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1. 发明申请

WO2008101979A1 QUINOXALINE COMPOUNDS AND USE THEREOF 审中-公开
标题翻译：喹啉化合物及其用途
公开(公告)号：WO2008101979A1
公开(公告)日：2008-08-28
申请号：PCT/EP2008/052102
申请日：2008-02-21
申请人： LABORATOIRES SERONO SA , GAILLARD, Pascale , POMEL, Vincent , JEANCLAUDE-ETTER, Isabelle , DORBAIS, Jérôme , KLICIC, Jasna , MONTAGNE, Cyril
发明人： GAILLARD, Pascale , POMEL, Vincent , JEANCLAUDE-ETTER, Isabelle , DORBAIS, Jérôme , KLICIC, Jasna , MONTAGNE, Cyril
IPC分类号： C07D241/44 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D407/12 , C07D407/14 , C07D409/14 , C07D451/02 , A61K31/498 , A61P35/00
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。

2. 发明申请

WO2002074741A1 PYRROLIDINE ESTER DERIVATIVES WITH OXYTOCIN MODULATING ACITVITY 审中-公开
标题翻译：具有氧化调节作用的吡咯烷酮衍生物
公开(公告)号：WO2002074741A1
公开(公告)日：2002-09-26
申请号：PCT/EP2002/003005
申请日：2002-03-19
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING NV , SCHWARZ, Matthias , QUATTROPANI, Anna , SCHEER, Alexander , DORBAIS, Jérôme , POMEL, Vincent
发明人： SCHWARZ, Matthias , QUATTROPANI, Anna , SCHEER, Alexander , DORBAIS, Jérôme , POMEL, Vincent
IPC分类号： C07D207/20
CPC分类号： C07D401/10 , A61K31/401 , C07D207/22 , C07D403/10
摘要： The present invention is related to the use of pyrrolidine esters of formula (I) for the treatment and/or prevention of premature labor, premature birth and dysmenorrhea. In particular, the present invention is related to the use of pyrrolidine esters of formula (I) to modulate, notably to antagonise the oxytocin receptor. The present invention is furthermore related to novel pyrrolidine esters. X is selected from the group consisting of CR 6 R 7 , NOR 6 , NNR 6 R 7 ;R is selected from the group comprising or consisting of C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, saturated or unsaturated 3-8-membered cycloalkyl which may contain 1 to 3 heteroatoms selected of N, O, S, aryl, heteroaryl, C 1 -C 6 -alkyl aryl, C 1 -C 6 -alkyl heteroaryl. R 1 is selected from the group comprising or consisting of C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, aryl, heteroaryl, 3-8-membered cycloalkyl, acyl, C 1 -C 6 -alkyl aryl, C 1 -C 6 -alkyl heteroaryl, said cycloalkyl or aryl or heteroaryl groups may be fused with 1-2 further cycloalkyl or aryl or heteroaryl group.
摘要翻译：本发明涉及式（I）的吡咯烷酯用于治疗和/或预防早产，早产和痛经的用途。特别地，本发明涉及式（I）的吡咯烷酯的用途，特别是拮抗催产素受体。本发明还涉及新的吡咯烷酯。 X选自CR 6 R 7，NOR 6，NNR 6 R 7; R选自C 1 -C 6烷基，C 2 -C 6烯基 C 2 -C 6炔基，饱和或不饱和的3-8元环烷基，其可以含有1-3个选自N，O，S，芳基，杂芳基，C 1 -C 6烷基芳基，C 1 -C 6烷基杂芳基的杂原子。 R 1选自由C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 炔基，芳基，杂芳基，3-8元环烷基，酰基，C 1 -C 6 - 烷基芳基，C 1 -C 6烷基杂芳基，所述环烷基或芳基或杂芳基可与1-2个其它环烷基或芳基或杂芳基稠合。

3. 发明申请

WO2007082956A1 THIAZOLE DERIVATIVES AND USE THEREOF 审中-公开
标题翻译：噻唑衍生物及其用途
公开(公告)号：WO2007082956A1
公开(公告)日：2007-07-26
申请号：PCT/EP2007/050618
申请日：2007-01-22
申请人： LABORATOIRES SERONO S.A. , QUATTROPANI, Anna , POMEL, Vincent , RUECKLE, Thomas , GRIPPI-VALLOTTON, Tania
发明人： QUATTROPANI, Anna , POMEL, Vincent , RUECKLE, Thomas , GRIPPI-VALLOTTON, Tania
IPC分类号： C07D417/04 , C07D417/14 , A61K31/427 , A61K31/4439 , A61P37/00
CPC分类号： C07D417/04 , C07D417/14
摘要： The present invention is related to thiazole 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）的噻唑衍生物，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。

4. 发明申请

WO2006125807A1 THIAZOLE DERIVATIVES AND USE THEREOF 审中-公开
标题翻译：噻唑衍生物及其用途
公开(公告)号：WO2006125807A1
公开(公告)日：2006-11-30
申请号：PCT/EP2006/062602
申请日：2006-05-24
申请人： Applied Research Systems ARS Holding N.V. , QUATTROPANI, Anna , COVINI, David , POMEL, Vincent , DORBAIS, Jérôme , RUECKLE, Thomas
发明人： QUATTROPANI, Anna , COVINI, David , POMEL, Vincent , DORBAIS, Jérôme , RUECKLE, Thomas
IPC分类号： C07D417/04 , A61K31/427 , A61P37/00 , A61P25/00 , A61P31/00
CPC分类号： C07D417/14 , C07D417/04
摘要： The present invention is related to thiazolc 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）的噻唑衍生物，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。

5. 发明申请

WO2010037765A3 4 -MORPHOLINO-PYRIDO [3, 2 -D] PYRIMIDINES ACTIVE ON PI3K 审中-公开
标题翻译：在PI3K上活化的4-吗啉基 - 吡啶并[3,2-D]吡啶
公开(公告)号：WO2010037765A3
公开(公告)日：2010-07-15
申请号：PCT/EP2009062664
申请日：2009-09-30
申请人： MERCK SERONO SA , POMEL VINCENT , GAILLARD PASCALE , DESFORGES GWENAELLE , QUATTROPANI ANNA , MONTAGNE CYRIL
发明人： POMEL VINCENT , GAILLARD PASCALE , DESFORGES GWENAELLE , QUATTROPANI ANNA , MONTAGNE CYRIL
IPC分类号： C07D471/04 , A61K31/519 , A61P35/00 , A61P37/00
CPC分类号： C07D471/04
摘要： This invention relates to compounds of Formula (I) as Pi3k inhibitors for treating autoimmune deseases, inflammatory disorders, multiple sclerosis and other deseases 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。

6. 发明申请

WO2003082278A1 THIAZOLIDINE CARBOXAMIDE DERIVATIVES AS MODULATORS OF THE PROSTAGLANDIN F RECEPTOR 审中-公开
标题翻译：作为PROSTAGLANDIN F受体的调节剂的噻唑烷羧酰胺衍生物
公开(公告)号：WO2003082278A1
公开(公告)日：2003-10-09
申请号：PCT/EP2003/050083
申请日：2003-03-27
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , PAGE, Patrick , JORAND-LEBRUN, Catherine , QUATTROPANI, Anna , POMEL, Vincent , SCHWARZ, Matthias , HAMELIN, Estelle , THOMAS, Russell J.
发明人： PAGE, Patrick , JORAND-LEBRUN, Catherine , QUATTROPANI, Anna , POMEL, Vincent , SCHWARZ, Matthias , HAMELIN, Estelle , THOMAS, Russell J.
IPC分类号： A61K31/426
CPC分类号： C07D417/12 , A61K31/426 , A61K31/427 , C07D277/06 , C07D417/14 , Y02P20/582
摘要： The present invention is related to thiazolidine carboxamide derivatives of formula (II) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery. G is selected from the group consisting of C 1 -C 6 -alkyl aryl, C 1 -C 6 -alkyl heteroaryl, C 1 -C 6 Alkyl cycloalkyl, C 1 -C 6 -alkyl heteroaryl, aryl, heteroaryl, C 3 -C 8 -cycloalkyl or -heterocycloalkyl, said cycloalkyl or aryl or heteroaryl groups may be fused with cycloalkyl or aryl or heteroaryl groups. R 1 is selected from the group consisting of aryl, heteroaryl, C 3 -C 8 -cycloalkyl or - heterocyclo-alkyl, said (hetero)cycloalkyl or aryl or heteroaryl groups may be fused with (hetero)cycloalkyl or aryl or heteroaryl groups. R 2 is selected from the group consisting of H, carboxy, acyl, alkoxycarbonyl, aminocarbonyl, C 1 -C 5 -alkyl carboxy, C 1 -C 5 -alkyl acyl, C 1 -C 5 -alkyl alkoxycarbonyl, C 1 -C 5 -alkyl aminocarbonyl, C 1 -C 5 -alkyl acyloxy, C 1 -C 5 -alkyl acylamino, C 1 -C 5 -alkyl ureido, C 1 -C 5 alkyl amino, C 1 -C 5 -alkyl alkoxy, C 1 -C 5 -alkyl sulfanyl, C 1 -C 5 -alkyl sulfinyl, C 1 -C 5 -alkyl sulfonyl, C 1 -C 5 -alkyl sulfonylamino, C 1 -C 5 -alkyl sulfonyloxy, C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, aryl, heteroaryl, C 3 -C 8 -cycloalkyl, heterocycloalkyl, C 1 -C 6 -alkyl aryl, C 2 -C 6 -alkyl heteroaryl, C 1 -C 6 -alkyl cycloalkyl, C 1 -C 6 -alkyl heterocycloalkyl, C 2 -C 6 -alkenyl aryl, C 2 -C 6 -alkenyl heteroaryl, C 2 -C 6 -alkynyl aryl, or C 2 -C 6 -alkynyl heteroaryl.
摘要翻译：本发明涉及式（II）的噻唑烷羧酰胺衍生物，其用于治疗和/或预防早产，早产，痛经和用于在剖宫产分娩前停止劳动。 G选自C1-C6-烷基芳基，C1-C6-烷基杂芳基，C1-C6烷基环烷基，C1-C6-烷基杂芳基，芳基，杂芳基，C3-C8-环烷基或 - 杂环烷基，所述环烷基或芳基或杂芳基可与环烷基或芳基或杂芳基稠合。 R 1选自芳基，杂芳基，C 3 -C 8 - 环烷基或 - - 杂环烷基，所述（杂）环烷基或芳基或杂芳基可与（杂）环烷基或芳基或杂芳基稠合。 R 2选自H，羧基，酰基，烷氧基羰基，氨基羰基，C 1 -C 5 - 烷基羧基，C 1 -C 5 - 烷基酰基，C 1 -C 5 - 烷基烷氧基羰基，C 1 -C 5 - 烷基氨基羰基，C 1 C 1 -C 5烷基酰氧基，C 1 -C 5烷基酰氨基，C 1 -C 5烷基脲基，C 1 -C 5烷基氨基，C 1 -C 5烷基烷氧基，C 1 -C 5烷基硫烷基，C 1 -C 5烷基亚磺酰基，烷基磺酰基，C 1 -C 5 - 烷基磺酰基氨基，C 1 -C 5 - 烷基磺酰氧基，C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6炔基，芳基，杂芳基，C 3 -C 8 - 环烷基，杂环烷基，C 1 -C 6 烷基芳基，C 2 -C 6烷基杂芳基，C 1 -C 6烷基环烷基，C 1 -C 6烷基杂环烷基，C 2 -C 6烯基芳基，C 2 -C 6链烯基杂芳基，C 2 -C 6炔基芳基或C 2 -C 6 - 炔基杂芳基。

7. 发明申请

WO2002102799A2 PYRROLIDINE OXADIAZOLE- AND THIADIAZOLE DERIVATIVES 审中-公开
标题翻译：吡咯烷氧基噻唑和噻唑并吡啶衍生物
公开(公告)号：WO2002102799A2
公开(公告)日：2002-12-27
申请号：PCT/EP2002/006629
申请日：2002-06-14
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , SCHWARZ, Matthias , PAGE, Patrick , POMEL, Vincent , QUATTROPANI, Anna , THOMAS, Russell, J.
发明人： SCHWARZ, Matthias , PAGE, Patrick , POMEL, Vincent , QUATTROPANI, Anna , THOMAS, Russell, J.
IPC分类号： C07D413/04
CPC分类号： C07D413/04 , C07D413/14
摘要： The present invention is related to pyrrolidine oxadiazole and thiadiazole derivatives for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such pyrrolidine oxadiazole derivatives. Said pyrrolidine derivatives are useful in the treatment and/or prevention of preterm labor, premature birth and dysmenorrhea. In particular, the present invention is related to pyrrolidine derivatives displaying a substantial modulatory, notably an antagonist activity of the oxytocin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin, including preterm labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. (I) B is a oxadiazole or thiadiazole group.
摘要翻译：本发明涉及用作药物活性化合物的吡咯烷恶二唑和噻二唑衍生物，以及含有这种吡咯烷恶二唑衍生物的药物制剂。所述吡咯烷衍生物可用于治疗和/或预防早产，早产和痛经。特别地，本发明涉及显示出显着调节，特别是催产素受体拮抗剂活性的吡咯烷衍生物。更优选地，所述化合物可用于治疗和/或预防催产素介导的疾病状态，包括早产，早产和痛经。本发明还涉及新型吡咯烷衍生物及其制备方法。（I）B是恶二唑或噻二唑基。

8. 发明申请

WO2011058149A1 TRICYCLIC PYRAZOL AMINE DERIVATIVES 审中-公开
标题翻译：三聚吡嗪胺衍生物
公开(公告)号：WO2011058149A1
公开(公告)日：2011-05-19
申请号：PCT/EP2010/067412
申请日：2010-11-12
申请人： MERCK SERONO S.A. , GAILLARD, Pascale , JEANCLAUDE-ETTER, Isabelle , POMEL, Vincent , SEBILLE, Eric , JEYAPRAKASHNARAYANAN, Seenisamy , MUZERELLE, Mathilde
发明人： GAILLARD, Pascale , JEANCLAUDE-ETTER, Isabelle , POMEL, Vincent , SEBILLE, Eric , JEYAPRAKASHNARAYANAN, Seenisamy , MUZERELLE, Mathilde
IPC分类号： C07D495/04 , C07D495/14 , A61K31/56 , A61P37/00
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。

9. 发明申请

WO2010037765A2 4-MORPHOLINO-PYRIDO[3,2-D]PYRIMIDINES 审中-公开
标题翻译： 4-吗啉代吡啶并[3,2-D]嘧啶类
公开(公告)号：WO2010037765A2
公开(公告)日：2010-04-08
申请号：PCT/EP2009/062664
申请日：2009-09-30
申请人： MERCK SERONO S.A. , POMEL, Vincent , GAILLARD, Pascale , DESFORGES, Gwenaelle , QUATTROPANI, Anna , MONTAGNE, Cyril
发明人： POMEL, Vincent , GAILLARD, Pascale , DESFORGES, Gwenaelle , QUATTROPANI, Anna , MONTAGNE, Cyril
IPC分类号： C07D471/04 , A61P35/00 , A61P37/00 , A61K31/519
CPC分类号： C07D471/04
摘要： This invention relates to compounds of Formula (I) as Pi3k inhibitors for treating autoimmune deseases, inflammatory disorders, multiple sclerosis and other deseases 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. 发明申请

WO2006024666A1 PYRIDINE METHYLENE AZOLIDINONES AND USE THEREOF PHOSPHOINOSITIDE INHIBITORS 审中-公开
标题翻译：吡啶甲基亚胺嘧啶酮及其用途磷酰胺抑制剂
公开(公告)号：WO2006024666A1
公开(公告)日：2006-03-09
申请号：PCT/EP2005/054339
申请日：2005-09-02
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , RUECKLE, Thomas , QUATTROPANI, Anna , POMEL, Vincent , DORBAIS, Jérôme , COVINI, David , BISCHOFF, Alexander
发明人： RUECKLE, Thomas , QUATTROPANI, Anna , POMEL, Vincent , DORBAIS, Jérôme , COVINI, David , BISCHOFF, Alexander
IPC分类号： C07D471/04 , C07D491/04 , A61K31/4355 , A61K31/519 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04 , C07D491/04
摘要： The present invention is related to fused pyridine methylene azolidinone 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）的稠合吡啶亚甲基唑烷酮衍生物，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，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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