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1. 发明申请

US20100305092A1 TRIAZOLE OXADIAZOLES DERIVATIVES 有权
标题翻译：三唑氧化酶衍生物
公开(公告)号：US20100305092A1
公开(公告)日：2010-12-02
申请号：US12809816
申请日：2008-12-17
申请人： Anna Quattropani , Christophe Cleva , Eric Sebille , Matthias Schwarz , Delphine Marin
发明人： Anna Quattropani , Christophe Cleva , Eric Sebille , Matthias Schwarz , Delphine Marin
IPC分类号： A61K31/397 , C07D413/04 , A61K31/4245 , C07D413/14 , A61K31/4439 , A61K31/5377 , C07D401/14 , A61K31/444 , A61K31/4545 , A61K31/4725 , A61K31/497 , A61P19/02 , A61P3/10 , A61P9/10 , A61P1/04 , A61P17/06 , A61P11/06 , A61P29/00
CPC分类号： C07D413/04 , C07D413/14
摘要： The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, X have the meanings given in claim 16. 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化合物：其中R1，R2，Ra，Rb，X具有权利要求1中给出的含义。治疗自身免疫性疾病，如多发性硬化症。

2. 发明授权

US08202856B2 Triazole oxadiazoles derivatives 有权
标题翻译：三唑恶二唑衍生物
公开(公告)号：US08202856B2
公开(公告)日：2012-06-19
申请号：US12809816
申请日：2008-12-17
申请人： Anna Quattropani , Christophe Cleva , Eric Sebille , Matthias Schwarz , Delphine Marin , Agnes Bombrun , Wesley Blackaby , Charles Baker-Glenn , Chris Knight , Craig Rouse
发明人： Anna Quattropani , Christophe Cleva , Eric Sebille , Matthias Schwarz , Delphine Marin , Agnes Bombrun , Wesley Blackaby , Charles Baker-Glenn , Chris Knight , Craig Rouse
IPC分类号： A61K31/397 , A61K31/4545 , A61K31/444 , A61K31/5377 , A61K31/4245 , A61K31/4439 , A61K31/4725 , A61K31/497 , C07D413/04 , C07D413/14 , C07D401/14 , A61P19/02 , A61P3/10 , A61P9/10 , A61P29/00 , A61P1/04 , A61P17/06 , A61P11/06
CPC分类号： C07D413/04 , C07D413/14
摘要： The invention relates to compounds of formula I: wherein R1, R2,Ra, Rb, X have the meanings given in claim 16. 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化合物：其中R1，R2，Ra，Rb，X具有权利要求1中给出的含义。治疗自身免疫性疾病，如多发性硬化症。

3. 发明申请

US20090029998A1 Thiazole Derivatives and Use Thereof 有权
标题翻译：噻唑衍生物及其用途
公开(公告)号：US20090029998A1
公开(公告)日：2009-01-29
申请号：US10585635
申请日：2005-01-11
申请人： Anna Quattropani , Thomas Rueckle , Matthias Schwarz , Jerome Dorbais , Wolfgang Sauer , Christophe Cleva , Gwenaelle Desforges
发明人： Anna Quattropani , Thomas Rueckle , Matthias Schwarz , Jerome Dorbais , Wolfgang Sauer , Christophe Cleva , Gwenaelle Desforges
IPC分类号： A61K31/427 , C07D277/38 , C07D401/04 , A61K31/5377 , A61P29/00 , A61P25/28 , A61P9/00 , A61P31/12 , A61P37/00 , A61K31/454 , C07D413/04
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. 发明授权

US08802861B2 Thiazole derivatives and use thereof 有权
标题翻译：噻唑衍生物及其用途
公开(公告)号：US08802861B2
公开(公告)日：2014-08-12
申请号：US10585635
申请日：2005-01-11
申请人： Anna Quattropani , Thomas Rueckle , Matthias Schwarz , Jerome Dorbais , Wolfgang Sauer , Christophe Cleva , Gwenaelle Desforges
发明人： Anna Quattropani , Thomas Rueckle , Matthias Schwarz , Jerome Dorbais , Wolfgang Sauer , Christophe Cleva , Gwenaelle Desforges
IPC分类号： A61K31/427 , C07D417/04 , C07D417/14
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

US20120115869A1 TETRAZOLE DERIVATIVES 审中-公开
标题翻译：四唑衍生物
公开(公告)号：US20120115869A1
公开(公告)日：2012-05-10
申请号：US13383848
申请日：2010-07-14
申请人： Stefano Crosignani , Christophe Cleva , Anna Quattropani , Gwenaelle Desforges , Agnès Bombrun
发明人： Stefano Crosignani , Christophe Cleva , Anna Quattropani , Gwenaelle Desforges , Agnès Bombrun
IPC分类号： A61K31/41 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D401/12 , A61K31/4439 , A61K31/4709 , A61K31/5377 , A61P37/08 , A61P11/06 , A61P27/02 , A61P27/00 , A61K31/422 , A61K31/428 , A61K31/4245 , A61K31/427 , A61K31/4155 , A61P17/00 , A61P29/00 , C07D257/04
CPC分类号： C07D257/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of formula (I) for use as pharmaceutical active compounds, as well as pharmaceutical formulations containing the same, for the treatment of allergic diseases.
摘要翻译：本发明涉及用作药物活性化合物的式（I）化合物，以及含有该化合物的用于治疗过敏性疾病的药物制剂。

6. 发明授权

US08202865B2 Oxadiazole derivatives 有权
标题翻译：恶二唑衍生物
公开(公告)号：US08202865B2
公开(公告)日：2012-06-19
申请号：US12675235
申请日：2008-10-01
申请人： Anna Quattropani , Cyril Montagne , Wolfgang Sauer , Stefano Crosignani , Agnes Bombrun , Mathilde Muzerelle , Jermone Dorbais , Delphine Marin , Jerome Gonzalez , Patrick Gerber
发明人： Anna Quattropani , Cyril Montagne , Wolfgang Sauer , Stefano Crosignani , Agnes Bombrun , Mathilde Muzerelle , Jermone Dorbais , Delphine Marin , Jerome Gonzalez , Patrick Gerber
IPC分类号： A61K31/5377 , A61K31/454 , A61K31/4439 , A61K31/4245 , C07D413/02 , C07D271/06
CPC分类号： C07D263/32 , C07D413/04 , C07D413/10
摘要： The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, W, Q and S have the meanings given in claim 16. 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化合物：其中R1，R2，Ra，Rb，W，Q和S具有权利要求16中给出的含义。治疗自身免疫性疾病，如多发性硬化症。

7. 发明申请

US20100240658A1 Oxadiazole Derivatives 有权
标题翻译：恶二唑衍生物
公开(公告)号：US20100240658A1
公开(公告)日：2010-09-23
申请号：US12675235
申请日：2008-10-01
申请人： Anna Quattropani , Cyril Montagne , Wolfgang Sauer , Stefano Crosignani , Agnes Bombrun , Mathilde Muzerelle , Jerome Dorbais , Delphine Marin , Jerome Gonzalez , Patrick Gerber
发明人： Anna Quattropani , Cyril Montagne , Wolfgang Sauer , Stefano Crosignani , Agnes Bombrun , Mathilde Muzerelle , Jerome Dorbais , Delphine Marin , Jerome Gonzalez , Patrick Gerber
IPC分类号： A61K31/5377 , C07D271/06 , C07D413/02 , A61K31/4245 , A61K31/4439 , A61K31/454
CPC分类号： C07D263/32 , C07D413/04 , C07D413/10
摘要： The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, W, Q and S have the meanings given in claim 16. 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化合物：其中R1，R2，Ra，Rb，W，Q和S具有权利要求16中给出的含义。治疗自身免疫性疾病，如多发性硬化症。

8. 发明授权

US07312358B2 Pharmaceutically active sulfanilide derivatives 有权
标题翻译：药物活性磺酰苯胺衍生物
公开(公告)号：US07312358B2
公开(公告)日：2007-12-25
申请号：US10399040
申请日：2001-10-15
申请人： Anna Quattropani , Matthias Schwarz , Catherine Joran-Lebrun , Dennis Church , Alexander Scheer
发明人： Anna Quattropani , Matthias Schwarz , Catherine Joran-Lebrun , Dennis Church , Alexander Scheer
IPC分类号： C07C303/00
CPC分类号： C07D213/53 , A61K31/18 , A61K31/4045 , A61K31/437 , A61K31/4402 , A61K31/4439 , A61K31/4706 , A61K31/472 , A61K31/5377 , A61K38/00 , C07D207/16 , C07D209/20 , C07D209/40 , C07D209/44 , C07D217/16 , C07D217/26 , C07D233/64 , C07D471/04 , C07K5/06026 , C07K5/06191
摘要： The present invention relates to sulfanilide derivatives of formula (I), in which R1 and R2 are optionally substituted aryl and heteroaryl groups and the other variables are as defined in the claims, for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such sulfanilide derivatives. Said derivatives are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to sulfanilide derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin and/or vasopressin, including preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. The present invention is furthermore related to novel sulfanilide derivatives as well as to methods of their preparation.
摘要翻译：本发明涉及式（I）的磺酰苯胺衍生物，其中R 1和R 2是任选取代的芳基和杂芳基，其它变量如用作药物活性化合物，以及含有这种磺酰苯胺衍生物的药物制剂。所述衍生物可用于治疗和/或预防早产，早产，痛经，不适当的血管加压素分泌，充血性心力衰竭，动脉高血压，肝硬化，肾病综合征和高眼压症。特别地，本发明涉及展示催产素和/或加压素受体的实质性调节，特别是拮抗活性的磺酰苯胺衍生物。更优选地，所述化合物可用于治疗和/或预防催产素和/或加压素介导的疾病状态，包括早产，早产，痛经，不适当的血管加压素分泌，充血性心力衰竭，动脉高血压，肝硬化，肾病综合征和高眼压症。本发明还涉及新的磺酰苯胺衍生物及其制备方法。

9. 发明授权

US07189754B2 Pyrrolidine ester derivatives with oxytocin modulating activity 有权
标题翻译：吡咯烷酯衍生物与催产素调节活性
公开(公告)号：US07189754B2
公开(公告)日：2007-03-13
申请号：US10471290
申请日：2002-03-19
申请人： Matthias Schwarz , Anna Quattropani , Alexander Scheer , Jerome Dorbais , Vincent Pomel
发明人： Matthias Schwarz , Anna Quattropani , Alexander Scheer , Jerome Dorbais , Vincent Pomel
IPC分类号： A61K31/40 , C07D207/00
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 antagonize the oxytocin receptor. The present invention is furthermore related to novel pyrrolidine esters. X is selected from the group consisting of CR6R7, NOR6, NNR6R7; R is selected from the group comprising or consisting of C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, saturated or unsaturated 3–8-membered cycloalkyl which may contain 1 to 3 heteroatoms selected of N, O, S, aryl, heteroaryl, C1–C6-alkyl aryl, C1–C6-alkyl heteroaryl. R1 is selected from the group comprising or consisting of C1–C6-alkyl, C2–C6-alkenyl, C2–C6-alkynyl, aryl, heteroaryl, 3–8-membered cycloalkyl, acyl, C1–C6-alkyl aryl, C1–C6-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，S 6，S 6，N 6，R 6，R 6， 7 ; R选自包含C 1 -C 6 -C 6烷基，C 2 -C 6 -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，杂芳基的杂原子 C 1 -C 6 - 烷基芳基，C 1 -C 6 - 烷基杂芳基，C 1 -C 6 - 烷基芳基，C 1 -C 6 - R 1选自由C 1 -C 6 - C 6 - 烷基，C 2 - （C 1 -C 6）烷基组成的组或由C 1 -C 6 - C 6 - 烯基，C 2 -C 6 - 炔基，芳基，杂芳基，3-8元环烷基，酰基，C

10. 发明授权

US07115639B2 Pyrrolidine oxadiazole- and thiadiazole oxime derivatives being oxytocin receptor antagonists 有权
标题翻译：吡咯烷恶二唑和噻二唑肟衍生物是催产素受体拮抗剂
公开(公告)号：US07115639B2
公开(公告)日：2006-10-03
申请号：US10480992
申请日：2002-06-14
申请人： Matthias Schwarz , Anna Quattropani , Patrick Page , Russell J. Thomas , Vincent Pomel
发明人： Matthias Schwarz , Anna Quattropani , Patrick Page , Russell J. Thomas , Vincent Pomel
IPC分类号： A61K31/433 , A61K31/4245 , C07D271/113 , C07D285/125
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。 B是恶二唑或噻二唑基

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