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US 10,308,607 B2Granted
Fucosidase inhibitors
AssigneeHorizon Orphan LLC
InventorsTodd C. Zankel, Sara Louise Isbell, Amanda Anne Ko
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Abstract
The present disclosure relates, in general, to compounds useful as inhibitors of fucosidase enzymes, and to methods and compositions for the treatment of tumors or cancers, such as liver disorders and liver tumors (e.g., hepatocellular carcinoma), with a compound as disclosed herein.
Claims14
A method for treating a tumor or cancer in a subject in need thereof comprising administering compound II, compound III, or a compound of formula I in a therapeutically effective amount:
- wherein:
- X1, X2, and X3 are independently selected from the group consisting of OH, halo, and O(C)OCH3;
- R is selected from the group consisting of C1-3alkyl and C1-3haloalkyl;
- R1 is selected from the group consisting of H, C1-3alkyl, OH, —CO2C1-3alkyl;
- R2 is selected from the group consisting of —NRbC(O)Ra, —NRbC(O)ORa, —NRbC(O)NRcRa, —NRbC(O)SRa, —C(O)Ra, and —C(O)NRbRa;
- Ra is —C0-3alkylene-G;
- G is selected from the group consisting of aryl, heteroaryl, cycloalkyl, and heterocycloalkyl;
- and
- Rb and Rc are independently selected from the group consisting of H and C1-3alkyl, wherein the tumor or cancer is selected from connective tissue cancer, brain cancer, cervical cancer, prostate cancer, or ovarian cancer.
6 more elements
Dependencies are inferred from the claim text.