camps , Pascale Gaillard , Jean-Pierre Gotteland
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。

3. 发明授权

US07259162B2 Benzazole derivatives and their use as JNK modulators 有权
标题翻译：苯并唑衍生物及其作为JNK调节剂的用途
公开(公告)号：US07259162B2
公开(公告)日：2007-08-21
申请号：US10168718
申请日：2000-12-20
申请人： Serge Halazy , Dennis Church , Montserrat Camps , Pascale Gaillard , Jean-Pierre Gotteland
发明人： Serge Halazy , Dennis Church , Montserrat Camps , Pascale Gaillard , Jean-Pierre Gotteland
IPC分类号： C07D417/06 , A61K31/506
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。

4. 发明授权

US07776854B2 Benzazole derivatives for the treatment of scleroderma 有权
标题翻译：苯唑衍生物用于治疗硬皮病
公开(公告)号：US07776854B2
公开(公告)日：2010-08-17
申请号：US10496785
申请日：2002-12-06
申请人： Jean-Pierre Gotteland , Pascale Gaillard , Yolande Chvatchko
发明人： Jean-Pierre Gotteland , Pascale Gaillard , Yolande Chvatchko
IPC分类号： A61K31/535
CPC分类号： A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/506
摘要： The present invention is related to the use of benzazole derivatives of formula (I) for the treatment and/or prevention of scleroderma and its therapeutic implications selected in the group consisting of systemic sclerosis, scleroderma-like disorders, sine scleroderma, liver cirrhosis, interstitial pulmonary fibrosis, Dupuytren's contracture, keloid and other scarring/wound healing abnormalities, postoperative adhesions and reactive fibrosis, as well as chronic heart failure, in particular after myocardial infarction.
摘要翻译：本发明涉及式（I）的苯并唑衍生物在治疗和/或预防硬皮病中的应用及其治疗意义，其选自系统性硬化症，硬皮病样疾病，正辛硬脂酸，肝硬化，间质性肺纤维化，Dupuytren挛缩，瘢痕疙瘩和其他瘢痕/伤口愈合异常，术后粘连和反应性纤维化，以及慢性心力衰竭，特别是心肌梗死后。

5. 发明申请

US20080051397A1 Benzothiazole Formulations and Use Thereof 有权
标题翻译：苯并噻唑配方及其用途
公开(公告)号：US20080051397A1
公开(公告)日：2008-02-28
申请号：US11667802
申请日：2005-11-16
申请人： Pierandrea Esposito , Daniela Chicco , Luca Donati , Andrea Leonardi , Stefania Bertero , Jean-Pierre Gotteland , Pascale Gaillard , Isabelle Jeanclaude-Etter , Simone Grandolini , Mario Maio
发明人： Pierandrea Esposito , Daniela Chicco , Luca Donati , Andrea Leonardi , Stefania Bertero , Jean-Pierre Gotteland , Pascale Gaillard , Isabelle Jeanclaude-Etter , Simone Grandolini , Mario Maio
IPC分类号： A61K31/428 , A61K31/497 , A61K31/506 , A61K31/5377 , A61P11/00 , A61P11/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P3/10 , A61P35/00 , A61P37/08 , A61P7/00
CPC分类号： A61K31/428 , A61K9/0014 , A61K9/0019 , A61K9/1617 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K47/10 , A61K47/14 , A61K47/26
摘要： The present invention is related to macrogol glyceride pharmaceutical formulations containing benzothiazole derivatives. In particular, the invention is related to benzothiazole stearoyl macrogol pharmaceutical formulations, method of preparation and use thereof.
摘要翻译：本发明涉及含有苯并噻唑衍生物的聚乙二醇甘油酯药物制剂。特别地，本发明涉及苯并噻唑硬脂酰聚乙二醇化学药物制剂，其制备方法和用途。

6. 发明授权

US07314878B2 Piperazine benzothiazoles as agents for the treatment of cerebral ischemic disorders or CNS disorders 有权
标题翻译：哌嗪苯并噻唑作为治疗脑缺血障碍或CNS疾病的药物
公开(公告)号：US07314878B2
公开(公告)日：2008-01-01
申请号：US10511438
申请日：2003-04-25
申请人： Pascale Gaillard , Jean-Pierre Gotteland , Pierre-Alain Vitte
发明人： Pascale Gaillard , Jean-Pierre Gotteland , Pierre-Alain Vitte
IPC分类号： C07D417/06 , C07D417/14 , A61K31/506
CPC分类号： C07D417/06
摘要： The present invention is related to piperazine henzothiazole derivatives, notably for use in the treatment and/or prophylaxis of cerebral ischemic disorders or CNS disorders. The present invention is furthermore related to methods of their preparation.
摘要翻译：本发明涉及哌嗪异噻唑衍生物，特别用于治疗和/或预防脑缺血障碍或CNS障碍。本发明还涉及它们的制备方法。

7. 发明申请

US20070060594A1 Pyridinyl acetonitriles 有权
标题翻译：吡啶基乙腈
公开(公告)号：US20070060594A1
公开(公告)日：2007-03-15
申请号：US10555960
申请日：2004-05-03
申请人： Matthias Schwarz , Pascale Gaillard , Jean-Pierre Gotteland , Russell Thomas , Patrick Page
发明人： Matthias Schwarz , Pascale Gaillard , Jean-Pierre Gotteland , Russell Thomas , Patrick Page
IPC分类号： A61K31/506 , C07D403/02
CPC分类号： C07D401/06 , A61K31/505 , A61K31/53
摘要： The present invention is related to pyridinyl acetonitriles as well as to pharmaceutical formulations containing such pyridinyl acetonitriles. Said pyridinyl acetonitriles are modulators of the protein kinase signalling pathways, particularly the one involving Glycogen Kinase Synthase 3 or JNK. The present invention is furthermore related to methods of preparing pyridinyl acetonitriles. X is a substituted or unsubstituted pyridinyl. G is an unsubstituted or substituted pyrimidinyl or triazinyl.
摘要翻译：本发明涉及吡啶基乙腈以及含有这种吡啶基乙腈的药物制剂。所述吡啶基乙腈是蛋白激酶信号通路的调节剂，特别是涉及糖原激酶合成酶3或JNK的调节剂。本发明还涉及制备吡啶基乙腈的方法。 X是取代或未取代的吡啶基。 G是未取代或取代的嘧啶基或三嗪基。

8. 发明申请

US20050261304A1 Piperazine benzothiazoles as agents for the treatment of cerebral ischemic disorders or cns disorders 有权
标题翻译：哌嗪苯并噻唑作为治疗脑缺血障碍或cns病症的药物
公开(公告)号：US20050261304A1
公开(公告)日：2005-11-24
申请号：US10511438
申请日：2003-04-25
申请人： Pascale Gaillard , Jean-Pierre Gotteland , Pierre-Alain Vitte
发明人： Pascale Gaillard , Jean-Pierre Gotteland , Pierre-Alain Vitte
IPC分类号： A61K31/506 , A61P25/28 , C07D417/06 , C07D417/14 , A61K31/513
CPC分类号： C07D417/06
摘要： The present invention is related to piperazine henzothiazole derivatives, notably for use in the treatment and/or prophylaxis of cerebral ischemic disorders or CNS disorders. The present invention is furthermore related to methods of their preparation.
摘要翻译：本发明涉及哌嗪异噻唑衍生物，特别用于治疗和/或预防脑缺血障碍或CNS障碍。本发明还涉及它们的制备方法。

9. 发明授权

US07855212B2 Pyridinyl acetonitriles 有权
标题翻译：吡啶基乙腈
公开(公告)号：US07855212B2
公开(公告)日：2010-12-21
申请号：US10555960
申请日：2004-05-03
申请人： Matthias Schwarz , Pascale Gaillard , Jean-Pierre Gotteland , Russell J. Thomas , Patrick Page
发明人： Matthias Schwarz , Pascale Gaillard , Jean-Pierre Gotteland , Russell J. Thomas , Patrick Page
IPC分类号： A01N43/54 , C07D239/42 , C07D401/04 , C07D239/02 , C07D401/00 , C07D403/00 , C07D405/00 , C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D419/00 , A61K31/505
CPC分类号： C07D401/06 , A61K31/505 , A61K31/53
摘要： The present invention is related to pyridinyl acetonitriles as well as to pharmaceutical formulations containing such pyridinyl acetonitriles. Said pyridinyl acetonitriles are modulators of the protein kinase signalling pathways, particularly the one involving Glycogen Kinase Synthase 3 or JNK. The present invention is furthermore related to methods of preparing pyridinyl acetonitriles. X is a substituted or unsubstituted pyridinyl. G is an unsubstituted or substituted pyrimidinyl or triazinyl.
摘要翻译：本发明涉及吡啶基乙腈以及含有这种吡啶基乙腈的药物制剂。所述吡啶基乙腈是蛋白激酶信号通路的调节剂，特别是涉及糖原激酶合成酶3或JNK的调节剂。本发明还涉及制备吡啶基乙腈的方法。 X是取代或未取代的吡啶基。 G是未取代或取代的嘧啶基或三嗪基。

10. 发明申请

US20070088017A1 Benzothiazole derivatives for the treatment of diabetes 审中-公开
标题翻译：苯并噻唑衍生物用于治疗糖尿病
公开(公告)号：US20070088017A1
公开(公告)日：2007-04-19
申请号：US10571291
申请日：2004-09-08
申请人： Pascale Gaillard , Jean-Pierre Gotteland , Pierre-Alain Vitte
发明人： Pascale Gaillard , Jean-Pierre Gotteland , Pierre-Alain Vitte
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/506 , C07D417/14
CPC分类号： C07D417/14 , A61K31/4184 , A61K38/28 , A61K45/06 , A61K2300/00
摘要： The present invention is related to the use of benzothiazole derivatives for the manufacture of a medicament for the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS) Formula (I). G is an unsubstituted or substituted pyrimidinyl group. L is an unsubstituted or substituted C1-C6-alkoxy, or an amino group, or an unsubstituted or a substituted 3-8 membered heterocycloalkyl, containing at least one heteroatom selected from N, O, S (e.g. a piperazine, a piperidine, a morpholine, a pyrrolidine). R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, unsubstituted or substituted C1-C6-alkyl, unsubstituted or substituted C2-C6-alkenyl, unsubstituted or substituted C2-C6-alkynyl or C1-C6-alkoxy, unsubstituted or substituted aryl, halogen, cyano or hydroxy.
摘要翻译：本发明涉及苯并噻唑衍生物在制备用于治疗由胰岛素抵抗或高血糖介导的代谢紊乱的药物中的用途，其包括II型糖尿病，葡萄糖耐量不足，胰岛素抵抗，肥胖，多囊卵巢综合征（PCOS）式（I）。 G是未取代或取代的嘧啶基。 L是未取代或取代的C 1 -C 6 - 烷氧基或氨基，或未取代或取代的3-8元杂环烷基，其含有至少一个杂原子选自N，O，S（例如哌嗪，哌啶，吗啉，吡咯烷）。 R 1选自氢，磺酰基，氨基，未取代或取代的C 1 -C 6 - 烷基，或未取代的或取代的C 2 -C 6 - 链烯基，未取代或取代的C 2 -C 6 - 炔基或C 氰基或羟基。未取代或取代的芳基，卤素，氰基或羟基。

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