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1. 发明申请

US20090215749A9 THIAZOLIDINE CARBOXAMIDE DERIVATIVES AS MODULATORS OF THE PROSTAGLANDIN F RECEPTOR 有权
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：US20090215749A9
公开(公告)日：2009-08-27
申请号：US12140682
申请日：2008-06-17
申请人： Patrick Naxos PAGE , Catherine Jorand-Lebrun , Anna Quattropani , Vincent Pomel , Matthias Schwarz , Estelle Hamelin , Russell J. Thomas
发明人： Patrick Naxos PAGE , Catherine Jorand-Lebrun , Anna Quattropani , Vincent Pomel , Matthias Schwarz , Estelle Hamelin , Russell J. Thomas
IPC分类号： A61K31/55 , C07D277/06 , A61K31/426 , A61P15/06 , A61P15/04 , C07D417/12
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.
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。

2. 发明授权

US08415480B2 Thiazolidine carboxamide derivatives as modulators of the prostaglandin F receptor 有权
标题翻译：噻唑烷羧酰胺衍生物作为前列腺素F受体的调节剂
公开(公告)号：US08415480B2
公开(公告)日：2013-04-09
申请号：US12140682
申请日：2008-06-17
申请人： Patrick Naxos Page , Catherine Jorand-Lebrun , Anna Quattropani , Vincent Pomel , Matthias Schwarz , Estelle Hamelin , Russell J. Thomas
发明人： Patrick Naxos Page , Catherine Jorand-Lebrun , Anna Quattropani , Vincent Pomel , Matthias Schwarz , Estelle Hamelin , Russell J. Thomas
IPC分类号： A61K31/4402 , A61K31/426 , C07D417/12 , C07D277/46
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.
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。

3. 发明申请

US20080255094A1 THIAZOLIDINE CARBOXAMIDE DERIVATIVES AS MODULATORS OF THE PROSTAGLANDIN F RECEPTOR 有权
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：US20080255094A1
公开(公告)日：2008-10-16
申请号：US12140682
申请日：2008-06-17
申请人： Patrick Naxos PAGE , Catherine Jorand-Lebrun , Anna Quattropani , Vincent Pomel , Matthias Schwarz , Estelle Hamelin , Russell J. Thomas
发明人： Patrick Naxos PAGE , Catherine Jorand-Lebrun , Anna Quattropani , Vincent Pomel , Matthias Schwarz , Estelle Hamelin , Russell J. Thomas
IPC分类号： A61K31/55 , C07D277/06 , A61K31/426 , A61P15/06 , A61P15/04 , C07D417/12
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.
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。

4. 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

5. 发明授权

US08404690B2 Piperazine-2-carboxamide derivatives 失效
标题翻译：哌嗪-2-甲酰胺衍生物
公开(公告)号：US08404690B2
公开(公告)日：2013-03-26
申请号：US10545296
申请日：2004-02-06
申请人： Patrick Page , Catherine Jorand-Lebrun , Russell J. Thomas , Matthias Schwarz
发明人： Patrick Page , Catherine Jorand-Lebrun , Russell J. Thomas , Matthias Schwarz
IPC分类号： A61K31/497 , C07D401/00
CPC分类号： C07D231/12 , A61K31/16 , A61K31/495 , C07D233/56 , C07D241/04 , C07D249/08 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14
摘要： The present invention is related to piperazine-2-carboxamide derivatives of formula (I) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery. Wherein A, X, Y, R1 and R2 are as defined in the description.
摘要翻译：本发明涉及式（I）的哌嗪-2-甲酰胺衍生物，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。其中A，X，Y，R 1和R 2如说明书中所定义。

6. 发明授权

US07468385B2 Triazoles as oxytocin antagonists 失效
标题翻译：三唑作为催产素拮抗剂
公开(公告)号：US07468385B2
公开(公告)日：2008-12-23
申请号：US10498356
申请日：2002-12-19
申请人： Anna Quattropani , Matthias Schwarz , Russell J. Thomas , Thomas Coulter
发明人： Anna Quattropani , Matthias Schwarz , Russell J. Thomas , Thomas Coulter
IPC分类号： A61K31/41 , C07D249/08
CPC分类号： C07D403/12 , C07D249/10 , C07D249/12 , C07D249/14 , C07D405/06 , C07D405/12
摘要： The present invention relates to triazole derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such triazole derivatives. Said triazoles 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 triazole 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. The present invention is furthermore related to novel triazole derivatives as well as to methods of their preparation.
摘要翻译：本发明涉及特别用作药物活性化合物的式（I）的三唑衍生物以及含有这种三唑衍生物的药物制剂。所述三唑可用于治疗和/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，本发明涉及显示催产素和/或加压素受体的显着调节，特别是拮抗活性的三唑衍生物。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。本发明还涉及新的三唑衍生物及其制备方法。

7. 发明申请

US20080167318A1 Pharmaceutically active pyrrolidine derivatives 审中-公开
标题翻译：药用活性吡咯烷衍生物
公开(公告)号：US20080167318A1
公开(公告)日：2008-07-10
申请号：US11783341
申请日：2007-04-09
申请人： Serge Halazy , Anna Quattropani , Alexander Scheer , Matthias Schwarz , Russell J. Thomas , Anthony Baxter
发明人： Serge Halazy , Anna Quattropani , Alexander Scheer , Matthias Schwarz , Russell J. Thomas , Anthony Baxter
IPC分类号： A61K31/497 , A61K31/40 , A61K31/403 , A61P15/06 , C07D209/56 , C07D455/02 , C07D403/02 , C07D207/02 , A61P15/02 , A61K31/47
CPC分类号： C07D401/12 , C07D207/22 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12
摘要： The present invention is related to pyrrolidine derivatives of formula I. Said compounds are preferably for use as pharmaceutically active compounds. Specifically, pyrrolidine derivatives of formula I are useful in the treatment and/or prevention of premature 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 premature labor, premature birth and dysmenorrhea. The present invention is furthermore related to novel pyrrolidine derivatives as well as to methods of their preparation. wherein X is selected from the group consisting of CR6R7, NOR6, NNR6R7; A is selected from the group consisting of —(C═O)—, —(C═O)—O—, —C(═NH)—, —(C═O)—NH—, —(C═S)—NH, —SO2—, —SO2NH—, —CH2—, B is either a group —C═O)—NR8R9 or represents a heterocyclic residue having the formula wherein Q is NR10, O or S; n is an integer selected of 0, 1 or 2; Y, Z and E form together with the 2 carbons to which they are attached a 5-6 membered aryl or heteroaryl ring.
摘要翻译：本发明涉及式I的吡咯烷衍生物。所述化合物优选用作药物活性化合物。具体地，式I的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。其中X选自CR 6，S 6，S 6，N 6，R 6，O 6， > 7 ; A选自 - （CO） - ， - （CO）-O-，-C（-NH） - ， - （CO）-NH-， - （CS）-NH， 2 - ， - SO 2 NH - ， - CH 2 - ， - B是基团-CO）-NR 8 - 或者表示具有下式的杂环残基：其中Q是NR 10，O或S; n是选自0,1或2的整数; Y，Z和E与它们所连接的2个碳原子一起形成5-6元芳基或杂芳基环。

8. 发明申请

US20130143893A1 PIPERAZINE DERIVATIVES AND METHODS OF USE 审中-公开
标题翻译：哌嗪衍生物及其使用方法
公开(公告)号：US20130143893A1
公开(公告)日：2013-06-06
申请号：US13754345
申请日：2013-01-30
申请人： Sharad Magar , Andreas Goutopoulos , Yihua Liao , Matthias Schwarz , Russell J. Thomas
发明人： Sharad Magar , Andreas Goutopoulos , Yihua Liao , Matthias Schwarz , Russell J. Thomas
IPC分类号： C07D409/14 , C07D403/12 , C07D471/04 , C07D403/14
CPC分类号： C07D409/14 , A61K31/496 , C07D401/14 , C07D403/12 , C07D403/14 , C07D471/04 , C07D487/04
摘要： The invention provides 2-carboxamide piperazine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility.
摘要翻译：本发明提供2-甲酰胺哌嗪化合物，以及使用或包含一种或多种这些化合物的治疗方法和药物组合物。本发明的化合物可用于治疗哺乳动物不育症。

9. 发明授权

US07754722B2 Piperazine derivatives and methods of use 失效
标题翻译：哌嗪衍生物和使用方法
公开(公告)号：US07754722B2
公开(公告)日：2010-07-13
申请号：US10528437
申请日：2003-09-19
申请人： Sharad Magar , Andreas Goutopoulos , Yihua Liao , Matthias Schwarz , Russell J. Thomas
发明人： Sharad Magar , Andreas Goutopoulos , Yihua Liao , Matthias Schwarz , Russell J. Thomas
IPC分类号： A61K31/497 , C07D241/04 , C07D295/00 , C07D403/00
CPC分类号： C07D409/14 , A61K31/496 , C07D401/14 , C07D403/12 , C07D403/14 , C07D471/04 , C07D487/04
摘要： The invention provides 2-carboxamide piperazine compounds of formula I, R3.IN\′N˜′R2I(0)z-oR4I wherein R′, R2, R3 and R4 are as defined in the claims and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility.
摘要翻译：本发明提供了式I的R 2，R 3，R 1，R 2，R 3和R 4如权利要求书和治疗方法和药物组合物中所定义的2-羧酰胺哌嗪化合物，使用或包含一种或多种这样的化合物。本发明的化合物可用于治疗哺乳动物不育症。

10. 发明授权

US08946227B2 Piperazine derivatives and methods of use 有权
标题翻译：哌嗪衍生物和使用方法
公开(公告)号：US08946227B2
公开(公告)日：2015-02-03
申请号：US13754345
申请日：2013-01-30
申请人： Sharad Magar , Andreas Goutopoulos , Yihua Liao , Matthias Schwarz , Russell J. Thomas
发明人： Sharad Magar , Andreas Goutopoulos , Yihua Liao , Matthias Schwarz , Russell J. Thomas
IPC分类号： A61K31/4965 , C07D295/00 , C07D409/14 , A61K31/496 , C07D401/14 , C07D403/12 , C07D487/04 , C07D471/04
CPC分类号： C07D409/14 , A61K31/496 , C07D401/14 , C07D403/12 , C07D403/14 , C07D471/04 , C07D487/04
摘要： The invention provides 2-carboxamide piperazine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility.
摘要翻译：本发明提供2-甲酰胺哌嗪化合物，以及使用或包含一种或多种这些化合物的治疗方法和药物组合物。本发明的化合物可用于治疗哺乳动物不育症。

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