Inventors:
Mark Becker - Belmont CA, US
Harlan Chapman - La Honda CA, US
Tomas Cihlar - Foster City CA, US
Eugene Eisenberg - San Carlos CA, US
Gong-Xin He - Fremont CA, US
Michael Kernan - Pacifica CA, US
William Lee - Los Altos CA, US
Ernest Prisbe - Los Altos CA, US
John Rohloff - Mountain View CA, US
Mark Sparacino - Morgan Hill CA, US
International Classification:
C12Q001/70
Abstract:
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 (5)
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.