[EN] COMPOUNDS USEFUL AS MODULATORS OF MELANOCORTIN RECEPTORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME<br/>[FR] COMPOSES UTILES COMME MODULATEURS DE RECEPTEURS DE LA MELANOCORTINE ET COMPOSITIONS PHARMACEUTIQUES LES COMPRENANT
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2002070511A1
公开(公告)日:2002-09-12
Compounds having the formula (I), wherein E is formula (E1), (E2), (E3), or -NR11R12; G is a novel side chain selected from C2-6alkenyl, A3-aryl, -OR18, heteroaryl, A1-cyano, A2-OR17, A1-C(=O)R18, A1-CO2R18, A1-CO2R18, A1-C(=O)NR18R19, A1-OC(=O)R18, A1-NR18C(=O)R19, A1-OC(=O)NR18R19, A1-NR18CO2R19, A1-NR18SO2R17, A1-SO2R17, A1-NR20C(=O)NR18R19, and A1-SR18; or when y is O or when W is not NHR22, G may be A1-heterocyclo, wherein A1 is a bond, C1-6alkylene or C2-6alkenylene, A2 is C1-6alkylene or C2-6alkenylene, and A3 is C2-6alkenylene; W is selected from-NR21R22, -OR23, -NR21C(=O)R24, -NR21CO2R24, amidino, guanidino, or a heteroaryl, heterocyclo, or C3-7cycloalkyl as defined in the specification, and X and R1 through R24 are as defined in the specification, are effective as modulators of melanocortin-receptors, particularly MC-1R and MC-4R.
具有公式(I)的化合物,其中E是公式(E1),(E2),(E3)或-NR11R12; G是从C2-6烯基,A3-芳基,-OR18,杂环芳基,A1-氰基,A2-OR17,A1-C(= O)R18,A1-CO2R18,A1-CO2R18,A1-C(= O)NR18R19,A1-OC(= O)R18,A1-NR18C(= O)R19,A1-OC(= O)NR18R19,A1-NR18CO2R19,A1-NR18SO2R17,A1-SO2R17,A1-NR20C(= O)NR18R19和A1-SR18中选择的新侧链; 或当y为O或W不为NHR22时,G可以是A1-杂环,其中A1是键,C1-6烷基或C2-6烯基,A2是C1-6烷基或C2-6烯基,A3是C2-6烯基; W从-NR21R22,-OR23,-NR21C(= O)R24,-NR21CO2R24,氨基甲酰基,胍基或在规范中定义的杂环芳基,杂环,或C3-7环烷基中选择,而X和R1到R24如规范中所定义,对于黑色素皮质素受体的调节剂,特别是MC-1R和MC-4R,是有效的。