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1. 发明申请

WO2010142628A1 PYRAZOLE OXADIAZOLE DERIVATIVES AS S1P1 AGONISTS 审中-公开
标题翻译：作为S1P1激动剂的吡唑氧杂衍生物
公开(公告)号：WO2010142628A1
公开(公告)日：2010-12-16
申请号：PCT/EP2010/057893
申请日：2010-06-07
申请人： MERCK SERONO S.A. , QUATTROPANI, Anna , BAKER-GLENN, Charles , BLACKABY, Wesley , KNIGHT, Chris
发明人： QUATTROPANI, Anna , BAKER-GLENN, Charles , BLACKABY, Wesley , KNIGHT, Chris
IPC分类号： C07D413/04 , C07D413/14 , C07D471/04 , A61K31/4245 , A61P37/06
CPC分类号： C07D231/10 , C07D271/06 , C07D413/04 , C07D413/14 , C07D471/04
摘要： The present invention relates to pyrazole oxadiazoles derivatives of Formula (I), and their use for treating multiple sclerosis and other diseases. Wherein R 1 , R 2 and R 3 are as defined in the description.
摘要翻译：本发明涉及式（I）的吡唑恶二唑衍生物及其治疗多发性硬化症等疾病的用途。其中R1，R2和R3如说明书中所定义。

2. 发明申请

WO2005068444A2 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：WO2005068444A2
公开(公告)日：2005-07-28
申请号：PCT/EP2005/050102
申请日：2005-01-11
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , QUATTROPANI, Anna , RUECKLE, Thomas , SCHWARZ, Matthias , DORBAIS, Jerôme , SAUER, Wolfgang , CLEVA, Christophe , DESFORGES, Gwénaëlle
发明人： QUATTROPANI, Anna , RUECKLE, Thomas , SCHWARZ, Matthias , DORBAIS, Jerôme , SAUER, Wolfgang , CLEVA, Christophe , DESFORGES, Gwénaëlle
IPC分类号： C07D277/46
CPC分类号： C07D417/04 , C07D277/46 , 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/或预防自身免疫性疾病和/或炎性疾病，心血管疾病，神经退行性疾病，细菌或病毒感染，肾脏疾病，血小板聚集，癌症，移植，移植排斥或肺损伤。

3. 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。

4. 发明申请

WO2010115751A2 OXADIAZOLE DERIVATIVES 审中-公开
标题翻译：恶二唑衍生物
公开(公告)号：WO2010115751A2
公开(公告)日：2010-10-14
申请号：PCT/EP2010/054100
申请日：2010-03-29
申请人： MERCK SERONO S.A. , QUATTROPANI, Anna , MONTAGNE, Cyril , SAUER, Wolfgang , CROSIGNANI, Stefano , BOMBRUN, Agnès
发明人： QUATTROPANI, Anna , MONTAGNE, Cyril , SAUER, Wolfgang , CROSIGNANI, Stefano , BOMBRUN, Agnès
IPC分类号： C07D271/06 , A61K31/4245 , A61P37/00
CPC分类号： A61K31/4245 , A61K31/192 , A61K31/197 , C07C57/30 , C07D271/06
摘要： The invention relates to compounds of formula I: wherein R 1 , R 2 , R a , R b , W, Q and S have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
摘要翻译：本发明涉及式I的化合物：其中R 1，R 2，R 1，R 2，R 3，R 4，R 5，其中W，Q和S具有权利要求1中给出的含义用于治疗自身免疫性疾病，如多发性硬化症。

5. 发明申请

WO2010069949A1 OXADIAZOLE FUSED HETEROCYCLIC DERIVATIVES USEFUL FOR THE TREATMENT OF MULTIPLE SCLEROSIS 审中-公开
标题翻译：用于治疗多发性硬化症的OXADIAZOLE FUSED HETEROCYCLIC DERIVATIVES
公开(公告)号：WO2010069949A1
公开(公告)日：2010-06-24
申请号：PCT/EP2009/067171
申请日：2009-12-15
申请人： MERCK SERONO S.A. , MUZERELLE, Mathilde , QUATTROPANI, Anna , MONTAGNE, Cyril , DORBAIS, Jérôme
发明人： MUZERELLE, Mathilde , QUATTROPANI, Anna , MONTAGNE, Cyril , DORBAIS, Jérôme
IPC分类号： C07D413/04 , C07D413/14 , A61K31/4525 , A61K31/435 , A61K31/4245 , A61P21/00 , A61P29/00 , A61P37/00
CPC分类号： C07D413/04 , C07D413/14
摘要： The invention provides compounds of Formula (I) for the treatment of multiple sclerosis and other diseases.
摘要翻译：本发明提供式（I）化合物用于治疗多发性硬化症和其它疾病。

6. 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。

7. 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。

8. 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。

9. 发明申请

WO2009043889A3 OXADIAZOLE DERIVATIVES 审中-公开
公开(公告)号：WO2009043889A3
公开(公告)日：2009-04-09
申请号：PCT/EP2008/063180
申请日：2008-10-01
申请人： MERCK SERONO S.A. , QUATTROPANI, Anna , MONTAGNE, Cyril , SAUER, Wolfgang , CROSIGNANI, Stefano , BOMBRUN, Agnes , MUZERELLE, Mathilde , DORBAIS, Jerome , MARIN, Delphine , GONZALEZ, Jérôme , GERBER, Patrick
发明人： QUATTROPANI, Anna , MONTAGNE, Cyril , SAUER, Wolfgang , CROSIGNANI, Stefano , BOMBRUN, Agnes , MUZERELLE, Mathilde , DORBAIS, Jerome , MARIN, Delphine , GONZALEZ, Jérôme , GERBER, Patrick
IPC分类号： C07D263/32 , C07D413/04 , C07D413/10 , A61K31/4245 , A61P37/00
摘要： The invention relates to compounds of formula (I). The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.

10. 发明申请

WO2006125805A1 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：WO2006125805A1
公开(公告)日：2006-11-30
申请号：PCT/EP2006/062595
申请日：2006-05-24
申请人： APPLIED RESEARCH SYSTEMS ARS HOLDING N.V. , QUATTROPANI, Anna , DORBAIS, Jérôme , COVINI, David , DESFORGES, Gwenaelle , RUECKLE, Thomas
发明人： QUATTROPANI, Anna , DORBAIS, Jérôme , COVINI, David , DESFORGES, Gwenaelle , RUECKLE, Thomas
IPC分类号： C07D277/46 , C07D277/48 , C07D277/56 , C07D417/14 , C07D491/10 , C07D493/08 , A61K31/427 , A61K31/433 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/553 , A61P9/00 , A61P25/00
CPC分类号： C07D277/46 , C07D277/48 , C07D277/56 , C07D417/14 , C07D491/10 , C07D493/08
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。

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