Phosphoramidates and methods therefor

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...

Reexamination Certificate

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C514S007600, C514S043000, C514S049000, C514S075000, C514S119000

Reexamination Certificate

active

06903081

ABSTRACT:
Novel phosphoramidate derivatives of hydroxy functional or amino functional compounds, including amino acids, peptides, peptidomimetics and nucleotide analogs, are described. The compounds enable enhanced intracellular delivery of drugs as their corresponding phosphate esters or amides. Described phosphoramidate compounds exhibit antiproliferative activity. Pharmaceutical formulations are provided for treatment of cancers.

REFERENCES:
patent: 5472956 (1995-12-01), Borch et al.
patent: WO 93/06120 (1993-04-01), None
“The Synthesis of O-monosaccharidyl-methoxycarbonyl-phosphonamidates by Arbuzov reaction” R. Y. Chen, et al. Chinese Chemical Letters, vol. 6, no. 1, 1995, pp. 23-26.
“Design and Synthesis of Lipophilic Phosphoramidate d4T-MP Prodrugs Expressing High Potency Against HIV in Cell Culture: Structural Determinants For In Vitro Activity and QSAR” A. Q. Siddiqui, et al., Journal of Medicinal Chemistry, vol. 42, No. 20, 1999, pp. 4122-4128.
“Phosphoramidates as Potent Prodrugs of Anti-HIV Nucleotides: Studies in the Amino Region,” C. McGuigan, et al. Antiviral Chemistry & Chemotherapy, vol. 7, No. 1, 1996, pp. 31-36.
“Design and Synthesis of Novel Nucleotide Prodrugs,” Caren F. Meyers, et al., American Association for Cancer Research 2000, Abstract No. 100710.

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