Lithocholic acid analogues that inhibit sialyltransferase
AssigneeAcademia Sinica
InventorsWen-Shan Li, Yi-Ching Wang, Hsueh-Fen Juan
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Abstract
Certain chemical entities chosen from compounds of Formula I: and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof are described. Pharmaceutical compositions comprising at least one chemical entity chosen from compounds of Formula I and a pharmaceutically acceptable vehicle are described. Also described are methods for inhibiting α-2,3-sialyltransferase activity in cells, and methods for treating a patient having a disease responsive to inhibition of α-2,3-sialyltransferase activity.
Claims24
At least one chemical entity chosen from the compounds of Formula I:
- and pharmaceutically acceptable salts thereof, wherein
- R1 is —CHR4(CH2)nR5 where
- n is chosen from 2 and 3,
- R4 is chosen from hydrogen and optionally substituted lower alkyl;
- and
- R5 is an optionally substituted triazole;
- R2 is chosen from hydroxy and acyloxy;
- R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form an oxo group.
At least one chemical entity chosen from
- (3R,5R,10S,13R,14S)-17-((R)-5-(4-(2-hydroxyethyl)-1H-1,2,3-triazol-1-yl)pentan-2-yl)-10,13-dimethyl-hexadecahydro-1H-cyclopenta[a]phenanthren-3-ol;
- 2-amino-3-(1-((R)-4-((3R,5R,10S,13R,14S)-3-hydroxy-10,13-dimethyl-hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentyl)-1H-1,2,3-triazol-4-yl)propanoic acid;
- 2-(diethoxyphosphoryl)-3-(1-((R)-4-((3R,5R,10S,13R,14S)-3-hydroxy-10,13-dimethyl-hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentyl)-1H-1,2,3-triazol-4-yl)propanoic acid;
- 3-(1-((R)-4-((3R,5R,10S,13R,14S)-3-hydroxy-10,13-dimethyl-hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentyl)-1H-1,2,3-triazol-4-yl)propanoic acid;
- 4-(1-((R)-4-((3R,5R,10S,13R,14S)-3-hydroxy-10,13-dimethyl-hexadecahydro-1H-cyclopenta[a]phenanthren-17-yl)pentyl)-1H-1,2,3-triazol-4-yl)butanoic acid;
- and pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.