HINAZOLIN DERIVATIVES AS MTKI

摘要

The present invention relates to compounds of formula (I), their N-oxide forms, pharmaceutically acceptable addition salts and stereochemically isomeric forms, where Z is NH; Y is -C-alkyl-, -C-alkyl-NR-C-alkyl-, -C-alkyl-NR-CO-C-alkyl-, -C-alkyl-NR-H-CO-NH-C-alkyl - or -C-alkyl-NR-CO-CRR-NH-; X is O or —O — C-alkyl-; X is a direct bond, C-alkyl, -CO-C-alkyl- or NR-C-alkyl; R is hydrogen or halogen; R is halogen, acetylene or Het; R is hydrogen or cyano; R 1 represents an Ar-C-alkyloxy group, a C-alkyloxy group or a C-alkyloxy group substituted with one or, where possible, two or more substituents selected from Het, NRR, a hydroxy group and a C-alkyloxy-C-alkyloxy group; R is hydrogen or C-alkyl; R is C-alkyl substituted with NR R or C-alkylsulfonyl; R is hydrogen or C-alkyl-; R 1 is Ar-sulfonyl or C-alkyloxycarbonyl optionally substituted with phenyl; R and R are hydrogen, C-alkyl or R and R, taken together with the carbon atom to which they are attached, form C-cycloalkyl; R is C-alkyl and R is hydrogen when R and R, taken together with the carbon atom to which they are bonded, form C-cycloalkyl; R, R, R and R, each independently, are hydrogen or C-alkylcarbonyl; Het means 2-boron-1,3-dioxolanyl; Het means piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl or 1,1-dioxothiomorpholinyl, wherein said Het is optionally substituted with C-alkyloxycarbonyl or NRR-C-alkyl; Ar and Ar are phenyl; Ar is phenyl optionally substituted with a nitro group.