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US 11,767,298 B2Granted
Substituted benzimidazoles as inhibitors of transforming growth factor-β kinase
AssigneeDuke University
InventorsEmily Derbyshire, Timothy A. J. Haystead, Philip F. Hughes
Life of this patent
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Abstract
The present invention provides inhibitors of TAK1 having formula (I) and methods of using such compounds to treat various diseases.
Claims17
A compound according to Formula (I):
- or a pharmaceutically acceptable salt or tautomer thereof,
- wherein:
- X is NR1;
- R1 is C1-4 alkyl, C0-3 alkylene-C(O)R, or C0-3 alkylene-OC(O)R, wherein the C1-4 alkyl is optionally substituted by one or more substituents independently selected from the group consisting of halogen, NRN1RN2, and OH;
- R2 is H, halogen, C1-4 alkyl, or OC1-4 alkyl, wherein the C1-4 alkyl is optionally substituted by one or more substituents independently selected from the group consisting of halogen, NRN1RN2, and OH;
- R3 is NRN1RN2, OH, or OC1-4 alkyl;
- R4 is H, halogen, C1-4 alkyl, or OC1-4 alkyl, wherein the C1-4 alkyl is optionally substituted by one or more substituents independently selected from the group consisting of halogen, NRN1RN2, and OH;
- R is alkyl, heteroalkyl, alkenyl, alkynyl, NH2, O(alkyl), cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- each RN1 is independently H, alkyl, heteroalkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- and
- each RN2 is independently H, alkyl, heteroalkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl, aryl, or heteroaryl;
- with the proviso that if R3 is NH2, then R1 is not CH2CH2CH3.
9 more elements
A compound selected from the group consisting of:
- or a pharmaceutically acceptable salt or tautomer thereof.
Dependencies are inferred from the claim text.