Antiviral phosphonomethoxy nucleotide analogs having increased oral bioavailability
Patent 6043230 Issued on March 28, 2000. Estimated Expiration Date: 
May 19, 2019. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.
May 19, 2019. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.Patent ReferencesAntiviral (phosphonomethoxy)methoxy purine/pyrimidine derivatives Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability Patent #: 5922695 Inventors
ApplicationNo. 314606 filed on 05/19/1999US Classes:514/81, Nonshared hetero atoms in at least two rings of the polycyclo ring system514/86, Nitrogen atoms occupy 1 and 3- positions544/243, Phosphorus attached directly or indirectly to the diazine ring by nonionic bonding544/244Polycyclo ring system having the diazine ring as one of the cyclosExaminersPrimary: Shah, Mukund J.Assistant: Sripada, Pavanaram K. Attorney, Agent or FirmInternational ClassesA61K 031/675C07F 009/651.2 AbstractNovel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure -OC(R2)2 OC(O) X(R)a, wherein R2 independently is H, C1 -C12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro or OR3 in which R3 is C1 -C12 alkyl; X is N or O; R is independently H, C1 -C12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, axido, nitro, --O--, --N=, --NR4 --, --N(R4)2 -- or OR3, R4 independently is --H or C1 -C8 alkyl, provided that at least one R is not H; and a is 1 or 2, with the proviso that when a is 2 and X is N, (a) two R groups can be taken together to form a carbocycle or oxygen-containing heterocycle, or (b) one R additionally can be OR3. The compounds are useful as intermediates for the preparation of antiviral compounds or oligonucleotides, or are useful for administration directly to patients for antiviral therapy or prophylaxis. Embodiments are particularly useful when administered orally. |
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