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3-(2-aminoalkyl)-1-(2,6-difluorobenzyl)-5- (2-fluoro-3-methoxyphenyl)-6-methyl-uracils as orally bioavailable antagonists of the human gonadotropin releasing hormone receptor |
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| Authors: | Tucci Fabio C Zhu Yun-Fei Guo Zhiqiang Gross Timothy D Connors Patrick J Gao Yinghong Rowbottom Martin W Struthers R Scott Reinhart Greg J Xie Qiu Chen Ta Kung Bozigian Haig Killam Bonneville Anne L Fisher Andrew Jin Liping Saunders John Chen Chen |
| Affiliation: | Departments of Medicinal Chemistry, Endocrinology, and Preclinical Development, Neurocrine Biosciences Inc., 10555 Science Center Drive, San Diego, CA 92121, USA. ftucci@neurocrine.com |
| Abstract: | Uracils possessing N-3 side chains derived from various amino alcohols were designed and synthesized as potent human gonadotropin releasing hormone receptor antagonists. The compounds herein presented displayed superior metabolic stability than their predecessor molecules. Selected compounds from this series featured good oral bioavailability in mice and cynomolgus monkeys. |
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