478010-70-7Relevant academic research and scientific papers
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist
Li, Haitao,Anderes, Kenna L.,Kraynov, Eugenia A.,Luthin, David R.,Do, Quyen-Quyen,Hong, Yufeng,Tompkins, Eileen,Sun, Eric T.,Rajapakse, Ranjan,Pathak, Ved P.,Christie, Lance C.,Vazir, Haresh,Castillo, Rosemary,Gregory, Margaret L.,Castro, Mary,Nared-Hood, Karen,Paderes, Genevive,Anderson, Mark B.
, p. 3362 - 3367 (2006)
Gonadotropin releasing hormone (GnRH) plays an important role in the biology of reproduction. The use of GnRH receptor antagonists has been reported in the literature for the treatment of breast, ovarian, and prostate cancers. In this article, we report the synthesis, in vitro characterization, pharmacokinetics, and pharmacodynamics of an orally bioavailable, potent, small molecule GnRH receptor antagonist N-{4,6-dimethoxy-2-[(3-morpholin-4-ylpropyl) amino]pyrimidin-5-yl}-5-[3,3,6-trimthyl-2,3-dihydro-1H-inden-5-yl)oxy] -2-furamide (compound 1).
RADIOLABELED GNRH ANTAGONISTS AS PET IMAGING AGENTS
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Page/Page column 11, (2014/12/12)
Provided herein is technology relating to imaging agents for positron emission tomography (PET) and particularly, but not exclusively, to a gonadotropin-releasing hormone (GnRH) antagonist radiolabeled with positron emitting nuclides and to methods of visualizing GnRH receptors in the central nervous system by PET from administration of such compounds to warm-blooded animals for diagnostic purposes.
Non-peptide GnRH agents, pharmaceutical compositions and methods for their use
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, (2008/06/13)
Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, 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.
NON-PEPTIDE GNRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE
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Page 43, (2010/02/06)
Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression o£ gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
