4-amino-6, 7-dimethoxy-2-piperazinylquinazoline derivatives,...

C - Chemistry – Metallurgy – 07 – D

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C07D 403/04 (2006.01) C07D 239/95 (2006.01)

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CA 1154765

ABSTRACT Compounds of formula (1): (I) Image in which: m is 2 or 3, and R represents a C2-C9 alkenyl group, a C2-C9 alkynyl group, a C4-C9 alkadienyl group, a group of formula: Image (where: R1 represents a hydrogen atom or an alkyl group and the two groups R1 may be the same or different, R2 represents a phenyl group optionally having one or more alkyl, alkoxy or halogen substituents, R3 represents an alkyl group, an alhoxy group, a hydroxy group, a halogen atom, or a group of formula -[O(CR12)? R2] and, where there is more than one group R3, they may be the same or different, n is 0 or an integer from 1 to 3, and p is 0, 1 or 2), a group of formula: Image (where: A represents a bivalent saturated aliphatic hydrocarbon group, Y represents an oxygen atom or a sulphur atom, q is 0 or 1, R4 represents an alkyl group, a hydroxy group, an alkoxy group, a halogen atom or an amino group optionally having one or two alkyl and/or acyl substituents, and n is as defined above), a group of formula: Image (where: r is an integer from 1 to 5), or a group of formula: Image (where: KS represents a hydrogen atom, an alkyl group, an alkoxy group or a halogen atom, one of the symbols R6 represents a hydrogen atom, a phenyl group or a substituted phenyl group having one or more alkyl, alkoxy or halogen atom substituents and the other symbols R6 all represent hydrogen atoms, R7 represents a hydrogen atom, an alkyl group or a halogen atom, and q and r are as defined above; provided that, when q is 0, one of the symbols R6 represents a substituted or unsubstituted phenyl group), and pharmaceutically acceptable acid addition salts thereof are useful as antihypertensive agents and may be prepared either by reacting a 4-amino-2-halo-6,7- dimethoxyquinazoline with a piperazine or homopiperazine derivative having a -COR group at the 1- position or by reacting a compound corresponding to the compound of formula (I) which it is desired to obtain but in which the -COR group is replaced by a hydrogen atom)with an acid of formula HOOC-R or with a reactive derivative of such an acid.

370761

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