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：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：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：US06297354B1

公开(公告)日：2001-10-02

申请号：US09373180

申请日：1999-08-12

申请人： Fortuna Haviv ,  Wesley Dwight ,  Jonathan Greer

发明人： Fortuna Haviv ,  Wesley Dwight ,  Jonathan Greer

IPC分类号： C07K1600

CPC分类号： C07K7/23 ,  A61K38/00

摘要： The present invention relates to a class of pentapeptide analogs of LHRH. These compounds are useful in the treatment of disease conditions which are mediated by reproductive hormones, including benign prostate hyperplasia, prostate tumors, breast and ovaries tumors, cryptorchidism, hirsuitism, gastric motility disorders, dysmenorrhea, and endometriosis.

摘要翻译： 本发明涉及一类LHRH的五肽类似物。 这些化合物可用于治疗由生殖激素介导的疾病状况，包括良性前列腺增生，前列腺肿瘤，乳腺和卵巢肿瘤，隐睾症，多毛症，胃动力障碍，痛经和子宫内​​膜异位症。