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：US20050234082A1

公开(公告)日：2005-10-20

申请号：US11016551

申请日：2004-12-17

申请人： Yun-Fei Zhu ,  Chen Chen ,  Fabio Tucci ,  Zhiqiang Guo ,  Timothy Gross ,  Martin Rowbottom ,  R. Struthers

发明人： Yun-Fei Zhu ,  Chen Chen ,  Fabio Tucci ,  Zhiqiang Guo ,  Timothy Gross ,  Martin Rowbottom ,  R. Struthers

IPC分类号： C07D239/52 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P1/04 ,  A61P5/24 ,  A61P13/08 ,  A61P15/00 ,  A61P15/18 ,  A61P25/20 ,  A61P35/00 ,  A61P37/06 ,  C07D239/54 ,  C07D239/553 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/18 ,  C07D513/04

CPC分类号： C07D239/54 ,  A61K31/513 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/08 ,  C07D513/04

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 A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n 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A，Q，R 1，R 2，R 3a，R 3b， R 4，R 5，R 6和n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：US20070208049A1

公开(公告)日：2007-09-06

申请号：US11520022

申请日：2006-09-11

申请人： Yun-Fei Zhu ,  Chen Chen ,  Fabio Tucci ,  Zhiqiang Guo ,  Timothy Gross ,  Martin Rowbottom ,  R. Struthers

发明人： Yun-Fei Zhu ,  Chen Chen ,  Fabio Tucci ,  Zhiqiang Guo ,  Timothy Gross ,  Martin Rowbottom ,  R. Struthers

IPC分类号： A61K31/513 ,  C07D239/06 ,  C07D239/10

CPC分类号： C07D239/54 ,  A61K31/513 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08 ,  C07D498/08 ,  C07D513/04

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 A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n 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A，Q，R 1，R 2，R 3a，R 3b， R 4，R 5，R 6和n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：US20050272733A1

公开(公告)日：2005-12-08

申请号：US11122246

申请日：2005-05-04

申请人： Chen Chen ,  Dongpei Wu ,  Zhiqiang Guo ,  Martin Rowbottom

发明人： Chen Chen ,  Dongpei Wu ,  Zhiqiang Guo ,  Martin Rowbottom

IPC分类号： A61K31/44 ,  A61K31/4418 ,  A61K31/50 ,  A61K31/501 ,  A61P1/04 ,  A61P5/04 ,  A61P5/24 ,  A61P13/08 ,  A61P15/00 ,  A61P15/08 ,  A61P25/20 ,  A61P35/00 ,  A61P37/02 ,  C07D213/64 ,  C07D401/12 ,  C07D41/02 ,  C07D43/02

CPC分类号： C07D213/64 ,  C07D401/12

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 A, R1, R2, R3a, R3b, R4, R5, R6, and n 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A 1，R 1，R 2，R 3a，R 3b， R 4，R 5，R 6和n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：US06750350B2

公开(公告)日：2004-06-15

申请号：US10211972

申请日：2002-08-02

申请人： Chen Chen ,  Dongpei Wu ,  Zhiqiang Guo ,  Martin Rowbottom

发明人： Chen Chen ,  Dongpei Wu ,  Zhiqiang Guo ,  Martin Rowbottom

IPC分类号： C07D21174

CPC分类号： C07D213/64 ,  C07D401/12

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 A, R1, R2, R3a, R3b, R4, R5, R6, and n 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：US07081459B2

公开(公告)日：2006-07-25

申请号：US11122246

申请日：2005-05-04

申请人： Chen Chen ,  Dongpei Wu ,  Zhiqiang Guo ,  Martin Rowbottom

发明人： Chen Chen ,  Dongpei Wu ,  Zhiqiang Guo ,  Martin Rowbottom

IPC分类号： C07D211/14 ,  C07D213/63 ,  C07D237/14 ,  A61K31/44 ,  A61P35/00

CPC分类号： C07D213/64 ,  C07D401/12

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 A, R1, R2, R3a, R3b, R4, R5, R6, and n 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A 1，R 1，R 2，R 3a，R 3b， R 4，R 5，R 6和n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：US06921761B2

公开(公告)日：2005-07-26

申请号：US10832092

申请日：2004-04-26

申请人： Chen Chen ,  Dongpei Wu ,  Zhiqiang Guo ,  Martin Rowbottom

发明人： Chen Chen ,  Dongpei Wu ,  Zhiqiang Guo ,  Martin Rowbottom

IPC分类号： A61K31/44 ,  A61K31/4418 ,  A61K31/50 ,  A61K31/501 ,  A61P1/04 ,  A61P5/04 ,  A61P5/24 ,  A61P13/08 ,  A61P15/00 ,  A61P15/08 ,  A61P25/20 ,  A61P35/00 ,  A61P37/02 ,  C07D213/64 ,  C07D401/12 ,  C07D237/14 ,  A61K31/51

CPC分类号： C07D213/64 ,  C07D401/12

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 A, R1, R2, R3a, R3b, R4, R5, R6, and n 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：US20070015778A1

公开(公告)日：2007-01-18

申请号：US11446583

申请日：2006-06-02

申请人： Yun-Fei Zhu ,  Collin Regan ,  Jaimie Rueter ,  Zhiqiang Guo ,  Yongsheng Chen ,  Charles Huang

发明人： Yun-Fei Zhu ,  Collin Regan ,  Jaimie Rueter ,  Zhiqiang Guo ,  Yongsheng Chen ,  Charles Huang

IPC分类号： A61K31/513 ,  C07D239/52

CPC分类号： C07D239/54 ,  C07D401/06

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, R2a, R2b, R3, R4, R5, R6, R7 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 2a，R 2b， R 3，R 4，R 5，R 6，R 7和R 7， 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：US20050043338A1

公开(公告)日：2005-02-24

申请号：US10885511

申请日：2004-07-06

申请人： Yun-Fei Zhu ,  Collin Regan ,  Jaimie Rueter ,  Zhiqiang Guo ,  Yongsheng Chen ,  Charles Huang

发明人： Yun-Fei Zhu ,  Collin Regan ,  Jaimie Rueter ,  Zhiqiang Guo ,  Yongsheng Chen ,  Charles Huang

IPC分类号： A61P5/02 ,  C07D239/54 ,  C07D401/06 ,  A61K31/513 ,  C07D43/02

CPC分类号： C07D239/54 ,  C07D401/06

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, R2a, R2b, R3, R4, R5, R6, R7 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，R2a，R2b，R3，R4，R5，R6，R7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：US06951858B2

公开(公告)日：2005-10-04

申请号：US10705762

申请日：2003-11-10

申请人： Joseph Pontillo ,  Zhiqiang Guo ,  Dongpei Wu

发明人： Joseph Pontillo ,  Zhiqiang Guo ,  Dongpei Wu

IPC分类号： C07D253/06 ,  A61K31/53 ,  A61P1/12 ,  A61P5/02 ,  A61P13/08 ,  A61P15/00 ,  A61P15/08 ,  A61P15/18 ,  A61P17/00 ,  A61P17/02 ,  A61P25/20 ,  A61P35/00 ,  A61P43/00 ,  C07D253/075 ,  C07D401/04 ,  C07D409/04 ,  A61P15/018

CPC分类号： C07D253/075 ,  C07D401/04 ,  C07D409/04

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 R1, R2, R3a, R3b, R4, R5, and n 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R 1，R 2，R 3，R 3，R 3， R 4，R 5和n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。