Thymidylate analogs and the use thereof

Details Thymidylate analogs and the use thereof Thymidylate analogs and the use thereof

1996-08-21

1998-06-02

Wilson, James O.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

514 50, 514885, 536 221, 536 231, 536 2534, 536 256, 536 268, 536 282, 536 2854, A61K 3170

Patent

active

057600139

ABSTRACT:
Novel thymidylate analogs having the following formula are synthesized in the present invention, which are found active against human immunodeficiency virus type 1 (HIV-1): ##STR1## wherein R.sup.1 is hydrogen, cyano (--CN), halogen or azido (--N.sub.3); R.sup.2 is hydroxyl or an amino ester radical having a formula of --NHR.sup.4 COOR.sup.5, wherein R.sup.4 is a bivalent C.sub.1 -C.sub.4 saturated hydrocarbon and R.sup.5 is C.sub.1 -C.sub.4 alkyl; Me is methyl; and R.sup.3 is hydroxyl or thymidinyl having a formula as follows: ##STR2##

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