Use of cinnamic acid derivatives as modulators of an EP2 receptor

摘要

Cinnamic acid derivatives (I), their isomer, diastereomer, enantiomer and salts and/or cyclodextrin clathrate, for the preparation of drug for the fertility control, are new. Cinnamic acid derivatives of formula (I), their isomer, diastereomer, enantiomer and salts and/or cyclodextrin clathrate, for the preparation of drug for the fertility control, are new. X : -CH=CH- or -CH 2-CH 2-; Y 1>-CH 2- or -(CH 2) n-; A : phenyl- or 5-16C-heteroaryl (optionally substituted by one or two R 4> and/or R 3>); R 1>H or 1-4C-alkyl (optionally substituted); R 2>H, halo, CN, 1-4C-alkoxy or 1-4C-alkyl; and R 3>, R 4>H, halo, amino, CF 3, OH, CN, 1-4C-alkyl, 1-4C-acyl, 1-4C-alkoxy, CO 2-(1-4C-alkyl), N-(1-4C-alkyl) 2, CO-NH(1-4C-alkyl), CO-N(1-4C-alkyl) 2 or a phenyl (optionally substituted by halo, 1-4C-alkyl or 1-4C-alkoxy). [Image] ACTIVITY : Antiinfertility; Gynecological; Analgesic; Osteopathic; Antiinflammatory; Gastrointestinal-Gen.; Contraceptive; Antiparasitic; Cytostatic; Virucide; Hepatotropic; Anti-HIV; Cardiovascular-Gen.; Vasotropic; Antiarteriosclerotic; Ophthalmological; Angiogenesis-inhibitor; Neuroprotective; Nootropic; Immunomodulator; Nephrotropic. MECHANISM OF ACTION : Prostaglandin E 2 (EP 2) receptor modulator. The ability of (I) to modulate prostaglandin EP 2 receptor was tested using cumulos expansion assay. The results showed that (E)-3-(3,5-difluorophenyl)-N-[2-(7-fluoro-2,4-dimethyl-1H-indol-3-yl)-ethyl]-acrylamide exhibited an IC 5 0 value of 0.83 mu M.