公开(公告)号：US07067509B2

公开(公告)日：2006-06-27

申请号：US10797487

申请日：2004-03-08

申请人： Val Goodfellow ,  Martin Rowbottom ,  Brian P Dyck ,  Junko Tamiya ,  Mingzhu Zhang ,  Jonathan Grey ,  Troy D Vickers ,  Mehrak Kiankarimi ,  Warren Wade ,  Sarah Clough ,  Joseph Pontillo ,  Dongpei Wu

发明人： Val Goodfellow ,  Martin Rowbottom ,  Brian P Dyck ,  Junko Tamiya ,  Mingzhu Zhang ,  Jonathan Grey ,  Troy D Vickers ,  Mehrak Kiankarimi ,  Warren Wade ,  Sarah Clough ,  Joseph Pontillo ,  Dongpei Wu

IPC分类号： A61K31/397 ,  A61K31/401 ,  A61K31/4025 ,  C07D207/14

CPC分类号： C07D207/14 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

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 and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R3, R4, R5, and R6 are as defined herein. Pharmaceutical compositions containing a compound of this invention, as well as methods relating to the use thereof, are also disclosed.

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：包括其立体异构体及其可药用盐，其中n，R 1，R 2，R 3， R 4，R 5和R 6如本文所定义。 还公开了含有本发明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：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。

公开(公告)号：US20060276454A1

公开(公告)日：2006-12-07

申请号：US11422843

申请日：2006-06-07

申请人： Joseph Pontillo ,  Yinghong Gao ,  Warren Wade ,  Dongpei Wu ,  Wendy Eccles

发明人： Joseph Pontillo ,  Yinghong Gao ,  Warren Wade ,  Dongpei Wu ,  Wendy Eccles

IPC分类号： A61K31/55 ,  A61K31/453 ,  A61K31/4025 ,  A61K31/382 ,  A61K31/353 ,  A61K31/277 ,  A61K31/137 ,  C07D409/02 ,  C07D405/02

CPC分类号： C07C215/42 ,  C07C217/74 ,  C07C323/32 ,  C07C2602/08 ,  C07D265/34 ,  C07D317/64 ,  C07D333/54

摘要： Monoamine re-uptake inhibitors and more specifically serotonin and noradrenaline re-uptake inhibitors are disclosed that have utility in the treatment of disorders of the central or peripheral nervous system in both men and women. The compounds of this invention have the structure: wherein R1, R2, R3, R4, R5, R6, m, n, W, X, Y, and Z are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts, esters and solvates 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 inhibiting monoamine re-uptake in a subject in need thereof.

摘要翻译： 公开了单胺再摄取抑制剂，更具体地说可用于治疗男性和女性中枢或周围神经系统疾病的5-羟色胺和去甲肾上腺素再摄取抑制剂。 本发明的化合物具有以下结构：其中R 1，R 2，R 3，R 4， R 5，R 6，m，n，W，X​​，Y和Z如本文所定义，包括立体异构体，前药和药学上可接受的盐，酯和溶剂合物 。 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抑制单胺再摄取的方法。

公开(公告)号：US20060252818A1

公开(公告)日：2006-11-09

申请号：US11429018

申请日：2006-05-05

申请人： Mehrak Kiankarimi ,  Sarah Hudson ,  Wesley Dwight ,  Warren Wade

发明人： Mehrak Kiankarimi ,  Sarah Hudson ,  Wesley Dwight ,  Warren Wade

IPC分类号： A61K31/382 ,  A61K31/353 ,  C07D335/06

CPC分类号： C07D335/06 ,  C07D307/83 ,  C07D311/22 ,  C07D311/76 ,  C07D407/12 ,  C07D409/12

摘要： Monoamine re-uptake inhibitors and more specifically serotonin and noradrenaline re-uptake inhibitors are disclosed that have utility in the treatment of disorders of the central or peripheral nervous system in both men and women. The compounds of this invention have the structure: wherein R1, R2, R3, R4, R5, R6, m, n, W, X, and Y are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts, esters and solvates 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 inhibiting monoamine re-uptake in a subject in need thereof.

摘要翻译： 公开了单胺再摄取抑制剂，更具体地说可用于治疗男性和女性中枢或周围神经系统疾病的5-羟色胺和去甲肾上腺素再摄取抑制剂。 本发明的化合物具有以下结构：其中R 1，R 2，R 3，R 4， R 5，R 6，m，n，W，X​​和Y如本文所定义，包括立体异构体，前药及其药学上可接受的盐，酯和溶剂化物。 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抑制单胺再摄取的方法。

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：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：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：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：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。