公开(公告)号：US07176211B2

公开(公告)日：2007-02-13

申请号：US11251085

申请日：2005-10-14

申请人： Zhiqiang Guo ,  Yongsheng Chen ,  Dongpei Wu ,  Chen Chen ,  Warren Wade ,  Wesley J. Dwight ,  Charles Q. Huang ,  Fabio C. Tucci

发明人： Zhiqiang Guo ,  Yongsheng Chen ,  Dongpei Wu ,  Chen Chen ,  Warren Wade ,  Wesley J. Dwight ,  Charles Q. Huang ,  Fabio C. Tucci

IPC分类号： A61K31/513 ,  C07D239/54

CPC分类号： C07D239/54 ,  C07D239/52 ,  C07D403/12 ,  C07D405/04

摘要： GnRH receptor antagonists are disclosed that 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, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs 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： 公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。 本发明的化合物具有以下结构：其中R 1a，R 1b，R 1c，R 2a， R 2b，R 3，R 4，R 5，R 6和R 6，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：US07056927B2

公开(公告)日：2006-06-06

申请号：US10885491

申请日：2004-07-06

申请人： Zhiqiang Guo ,  Yongsheng Chen ,  Dongpei Wu ,  Chen Chen ,  Warren Wade ,  Wesley J. Dwight ,  Charles Q. Huang ,  Fabio C. Tucci

发明人： Zhiqiang Guo ,  Yongsheng Chen ,  Dongpei Wu ,  Chen Chen ,  Warren Wade ,  Wesley J. Dwight ,  Charles Q. Huang ,  Fabio C. Tucci

IPC分类号： C07D239/54 ,  A61K31/513

CPC分类号： C07D239/54 ,  C07D239/52 ,  C07D403/12 ,  C07D405/04

摘要： GnRH receptor antagonists are disclosed that 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, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs 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： 公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。 本发明的化合物具有以下结构：其中R 1a，R 1b，R 1c，R 2a， R 2b，R 3，R 4，R 5，R 6和R 6，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：US07419983B2

公开(公告)日：2008-09-02

申请号：US11627204

申请日：2007-01-25

申请人： Zhiqiang Guo ,  Yongsheng Chen ,  Dongpei Wu ,  Chen Chen ,  Warren Wade ,  Wesley J. Dwight ,  Charles Q. Huang ,  Fabio C. Tucci

发明人： Zhiqiang Guo ,  Yongsheng Chen ,  Dongpei Wu ,  Chen Chen ,  Warren Wade ,  Wesley J. Dwight ,  Charles Q. Huang ,  Fabio C. Tucci

IPC分类号： C07D239/54 ,  A61K31/513

CPC分类号： C07D239/54 ,  C07D239/52 ,  C07D403/12 ,  C07D405/04

摘要： GnRH receptor antagonists are disclosed that 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, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs 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： 公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。 本发明的化合物具有以下结构：其中R 1a，R 1b，R 1c，R 2a， R 2b，R 3，R 4，R 5，R 6和R 6，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：US20060122202A1

公开(公告)日：2006-06-08

申请号：US11251085

申请日：2005-10-14

申请人： Zhiqiang Guo ,  Yongsheng Chen ,  Dongpei Wu ,  Chen Chen ,  Warren Wade ,  Wesley Dwight ,  Charles Huang ,  Fabio Tucci

发明人： Zhiqiang Guo ,  Yongsheng Chen ,  Dongpei Wu ,  Chen Chen ,  Warren Wade ,  Wesley Dwight ,  Charles Huang ,  Fabio Tucci

IPC分类号： A61K31/513

CPC分类号： C07D239/54 ,  C07D239/52 ,  C07D403/12 ,  C07D405/04

摘要： GnRH receptor antagonists are disclosed that 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, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs 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：US20050038057A1

公开(公告)日：2005-02-17

申请号：US10885491

申请日：2004-07-06

申请人： Zhiqiang Guo ,  Yongsheng Chen ,  Dongpei Wu ,  Chen Chen ,  Warren Wade ,  Wesley Dwight ,  Charles Huang ,  Fabio Tucci

发明人： Zhiqiang Guo ,  Yongsheng Chen ,  Dongpei Wu ,  Chen Chen ,  Warren Wade ,  Wesley Dwight ,  Charles Huang ,  Fabio Tucci

IPC分类号： A61K31/513 ,  A61P5/02 ,  C07D239/54 ,  C07D403/12 ,  C07D405/04 ,  C07D45/02

CPC分类号： C07D239/54 ,  C07D239/52 ,  C07D403/12 ,  C07D405/04

摘要： GnRH receptor antagonists are disclosed that 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, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs 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： 公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。 本发明的化合物具有以下结构：其中R1a，R1b，R1c，R2a，R2b，R3，R4，R5，R6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：US20070191403A1

公开(公告)日：2007-08-16

申请号：US11627204

申请日：2007-01-25

申请人： Zhiqiang Guo ,  Yongsheng Chen ,  Dongpei Wu ,  Chen Chen ,  Warren Wade ,  Wesley Dwight ,  Charles Huang ,  Fabio Tucci

发明人： Zhiqiang Guo ,  Yongsheng Chen ,  Dongpei Wu ,  Chen Chen ,  Warren Wade ,  Wesley Dwight ,  Charles Huang ,  Fabio Tucci

IPC分类号： A61K31/513 ,  C07D239/52

CPC分类号： C07D239/54 ,  C07D239/52 ,  C07D403/12 ,  C07D405/04

摘要： GnRH receptor antagonists are disclosed that 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, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs 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： 公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。 本发明的化合物具有以下结构：其中R 1a，R 1b，R 1c，R 2a， R 2b，R 3，R 4，R 5，R 6和R 6，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：US07229995B2

公开(公告)日：2007-06-12

申请号：US11264702

申请日：2005-11-01

申请人： Charles Q. Huang ,  Chen Chen ,  Yongsheng Chen ,  Zhiqiang Guo ,  Warren Wade ,  Martin Rowbottom ,  Jaimie K. Rueter

发明人： Charles Q. Huang ,  Chen Chen ,  Yongsheng Chen ,  Zhiqiang Guo ,  Warren Wade ,  Martin Rowbottom ,  Jaimie K. Rueter

IPC分类号： C07D239/54 ,  A61K31/513

CPC分类号： C07D239/54 ,  C07D403/12

摘要： GnRH receptor antagonists are disclosed that 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 n, R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs 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： 公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。 本发明的化合物具有如下结构：其中n，R 1a，R 1b，R 1c，R 2a， R 2，R 3，R 3，R 4，R 5，R 6， >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：US07015226B2

公开(公告)日：2006-03-21

申请号：US10885490

申请日：2004-07-06

申请人： Charles Q. Huang ,  Chen Chen ,  Yongsheng Chen ,  Zhiqiang Guo ,  Warren Wade ,  Martin Rowbottom ,  Jaimie K. Rueter

发明人： Charles Q. Huang ,  Chen Chen ,  Yongsheng Chen ,  Zhiqiang Guo ,  Warren Wade ,  Martin Rowbottom ,  Jaimie K. Rueter

IPC分类号： C07D239/54 ,  A61K31/513

CPC分类号： C07D239/54 ,  C07D403/12

摘要： GnRH receptor antagonists are disclosed that 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 n, R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs 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：US20060122204A1

公开(公告)日：2006-06-08

申请号：US11264702

申请日：2005-11-01

申请人： Charles Huang ,  Chen Chen ,  Yongsheng Chen ,  Zhiqiang Guo ,  Warren Wade ,  Martin Rowbottom ,  Jaimie Rueter

发明人： Charles Huang ,  Chen Chen ,  Yongsheng Chen ,  Zhiqiang Guo ,  Warren Wade ,  Martin Rowbottom ,  Jaimie Rueter

IPC分类号： A61K31/513

CPC分类号： C07D239/54 ,  C07D403/12

摘要： GnRH receptor antagonists are disclosed that 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 n, R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs 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： 公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。 本发明的化合物具有以下结构：其中n，R 1a，R 1b，R 1c，R 2a， R 2，R 3，R 3，R 4，R 5，R 6， >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：US20050038056A1

公开(公告)日：2005-02-17

申请号：US10885490

申请日：2004-07-06

申请人： Charles Huang ,  Chen Chen ,  Yongsheng Chen ,  Zhiqiang Guo ,  Warren Wade ,  Martin Rowbottom ,  Jaimie Rueter

发明人： Charles Huang ,  Chen Chen ,  Yongsheng Chen ,  Zhiqiang Guo ,  Warren Wade ,  Martin Rowbottom ,  Jaimie Rueter

IPC分类号： A61P5/06 ,  C07D239/54 ,  C07D403/12 ,  A61K31/513 ,  C07D45/02

CPC分类号： C07D239/54 ,  C07D403/12

摘要： GnRH receptor antagonists are disclosed that 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 n, R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs 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： 公开了具有用于治疗男性和女性中各种性激素相关病症的GnRH受体拮抗剂。 本发明的化合物具有以下结构：其中n，R1a，R1b，R1c，R2a，R2b，R3，R4，R5，R6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。