Prodrugs of phosphonate nucleotide analogues and methods for...

Details Prodrugs of phosphonate nucleotide analogues and methods for... Prodrugs of phosphonate nucleotide analogues and methods for...

C - Chemistry, Metallurgy

12

Q

C12Q 1/02 (2006.01) A61K 31/675 (2006.01) A61P 31/12 (2006.01) A61P 35/00 (2006.01) C07F 9/6561 (2006.01) C12Q 1/18 (2006.01) C12Q 1/70 (2006.01)

Patent

CA 2725819

A novel method is provided for screening prodrugs of methoxyphosphonate nucleotide analogues to identify prodrugs selectively targeting desired tissues with antiviral or antitumor activity. This method has led to the identification of novel mixed ester-amidates of PMPA for retroviral or hepadnaviral therapy, including compounds of structure (5a) having substituent groups as defined herein. Compositions of these novel compounds in pharmaceutically acceptable excipients and their use in therapy and prophylaxis are provided. Also provided is an improved method for the use of magnesium alkoxide for the preparation of starting materials and compounds for use herein.

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