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Generated: June 23, 2018

DrugPatentWatch Database Preview

Details for Patent: 5,041,449

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Title: 4-(nucleoside base)-substituted-1,3-dioxolanes useful for treatment of retroviral infections
Abstract:There are provided novel 2-substituted-4-substituted-1,3-dioxolanes which are particularly useful as antiviral agents.
Inventor(s): Belleau; Bernard (Westmount, CA), Dixit; Dilip (Roxboro, CA), Nguyen-Ba; Nghe (La Prairie, CA)
Assignee: IAF BioChem International, Inc. (Montreal, CA)
Filing Date:Jun 29, 1990
Application Number:07/546,676
Claims:1. 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.

2. The compound of claim 1. which is the 2-acetoxymethyl-4-(thymin-1'-yl)-1,3-dioxolane.

3. The compound of claim 1 which is the 2-hydroxymethyl-4-(thymin-1'-yl)-1,3-dioxolane.

4. The compound of claim 1 which is the 2-benzoyloxymethyl-4-(cytosin-1'-yl)-1,3-dioxolane.

5. The compound of claim 1 which is the trans-2-hydromethyl-4-(cytosin-1'-yl)-1,3-dioxolane.

6. 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.

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Serving hundreds of leading biopharmaceutical companies globally:

Cerilliant
Colorcon
McKinsey
Citi
Farmers Insurance
Dow
Medtronic
Harvard Business School
UBS

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