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US 9,505,782 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 2: and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins.
Claims26
A compound of Formula 2:
- or a pharmaceutically acceptable salt thereof, wherein:
- each of R1 and R2 is independently H, alkyl, substituted alkyl, alcohol, ether, amine, thioalkyl, halogen, ketone, carbocyclic ring, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, thiol, disulfide, sulfoxide, or sulfone;
- Y is N, C—H, or C—Ra;
- Ra is alkyl, heteroalkyl, alkyl-substituted aryl, substituted alkyl, alcohol, ether, amino, cyano, aldehyde, heterocycloalkyl, or aromatic group;
- L is alkylene, oxalkylene, or absent;
- wherein when L is absent the bonds attached to L do not exist;
- Q is alkylene or heteroalkylene;
- each R3 is independently H, alkyl, substituted alkyl, alcohol, ether, amine, thioalkyl, halogen, ketone, carbocyclic ring, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, or substituted heterocycloalkyl;
- n is 1, 2, 3, or 4;
- and
- Z is CHR4SO2R5 or —NR4SO2R5, wherein R4 is H, alkyl, substituted alkyl, alcohol, ether, amine, or carbocyclic ring and R5 is H, alkyl, substituted alkyl, alcohol, ether, amine, thioalkyl, ketone, carbocyclic ring, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, or substituted heterocycloalkyl.
8 more elements
Dependencies are inferred from the claim text.