199861-89-7

Upstream product

• 5900-58-3 2-amino-4-chloro-benzoic acid methyl ester 
• 199850-56-1 methyl 2-amino-4-chloro-5-iodobenzoate 
• 119423-95-9 3,5-dimethylphenylacetyl chloride 
• 42288-46-0 (3,5-dimethylphenyl)acetic acid 
• 199861-83-1 4-chloro-2-[2-(3,5-dimethylphenyl)-acetylamino]-5-iodo-benzoic acid methyl ester 

Downstream Products

• 199861-90-0 2-{2-[7-chloro-3-(3.5-dimethylphenyl)-6-iodo-2-oxo-1,2-dihydroquinolin-4-yloxy]-ethyl}-piperidine-1-carboxylic acid tert-butyl ester 
• 265324-93-4 7-chloro-3-(3,5-dimethyl-phenyl)-6-iodo-4-[2-(1-methyl-piperidin-2-yl)-ethoxy]-1H-quinolin-2-one 

Relevant academic research and scientific papers

Quinolones as gonadotropin releasing hormone (GnRH) antagonists: Simultaneous optimization of the C(3)-aryl and C(6)-substituents

A series of 3-arylquinolones was prepared and evaluated for their ability to act as gonadotropin releasing hormone (GnRH) antagonists. A variety of substitution patterns of the 3-aryl substituent are described. The 3,4,5-trimethylphenyl substituent (23h) was found to be optimal. (C) 2000 Elsevier Science Ltd. All rights reserved.

Potent antagonists of gonadotropin releasing hormone receptors derived from quinolone-6-carboxamides

SAR studies which focused upon the C-6 position of a recently described series of quinolone gonadotropin releasing hormone antagonists are reported. Synthetic access to diverse quinolone-6-carboxamides was achieved via the palladium-catalyzed amino-carbonylation reactions of iodide 4 with various amines. Amides related to 9y were especially potent, functional antagonists of rat and human GnRH receptors. (C) 2000 Elsevier Science Ltd. All rights reserved.

Antagonists of gonadotropin releasing hormone

PCT No. PCT/US97/08432 Sec. 371 Date Nov. 12, 1998 Sec. 102(e) Date Nov. 12, 1998 PCT Filed May 16, 1997 PCT Pub. No. WO97/44339 PCT Pub. Date Nov. 27, 1997There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related conditions in both men and women.