Antiviral, highly water soluble, stable, crystalline salts of 2′, 3′-dideoxyinosine, 2′, 3′-dideoxy-2′, 3′-didehydrothymidine and 2′, 3′-dideoxy-2′-fluoroinosine
AssigneeBristol-Myers Squibb Company
InventorsJoseph B. Bogardus, Murray A. Kaplan, Robert K. Perrone
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Abstract
Provided are very highly water soluble, stable, crystalline salts of 2′,3′-dideoxy-2′,3′-didehydrothymidine (“d4T”), 2′,3′-dideoxyinosine (“ddI”), and 2′,3′-dideoxy-2′-fluoroinosine (“F-ddI”). Such salts are useful as intermediates or as antiviral agents.
Claims24
A highly water soluble, stable, crystalline salt of 2′,3′-dideoxy-2′,3′-didehydrothymidine of Formula (I):
- wherein X is an alkali or alkaline earth metal ion, an ammonium ion or a quaternary amino ion and n is 0.5 to 2.0.
Sodium 2′,3′-dideoxy-2′,3′didehydrothymidine monohydrate.
Potassium 2′,3′-dideoxy-2′,3′-didehydrothymidine monohydrate.
A highly water soluble, stable, crystalline sodium salt of 2′,3′-dideoxyinosine of Formula
- wherein X is an alkali or alkaline earth metal ion, an ammonium ion or a quaternary amino ion and n is 0.5 to 2.0.
Sodium 2′,3′-dideoxyinosine monohydrate.
Potassium 2,3′-dideoxyinosine hemihydrate.
A highly water-soluble, stable, crystalline salt of 2′,3′-dideoxy-2′-fluoroinosine of Formula (III):
- wherein X is an alkali or alkaline earth metal ion, an ammonium ion or a quaternary amino ion and n is 0.5 to 2.0.
Sodium 2′,3′-dideoxy-2′-fluoroinosine hemihydrate.
Dependencies are inferred from the claim text.