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：US20050119252A1

公开(公告)日：2005-06-02

申请号：US10971732

申请日：2004-10-22

申请人： Fabio Tucci ,  Joe Tran ,  Wei-Chuan Chen ,  Wanlong Jiang ,  Chen Chen

发明人： Fabio Tucci ,  Joe Tran ,  Wei-Chuan Chen ,  Wanlong Jiang ,  Chen Chen

IPC分类号： A61K31/495 ,  A61K31/506 ,  A61K31/551 ,  C07D207/26 ,  C07D207/27 ,  C07D213/75 ,  C07D241/04 ,  C07D295/185 ,  C07D295/215 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D43/14

CPC分类号： C07D295/185 ,  C07D207/27 ,  C07D213/75 ,  C07D295/215 ,  C07D401/04

摘要： Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders. The compounds have the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein m, n, q, s, R1, R1a, R1b, R2, R3, R4a, R4b, R5a, R5b, X1, X2, X3, X4 and Ar are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.

摘要翻译： 作为黑皮质素受体配体起作用并可用于治疗基于黑皮质素受体的疾病的化合物。 所述化合物具有以下结构（I）：包括其立体异构体，前药和药学上可接受的盐，其中m，n，q，s，R 1，R 1a， R 1b，R 2，R 3，R 4a，R 4b， R 5a，R 5b，X 1，X 2，X 3， X 4和Ar如本文所定义。 还公开了含有结构（I）化合物的药物组合物以及与其用途有关的方法。

公开(公告)号：US20050192286A1

公开(公告)日：2005-09-01

申请号：US10972064

申请日：2004-10-22

申请人： Joe Tran ,  Fabio Tucci ,  Wanlong Jiang ,  Wei-Chuan Chen ,  Dragan Marinkovic ,  Melissa Arellano ,  Nicole White ,  Chen Chen

发明人： Joe Tran ,  Fabio Tucci ,  Wanlong Jiang ,  Wei-Chuan Chen ,  Dragan Marinkovic ,  Melissa Arellano ,  Nicole White ,  Chen Chen

IPC分类号： A61K31/496 ,  C07D207/16 ,  C07D207/26 ,  C07D207/277 ,  C07D263/24 ,  C07D277/14 ,  C07D295/185 ,  C07D307/24 ,  C07D307/33 ,  C07D317/32 ,  C07D333/38 ,  C07D333/48 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D43/02

CPC分类号： C04B35/632 ,  C07D207/16 ,  C07D207/277 ,  C07D263/24 ,  C07D295/185 ,  C07D307/24 ,  C07D307/33 ,  C07D317/32 ,  C07D333/38 ,  C07D333/48 ,  C07D401/12 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

摘要： Compounds which function as melanocortin receptor ligands and having utility in the treatment of melanocortin receptor-based disorders. The compounds have the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts thereof, wherein m, n, q, s, R1, R1a, R1b, R2, R3, R4, X1, X2 and X3 are as defined herein. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.

摘要翻译： 作为黑皮质素受体配体起作用并可用于治疗基于黑皮质素受体的疾病的化合物。 所述化合物具有以下结构（I）：包括立体异构体，前药和其药学上可接受的盐，其中m，n，q，s，R 1，R 1 a R 1b，R 2，R 3，R 4，X 1， X 2和X 3如本文所定义。 还公开了含有结构（I）化合物的药物组合物以及与其用途有关的方法。