4,5-DIAMINOPYRIMIDINE DERIVATIVES AND A METHOD FOR THE PREPARATION THEREOF

摘要

Novel 4,5-diamino pyrimidine derivatives having the inhibitory activity of cyclic guanosine 3',5'-monophosphate phosphodiesterase and tumor necrosis factor, physiologically acceptable salt, solvate or metabolically readily conversible ester thereof and a process for producing the same are described. The present compounds are represented as general formula (I) in which X is a direct bond, C1-4 alkylene, C1-4 alkyleneoxy, C1-4 alkoxyphenyl or phenyl C1-4 alkylene; Y is a direct bond or C1-2 alkyl; R<1> is (i) 5-15 membered cyclic or branched chain heterocompound which includes one or two selected from a group consisting of nitrogen, oxygen and sulfur and which is substituted with one or two selected from a group consisting of hydrogen, halogen, nitro, hydroxy, C1-6 alkyl, C3-6 alkenyl and halogen C1-4 alkoxy, (ii) C4-10 carbocyclic compound or (iii) hydroxy C1-4 alkoxy; R<2> is 5-15 membered cyclic or branched chain heterocompound which includes one or two selected from a group consisting of nitrogen, oxygen and sulfur and which is substituted with one or two selected from a group consisting of hydrogen, hydroxy, halogen, nitro, hydroxy C1-5 alkyl, C1-6 alkyl, C3-6 alkenyl and halogen C1-4 alkoxy; R<3> is hydrogen, (a) or (b) in which R<4> and R<5> are each independently selected from a group consisting of hydroxy, C1-6 alkyl, C3-7 cycloalkyl, C3-6 alkenyl, halogen C1-6 alkyl, halogen C2-6 alkenyl and C1-4 alkoxy or R<4> and R<5> represent each independently (c) in which R<6> is selected from a group consisting of hydrogen, hydroxy, C1-6 alkyl, C3-6 alkenyl, halogen C1-6 alkyl, halogen, nitro and C1-4 alkoxy.