S-substituted 1,3,7-trialkyl-xanthine derivatives

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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544229, 544267, 544271, 544272, 544273, C07D47312, C07D47306, A61K 3152

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active

058614052

ABSTRACT:
The present invention provides 8-substituted 1,3,7-trialkylxanthines useful as A.sub.2 -selective adenosine receptor antagonists and compositions comprising such compounds. Examples of the 8-substituted 1,3,7-trialkyl xanthines include: ##STR1## In compound (a), R.sub.1, R.sub.3, and R.sub.7 are methyl and X is one to three substituents, which may be the same or different and selected from the group consisting of amino, C.sub.1 -C.sub.4 alkylcarbonylamino, carboxy C.sub.2 -C.sub.4 alkylcarbonylamino, halo, C.sub.1 -C.sub.3 alkyloxy, amino C.sub.1 -C.sub.4 alkyloxy, C.sub.1 -C.sub.4 alkyloxy carbonylamino, amino C.sub.1 -C.sub.4 alkenyloxy, isothiocyanato, and diazonium tetrafluoroborate. In compound (b), R.sub.1, R.sub.3, and R.sub.7 are methyl, R.sub..beta. is hydrogen or methyl, and X is selected from the group consisting of R, C(.dbd.O)OR, and C(.dbd.O)NH--R, wherein R is a C.sub.1 -C.sub.6 alkyl.

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