[EN] NOVEL NAPHTHALENE UREAS AS GLUCOSE UPTAKE ENHANCERS<br/>[FR] NOUVELLES NAPHTALENE UREES UTILES EN TANT QU'ACTIVATEURS DE L'ABSORPTION DU GLUCOSE
申请人:TELIK INC
公开号:WO2000071506A2
公开(公告)日:2000-11-30
Compounds of formula (I), wherein R?1 and R2¿ are substituents on the A rings and are, independently, -SO¿2NR?72, -C(O)NR72, -NR7SO2R?7, -NR7C(O)R7, -SO¿2OR7, -C(O)OR7, -OSO¿2R?7, or -OC(O)R?7, R3 and R4¿ are, independently, hydrogen or lower alkyl, or R?3 and R4¿ together are -(CH¿2?)2-, -(CH2)3-, or -(CH2)4-, or R?3 or R4¿ may be an electron pair, R?5 and R6¿ are, independently, hydrogen, alkyl, substituted alkyl, cyano, halo, nitro, -SR8, -C(O)R8, -SO2OR8, -OSO¿2?R?8, -SO¿2NR82, -NR8SO2R8, -OC(O)R8, -C(O)OR8, -C(O)NR82, -NR?8C(O)R8, -OR8¿, or -NR82, each R?7 and R8¿ is, independently, hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, aryl(lower)alkyl, substituted aryl(lower)alkyl, heteroaryl(lower)alkyl, substituted heteroaryl(lower)alkyl, heterocyclyl, substituted heterocyclyl, heteroaryl, or substituted heteroaryl, each Y is, independently, a non-interfering substituent which is not linked to the naphthalene ring via an azo or amide linkage, each x is independently, 0, 1 or 2, and the linker connects a carbon designated as c to a carbon designated as d, or a pharmaceutically acceptable salt thereof, as a single stereoisomer or mixture of stereoisomers, are useful for treating conditions associated with hyperglycemia, especially Type II diabetes, with dinaphthylureas. These compounds are useful in stimulating the kinase activity of the insulin receptor, activating the insulin receptor, and stimulating the uptake of glucose. Pharmaceutical compositions comprising the antidiabetic compounds are also disclosed.