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Usage

Uses

Used in Pharmaceutical Industry:
1-(2-fluoro-6-(trifluoroMethyl)benzyl)-6-Methyl-5-(piperazin-1-yl)pyriMidine-2,4(1H,3H)-dione is used as a potential pharmaceutical candidate for [specific application reason, if known]. Its unique structure and properties may contribute to its effectiveness in [specific medical condition or therapeutic area, if known]. Further research is required to fully understand its potential and optimize its use in medical treatments.

Upstream product

• 1308380-31-5 5-(4-benzyl-piperazin-1-yl)-1-(2-fluoro-6-trifluoromethyl-benzyl)-6-methyl-1H-pyrimidine-2,4-dione 
• 830346-48-0 5-bromo-1-[2-fluoro-6-(trifluoromethyl)benzyl]-6-methylpyrimidine-2,4-(1H,3H)-dione 

Downstream Products

• 1308378-32-6 1-(2-fluoro-6-(trifluoromethyl)benzyl)-6-methyl-5-(4-(3-nitrobenzyl)piperazin-1-yl)pyrimidine-2,4(1H,3H)-dione 
• 1308380-37-1 [(R)-2-{3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-5-[4-(3-nitro-benzyl)-piperazin-1-yl]-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl}-1-(2-methoxy-phenyl)-ethyl]-carbamic acid tert-butyl ester 
• 1308379-59-0 3-[(R)-2-amino-2-(2-hydroxy-phenyl)-ethyl]-1-(2-fluoro-6-trifluoromethyl-benzyl)-6-methyl-5-[4-(3-nitro-benzyl)-piperazin-1-yl]-1H-pyrimidine-2,4-dione 
• 1308379-69-2 (R)-2-(2-(1-amino-2-(3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-5-(4-(3-nitrobenzyl)piperazin-1-yl)-2,6-dioxo-2,3-dihydropyrimidin-1(6H)-yl)ethyl)phenoxy)acetic acid 
• 1308379-70-5 4-[2-((R)-1-amino-2-{3-(2-fluoro-6-trifluoromethyl-benzyl)-4-methyl-5-[4-(3-nitro-benzyl)-piperazin-1-yl]-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl}-ethyl)-phenoxy]-butyric acid 
• 1308378-34-8 1-(2-fluoro-6-(trifluoromethyl)benzyl)-6-methyl-5-(4-((5-(trifluoromethyl)furan-2-yl)methyl)piperazin-1-yl)pyrimidine-2,4(1H,3H)-dione 
• 1308378-96-2 (R)-4-((1-(3-fluoro-5-methylphenyl)-2-(3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-5-(4-((5-(trifluoromethyl)furan-2-yl)methyl)piperazin-1-yl)-2,3-dihydropyrimidin-1(6H)-yl)ethyl)amino)butanoic acid 
• 1308378-99-5 (R)-4-((1-(5-fluoro-2-methoxyphenyl)-2-(3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-5-(4-((5-(trifluoromethyl)furan-2-yl)methyl)piperazin-1-yl)-2,3-dihydropyrimidin-1(6H)-yl)ethyl)amino)butanoic acid 
• 1308379-02-3 (R)-4-((2-(3-(2-fluoro-6-(trifluoromethyl)benzyl)-4-methyl-2,6-dioxo-5-(4-((5-(trifluoromethyl)furan-2-yl)methyl)piperazin-1-yl)-2,3-dihydropyrimidin-1(6H)-yl)-1-(2-methoxyphenyl)ethyl)amino)butanoic acid 
• 1308378-51-9 (R)-3-(2-amino-2-(3-fluoro-5-methylphenyl)ethyl)-1-(2-fluoro-6-(trifluoromethyl) benzyl)-6-methyl-5-(4-((5-(trifluoromethyl)furan-2-yl)methyl)piperazin-1-yl)pyrimidine-2,4(1H,3H)-dione 
• 1308378-49-5 (R)-3-(2-amino-2-(5-fluoro-2-methoxyphenyl)ethyl)-1-(2-fluoro-6-(trifluoromethyl) benzyl)-6-methyl-5-(4-((5-(trifluoromethyl)furan-2-yl)methyl)piperazin-1-yl)pyrimidine-2,4(1H,3H)-dione 
• 1308378-48-4 (R)-3-(2-amino-2-(2-methoxyphenyl)ethyl)-1-(2-fluoro-6-(trifluoromethyl)benzyl)-6-methyl-5-(4-((5-(trifluoromethyl)furan-2-yl)methyl)piperazin-1-yl)pyrimidine-2,4(1H,3H)-dione 
• 1308376-62-6 (R)-3-(2-amino-2-phenylethyl)-1-(2-fluoro-6-(trifluoromethyl)benzyl)-6-methyl-5-(4-((5-(trifluoromethyl)furan-2-yl)methyl)piperazin-1-yl)pyrimidine-2,4(1H,3H)-dione 
• 1308375-83-8 (S)-3-(2-amino-2-(3-fluoro-5-methylphenyl)ethyl)-1-(2-fluoro-6-(trifluoromethyl) benzyl)-6-methyl-5-(4-(3-nitrobenzyl)piperazin-1-yl)pyrimidine-2,4(1H,3H)-dione 

Relevant academic research and scientific papers

Synthesis and biological evaluation of 3-(2-aminoethyl) uracil derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists

We investigated a series of uracil analogues by introducing various substituents on the phenyl ring of the N-3 aminoethyl side chain and evaluated their antagonistic activity against human gonadotropin-releasing hormone (GnRH) receptors. Analogues with su

Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist

We developed a compound library for orally available gonadotropin-releasing hormone (GnRH) receptor antagonists that were based on a uracil scaffold. On the basis of in vitro activity and CYP inhibition profile, we selected 18a (SKI2496) for further in vivo studies. Compound 18a exhibited more selective antagonistic activity toward the human GnRH receptors over the GnRHRs in monkeys and rats, and this compound also showed inhibitory effects on GnRH-mediated signaling pathways. Pharmacokinetic and pharmacodynamic evaluations of 18a revealed improved bioavailability and superior gonadotropic suppression activity compared with Elagolix, the most clinically advanced compound. Considering that 18a exhibited highly potent and selective antagonistic activity toward the hGnRHRs along with favorable pharmacokinetic profiles, we believe that 18a may represent a promising candidate for an orally available hormonal therapy.

Gonadotropin Releasing Hormone Receptor Antagonist, Preparation Method Thereof And Pharmaceutical Composition Comprising The Same

Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.

GONADOTROPIN RELEASING HORMONE RECEPTOR ANTAGONISTS, MANUFACTURING METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME

Disclosed are compounds useful as gonadotropin-releasing hormone ("GnRH") receptor antagonist.