MELANOCORTIN RECEPTOR AGONISTS

摘要

A novel compound is provided to be effective as melanocortin receptor agonists and particularly effective as selective agonists of melanocortin-4 receptor(MC-4R), thereby being useful for preventing and treating obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction, and inflammation. A compound as a melanocortin receptor agonist is represented by the formula(1), wherein R^1 is H, amidino, C1-4 alkylamidino, C1-4 alkanoylamidino, C1-10 alkyl, C3-7 cycloalkyl, C6-10 aryl, heterocycle, heteroaryl, C1-6 alkylcarbonyl, C3-7 cycloalkylcarbonyl, C1-4 alkoxycarbonyl, (C6-10)-aryl-(C1-4)alkoxycarbonyl, SO2-(C1-4)alkyl, C(O)N(R^5)(R^6) or C(S)N(R^5)(R^6)(each R^5 and R^6 is independently H, C1-6 alkyl or C3-7 cycloalkyl); R^2 is C6-10 aryl which may be mono- or di-substituted by a substituent selected from the group consisting of halogen, hydroxy, C1-4 alkyl and C1-4 alkoxy; R^3 is C3-8 cycloalkyl, heterocycle, C6-10 aryl or heteroaryl; and R^4 is H, C1-6 alkyl, C(O)R^7, (CH2)p-(C6-10)aryl, (CH2)p-heterparyl or (CH2)p-(C3-8)cycloalkyl(where p is 1 or 2, and R^7 is C1-10 alkyl, C2-6 alkenyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, amino, C1-4 alkylamino, (C1-4)alkyl(C1-4 alkyl)amino, SO2-(C1-7)alkyl, C6-10 aryl, heteroaryl or heterocycle). A method for preparing the compound of the formula(1) comprises a step of amide-coupling a compound represented by the formula(2) with a compound represented by the formula(3). A functional agonist composition of melanocortin receptor comprises a pharmaceutically acceptable carrier and the compound of the formula(1), a pharmaceutically acceptable salt thereof or an isomer thereof.