496929-84-1Relevant academic research and scientific papers
Structure-activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists
Guo, Zhiqiang,Wu, Dongpei,Zhu, Yun-Fei,Tucci, Fabio C.,Regan, Collin F.,Rowbottom, Martin W.,Struthers, R. Scott,Xie, Qiu,Reijmers, Shelby,Sullivan, Susan K.,Sai, Yang,Chen, Chen
, p. 3685 - 3690 (2007/10/03)
SAR studies of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists resulted in potent compounds. The best compound from the series had a binding affinity of 2 nM.
A convenient one-pot synthesis of asymmetric 1,3,5-triazine-2,4,6-triones and its application towards a novel class of gonadotropin-releasing hormone receptor antagonists
Guo, Zhiqiang,Wu, Dongpei,Zhu, Yun-Fei,Tucci, Fabio C.,Pontillo, Joseph,Saunders, John,Xie, Qiu,Struthers, R. Scott,Chen, Chen
, p. 693 - 698 (2007/10/03)
A convenient one-pot synthetic route was developed for the preparation of asymmetric 1,3-dialkyl-1,3,5-triazine-2,4,6-triones from readily available alkyl- or aryl-isocyanates, primary amines and N-chlorocarbonyl isocyanate in excellent yields. Subsequent alkylation with N-protected amino alcohols afforded the desired 1,3,5-triazine-2,4,6-triones in good yields. This methodology was applied to the synthesis of a chemical library acting as antagonists of the hGnRH receptor.
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
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, (2008/06/13)
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 R1, R2, R3a, Rs
