Xanthines in the 7th position with a benzyl acetic acid moiety

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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544268, 544269, 544270, 544271, A61K 3152, C07D47308, C07D47322, C07D47306

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057144940

ABSTRACT:
Substituted xanthines of formula ##STR1## in which A represents a radical of the formula ##STR2## in which R.sup.3, R.sup.4, R.sup.6 and R.sup.7 denote hydrogen, cycloalkyl, aryl having 6 to 10 carbon atoms, or denote straight-chain of branched alkyl or alkenyl, each of which is optionally substituted; T, V, X and Y are identical or different and denote an oxygen or sulphur atom; R.sup.5 and R.sup.8 are identical or different and denote hydrogen, halogen, cycloalkyl having 3 to 8 carbon atoms or straight-chain or branched alkyl or alkenyl in each case having up to 8 carbon atoms, optionally substituted or R.sup.5 and R.sup.8 denote aryl having 6 to 10 carbon atoms or a 5- to 7-membered aromatic, optionally benzo-fused heterocycle having up to 3 heteroatoms S, N and/or O, each of which is optionally substituted; L represents an oxygen or sulphur atom; R.sup.2 represents mercapto, hydroxyl, straight-chain or branched alkoxy having up to 8 carbon atoms or the group of the formula ##STR3## in which R.sup.13 denotes hydrogen or straight-chain or branched alkyl having up to 4 carbon atoms; R.sup.14 denotes hydrogen, phenyl or a 5- to 6-membered aromatic heterocycle having up to 3 heteroatoms S, N and/or O; and R.sup.15 denotes hydrogen or straight-chain or branched alkyl having up to 8 carbon atom, optionally substituted by hydroxyl, and their salts are prepared by reaction of the suitable unsubstituted xanthines with halogenomethylphenylacetic acids and subsequent reaction of the carboxylic esters or acids with phenylglycinolamine. The substituted xanthines are suitable as active compounds in medicaments, in particular in antiatherosclerotic medicaments.

REFERENCES:
patent: 4061753 (1977-12-01), Bodor
patent: 5352687 (1994-10-01), Muller et al.
patent: 5420149 (1995-05-01), Muller et al.
patent: 5521206 (1996-05-01), Muller et al.
patent: 5527809 (1996-06-01), Muller-Gliemann et al.
F. Carey, "Organic Chemistry" (2nd Edition), p. 1217 (1992).

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