352303-66-3

Usage

InChI:InChI=1/C12H9BrF2N2O2/c1-6-10(13)11(18)16-12(19)17(6)5-7-8(14)3-2-4-9(7)15/h2-4H,5H2,1H3,(H,16,18,19)

Upstream product

• 17751-24-5 N-(2,6-difluorobenzyl) urea 
• 618914-13-9 1-(2,6-difluorobenzyl)-3-(3-oxobutyryl)urea 

Downstream Products

• 618914-14-0 5-bromo-1-(2,6-difluoro-benzyl)-6-methyl-3-(2-methyl-allyl)-1H-pyrimidine-2,4-dione 
• 352303-75-4 5-bromo-1-(2,6-difluorobenzyl)-3-[2-(R)-N-Boc-aminopropyl]-6-methyluracil 
• 675605-94-4 5-bromo-1-(2,6-difluorobenzyl)-3-[2-(S)-N-Boc-aminopropyl]-6-methyluracil 
• 618902-05-9 3-[5-bromo-3-(2,6-difluoro-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-pyrrolidine-1-carboxylic acid tert-butyl ester 
• 618902-01-5 3-[2-N-Boc-amino-1-(S)-methylethyl]-5-bromo-1-(2,6-difluorobenzyl)-6-methyluracil 
• 352303-74-3 3-[2-N-Boc-amino-1-(R)-methylethyl]-5-bromo-1-(2,6-difluorobenzyl)-6-methyluracil 
• 352296-26-5 (S)-5-bromo-3-(N-tert-butoxycarbonyl-2-amino-3-phenylpropyl)-1-(2,6-difluorobenzyl)-6-methyluracil 
• 732282-75-6 (S)-5-bromo-3-(N-tert-butoxycarbonyl-2-amino-4-methylpentyl)-1-(2,6-difluorobenzyl)-6-methyluracil 
• 732282-71-2 {1-[5-bromo-3-(2,6-difluoro-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-ylmethyl]-2-methyl-propyl}-carbamic acid tert-butyl ester 
• 732282-70-1 {1-[5-bromo-3-(2,6-difluoro-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-ylmethyl]-2-methyl-propyl}-carbamic acid tert-butyl ester 
• 732282-62-1 (R)-5-bromo-3-(N-tert-butoxycarbonyl-2-amino-4-methylpentyl)-1-(2,6-difluorobenzyl)-6-methyluracil 
• 352296-29-8 (R)-5-bromo-3-(N-tert-butoxycarbonyl-2-amino-3-phenylpropyl)-1-(2,6-difluorobenzyl)-6-methyluracil 
• 732282-74-5 (S)-5-bromo-3-(N-tert-butoxycarbonyl-2-amino-2-cyclohexylethyl)-1-(2,6-difluorobenzyl)-6-methyluracil 
• 732282-77-8 {1-[5-bromo-3-(2,6-difluoro-benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-ylmethyl]-3-phenyl-propyl}-carbamic acid tert-butyl ester 

Relevant academic research and scientific papers

PYRIMIDINE-2,4-DIONE DERIVATIVES AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS

GnRH receptor antagonists are disclosed that 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 formula (I) wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

PYRIMIDINE-2, 4-DIONE DERIVATIVES AS GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS

GnRH receptor antagonists are disclosed that 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: wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO

GnRH receptor antagonists are disclosed that 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: wherein n, R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.

Synthesis and structure-activity relationships of uracil derived human GnRH receptor antagonists: (R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6- methyluracils containing a substituted thiophene or thiazole at C-5

The design and synthesis of a number of 5-thiazolyl and 5-thienyl substituted uracils is described and results from SAR studies are summarized. The best compound showed Ki = 2 nM. The synthesis of a series of (R)-3-[2-(2-amino)phenethyl]-1-(2,6

Synthesis and Structure-Activity Relationships of 1-Arylmethyl-5-aryl-6-methyluracils as Potent Gonadotropin-Releasing Hormone Receptor Antagonists

Based on the SAR from bicyclic gonadotropin-releasing hormone (GnRH) antagonists such as 6-aminomethyl-7-aryl-pyrrolo [1,2-a] pyrimid-4-ones (5) and 2-aryl-3-aminomethyl-imidazolo-[1,2-a]pyrimid-5-ones (6a,b), a series of novel uracil compounds (8) were d

Synthesis and structure-activity relationships of 1-arylmethyl-3-(2-aminopropyl)-5-aryl-6-methyluracils as potent GnRH receptor antagonists

The novel synthesis and SAR studies of 6-methyluracils as human GnRH receptor antagonists are discussed. Introduction of a small methyl substituent at the β-position from N3 of the uracil improved the GnRH binding potency by 5- to 10-fold. The best compou