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AssigneeUniversity of Georgia Research Foundation, Inc.
InventorsChung K. Chu, Lakshmi P. Kotra, Konstantine K. Manouilov, Jinfa Du, Raymond Schinazi
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Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2′-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.
A pharmaceutical composition comprising:
N6-azido-β-D-3′-deoxyribofuranosyl purine, or a monophosphate, diphosphate or triphosphate or pharmaceutically acceptable salt thereof.
6-azido-2′,3′-dideoxy-2′-fluoro-β-D-arabinofurasylpurine or a monophosphate, diphosphate or triphosphate or pharmaceutically acceptable salt thereof.
9-(β-D-arabinofuranosyl)-6-azidopurine or a monophosphate, diphosphate or triphosphate or pharmaceutically acceptable salt thereof.
2-amino-6-azido-1,9-dihydro9[(2-hydroxyethoxy)methyl]-purineoramonophosphate, diphosphate or triphosphate or pharmaceutically acceptable salt thereof.
2-amino-6-azido-1,9-dihydro-9-[dihydroxymethyl]propyl-purine or a monophosphate, diphosphate or triphosphate or pharmaceutically acceptable salt thereof.
A method of increasing the half-life of a drug in a subject, which drug comprises an amino, carbonyl or hydroxy moiety, comprising the steps of:
A method for ameliorating a pathological condition in a patient, which pathological condition is capable of being ameliorated by a selected drug which comprises an amino, carbonyl or hydroxy moiety, comprising treating the patient with a therapeutically effective azide compound which is capable of metabolizing in vivo to said selected drug by replacement of an azide group thereof with an amino, carbonyl or hydroxy moiety to form said drug effective for the treatment of said pathological condition.
Dependencies are inferred from the claim text.