Patent Evaluation: Inhibition of Purine Nucleoside Phosphorylase: Current Opinion on Therapeutic Patents: Vol 2, No 8

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Summary

Novelty: Xanthines are disclosed which are said to inhibit purine nucleoside phosphorylase (PNPase) and thus may be effective antiviral agents.

Biology: The purification of PNPase and an assay for its inhibition are described. IC₅₀ values for the compounds range from 1 nM to 5μM. 3-(2-Amino-1,1-dihydro-6-oxo-9H-purinyl)-methyl)benzylthio)methyl phosphonic acid gave an IC₅₀= 1.1 nM.

Chemistry: The preparation of fourteen compounds is described in detail. The aforementioned compound is the only explicitly claimed compound.

Structure:

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Patent Evaluation: Inhibition of Purine Nucleoside Phosphorylase

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Patent Evaluation: Inhibition of Purine Nucleoside Phosphorylase

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