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US 10,207,998 B2Granted
Substituted benzimidazole and substituted benzothiazole inhibitors of transforming growth factor-β kinase and methods of use thereof
AssigneeDuke University
InventorsEmily Derbyshire, Timothy A. J. Haystead, Philip F. Hughes
Life of this patent
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Abstract
The present invention provides novel inhibitors of TAK1 having formula (I) and methods of using such compounds to treat various diseases.
Claims21
A pharmaceutical composition comprising a compound of Formula (I):
- or a tautomer or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier;
- wherein
- X is NR1;
- R1 is H, C1-6 alkyl, C1-4 carbonyl, or C1-4 carboxy, wherein the C1-4 carbonyl is a group —C(O)R attached by an alkyl group of up to 3 carbon atoms and R is aryl, alkoxy, or amino;
- R2 is H, C1-4 alkyl, C1-4 alkoxy, or halogen;
- R3 is OH, C1-4 alkoxy, NH2, NH(C1-4 alkyl), or N(C1-4 alkyl)(C1-4 alkyl);
- and
- R4 is H, C1-4 alkyl, C1-4 alkoxy, or halogen;
- wherein the C1-4 alkyl and C1-6 alkyl of R1, R2, and R4 are optionally and independently substituted by halo, OH, NH2, NH(C1-4 alkyl), or N(C1-4 alkyl)(C1-4 alkyl).
6 more elements
A compound according to Formula (I):
- or a tautomer or pharmaceutically acceptable salt thereof;
- wherein
- X is NR1;
- R1 is C1-6 alkyl, C1-4 carbonyl, or C1-4 carboxy, wherein the C1-4 carbonyl is a group —C(O)R attached by an alkyl group of up to 3 carbon atoms and R is aryl, alkoxy, or amino;
- R2 is H, C1-4 alkyl, C1-4 alkoxy, or halogen;
- R3 is OH, C1-4 alkoxy, NH2, NH(C1-4 alkyl), or N(C1-4 alkyl)(C1-4 alkyl);
- and
- R4 is H, C1-4 alkyl, C1-4 alkoxy, or halogen;
- wherein the C1-4 alkyl and C1-6 alkyl of R1, R2, and R4 are optionally and independently substituted by halo, OH, NH2, NH(C1-4 alkyl), or N(C1-4 alkyl)(C1-4 alkyl);
- wherein the compound of Formula (I) is not
7 more elements
A method for modulating transforming growth factor β activated kinase 1 activity in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a compound according to Formula (I):
- or a tautomer or pharmaceutically acceptable salt thereof;
- wherein
- X is NR1 or S;
- R1 is H, C1-6 alkyl, C1-4 carbonyl, or C1-4 carboxy, wherein the C1-4 carbonyl is a group —C(O)R attached by an alkyl group of up to 3 carbon atoms and R is aryl, alkoxy, or amino;
- R2 is H, C1-4 alkyl, C1-4 alkoxy, or halogen;
- R3 is OH, C1-4 alkoxy, NH2, NH(C1-4 alkyl), or N(C1-4 alkyl)(C1-4 alkyl);
- and
- R4 is H, C1-4 alkyl, C1-4 alkoxy, or halogen;
- wherein the C1-4 alkyl and C1-6 alkyl of R1, R2, and R4 are optionally and independently substituted by halo, OH, NH2, NH(C1-4 alkyl), or N(C1-4 alkyl)(C1-4 alkyl).
6 more elements
Dependencies are inferred from the claim text.