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Last Updated: March 28, 2024

Claims for Patent: 5,821,236


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Summary for Patent: 5,821,236
Title: Tumor treatment with arabinofuranosyl purine derivatives
Abstract:6-Alkoxy derivatives of Ara-G, and pharmaceutically acceptable esters thereof, are described as being useful in tumor therapy. Novel pharmaceutically acceptable esters, their preparation and pharmaceutical formulations containing them are also disclosed.
Inventor(s): Krenitsky; Thomas Anthony (Chapel Hill, NC), Averett; Devron Randolph (Raleigh, NC), Koszalka; George Walter (Chapel Hill, NC)
Assignee: Glaxo Wellcome Inc. (Research Triangle Park, NC)
Application Number:08/449,078
Patent Claims: 1. A method for the inhibition of susceptible tumours in a mammal which comprises administering to said mammal an effective tumour inhibiting amount of a compound of the formula (I) ##STR2## wherein R.sup.1 is a C.sub.1-5 alkoxy group or a pharmaceutically acceptable ester or salt thereof.

2. A method according to claim 1 wherein R.sup.1 is methoxy.

3. The method of claim 1, wherein said compound is selected from the group consisting of

9-(3,5-di-O-Acetyl-.beta.-D-arabinofuranosyl)-2-amino-6-methoxy-9H-purine,

9-(2,5-di-O-Acetyl-.beta.-D-arabinofuranosyl)-2-amino-6-methoxy-9H-purine,

9-(2-O-Acetyl-.beta.-D-arabinofuranosyl)-2-amino-6-methoxy-9H-purine,

9-(2,3,5-tri-O-Acetyl-.beta.-D-arabinofuranosyl)-2-amino-6-methoxy-9H-purin e,

9-(5-O-isobutyryl-.beta.-D-arabinofuranosyl)-2-amino-6-methoxy-9H-purine,

9-(2,3-di-O-Acetyl-.beta.-D-arabinofuranosyl)-2-amino-6-methoxy-9H-purine, and

2-amino-6-methoxy-9-(5-O-acetyl-.beta.-D-arabinofuranosyl)-9H-purine,

or a pharmaceutically acceptable salt thereof.

4. The method of claim 1, wherein said compound is 2-amino-6-methoxy-9-(5-O-acetyl-.beta.-D-arabinofuranosyl)-9H-purine.

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