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US 12,521,442 B2Granted
ASH1L inhibitors and methods of treatment therewith
AssigneeThe Regents of the University of Michigan
InventorsJolanta Grembecka, Szymon Klossowski, Jing Deng, Tomasz Cierpicki, Hao Li, Hongzhi Miao, Trupta Purohit, EunGi Kim
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Abstract
Provided herein are small molecules that bind to ASH1L and inhibit ASH1L activity, and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.
Claims14
A compound comprising the structure of:
- wherein X is S or O;
- wherein Y is C, N, or O;
- wherein, when Y is O, R1 is absent,
- wherein, when Y is N, R1 is selected from H, SO2CH3, and SO2CF3,
- wherein, when Y is C, two R1 are present and the two R1 are both H or both F;
- wherein R6 is selected from H, alkyl, substituted alkyl, hydroxy, alkoxy, amine, substituted amine, alkylamine, substituted alkylamine, thioalkyl, halogen, ketone, amide, substituted amide, alkylamide, substituted alkylamide, cyano, sulfonyl, carboxy, dialkylphosphine oxide, a carbocyclic ring, a substituted carbocyclic ring, an aromatic ring, a substituted aromatic ring, a heterocyclic aromatic ring, a substituted heterocyclic aromatic ring, a substituted or non-substituted heterocyclic non-aromatic ring, carbocyclic or heterocyclic aromatic ring fused to another aromatic ring, and combinations thereof;
- and wherein R7 is selected from H and a halogen;
- or a salt thereof.
5 more elements
Dependencies are inferred from the claim text.