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US 12,364,688 B2Granted
NSD family inhibitors and methods of treatment therewith
AssigneeThe Regents of the University of Michigan
InventorsTomasz Cierpicki, Jolanta Grembecka, Huang Huang, Sergei Zari, Hyo Je Cho, Mykhaylo Potopnyk, Sergii Dudkin, Wenbing Chen, Yassir Adam, Christina Howard, EunGi Kim
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Abstract
Provided herein are small molecule inhibitors of NSD1, NSD2 and/or NSD3 activity, and methods of use thereof for the treatment of disease, including leukemia, breast cancer, osteosarcoma, lung and prostate cancers and other solid tumors as well as other diseases dependent on the activity of NSD1, NSD2 and/or NSD3.
Claims3
A composition comprising a compound having a structure of
- or a salt thereof;
- wherein X is CH2 or NH;
- wherein R2 is selected from H and C1-C4 alky;
- wherein R4 is selected from H, halogen, OH, OCH3, OCH2CH3, CH2OH, NH2, CH2NH3, NHCH3, CH3, CH2CH3, trihalomethyl, trihaloethyl, dihalomethyl, dihaloethyl, halomethyl, and haloethyl;
- wherein R5 is selected from H, CH3, CH2CH3, OH, OCH3, NH2, and halogen;
- wherein Z is NH, S, O, CH2, or is absent;
- wherein A is selected from a 5- or 6-membered aryl ring, 5- or 6-membered heteroaryl ring, 5- or 6-membered cycloalkyl ring, or a 5- or 6-membered heterocyclic ring;
- wherein A is unsubstituted or substituted with one or more of halogen, OH, OCH3, OCH2CH3, OCH (CH3)2, OCH2CH (CH3)2, CH2OCH3, NH2, CH2NH3, NHCH3, CH3, CH2CH3, CH2CH (CH3)2, and amide;
- wherein L is —NHC (O) CH2—, —NHC (O) (CH2)2—, —NHC (O) (CH2)3—, —NHC (O) CH═CH—, —NHCH2—, —NH (CH2)2—, —NH (CH2)3—, —O—, —OCH2—, —O (CH2)2—, —O (CH2)3—, —CH2—, —CH2O—, or absent;
- wherein E is selected from a 5- or 6-membered aryl ring, 5- or 6-membered heteroaryl ring, 5- or 6-membered cycloalkyl ring, or a 5- or 6-membered heterocyclic ring;
- wherein Y is absent or a Michael acceptor;
- wherein R7 is H, D, F, OH, NH2, or CH3.
9 more elements
Dependencies are inferred from the claim text.