Patent ID: 6271212
Filing Date: 2001-08-07
Classification: A61K,A61P,C07H

Abstract:
A prodrug pharmaceutical composition comprising:a) a An azide derivative of a biologically active therapeutic purine, pyrimidine nucleoside or phosphorylated nucleoside compound other than 3'-deoxy-3'-azidothymidine (AZT) or a mono-, di- or tri-phosphate ester thereof, which compound has an active amino, oxygen or hydroxy substituent, wherein in said azide derivative an azide group replaces said amino, oxygen or hydroxy substituent, said azide derivative being capable of being converted to said biologically active therapeutic compound in vivo by replacement of said azide group with said amino, oxygen or hydroxy substituent of said biologically active therapeutic compoundb) in combination with a pharmaceutically acceptable carrier;wherein the prodrug azide derivative is selected from the group consisting ofi) 6-azido-(2,3-dideoxy-.beta.-D-glyceropentofuranosyl)purine,ii) 9-(.beta.-D-arabinofuranosyl)-6-azidopurine (6-AAP),iii) 6-azido-9-(3-deoxy-.beta.-D-ribofuranosyl)purine,iv) 4-azido-5-fluoro-2(1H)-pyrimidinoine,v) 4-azido-1-(.beta.-D-arabinofuranosyl)-2(1H)-pyrimidinone,vi) 2,4-diazido-5-(3,4,5-trimethoxybenzyl)pyrimidine,vii) 4-azido-5-fluoro-1-(.beta.-D-arabinofuranosyl)-2(1H)-pyrimidinone,viii) 2-chloro-6-azido-9-(2-deoxy-.beta.-D-arabinofuranosyl)purine,ix) 6-azido-9-(2-fluoro-2,3-dideoxyarabinofuranosyl)purine, andx) 2-amino-6-azido-9-{3,3-di(hydroxymethyl)propyl}-purine,wherein the individual therapeutic compounds produced in vivo arei) 2',3'-dideoxyinosine (ddI),ii) arabinofuranosyladenine (araA),iii) 3'-deoxyadenosine (cordycepin),iv) 5-fluorocytosine (flucytosine),v) 1-(.beta.-D-arabinofuranosyl)cytosine (cytarabine),vi) 2,4-diamino-5-(3,4,5-trimethoxybenzyl)pyrimidine (tri-methoprim),vii) 5-fluoro-1-(.beta.-D-arabinofuranosyl)cytosine,xiii) 2-chloro-9-(2-deoxy-.beta.-D-arabinofuranosyl)adenine,ix) 9-(2-fluoro-2,3-dideoxyarabinofuranosyl)purine (2'-F-ara-ddI), andx) 2,6-diamino-9-{3,3-di(hydroxymethyl)propyl}purine (penciclovir), respectively.