US 5,708,000 A · N4-substituted cytosinyl 1,3-oxathiolane nucleoside analogues, and their antiviral activity

Abstract

The present invention pertains to the field of organic chemistry, and particularly therapeutic chemistry. The invention provides cis-form 5-(cytosinyl-1) 1,3-oxathiolanes of general formula (I), wherein R is an acyl or aralkoyl radical, derivatized from a nitrogen monocyclic or bicyclic heterocycle, and the hydroxymethyl group in position 2 is in cis position in relation to the plane defined by positions 2 and 5. The compounds of general formula (I) are useful as active ingredients in pharmaceutical compositions, particularly with antiviral activity.

Claims15

Dependent claims

A 5-(cytosinyl-1) 1,3-oxathiolane of cis configuration (2R-5S) or (2S-5R) of the formula ##STR10## wherein R is an acyl group derived from a monocyclic or bicyclic nitrogenous heteroring or aralkyl derived from a monocyclic or bicyclic nitrogenous heteroring and its non-toxic, pharmaceutically acceptable acid addition salts.

Dependencies are inferred from the claim text.

Facts

Application

08/586,892Filed 25 Mar 1996

Priority

FR 94 0626224 May 1994

Granted

13 Jan 1998

Term ends

Not estimatedThe source records don’t support an estimate.

Classification7 codes

C07D 411/14
Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen and sulfur atoms as the only ring hetero atoms:…
A61P 31/12
Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics: antivirals
A61P 37/04
Immunomodulators: immunostimulants
C07F 7/1804
Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages: compounds having Si-O-C linkages

N4-substituted cytosinyl 1,3-oxathiolane nucleoside analogues, and their antiviral activity

Life of this patent

N4-substituted cytosinyl 1,3-oxathiolane nucleoside analogues, and their antiviral activity

Life of this patent

Abstract

Claims15