Nucleoside compounds and uses thereof
AssigneeRibapharm, Inc.
InventorsZhi Hong, Jean-Luc Girardet, Kanda Ramasamy, Johnson Lau
Life of this patent
Estimating the term…
Abstract
Nucleosides, novel nucleoside analog compounds and their novel prodrug forms are disclosed. The novel compounds, prodrugs, or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Type 1 and Type 2 activity.
Claims6
A nucleoside analog of Formula 1, in which the sugar is either in the L- or D-configuration:
- 68
- wherein Z is O, CH2, or S;
- R is independently H, hydroxyl, protected hydroxyl or halogen;
- R1, R2, R3, R4, R5, are independently selected from H, halogen, CN, CH2OH, lower alkyl, vinyl, and acetylene radical;
- with the proviso that
- when R2 is hydroxyl, then, R that is attached to the same carbon as that of R2 is not halogen;
- when R3 is hydroxyl, then, R that is attached to the same carbon as that of R3 is not halogen;
- R6 is O-monoboranophosphate radical, O-diboranophosphate radical, O-triboranophosphate radical, O-monoboranophosphate derivative radical, O-diboranophosphate derivative radical, or O-triboranophosphate derivative radical;
- R7 is selected from H, alkyl, CH3COO—, CH3COO-phenyl-CH2—O—CO—, phenyl, —(CH2)n-COOH, coumarinic acid, salicylic acid, dithiosuccinoyl derivative radical, reductase mediated cleavable group, phosphonoformic acid radical, and phosphoramidate group radical;
- R8 is selected from H, H*HCl, H*HBr, lower alkyl, phenyl, CH3COO—, CH3COO— Phenyl-CH2—O—CO—, carbamate, and phenyl;
- and
- wherein the nucleoside analog optionally forms a pharmacologically acceptable salt with an acid or a base.
A nucleoside analog of Formula 2, in which the sugar is either in the L- or D-configuration:
- 69
- wherein X is O or NH;
- R1 is a masking group of the amino group;
- R2 is monoboranophosphate radical, diboranophosphate radical, triboranophosphate radical, monoboranophosphate derivative radical, diboranophosphate derivative radical, triboranophosphate derivative radical, monophosphate radical, diphosphate radical, triphosphate radical, stabilized monophosphate radical, stabilized diphosphate radical, or stabilized triphosphate radical;
- R3 is independently H or C1-C18 acyl;
- and
- wherein the nucleoside analog optionally forms a pharmacologically acceptable salt with an acid or a base.
A nucleoside analog of Formula 5, in which the sugar is either in the L- or D-configuration:
- 74
- wherein Y is O or NH;
- wherein X is R2 is monoboranophosphate radical, diboranophosphate radical, triboranophosphate radical, monoboranophosphate derivative radical, diboranophosphate derivative radical, triboranophosphate derivative radical, stabilized monophosphate radical, stabilized diphosphate radical, or stabilized triphosphate radical;
- and
- wherein the nucleoside analog optionally forms a pharmacologically acceptable salt with an acid or a base.
A nucleoside analog of Formula 6, in which the sugar is either in the L- or D-configuration:
- 75
- wherein the nucleoside analog optionally forms a pharmacologically acceptable salt with an acid or a base.
Dependencies are inferred from the claim text.