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US 5,041,449 AGranted
4-(nucleoside base)-substituted-1,3-dioxolanes useful for treatment of retroviral infections
AssigneeIAF BioChem International, Inc.
InventorsBernard Belleau, Dilip Dixit, Nghe Nguyen-Ba
Life of this patent
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Abstract
There are provided novel 2-substituted-4-substituted-1,3-dioxolanes which are particularly useful as antiviral agents.
Claims6
A 1,3-dioxolane derivative of the general formula L, the geometric and optical isomers thereof and mixtures of these isomers:
- ##STR11## wherein:
- R.sub.1 is selected from the group consisting of hydrogen, an aliphatic acyl group having 2 to 16 carbon atoms, benzoyl and a benzoyl substituted in any position by a halogen, a lower alkyl, a lower alkoxy, a nitro or a trifluoromethyl group;
- R.sub.2 is a heterocyclic radical selected from:
- ##STR12## wherein R.sub.3 is selected from the group consisting of hydrogen and lower alkyl radicals having from 1 to 3 carbon atoms;
- R.sub.4 is selected from the group consisting of hydrogen, lower alkyl or alkenyl radicals having from 1 to 3 carbon atoms;
- and
- R.sub.5 is selected from the group consisting of lower alkyl or alkenyl radicals having from 1 to 3 carbon atoms, fluoro and iodo.
4 more elements
A method for treating retroviral infections by administering to an infected host a therapeutically effective amount of a 2-substituted-4-substituted-1,3-dioxolane of Formula (L), the geometric and optical isomers thereof, and mixtures of those isomers:
- ##STR13## wherein:
- R.sub.1 is selected from the group consisting of hydrogen, an aliphatic acyl group having 2 to 16 carbon atoms, benzoyl and a benzoyl substituted in any position by a halogen, a lower alkyl, a lower alkoxy, a nitro or a trifluoromethyl group;
- R.sub.2 is a heterocyclic radical selected from:
- ##STR14## wherein R.sub.3 is selected from the group consisting of hydrogen and lower alkyl radicals having from 1 to 3 carbon atoms;
- R.sub.4 is selected from the group consisting of hydrogen, lower alkyl or alkenyl radicals having from 1 to 3 carbon atoms;
- and
- R.sub.5 is selected from the group consisting of lower alkyl or alkenyl radicals having from 1 to 3 carbon atoms, fluoro and iodo.
4 more elements
Dependencies are inferred from the claim text.