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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. | LitMetric
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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.

Fabio C Tucci Yun-Fei Zhu Zhiqiang Guo Timothy D Gross Patrick J Connors Yinghong Gao Martin W Rowbottom R Scott Struthers Greg J Reinhart Qiu Xie Ta Kung Chen Haig Bozigian Anne L Killam Bonneville Andrew Fisher Liping Jin John Saunders Chen Chen

J Med Chem

Departments of Medicinal Chemistry, Endocrinology, and Preclinical Development, Neurocrine Biosciences Inc., 10555 Science Center Drive, San Diego, CA 92121, USA.

Published: July 2004

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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http://dx.doi.org/10.1021/jm049791wDOI Listing

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