L-nucleoside analogues and pharmaceutical compositions

Details L-nucleoside analogues and pharmaceutical compositions L-nucleoside analogues and pharmaceutical compositions

1995-08-18

1998-05-05

Kight, John

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514 46, 514 49, 514 50, 514 51, 514 81, 514 86, 536 2623, 536 2626, 536 267, 536 268, 536 276, 536 278, 536 2781, 536 285, 536 2851, 536 2852, 536 2853, 536 2854, 536 2855, 544264, 544265, 544323, 544322, 544298, 544309, 544326, 544242, C07H 1910, C07H 1920, A61K 3170

Patent

active

057474737

ABSTRACT:
##STR1## Novel antiviral compounds of formulae (1A) and (1B), wherein X and R.sub.1 -R.sub.4 are as stated in claim 1 in the form of an .alpha.- or .beta.-anomer or a mixture thereof, and pharmaceutically acceptable salts thereof, are disclosed, as well as a new method for preparation thereof. Said compounds can be used for treatment of infections caused by viruses requiring reverse transcriptase for replication, such as HIV and hepatitis B virus.

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Okabe et al., "Synthesis of Dideoxynucleosides ddC and CNT from Glutamic Acid, Ribonolactone, and Pyrimidine Bases," J. Org. Chem., 53(20), 4780-4786 (1988).
Chong et al., "Facile Preparation of (2R,3S)-and Epoxidation," J. Org. Chem., 52(12), 2596-2598 (1987).
Barr et al., "The Synthesis of Nucleosides Derived From 5-Ethynyluracil and 5-Ethynylcytosine," J. Chem. Soc., Perkin Trans. I, (10), 1263-1267 (1978).
Swierkowski et al., "A Nonmutagenic Thymidine Analog with Antiviral Activity. 5-Ethyldeoxyuridine," J. Medicinal Chem., 12, 533-534 (May 1969) .

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