Modified 5′-phosphonate...

Details Modified 5′-phosphonate... Modified 5′-phosphonate...

2011-08-16

2011-08-16

Crane, Lawrence E (Department: 1623)

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

C514S051000

Reexamination Certificate

active

07999099

ABSTRACT:
The invention relates to the field of molecular biology, virology and medicine and, more specifically, to novel derivatives of 3′-azido-3′-deoxythymidine phosphonates with the following general formulawhere R=alkyl groups, including those containing halogen atoms, carboxy-, hydroxy-, alkoxy- and acyloxy- groups as well as substituted aminocarbonyl groups. The compounds can be used as antiviral agents as they have low toxicity and can effectively inhibit replication of type 1 immunodeficiency virus in MT-4 cell culture and generate AZT in mammalians ensuring a gradual increase of its concentration in the blood.

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patent: WO92/00988 (1992-01-01), None
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(S) Shirokova et al. (II), “New Phosphonoformic Acid Derivatives of 3′-Azido-3′-deoxythymidine,” Russian Journal of Bioorganic Chemistry, 30(3), 242-249 (2004): for Abstract see CAPLUS Search Notes; Answer 7 of 10.
(T) Shirokova et al. (III), “New Lipophilic Derivatives of AZT and d4T 5′-Phosphates,” Nucleosides, Nucleotides & Nucleic Acids, 22(5-8), 981-985 (2003); CAPLUS entry date: Sep. 11, 2003: for Abstract see Search Notes; Answer 9 of 10.
(U) Orlov et al., “Investigation of Nucleoside and Nucleotide Derivatives by Plasma Desorption Mass Spectrometry,” Molekulyarnaya Biologiya (Moscow),. 28(3), 708-713 (1994): for Abstract see CAPLUS Search Notes: Answer 10 of 10.
(V) Casara et al., “Synthesis of Acid Stable 5′-o-fluoromethylphosphonates of Nucleosides. Evaluation as Inhibitors of Reverse Transcriptase,” Bioorganic & Medicinal Chemistry Letters, 2(2), 145-148 (1992); only Abstract supplied.

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