5-Substituted pyrimidine derivatives of conformationally locked nucleoside analogues
AssigneeThe United States of America as represented by the Department of Health and Human Services
InventorsVictor E. Marquez, Pamela L. Russ
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Abstract
The embodiments described herein concern 5-substituted pyrimidine derivatives of conformationally locked nucleoside analogues and to the use of these derivatives as anti-viral and anti-cancer agents. The compounds are of the formula: wherein B is uracil-1-yl or cytosin-1-yl having a 5-substituent selected from halogen, alkyl, alkenyl, and alkynyl, with the proviso that where B is uracil-1-yl, the 5-substituent is not methyl. The compounds are useful in the treatment of Herpes simplex virus (HSV).
Claims37
A conformationally locked nucleoside analogue comprising the formula:
- wherein B is
- a 5-substituted cytosin-1-yl and the 5-substituent is a member of the group consisting of F, Cl, Br, I, CH═CH2, C≡CH, C≡CHCH3, CH═CHF, CH═CHCl, CH═CHBr, and CH═CHI.
A conformationally locked nucleoside analogue comprising the formula:
- wherein B is uracil-1-yl having a 5-substituent, wherein the 5-substituent is bromine.
A conformationally locked nucleoside analogue comprising the formula:
- wherein B is uracil-1-yl having a 5-substituent, wherein the 5-substituent is iodine.
A conformationally locked nucleoside analogue comprising the formula:
- wherein B is uracil-1-yl having a 5-substituent wherein the 5-substituent is bromovinyl.
A pack comprising a conformationally locked nucleoside analogue in unit dosage form, wherein the conformationally locked nucleoside analogue comprises the formula:
- wherein B is uracil-1-yl having a 5-substituent or cytosin-1-yl having a 5-substituent, wherein the 5-substituent is selected from the group consisting of halogen, alkyl alkenyl, and alkynyl.
Dependencies are inferred from the claim text.