Neuropeptide Y5 receptor antagonist comprises new or known aminosulfinyl or aminosulfonyl derivatives (I). Neuropeptide Y5 receptor antagonist comprises aminosulfinyl or aminosulfonyl derivatives of formula (I), their prodrugs, salts or solvates. [Image] R 1optionally substituted lower alkyl, cycloalkyl or aryl, or R 1 + R 2lower alkylene； n : 1 or 2； X : (CR 3R 4) pA(CR 5R 6) q, HetU, NR 2X or optionally substituted lower alkylene, lower alkenylene, CO-lower alkylene or CO-lower alkenylene； A : optionally substituted cycloalkylene, cycloalkenylene, bicycloalkylene, arylene or divalent heterocycle； p, q : 0 or 1； Het : piperidinediyl, piperazinediyl, pyridinediyl, pyrazinediyl, pyrrolidinediyl or pyrrolediyl all attached to NR 2 via N； U : a bond, lower alkylene or lower alkenylene； Y : OCONR 7, CONR 7, CSNR 7, NR 7CO or NR 7CS； R 2-R 7H or lower alkyl； Z : optionally substituted lower alkyl, lower alkenyl, amino, lower alkoxy, carbocyclyl or heterocyclyl. Independent claims are also included for compounds (I), their salts, prodrugs and solvates in which: (i) X = 2-6C alkylene or 3-6C alkenylene； and R 1 = optionally substituted 3-10C alkyl or 5 or 6C cycloalkyl； provided that when Y = NR 7, the Z is not lower alkylphenylamino, lower hydroxyalkylphenylamino or acylphenylamino； (ii) A = heteroarylene or optionally substituted cycloalkylene, cycloalkenylene, bicycloalkylene or piperidinylene； and R 1 = optionally substituted 3-10C alkyl or 5 or 6C cycloalkyl； and (iii) A = p-phenylene； R 1 = 3-10C alkyl or 5 or 6C cycloalkyl and Z = p-lower alkylphenylene； provided that when R 1 = isopropyl, the Z is not p-n-butylphenylene. ACTIVITY : Anorectic； antidiabetic； hypotensive； antilipemic； antiarteriosclerotic； cardiant. MECHANISM OF ACTION : Neuropeptide-Y5 antagonist. In assays, a compound of formula (Ia) exhibited IC 50 values for neuropeptide Y5 binding of 0.1 nM and for cAMP in Chinese hamster ovary cells of 1.9 nM. [Image].
