2805-16-5Relevant academic research and scientific papers
Gonadotropin-releasing hormone receptor antagonists and methods relating thereto
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Page column 41-42, (2010/01/30)
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: including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein Ar, B, R1, R2, R3a, R3b, R4, R5, R6and m are as defined herein.
A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists.
Tucci, Fabio C,Zhu, Yun-Fei,Guo, Zhiqiang,Gross, Timothy D,Connors Jr., Patrick J,Struthers, R Scott,Reinhart, Greg J,Wang, Xiaochuan,Saunders, John,Chen, Chen
, p. 3491 - 3495 (2007/10/03)
A new class of small molecule GnRH antagonists, the 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones, was designed and a novel synthesis for these compounds was developed. The synthesis utilizes a base-catalyzed intramolecular cyclization of fluoromethyl pyrimidone 5 to generate the bicyclic core. Amongst the compounds synthesized, we discovered some highly potent GnRH receptor antagonists (e.g., 12, K(i)=9 nM), which showed enhanced stability towards acidic physiological conditions compared to the des-fluoro analogues.
