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US 11,833,210 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
Life of this patent
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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.
Claims19
A compound comprising the structure of:
- wherein X, when present, is CH or N;
- wherein R1 is selected from H, alkyl, substituted alkyl, branched alkyl, a substituted brached alkyl, alkoxy, amine, substituted amine, thioalkyl, ketone, amide, a substituted amide, cyano, sulfonyl, carboxy, dialkylphosphine oxide, a carbocyclic ring, s sustituted carobocyclic 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, a hydrogen bond donor, a hydrogen bond acceptor, and combinations thereof;
- wherein R2, R3, R4, R5, and R7, when present, are independently selected from H, halogen, CH3, OH, SH, NH2, CN, CF3, CCl3, —CH2—CH3, —CH2—OH, —CH2NH2, —C(O)NH2, CH3SH, CH2Cl, CH2Br, CH2F, CHF2, CH2CN, CH2CF3, CH2Cl3, alkyl, haloalkyl, and alcohol;
- and
- 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, a hydrogen bond donor, a hydrogen bond acceptor, and combinations thereof;
- or a salt thereof.
3 more elements
Dependencies are inferred from the claim text.