公开(公告)号：US08507536B2

公开(公告)日：2013-08-13

申请号：US13572510

申请日：2012-08-10

申请人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Jinghua Yu ,  Willy Moree ,  Warren Wade ,  Liren Zhao ,  Yun-fei Zhu ,  Martin Rowbottom ,  Neil Ashweek

发明人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Jinghua Yu ,  Willy Moree ,  Warren Wade ,  Liren Zhao ,  Yun-fei Zhu ,  Martin Rowbottom ,  Neil Ashweek

IPC分类号： C07D211/06 ,  C07D213/78 ,  C07D211/70 ,  A61K31/44 ,  A61P25/00

CPC分类号： C07D213/61 ,  C07D213/84 ,  C07D239/36 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

摘要： GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

摘要翻译： 公开了GnRH受体拮抗剂，其可用于治疗男性和女性中各种性激素相关病症。 本发明的化合物具有以下结构：其中R1a，R1b，R1c，R1d，R2，R2a和A如本文所定义，包括立体异构体，酯，溶剂化物和药学上可接受的盐。 还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

公开(公告)号：US20130040975A1

公开(公告)日：2013-02-14

申请号：US13572510

申请日：2012-08-10

申请人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Jinghua Yu ,  Willy Moree ,  Warren Wade ,  Liren Zhao ,  Yun-fei Zhu ,  Martin Rowbottom ,  Neil Ashweek

发明人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Jinghua Yu ,  Willy Moree ,  Warren Wade ,  Liren Zhao ,  Yun-fei Zhu ,  Martin Rowbottom ,  Neil Ashweek

IPC分类号： C07D213/61 ,  C07D239/36 ,  A61K31/513 ,  C07D213/84 ,  A61K31/444 ,  C07D405/12 ,  A61K31/443 ,  C07C311/15 ,  C07D215/14 ,  C07D495/04 ,  A61P5/24 ,  A61P15/00 ,  A61P17/00 ,  A61P35/00 ,  A61P13/08 ,  A61P15/08 ,  A61K31/4418

CPC分类号： C07D213/61 ,  C07D213/84 ,  C07D239/36 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

摘要： GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

摘要翻译： 公开了GnRH受体拮抗剂，其可用于治疗男性和女性中各种性激素相关病症。 本发明的化合物具有以下结构：其中R1a，R1b，R1c，R1d，R2，R2a和A如本文所定义，包括立体异构体，酯，溶剂化物和药学上可接受的盐。 还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

公开(公告)号：US08263588B2

公开(公告)日：2012-09-11

申请号：US12594815

申请日：2008-04-04

申请人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Jinghua Yu ,  Willy Moree ,  Warren Wade ,  Liren Zhao ,  Yun-fei Zhu ,  Martin Rowbottom ,  Neil Ashweek

发明人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Jinghua Yu ,  Willy Moree ,  Warren Wade ,  Liren Zhao ,  Yun-fei Zhu ,  Martin Rowbottom ,  Neil Ashweek

IPC分类号： C07D213/61 ,  C07D213/84 ,  C07D401/12 ,  C07D403/12 ,  A61K31/435 ,  A61P35/00

CPC分类号： C07D213/61 ,  C07D213/84 ,  C07D239/36 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

摘要： GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

摘要翻译： 公开了GnRH受体拮抗剂，其可用于治疗男性和女性中各种性激素相关病症。 本发明的化合物具有以下结构：其中R1a，R1b，R1c，R1d，R2，R2a和A如本文所定义，包括立体异构体，酯，溶剂化物和药学上可接受的盐。 还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

公开(公告)号：US20100184741A1

公开(公告)日：2010-07-22

申请号：US12594815

申请日：2008-04-04

申请人： Neil Ashweek ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Willy Moree ,  Martin Rowbottom ,  Warren Wade ,  Liren Zhao ,  Yun-fei Zhu ,  Jinghua Yu ,  Graham Beaton

发明人： Neil Ashweek ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Willy Moree ,  Martin Rowbottom ,  Warren Wade ,  Liren Zhao ,  Yun-fei Zhu ,  Jinghua Yu ,  Graham Beaton

IPC分类号： C07D213/84 ,  A61K31/444 ,  C07D215/12 ,  C07D403/12 ,  A61K31/44 ,  A61K31/55 ,  C07D223/16 ,  A61K31/47 ,  A61P35/04 ,  A61P15/00

CPC分类号： C07D213/61 ,  C07D213/84 ,  C07D239/36 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

摘要： GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

摘要翻译： 公开了GnRH受体拮抗剂，其可用于治疗男性和女性中各种性激素相关病症。 本发明的化合物具有以下结构：其中R1a，R1b，R1c，R1d，R2，R2a和A如本文所定义，包括立体异构体，酯，溶剂化物和药学上可接受的盐。 还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

公开(公告)号：US20120122891A1

公开(公告)日：2012-05-17

申请号：US13293943

申请日：2011-11-10

申请人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Richard Lowe ,  Willy Moree ,  Nicole Smith ,  Warren Wade ,  Liren Zhao ,  Yun-Fei Zhu ,  Martin Rowbottom ,  Neil Ashweek

发明人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Richard Lowe ,  Willy Moree ,  Nicole Smith ,  Warren Wade ,  Liren Zhao ,  Yun-Fei Zhu ,  Martin Rowbottom ,  Neil Ashweek

IPC分类号： A61K31/519 ,  C07D471/04 ,  C07D495/04 ,  A61K31/513 ,  A61K31/4375 ,  A61P13/02 ,  A61P5/08 ,  A61P17/00 ,  A61P15/08 ,  A61P1/00 ,  A61P35/00 ,  C07D239/36 ,  A61P15/00

CPC分类号： C07D495/04 ,  C07C233/88 ,  C07C235/42 ,  C07C255/57 ,  C07D213/56 ,  C07D213/58 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D215/14 ,  C07D215/54 ,  C07D239/36 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

摘要： GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

摘要翻译： 公开了GnRH受体拮抗剂，其可用于治疗男性和女性中各种性激素相关病症。 本发明的化合物具有以下结构：其中R1a，R1b，R1c，R1d，R2，R2a和A如本文所定义，包括其立体异构体，酯，溶剂化物和药学上可接受的盐。 还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

公开(公告)号：US08084614B2

公开(公告)日：2011-12-27

申请号：US12594809

申请日：2008-04-04

申请人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Richard Lowe ,  Willy Moree ,  Nicole Smith ,  Warren Wade ,  Liren Zhao ,  Yun-fei Zhu ,  Martin Rowbottom ,  Neil Ashweek

发明人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Richard Lowe ,  Willy Moree ,  Nicole Smith ,  Warren Wade ,  Liren Zhao ,  Yun-fei Zhu ,  Martin Rowbottom ,  Neil Ashweek

IPC分类号： C07D213/00 ,  C07D211/70 ,  C07D233/00 ,  A61K31/44

CPC分类号： C07D495/04 ,  C07C233/88 ,  C07C235/42 ,  C07C255/57 ,  C07D213/56 ,  C07D213/58 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D215/14 ,  C07D215/54 ,  C07D239/36 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

摘要： GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

摘要翻译： 公开了GnRH受体拮抗剂，其可用于治疗男性和女性中各种性激素相关病症。 本发明的化合物具有以下结构，其中R1a，R1b，R1c，R1d，R2，R2a和A如本文所定义，包括其立体异构体，酯，溶剂合物及其药学上可接受的盐。 还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

公开(公告)号：US20100152207A1

公开(公告)日：2010-06-17

申请号：US12594809

申请日：2008-04-04

申请人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Willy Moree ,  Martin Rowbottom ,  Warren Wade ,  Liren Zhao ,  Richard Lowe ,  Nicole Smith ,  Neil Ashweek ,  Yun-Fei Zhu

发明人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Willy Moree ,  Martin Rowbottom ,  Warren Wade ,  Liren Zhao ,  Richard Lowe ,  Nicole Smith ,  Neil Ashweek ,  Yun-Fei Zhu

IPC分类号： A61K31/519 ,  C07D213/56 ,  A61K31/4418 ,  C07D215/38 ,  A61K31/47 ,  C07D495/04 ,  C07C233/67 ,  A61K31/165 ,  C07D213/84 ,  A61K31/44 ,  C07D401/04 ,  A61K31/4439 ,  C07D213/62 ,  C07D239/02 ,  A61K31/505 ,  C07D401/12 ,  C07D413/12 ,  C07D403/02 ,  A61K31/444 ,  A61P15/00

CPC分类号： C07D495/04 ,  C07C233/88 ,  C07C235/42 ,  C07C255/57 ,  C07D213/56 ,  C07D213/58 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D215/14 ,  C07D215/54 ,  C07D239/36 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

摘要： GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure, wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

摘要翻译： 公开了GnRH受体拮抗剂，其可用于治疗男性和女性中各种性激素相关病症。 本发明的化合物具有以下结构，其中R1a，R1b，R1c，R1d，R2，R2a和A如本文所定义，包括其立体异构体，酯，溶剂合物及其药学上可接受的盐。 还公开了含有本发明化合物与药学上可接受的载体组合的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

公开(公告)号：US08481738B2

公开(公告)日：2013-07-09

申请号：US13293943

申请日：2011-11-10

申请人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Richard Lowe ,  Willy Moree ,  Nicole Smith ,  Warren Wade ,  Liren Zhao ,  Yun-fei Zhu ,  Martin Rowbottom ,  Neil Ashweek

发明人： Graham Beaton ,  Mi Chen ,  Timothy Richard Coon ,  Todd Ewing ,  Wanlong Jiang ,  Richard Lowe ,  Willy Moree ,  Nicole Smith ,  Warren Wade ,  Liren Zhao ,  Yun-fei Zhu ,  Martin Rowbottom ,  Neil Ashweek

IPC分类号： C07D513/02 ,  C07D401/00

CPC分类号： C07D495/04 ,  C07C233/88 ,  C07C235/42 ,  C07C255/57 ,  C07D213/56 ,  C07D213/58 ,  C07D213/61 ,  C07D213/64 ,  C07D213/70 ,  C07D213/81 ,  C07D213/84 ,  C07D213/89 ,  C07D215/14 ,  C07D215/54 ,  C07D239/36 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

摘要： GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

公开(公告)号：US20080262005A1

公开(公告)日：2008-10-23

申请号：US11568961

申请日：2005-05-13

申请人： Yun-Fei Zhu ,  Zhiqiang Gou ,  Mi Chen ,  Liren Zhao

发明人： Yun-Fei Zhu ,  Zhiqiang Gou ,  Mi Chen ,  Liren Zhao

IPC分类号： A61K31/513 ,  C07D239/54 ,  A61P5/00 ,  A61P43/00 ,  A61P15/18

CPC分类号： C07D239/54 ,  C07D403/12

摘要： Compounds having utility as GnRH receptor antagonists and for treatment of a variety of sex-hormone related conditions in both men and women. Such compounds have the following structure (I): (I) wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6, R7, n and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of structure (I) in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

摘要翻译： 具有用作GnRH受体拮抗剂并用于治疗男性和女性中各种性激素相关病症的化合物。 这样的化合物具有以下结构（I）：（I）其中R 1a 1a，R 1b，R 1c，R 2a， R 1，R 2，R 3，R 4，R 5，R 6， R 3，R 7，n和X如本文所定义，包括其立体异构体，前药和药学上可接受的盐。 还公开了含有结构（I）的化合物与药学上可接受的载体的组合物的组合物，以及涉及其在有需要的受试者中拮抗促性腺激素释放激素的方法。

公开(公告)号：US20050256124A1

公开(公告)日：2005-11-17

申请号：US11107317

申请日：2005-04-15

申请人： Val Goodfellow ,  Brian Dyck ,  Liren Zhao ,  Junko Tamiya ,  Jonathan Grey ,  Warren Wade ,  Martin Rowbottom ,  Mingzhu Zhang ,  Troy Vickers

发明人： Val Goodfellow ,  Brian Dyck ,  Liren Zhao ,  Junko Tamiya ,  Jonathan Grey ,  Warren Wade ,  Martin Rowbottom ,  Mingzhu Zhang ,  Troy Vickers

IPC分类号： A61K31/4427 ,  A61K31/4439 ,  A61K31/4745 ,  A61K31/501 ,  A61K31/503 ,  A61K31/519 ,  C07D401/10 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D498/02 ,  C07D41/14 ,  C07D49/14

CPC分类号： C07D401/10 ,  C07D401/14 ,  C07D405/14 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04

摘要： Melanin-concentrating hormone (MCH) receptor antagonists are disclosed having utility for the treatment of MCH receptor-based disorders such as obesity. The compounds of this invention have the following structure: including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein R1, R2, R5, Het, X and Cyc are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.

摘要翻译： 公开了用于治疗基于MCH受体的疾病如肥胖症的黑色素浓缩激素（MCH）受体拮抗剂。 本发明的化合物具有以下结构：包括立体异构体，前药和药学上可接受的盐，其中R 1，R 2，R 5， >，Het，X和Cyc如本文所定义。 还公开了含有本发明化合物的组合物以及与其用途有关的方法。