537696-27-8Relevant academic research and scientific papers
NON-PEPTIDE GnRH AGENTS, METHODS AND INTERMEDIATES FOR THEIR PREPARATION
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Page/Page column 42, (2010/02/11)
Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
Characterization of mono- and diaminopyrimidine derivatives as novel, nonpeptide gonadotropin releasing hormone (GnRH) receptor antagonists.
Luthin, David R,Hong, Yufeng,Tompkins, Eileen,Anderes, Kenna L,Paderes, Genevieve,Kraynov, Eugenia A,Castro, Mary A,Nared-Hood, Karen D,Castillo, Rosemary,Gregory, Margaret,Vazir, Haresh,May, John M,Anderson, Mark B
, p. 3635 - 3639 (2007/10/03)
A novel series of derivatives of mono- and diaminopyrimidines 1 potently displaced binding of a radiolabeled GnRH analogue to human and rat GnRH receptors. Analogues from these series competitively antagonized GnRH-stimulated increases in extracellular acidification in vitro and suppressed GnRH-mediated increases in circulating luteinizing hormone (LH) in castrated rats and testosterone in intact rats. These compounds or their analogues may be useful in treating sex hormone-dependent disease.
