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1. 发明授权

US07465736B2 Azole methylidene cyanide derivatives and their use as protein kinase modulators 失效
标题翻译： Azole亚甲基氰化物衍生物及其作为蛋白激酶调节剂的用途
公开(公告)号：US07465736B2
公开(公告)日：2008-12-16
申请号：US10516330
申请日：2003-06-13
申请人： Pascale Gaillard , Jean-Pierre Gotteland , Isabelle Jeanclaude-Etter , Matthias Schwarz , Russel J. Thomas
发明人： Pascale Gaillard , Jean-Pierre Gotteland , Isabelle Jeanclaude-Etter , Matthias Schwarz , Russel J. Thomas
IPC分类号： C07D417/06 , C07D417/08 , C07D417/14 , A61K31/427 , A61P3/04 , A61P3/10 , C07D413/06 , C07D413/14 , A61K31/4523 , A61K31/497 , A61K31/502
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D417/06 , C07D417/12 , C07D417/14 , C07D495/10
摘要： An azole derivative of formula (I) a medicament that contains the azole derivative of formula (I), a method of treating a disease with the azole derivative of formula (I), and a method of preparing the azole derivative of formula (I).
摘要翻译：式（I）的唑衍生物含有式（I）的唑衍生物的药物，用式（I）的唑衍生物治疗疾病的方法，以及制备式（I）的唑衍生物的方法，。

2. 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。

3. 发明授权

US07838522B2 Benzothiazole formulations and use thereof 有权
标题翻译：苯并噻唑制剂及其用途
公开(公告)号：US07838522B2
公开(公告)日：2010-11-23
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： A61K31/5377 , A61K31/428 , C07D413/14 , C07D277/62
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。

4. 发明申请

US20070123530A1 Azole methylidene cyanide derivatives and their use as protein kinase modulators 失效
标题翻译： Azole亚甲基氰化物衍生物及其作为蛋白激酶调节剂的用途
公开(公告)号：US20070123530A1
公开(公告)日：2007-05-31
申请号：US10516330
申请日：2003-06-13
申请人： Pascale Gaillard , Jean-Pierre Gottenland , Isabelle Jeanclaude-Etter , Matthias Schwarz , Russel Thomas
发明人： Pascale Gaillard , Jean-Pierre Gottenland , Isabelle Jeanclaude-Etter , Matthias Schwarz , Russel Thomas
IPC分类号： A61K31/5377 , A61K31/53 , A61K31/506 , C07D417/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D417/06 , C07D417/12 , C07D417/14 , C07D495/10
摘要： An azole derivative of formula (I) a medicament that contains the azole derivative of formula (I), a method of treating a disease with the azole derivative of formula (I), and a method of preparing the azole derivative of formula (I).
摘要翻译：式（I）的唑衍生物含有式（I）的唑衍生物的药物，用式（I）的唑衍生物治疗疾病的方法，以及制备式（I）的唑衍生物的方法，。

5. 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。

6. 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。

7. 发明申请

US20070203134A1 Benzimidazole Acetonitriles 审中-公开
标题翻译：苯并咪唑乙腈
公开(公告)号：US20070203134A1
公开(公告)日：2007-08-30
申请号：US10571470
申请日：2004-09-10
申请人： Matthias Schwarz , Pascale Gaillard , Patrick Page , Jean-Pierre Gotteland , Russell Thomas
发明人： Matthias Schwarz , Pascale Gaillard , Patrick Page , Jean-Pierre Gotteland , Russell Thomas
IPC分类号： A61K31/5377 , A61K31/506 , C07D413/14 , C07D403/02
CPC分类号： C07D403/06 , C07D403/14 , C07D413/14 , C07D417/14
摘要： The present invention is related to benzimidazole acetonitriles as well as to pharmaceutical formulations containing such benzimidazole acetonitriles of formula (I). Said benzimidazole acetonitriles are useful in 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) (I). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles. G is pyrimidinyl; L is an amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom selected from N, O, S or L is an acylamino moiety; R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, carboxy, aminocarbonyl, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl or C1-C6-alkoxy, aryl, halogen, cyano or hydroxy; R2 is selected from the group comprising or consisting of hydrogen, C1-C6-alkyl, C2-C6alkenyl, C2-C6-alkynyl, or C1-C6-alkoxy.
摘要翻译：本发明涉及苯并咪唑乙腈和含有式（I）的苯并咪唑乙腈的药物制剂。所述苯并咪唑乙腈可用于治疗由胰岛素抵抗或高血糖介导的代谢紊乱，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）（I））。本发明还涉及制备苯并恶唑乙腈的方法。 G是嘧啶基; L是含有至少一个选自N，O，S或L的杂原子的氨基或3-8元杂环烷基是酰氨基部分; R 1选自氢，磺酰基，氨基，羧基，氨基羰基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷基， C 2 -C 6 - 烯基，C 2 -C 6 - 炔基或C 1 -C 6 - C 1 -C 6 - 烷氧基，芳基，卤素，氰基或羟基; R 2选自包含或由氢，C 1 -C 6 - 烷基，C 2 H 2基团组成的组 C 1 -C 6亚烷基，C 2 -C 6亚炔基或C 1 -C 6亚烷基， 6 - 烷氧基。

8. 发明申请

US20070185104A1 Benzoxazole acetonitriles 审中-公开
标题翻译：苯并恶唑乙腈
公开(公告)号：US20070185104A1
公开(公告)日：2007-08-09
申请号：US10571323
申请日：2004-09-10
申请人： Matthias Schwarz , Pascale Gaillard , Patrick Page , Jean-Pierre Gotteland , Russell Thomas
发明人： Matthias Schwarz , Pascale Gaillard , Patrick Page , Jean-Pierre Gotteland , Russell Thomas
IPC分类号： A61K31/5377 , A61K31/506 , C07D413/14
CPC分类号： C07D491/10 , C07D413/06 , C07D413/14
摘要： The present invention is related to benzoxazole acetonitriles as well as to pharmaceutical formulations containing such benzoxazole acetonitriles pof formula (I). Said benzoxazole acetonitriles are useful in 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). The present invention is furthermore related to methods of preparing benzoxazole acetonitriles (I). A is a pyrimidinyl.L is a secondary or tertiary amino group, or a 3-8 membered heterocycloalkyl, containing at least one heteroatom. selected from N, O, S or L is an acylamino moiety. R1 is selected from the group comprising or consisting of hydrogen, sulfonyl, amino, C1C6-alkYl, C2-C6-alkenYl, C2-C6-alkynyl or C1-C6-alkoxy, aryl, halogen, carboxy, aminocarbonyl, cyano or hydroxy.
摘要翻译：本发明涉及苯并恶唑乙腈和含有该苯并恶唑乙腈的配方（I）的药物制剂。所述苯并恶唑乙腈可用于治疗由胰岛素抵抗或高血糖介导的代谢紊乱，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）。本发明还涉及制备苯并恶唑乙腈（I）的方法。 A是嘧啶基，L是含有至少一个杂原子的仲或叔氨基或3-8元杂环烷基。选自N，O，S或L是酰氨基部分。 R 1选自包含或由氢，磺酰基，氨基，C 1 -C 6 - 烷基，C 2 -C 6 - 亚烷基，C 2 -C 6 - 炔基或C 1 -C 烷氧基，芳基，卤素，羧基，氨基羰基，氰基或羟基。

9. 发明授权

US09073940B2 Tricyclic pyrazol amine derivatives 有权
标题翻译：三环吡唑胺衍生物
公开(公告)号：US09073940B2
公开(公告)日：2015-07-07
申请号：US13509291
申请日：2010-11-12
申请人： Pascale Gaillard , Isabelle Jeanclaude-Etter , Vincent Pomel , Eric Sebille , Seenisamy Jeyaprakashnarayanan , Mathilde Muzerelle
发明人： Pascale Gaillard , Isabelle Jeanclaude-Etter , Vincent Pomel , Eric Sebille , Seenisamy Jeyaprakashnarayanan , Mathilde Muzerelle
IPC分类号： C07D495/04 , C07D495/14
CPC分类号： C07D495/04 , C07D495/14
摘要： This invention relates to compounds of Formula (I*) as Pi3k inhibitors for treating autoimmune diseases, inflammatory disorders, multiple sclerosis and other diseases like cancers.
摘要翻译：本发明涉及作为用于治疗自身免疫性疾病，炎症性疾病，多发性硬化和其它疾病如癌症的Pi3k抑制剂的式（I *）化合物。

10. 发明授权

US08614215B2 Quinoxaline inhibitors of phosphoinositide-3-kinases (PI3Ks) 有权
标题翻译：磷酸肌醇-3-激酶（PI3K）的喹喔啉抑制剂
公开(公告)号：US08614215B2
公开(公告)日：2013-12-24
申请号：US12525095
申请日：2008-02-21
申请人： Pascale Gaillard , Vincent Pomel , Isabelle Jeanclaude-Etter , Jerome Dorbais , Jasna Klicic , Cyril Montagne
发明人： Pascale Gaillard , Vincent Pomel , Isabelle Jeanclaude-Etter , Jerome Dorbais , Jasna Klicic , Cyril Montagne
IPC分类号： A61K31/495
CPC分类号： C07D403/12 , C07D241/44 , C07D401/12 , C07D401/14 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D451/02
摘要： The present invention is related to quinoxaline compounds of Formula (I) in particular for the treatment 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）的喹喔啉化合物，特别是用于治疗自身免疫性疾病和/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，癌症，移植，移植排斥或肺部受伤。

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