COMPUESTOS DERIVADOS DE N-(1-HETARIL-PIPERIDIN-4-IL)-(HET)ARILAMIDA, MODULADORES DEL RECEPTOR EP2; COMPOSICION FARMACEUTICA QUE COMPRENDE A DICHO COMPUESTO; Y USO DEL COMPUESTO PARA EL TRATAMIENTO DE TRASTORNOS DE LA FERTILIDAD, TRASTORNOS MENSTRUALE

摘要

N-(1-hetarylpiperidin-4-yl)(het)arylamide derivative, its isomers, salts, cyclodextrin clathrates are new. N-(1-hetarylpiperidin-4-yl)(het)arylamide derivative of formula (I), its isomers, salts, cyclodextrin clathrates are new. X and Y 1nitrogen radical or CH; R 15-12 membered mono or bicyclic aryl or heteroaryl ring which is optionally mono or polysubstituted; R 2-R 51-6C alkyl, 3-10C cycloalkyl ring, 2-6C alkenyl, 2-6C alkynyl, 5-12-membered mono or bicyclic aryl or heteroaryl ring (all optionally substituted), H, halo, cyano, OR 6, OC(O)R 6, S(O) nR 6, SO 2NHR 6, SO 2NHC(O)R 6, NR 6R 7, NHC(O)R 6, CH 2NR 6R 7, CH 2NHC(O)R 6, C(OH)R 6R 7, C(O)R 6, CO 2R 6 or C(O)NR 6R 7; R 6 and R 71-6C alkyl, 3-10C cycloalkyl, 5-12-membered mono or bicyclic aryl or heteroaryl ring (optionally substituted) or H; R 6+R 73-8-membered ring;and n : 0-2. Provided that at least one of X and Y 1 is a nitrogen radical. [Image] - ACTIVITY : Antiinfertility; Gynecological; Cytostatic; Analgesic; Osteopathic; Antimicrobial; Antiinflammatory; Hepatotropic; Virucide; Anti-HIV; Cardiovascular-Gen.; Vasotropic; Antiarteriosclerotic; Ophthalmological; Angiogenesis-Inhibitor; Angiogenesis-Stimulator; Neuroprotective; Nootropic; Immunomodulator; Nephrotropic. No biological data given. - MECHANISM OF ACTION : E-prostanoid-2 (EP2) receptor modulator. The efficacy of N-[1-(7-bromo-quinolin-4-yl)-piperidin-4-yl]-2,3-dichloro-benzamide (Ia) was evaluated for EP2 receptor modulatory activity using cumulus expansion assay and IC 5 0 value was calculated. (Ia) Showed IC 5 0 value of 0.1 mu M.