Discovery of sodium R-(+)-4-{2-[5-(2-Fluoro-3-methoxyphenyl)-3-(2-fluoro-6- [trifluoromethyl]-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl] -1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor

Journal of Medicinal Chemistry

Volumn 51, Issue 23, 2008, Pages 7478-7485

  Chen, Chen ^a   Wu, Dongpei ^a   Guo, Zhiqiang ^a   Xie, Qiu ^a   Reinhart, Greg J ^a   Madan, Ajay ^a   Wen, Jenny ^a   Chen, Takung ^a   Huang, Charles Q ^a   Chen, Mi ^a   Chen, Yongsheng ^a   Tucci, Fabio C ^a   Rowbottom, Martin ^a   Pontillo, Joseph ^a   Zhu, Yun Fei ^a   Wade, Warren ^a   Saunders, John ^a   Bozigian, Haig ^a   Struthers, R Scott ^a  

^a NEUROCRINE BIOSCIENCES INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 [2 [5 (2 FLUORO 3 METHOXYPHENYL) 3 [2 FLUORO 6 (TRIFLUOROMETHYL)BENZYL] 4 METHYL 2,6 DIOXO 43,6 DIHYDRO 2H PYRIMIDIN 1 YL] 1 PHENYLETHYLAMINO]BUTYRIC ACID; ELAGOLIX; GONADORELIN ANTAGONIST; PHENETHYLAMINE DERIVATIVE; UNCLASSIFIED DRUG; URACIL DERIVATIVE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; CHEMICAL REACTION KINETICS; CONTROLLED STUDY; DRUG POTENCY; DRUG SELECTIVITY; ENDOMETRIOSIS; ENZYME INHIBITION; GONADORELIN RELEASE; HORMONE RECEPTOR INTERACTION; LIVER MICROSOME; LUTEINIZING HORMONE RELEASE; MACACA; NONHUMAN; RAT; REACTION OPTIMIZATION; SINGLE DRUG DOSE;

ANIMALS; CACO-2 CELLS; CYTOCHROME P-450 CYP3A; DRUG DISCOVERY; DRUG EVALUATION, PRECLINICAL; HUMANS; HYDROCARBONS, FLUORINATED; MACACA FASCICULARIS; MALE; MICROSOMES, LIVER; MOLECULAR STRUCTURE; PYRIMIDINES; RECEPTORS, LHRH; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; TIME FACTORS;

EID: 57349195546     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm8006454     Document Type: Article

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