Patent ID: 6358954
Filing Date: 2002-03-19
Classification: A61P,C07D

Abstract:
A substantially purified tyrphostin isomer of a general formula: wherein,4, 5, 6, 7, 8 and 9 indicate positions on a terminal 6-member aromatic ring; A, D, X and Y are each a nitrogen; B is a carbon; R1, R3, R5 and R7 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, hydroxy, alkoxy, halo, carbonyl, thiocarbonyl, guanyl, sulfonyl, trihalomethane-sulfonyl and a pair of electrons; R2 is selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, hydroxy, alkoxy, halo, C-carboxy, carbonyl, thiocarbonyl, C-amido, guanyl, sulfonyl and trihalomethane-sulfonyl; or alternatively, R1 and R2 or R2 and R3 form a 5-7 member ring structure; R6 is selected from the group consisting of alkyl, trihaloalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, heteroalicyclic ring, hydroxy, alkoxy, aryloxy, thiohydroxy, thioalkoxy, thioaryloxy, sulfinyl, sulfonyl, trihalomethylsulfonamido, carbonyl, thiocarbonyl, C-carboxy, C-amido, cyano, nitro, halo, ureido, guanyl, guanidino, amino and a physiologically acceptable salt or an ester thereof; R4 and R8 are each independently selected from the group consisting of hydrogen, alkyl, trihaloalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, heteroalicyclic ring, hydroxy, alkoxy, aryloxy, thiohydroxy, thioalkoxy, thioaryloxy, sulfinyl, sulfonyl, trihalomethylsulfonamido, carbonyl, thiocarbonyl, C-carboxy, C-amido, cyano, nitro, halo, ureido, guanyl, guanidino, amino and â€”NR10R11, and, a physiologically acceptable salt or an ester thereof; R10 and R11, are each independently selected from the group consisting of hydrogen, alkyl, cycloalkyl, aryl, carbonyl and sulfonyl, or alternatively R10 and R11 form a five- or six-member heteroalicyclic ring; and, a physiologically acceptable salt or an ester thereof; whereas said R is at position 6; the tyrphostin isomer being capable of inhibiting PDGF receptor kinase activity.