Patent ID: 6562828
Filing Date: 2003-05-13
Classification: A61P,C07D

Abstract:
An amidine compound of the formula I whereinR is a group of the formula â€ƒwherein R4 is hydrogen atom, hydroxy group, lower alkyl group, lower alkoxy group or halogen atom, R5 is hydrogen atom, cyano group, carboxy group or lower alkoxycarbonyl group, R6 is hydrogen atom, cycloalkyl group, hydroxy group, carboxy group, lower alkoxycarbonyl group, aralkyloxycarbonyl group, wherein the aryl moiety of said aralkyloxycarbonyl group is optionally substituted by halogen atom, nitro group, alkyl group, alkoxy group or trifluoromethyl group, nitro group, amino group, lower alkylamino group, di(lower)alkylamino group, aryl group, heteroaryl selected from the group consisting of an imidazolyl group, a pyridyl group, a pyridine-1-oxide group, a pyrimidyl group, a thienyl group, a thiazolyl group, an isoxazolyl group, an oxadiazolyl group, a triazolyl group, an indolyl group, a quinolyl group, a furyl group, a benzofuryl group, a 1H-benzimidazolyl group and a 2-benzothiazolyl group, wherein said aryl group or heteroaryl group is optionally substituted by 1 to 3 substituents selected from lower alkyl group, hydroxy group, lower alkoxy group, carboxy group, lower alkoxycarbonyl group, aralkyloxycarbonyl group, nitro group, amino group, acylamino group, amidino group and hydroxyamidino group, 5- to 7-membered saturated heterocycle having one or two heteroatoms selected from O, S or N and three to six carbon atoms provided that at least one nitrogen atom is present, wherein said saturated heterocycle is optionally substituted by lower alkyl group, acyl group, di(lower)alkylamino(lower)alkanoyl group or imidoyl group, or R6 is â€ƒwherein Ak is lower alkyl group and Hal is halogen atom, X2 is oxygen atom, sulfur atom, â€”SO2â€”, â€”SO2NHâ€” or a single bond, X3 is â€”(CH2)mâ€” wherein m is 0 or an integer of 1 to 3, X4 is â€ƒor a single bond, X5 is alkylene group having 1 to 6 carbon atoms, alkenylene group having 2 to 6 carbon atoms, or a single bond, j is 1, k is 0 or 1, and m and n are the same or different and each is 0 or an integer of 1 to 3; and R1, R2 and R3 are the same or different and each is hydrogen atom, hydroxy group, lower alkyl group or aryl group, provided that when X4 is a single bond, R6 is hydrogen atom, carboxy group, lower alkoxycarbonyl group, aryl group or heteroaryl group (the aryl or heteroaryl group is optionally substituted by 1 to 3 substituents selected from the group consisting of lower alkyl group, hydroxy group, lower alkoxy group, carboxy group, lower alkoxycarbonyl group, aralkyloxycarbonyl group, nitro group, amino group, acylamino group, amidino group and hydroxyamidino group), or a pharmaceutically acceptable salt thereof.