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1. 发明申请

US20120251551A1 Substituted (Heteroarylmethyl)thiohydantoins 审中-公开
标题翻译：取代的（杂芳基甲基）硫代乙内酰脲
公开(公告)号：US20120251551A1
公开(公告)日：2012-10-04
申请号：US13394536
申请日：2010-08-28
申请人： Ulrich Lücking , Arwed Cleve , Bernard Haendler , Hortensia Faus Gimenez , Silke Köhr , Horst Irlbacher
发明人： Ulrich Lücking , Arwed Cleve , Bernard Haendler , Hortensia Faus Gimenez , Silke Köhr , Horst Irlbacher
IPC分类号： A61K31/4439 , C07D401/06 , C07D413/14 , A61K31/5377 , C07D417/14 , A61K31/541 , A61K31/551 , A61K31/4545 , C07D403/14 , A61K31/506 , C07D409/14 , A61K31/565 , A61K39/395 , A61P35/00 , C07D401/14
CPC分类号： C07D401/06 , C07D401/14 , C07D403/14 , C07D409/14 , C07D417/14
摘要： The invention relates to substituted (heteroarylmethyl) thiohydantoin compounds of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, and their use for the preparation of medicaments for the treatment and/or prophylaxis of disorders, in particular of prostate cancer.
摘要翻译：本发明涉及本文所述和定义的通式（I）的取代（杂芳基甲基）硫代乙内酰脲化合物及其制备方法，其用于治疗和/或预防疾病的用途及其用于制备药物的用途治疗和/或预防疾病，特别是前列腺癌。

2. 发明申请

US20120238533A1 (Heteroarylmethyl) Thiohydantoins as anticancer drugs 审中-公开
标题翻译：（杂芳基甲基）硫代乙内酰脲作为抗癌药物
公开(公告)号：US20120238533A1
公开(公告)日：2012-09-20
申请号：US13395087
申请日：2010-09-03
申请人： Arwed Cleve , Ulrich Lücking , Stefan Bäurle , Martin Fritsch , Jens Schröder , Bernd-Wolfgang Igl
发明人： Arwed Cleve , Ulrich Lücking , Stefan Bäurle , Martin Fritsch , Jens Schröder , Bernd-Wolfgang Igl
IPC分类号： A61K31/4166 , A61K31/4439 , A61K31/57 , A61K31/167 , A61K31/56 , A61K31/407 , A61P35/00 , A61K31/565 , A61K31/366 , A61K31/277 , A61K31/4704
CPC分类号： A61K31/275 , A61K31/4439
摘要： The invention refers to the use of androgen receptor antagonists for the treatment and/or prevention of fibroids, also known as uterine leiomyoma, leiomyomata. Particularly, the invention refers to the use of an androgen receptor antagonist being any one of the compounds according to the following list: cyproterone acetate, oxendolone, chlormadinone acetate, spironolactone, osaterone acetate, dienogest, flutamide, hydroxyflutamide, nilutamide, bicalutamide, RU 58841, LGD-2226, MDV3100, BMS-641988, BMS-779333, or 4-(3-{[6-(2-hydroxy-2-methylpropoxy)pyridin-3-yl]methyl}-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile (thioxoimidazolidine derivative) for the treatment of fibroids.
摘要翻译：本发明涉及雄激素受体拮抗剂用于治疗和/或预防子宫肌瘤，也称为子宫平滑肌瘤，平滑肌瘤的用途。特别地，本发明涉及使用根据以下列举的化合物中的任何一种的雄激素受体拮抗剂：醋酸环丙孕酮，羟考灵，乙酸氯地孕酮，螺内酯，醋酸奥托酮，依诺孕，氟他胺，羟基氟他胺，尼鲁替胺，比卡鲁胺，RU 58841 ，LGD-2226，MDV3100，BMS-641988，BMS-779333或4-（3 - {[6-（2-羟基-2-甲基丙氧基）吡啶-3-基]甲基} -4,4-二甲基-5 - 氧代-2-硫代咪唑烷-1-基）-2-（三氟甲基）苄腈（硫代咪唑烷衍生物）。

3. 发明授权

US08053426B2 Progesterone receptor antagonists 有权
标题翻译：孕激素受体拮抗剂
公开(公告)号：US08053426B2
公开(公告)日：2011-11-08
申请号：US11984331
申请日：2007-11-15
申请人： Ulrike Fuhrmann , Anja Schmidt , Arwed Cleve , Orlin Petrov , Gunnar Garke , Stefan Pruehs , Margarete Brudny-Kloeppel , Antje Rottmann , Rainer Hasselmann , Marcus Schultze-Mosgau , Carsten Moeller
发明人： Ulrike Fuhrmann , Anja Schmidt , Arwed Cleve , Orlin Petrov , Gunnar Garke , Stefan Pruehs , Margarete Brudny-Kloeppel , Antje Rottmann , Rainer Hasselmann , Marcus Schultze-Mosgau , Carsten Moeller
IPC分类号： A61K31/565 , C07J1/00
CPC分类号： C07J1/0081 , C07J21/006 , C07J51/00
摘要： The present invention relates to progesterone receptor antagonists of general formula I: in which R1 can be a hydrogen atom and R2 a hydroxyl group or R1 and R2 together can be an oxo group.
摘要翻译：本发明涉及通式I的孕酮受体拮抗剂：其中R 1可以是氢原子，R 2是羟基或R 1和R 2可以是氧代基。

4. 发明申请

US20100210630A1 Diamine Derivatives as Inhibitors of Leukotriene A4 Hydrolase 有权
标题翻译：二胺衍生物作为白三烯A4水解酶的抑制剂
公开(公告)号：US20100210630A1
公开(公告)日：2010-08-19
申请号：US12771659
申请日：2010-04-30
申请人： Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica J. Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Ping Wei , Bin Ye
发明人： Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica J. Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Ping Wei , Bin Ye
IPC分类号： A61K31/551 , C07D487/08 , A61K31/504 , C07D243/08 , C07D263/32 , A61K31/421 , C07D211/58 , A61K31/4468 , C07D207/09 , A61K31/40 , C07D413/00 , A61K31/5377 , A61P29/00
CPC分类号： C07D487/08 , C07B2200/07 , C07C217/58 , C07C229/08 , C07C229/38 , C07C233/78 , C07C255/57 , C07C271/20 , C07C2601/14 , C07D207/04 , C07D207/09 , C07D207/16 , C07D211/26 , C07D211/34 , C07D211/58 , C07D243/08 , C07D263/14 , C07D263/32 , C07D277/22 , C07D277/68 , C07D295/04 , C07D295/096 , C07D295/16 , C07D401/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D451/02 , C07D451/04
摘要： This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
摘要翻译：本发明涉及式（I）化合物：其中r，q，R，R2，R3，R4，R5a，R5b，R5c，R6a，R6b，R6c，R7，R8和R9在本文中描述为单立体异构体或作为立体异构体或其药学上可接受的盐，溶剂合物，包合物，多晶型物，铵离子，N-氧化物或前药的混合物; 其是白三烯A4水解酶抑制剂，因此可用于治疗炎症性疾病。还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。

5. 发明授权

US6096732A Steroid esters, process for their production and their pharmaceutical use 失效
标题翻译：类固醇酯，其生产过程及其药物用途
公开(公告)号：US6096732A
公开(公告)日：2000-08-01
申请号：US986592
申请日：1997-12-08
申请人： Ulrich Klar , Arwed Cleve , Wolfgang Schwede , Gunter Neef , Eckhard Ottow , Kristof Chwalisz , Martin Schneider
发明人： Ulrich Klar , Arwed Cleve , Wolfgang Schwede , Gunter Neef , Eckhard Ottow , Kristof Chwalisz , Martin Schneider
IPC分类号： A61K31/565 , A61P35/00 , C07J53/00 , A61K31/56
CPC分类号： C07J53/002 , Y10S514/843
摘要： Steroid esters of formula I ##STR1## are described, wherein m, n and x are as defined by the specification. The compounds are distinguished from the basic hydroxy compounds by considerably improved solubility as well by increased biological activity and selectivity.The compounds are suitable for the production of pharmaceutical agents.
摘要翻译：描述式I的类固醇酯，其中m，n和x如本说明书所定义。通过显着改善溶解度以及增加的生物活性和选择性，化合物与碱性羟基化合物的区别。该化合物适用于生产药剂。

6. 发明授权

US07951790B2 Progesterone receptor antagonists 有权
公开(公告)号：US07951790B2
公开(公告)日：2011-05-31
申请号：US11984331
申请日：2007-11-15
申请人： Ulrike Fuhrmann , Anja Schmidt , Arwed Cleve , Orlin Petrov , Gunnar Garke , Stefan Pruehs , Margarete Brudny-Kloeppel , Antje Rottmann , Rainer Hasselmann , Marcus Schultze-Mosgau , Carsten Moeller
发明人： Ulrike Fuhrmann , Anja Schmidt , Arwed Cleve , Orlin Petrov , Gunnar Garke , Stefan Pruehs , Margarete Brudny-Kloeppel , Antje Rottmann , Rainer Hasselmann , Marcus Schultze-Mosgau , Carsten Moeller
IPC分类号： A61K31/565 , C07J1/00
摘要： The present invention relates to progesterone receptor antagonists of general formula I: in which R1 can be a hydrogen atom and R2 a hydroxyl group or R1 and R2 together can be an oxo group.

7. 发明授权

US07910573B2 Crystalline forms of 11β-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one 失效
标题翻译： 11β-（4-乙酰基苯基）-20,20,21,21,21-五氟-17-羟基-19-去甲-17α-孕甾-4,9-二烯-3-酮的结晶形式
公开(公告)号：US07910573B2
公开(公告)日：2011-03-22
申请号：US11757118
申请日：2007-06-01
申请人： Wolfgang Beckmann , Gabriele Winter , Edda Kraemer , Thomas Ginko , Evelin Amoulong , Arwed Cleve
发明人： Wolfgang Beckmann , Gabriele Winter , Edda Kraemer , Thomas Ginko , Evelin Amoulong , Arwed Cleve
IPC分类号： A01N29/12 , A61K31/03 , C07C49/00
CPC分类号： C07J1/0081
摘要： The present invention relates to crystalline forms of 11β-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one. The invention relates in particular to two crystalline ansolvate/anhydrate forms of this compound, polymorphs I and II. However, the present invention also relates to crystalline solvates, for example methanol and ethanol solvates of 11β-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one as precursors for preparing these two polymorphs I and II. Processes for preparing polymorph I by displacement crystallization or by trituration are described. Selection of the last solvent before formation of the ansolvate can be based on the differences in the purification behaviour of the individual solvates of 11β-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one. Polymorph I according to the invention is particularly suitable for the manufacture of medicinal products.
摘要翻译：本发明涉及11β-（4-乙酰基苯基）-20,20,21,21,21-五氟-17-羟基-19-去甲-17α-孕甾-4,9-二烯-3-酮的结晶形式。本发明特别涉及这种化合物的两种结晶固体/无水物形式，即多晶型物I和II。然而，本发明还涉及结晶溶剂合物，例如11β-（4-乙酰基苯基）-20,20,21,21,21-五氟-17-羟基-19-去甲基-17α-前体的甲醇和乙醇溶剂合物 -4,9-二烯-3-酮作为制备这两种多晶型I和II的前体。描述了通过置换结晶或研磨制备多晶型I的方法。在形成溶剂化物之前，最后一种溶剂的选择可以基于11＆bgr-（4-乙酰基苯基）-20,20,21,21,21-五氟-17-羟基 - 19-nor-17α-前 - 4,9-二烯-3-酮。根据本发明的多晶型I特别适用于制造药用产品。

8. 发明授权

US07902178B2 Progesterone receptor antagonists 有权
公开(公告)号：US07902178B2
公开(公告)日：2011-03-08
申请号：US11984331
申请日：2007-11-15
申请人： Ulrike Fuhrmann , Anja Schmidt , Arwed Cleve , Orlin Petrov , Gunnar Garke , Stefan Pruehs , Margarete Brudny-Kloeppel , Antje Rottmann , Rainer Hasselmann , Marcus Schultze-Mosgau , Carsten Moeller
发明人： Ulrike Fuhrmann , Anja Schmidt , Arwed Cleve , Orlin Petrov , Gunnar Garke , Stefan Pruehs , Margarete Brudny-Kloeppel , Antje Rottmann , Rainer Hasselmann , Marcus Schultze-Mosgau , Carsten Moeller
IPC分类号： A61K31/565 , C07J1/00
摘要： The present invention relates to progesterone receptor antagonists of general formula I: in which R1 can be a hydrogen atom and R2 a hydroxyl group or R1 and R2 together can be an oxo group.

9. 发明授权

US07737145B2 Diamine derivatives as inhibitors of leukotriene A4 hydrolase 有权
标题翻译：二胺衍生物作为白三烯A4水解酶的抑制剂
公开(公告)号：US07737145B2
公开(公告)日：2010-06-15
申请号：US11644244
申请日：2006-12-22
申请人： Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica J. Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Ping Wei , Bin Ye
发明人： Damian Arnaiz , Greg Brown , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica J. Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Ping Wei , Bin Ye
IPC分类号： A01N43/60 , A61K31/495 , C07D241/36 , C07D271/00 , C07D487/00 , C07D491/00 , C07D495/00 , C07D497/00 , C07D498/00 , C07D513/00
CPC分类号： C07D487/08 , C07B2200/07 , C07C217/58 , C07C229/08 , C07C229/38 , C07C233/78 , C07C255/57 , C07C271/20 , C07C2601/14 , C07D207/04 , C07D207/09 , C07D207/16 , C07D211/26 , C07D211/34 , C07D211/58 , C07D243/08 , C07D263/14 , C07D263/32 , C07D277/22 , C07D277/68 , C07D295/04 , C07D295/096 , C07D295/16 , C07D401/10 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D451/02 , C07D451/04
摘要： This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
摘要翻译：本发明涉及式（I）化合物：其中r，q，R，R2，R3，R4，R5a，R5b，R5c，R6a，R6b，R6c，R7，R8和R9在本文中描述为单立体异构体或作为立体异构体或其药学上可接受的盐，溶剂合物，包合物，多晶型物，铵离子，N-氧化物或前药的混合物; 其是白三烯A4水解酶抑制剂，因此可用于治疗炎症性疾病。还公开了包含本发明化合物的药物组合物和制备本发明化合物的方法。

10. 发明申请

US20070155727A1 Amide inhibitors of leukotriene A4 hydrolase 审中-公开
标题翻译：白三烯A4水解酶的酰胺抑制剂
公开(公告)号：US20070155727A1
公开(公告)日：2007-07-05
申请号：US11644822
申请日：2006-12-22
申请人： Ming Chen , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Wei , Bin Ye , Hong Ye
发明人： Ming Chen , Emmanuel Claret , Arwed Cleve , David Davey , William Guilford , Seock-Kyu Khim , Thomas Kirkland , Monica Kochanny , Amy Liang , David Light , John Parkinson , David Vogel , Guo Wei , Bin Ye , Hong Ye
IPC分类号： A61K31/551 , A61K31/407 , C07D487/02 , C07D243/08
CPC分类号： C07D207/04 , C07C237/04 , C07C237/06 , C07C237/30 , C07C255/58 , C07C275/40 , C07C275/42 , C07C275/62 , C07C311/05 , C07C311/08 , C07C311/09 , C07C311/37 , C07C2601/08 , C07C2601/14 , C07D211/06 , C07D243/08 , C07D295/04 , C07D295/16 , C07D487/02 , C07D487/08
摘要： This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4a, R4b, R4c, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, R9 and R10 are described herein, or pharmaceutically acceptable salts, solvates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and which are therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of using and preparing the compounds of the invention are also disclosed.
摘要翻译：本发明涉及式（I）化合物：其中r，q，R，R 2，R 3，R 4a，R 4， R 4b，R 4c，R 5a，R 5b，R 5c，R 5，R 5， R 6b，R 6b，R 6，R 7，R 8，R 8，R 8，本文描述了本发明的其它药学上可接受的盐，溶剂合物，多晶型物，铵离子，N-氧化物或前体药物; 其是白三烯A 4水解酶抑制剂，因此其可用于治疗炎症性疾病。还公开了包含本发明化合物的药物组合物和使用和制备本发明化合物的方法。

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