Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist

被引：19

作者：

Li, Haitao ^{[1
]}

Anderes, Kenna L. ^{[1
]}

Kraynov, Eugenia A. ^{[1
]}

Luthin, David R. ^{[1
]}

Do, Quyen-Quyen ^{[1
]}

Hong, Yufeng ^{[1
]}

Tompkins, Eileen ^{[1
]}

Sun, Eric T. ^{[1
]}

Rajapakse, Ranjan ^{[1
]}

Pathak, Ved P. ^{[1
]}

Christie, Lance C. ^{[1
]}

Vazir, Haresh ^{[1
]}

Castillo, Rosemary ^{[1
]}

Gregory, Margaret L. ^{[1
]}

Castro, Mary ^{[1
]}

Nared-Hood, Karen ^{[1
]}

Paderes, Genevieve ^{[1
]}

Anderson, Mark B. ^{[1
]}

机构：

[1] Pfizer Global Res & Dev, Dept Med Chem Res Pharmacol & Pharmacokinet Dynam, San Diego, CA 92121 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2006年 / 49卷 / 11期

关键词：

D O I：

10.1021/jm060012g

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Gonadotropin releasing hormone (GnRH) plays an important role in the biology of reproduction. The use of GnRH receptor antagonists has been reported in the literature for the treatment of breast, ovarian, and prostate cancers. In this article, we report the synthesis, in vitro characterization, pharmacokinetics, and pharmacodynamics of an orally bioavailable, potent, small molecule GnRH receptor antagonist N-{4,6dimethoxy-2-[(3-morpholin-4-ylpropyl) amino]pyrimidin-5-yl}-5-[3,3,6-trimthyl-2,3-dihydro-1H-inden-5yl)oxy]-2-furamide(compound1).

引用

页码：3362 / 3367

页数：6

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