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US 2018/0244713 A1Published application
Sialyltransferase inhibitors and uses thereof
AssigneeAcademia Sinica
InventorsWen-Shan LI, Wen-Chun HUNG, Chia-Ning SHEN
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Abstract
Disclosed herein are novel sialyltransferase inhibitors, and compositions and methods for treating diseases and/or conditions associated with the activation of sialyltransferase, such as a cancer, an immune disease or an inflammatory disease.
Claims28
A compound having the structure of formula (1)
- and pharmaceutically acceptable salts and solvates thereof, wherein,
- n is an integral from 1 to 4;
- A, B, and C are independently a 6- or 7-membered saturated or unsaturated carbon cyclic ring, a homolactone or a homolactam, in which the saturated or unsaturated carbon cyclic ring, the homolactone or the homolactam is optionally substituted with one or more fluoro or hydroxy;
- X1 is O or N;
- or X1 is fluoro, provided that R1 is null;
- R1 is selected from the group consisting of null, H,
- R3 is selected from the group consisting of methyl, methoxy, RaCOOH, RaNH2, RaNHC(NH2)═NH, RaSRb,
- or
- R3 and the neighboring carbon and nitrogen atoms are taken together to form a 5-membered heterocyclic ring;
- Ra and Rb are independently H or C1-6 alkyl;
- R2 is COOH, CH(COOH)COOH, or COX2(CH2CH2O)mCH2CH2N3,
- X2 is O or N, and m is an integral from 1 to 4;
- and
- Ar is selected from the group consisting of, H,
11 more elements
Dependencies are inferred from the claim text.