公开(公告)号：US08507536B2

公开(公告)日：2013-08-13

申请号：US13572510

申请日：2012-08-10

Applicant: 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

Inventor： 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: C07D211/06 ,  C07D213/78 ,  C07D211/70 ,  A61K31/44 ,  A61P25/00

CPC classification number: C07D213/61 ,  C07D213/84 ,  C07D239/36 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12

Abstract: 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.

Abstract translation: 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：US07393865B2

公开(公告)日：2008-07-01

申请号：US11156252

申请日：2005-06-17

Applicant: Graham Beaton ,  Wilna (Willy) J Moree ,  Florence Jovic ,  Timothy Coon ,  Jinghua Yu

Inventor： Graham Beaton ,  Wilna (Willy) J Moree ,  Florence Jovic ,  Timothy Coon ,  Jinghua Yu

IPC: A61K31/44 ,  A61K31/425 ,  A61K31/381 ,  C07D277/20 ,  C07D333/52 ,  C07D409/06

CPC classification number: C07D409/04 ,  C07D333/58 ,  C07D417/04

Abstract: Compounds having the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts, esters and solvates thereof, wherein R1, R2, R3a, R3b, L1, L2 and n are as defined herein. Such compounds generally function as H1 receptor ligands, and thus have utility as sleep inducing agents. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.

Abstract translation: 具有以下结构（I）的化合物：包括其立体异构体，前药和药学上可接受的盐，酯和溶剂化物，其中R 1，R 2，R 3a R 3b，L 1，L 2和n如本文所定义。 这些化合物通常用作H 1 H 1受体配体，因此可用作睡眠诱导剂。 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：US20060014797A1

公开(公告)日：2006-01-19

申请号：US11156252

申请日：2005-06-17

Applicant: Graham Beaton ,  Wilna (Willy) Moree ,  Florence Jovic ,  Timothy Coon ,  Jinghua Yu

Inventor： Graham Beaton ,  Wilna (Willy) Moree ,  Florence Jovic ,  Timothy Coon ,  Jinghua Yu

IPC: C07D333/66 ,  C07D409/02 ,  A61K31/4436 ,  A61K31/381

CPC classification number: C07D409/04 ,  C07D333/58 ,  C07D417/04

Abstract: Compounds having the following structure (I): including stereoisomers, prodrugs, and pharmaceutically acceptable salts, esters and solvates thereof, wherein R1, R2, R3a, R3b, L1, L2 and n are as defined herein. Such compounds generally function as H1 receptor ligands, and thus have utility as sleep inducing agents. Pharmaceutical compositions containing a compound of structure (I), as well as methods relating to the use thereof, are also disclosed.

Abstract translation: 具有以下结构（I）的化合物：包括其立体异构体，前药和药学上可接受的盐，酯和溶剂化物，其中R 1，R 2，R 3a R 3b，L 1，L 2和n如本文所定义。 这些化合物通常用作H 1 H 1受体配体，因此可用作睡眠诱导剂。 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。