459841-29-3Relevant academic research and scientific papers
Further optimization of sulfonamide analogs as EP1 receptor antagonists: Synthesis and evaluation of bioisosteres for the carboxylic acid group
Naganawa, Atsushi,Matsui, Toshiaki,Ima, Masaki,Saito, Tetsuji,Murota, Masayuki,Aratani, Yoshiyuki,Kijima, Hideomi,Yamamoto, Hiroshi,Maruyama, Takayuki,Ohuchida, Shuichi,Nakai, Hisao,Toda, Masaaki
, p. 7121 - 7137 (2007/10/03)
4-{[2-[(2-Furylsulfonyl)(isobutyl)amino]-5-(trifluoromethyl)phenoxy]methyl}benzoic acid analogs 2a and b and a series of the acid analogs, in which the carboxylic acid residue of 2b was replaced with various kinds of carboxylic acid bioisosteres, were synthesized and evaluated as EP1 receptor antagonists. Compound 2b and its monocyclic acid analogs, in which the carboxylic acid residue of 2b was replaced with monocyclic acid bioisosteres, were found to show potent EP1 receptor antagonist activity. Optimization of the linker Y between the phenyl moiety and the carboxylic acid residue of 2b was also carried out (Table 5). Compounds 2b and 16 and 17 possessing conformationally restricted linker Y were found to show the most optimized potency among the tested compounds. Cytochrome P450 inhibition of optimized compounds was also investigated. Details of the structure-activity relationship study are presented.
REMEDIES FOR DEPRESSION CONTAINING EP1 ANTAGONIST AS THE ACTIVE INGREDIENT
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Page 28, (2008/06/13)
A pharmaceutical composition for the treatment and/or prevention of depression comprising a compound having an antagonistic activity for EP1 receptor which a prostaglandin E2 receptor subtype. EP1 antagonist is useful for
N-PHENYLARYLSULFONAMIDE COMPOUND, DRUG CONTAINING THE COMPOUND AS ACTIVE INGREDIENT, INTERMEDIATE FOR THE COMPOUND, AND PROCESSES FOR PRODUCING THE SAME
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Page 25, 26, (2008/06/13)
(R1 is COOH etc.; R2 is hydrogen, methyl, etc.; R3 and R4 are a combination of methyl and methyl, etc.; R5 is isopropyl etc.; Ar is thiazolyl, pyridyl, 5-methyl-2-furyl each optionally substituted wit
