Anti-tumour agents

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 239/88 (2006.01) C07D 239/90 (2006.01) C07D 239/96 (2006.01) C07D 401/12 (2006.01) C07D 409/12 (2006.01)

Patent

CA 1301756

A B S T R A C T ANTI-TUMOUR AGENTS A quinazoline of the formula:- Image wherein R1 is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkylthio, aryl, aryloxy, arylthio, arylalkyl, halogeno, hydroxy or mercapto, or substituted alkyl or alkoxy wherein R2 is hydrogen, alkyl, alkenyl or alkynyl, or substituted alkyl or alkanoyl: wherein Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or bears one or more substituents; wherein R3 is such that R3 NH2 is an amino acid wherein R4 is hydrogen or alkyl; wherein R5 is hydrogen or alkyl; and wherein each of R6, R7 and R8 is hydrogen, hydroxy, alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, phenyl, halogeno, nitro, cyano or amino, or substituted alkyl, alkoxy or alkylthio: provided that at least one of R4, R5, R6, R7 and R8 is other than hydrogen or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumour activity.

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