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US 9,216,993 B2Granted
Compositions comprising thienopyrimidine and thienopyridine compounds and methods of use thereof
AssigneeThe Regents of the University of Michigan
InventorsJolanta Grembecka, Tomasz Cierpicki, Dmitry Borkin, Jay L. Hess, Duxin Sun, Xiaoqin Li
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Abstract
The present disclosure relates generally to thienopyrimidine and thienopyridine compounds and methods of use thereof. In particular embodiments, the present disclosure provides compositions comprising thienopyrimidine and thienopyridine compounds of Formula 4: and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins.
Claims54
A compound of Formula 4:
- or a pharmaceutically acceptable salt thereof, wherein
- each of R1, R2, R3, R4, R5, R6, R7, and R8 is independently H, alkyl, substituted alkyl, alcohol, ether, amine, halogen, ketone, amide, cyano, sulfonylmethane, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, or substituted heterocycloalkyl;
- wherein R6 is present at one or more positions of the indole;
- Y is N, C—H, or
- Ra is alkyl, heteroalkyl, alkyl-substituted aryl, substituted alkyl, alcohol, ether, amino, cyano, aldehyde, heterocycloalkyl, or aromatic group;
- and
- L is alkylene, oxalkylene, or absent;
- wherein when L is absent the bonds attached to L do not exist.
5 more elements
Dependencies are inferred from the claim text.