Substituted tropolone derivatives and methods of use
AssigneeUniversity of Connecticut
InventorsDennis L. Wright, Amy C. Anderson, Michael Van Heyst, Sophia Ononye
Life of this patent
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Abstract
The compositions and methods described herein relate generally to substituted tropolone derivatives, which, among other features, are useful as histone deacetylase (HDAC) inhibitors.
Claims28
A pharmaceutical formulation comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof:
- wherein:
- Rx is hydrogen, hydroxyl, or amino;
- R1, R2, and R3 are hydrogen;
- wherein when Rx is hydrogen, then R4 and R5 are independently hydrogen, C4-C6 alkyl, C3-C6 cycloalkyl, naphthyl, or alkoxy substituted phenyl, wherein when the alkoxy substitution is methoxy, then the phenyl includes at least two substitutions;
- wherein when Rx is hydroxyl, then R4 and R5 are independently hydrogen, C4-C6 alkyl, C3-C6 cycloalkyl, naphthyl, or alkoxy substituted phenyl;
- wherein when Rx is amino, then R4 and R5 are independently hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, naphthyl, phenyl, or alkoxy substituted phenyl;
- provided that R4 and R5 are not both hydrogen;
- and a pharmaceutically acceptable carrier.
A method of inhibiting histone deacetylase (HDAC) activity, comprising contacting an HDAC isoform with a compound of Formula (I) or a pharmaceutically acceptable salt thereof:
- wherein:
- Rx is hydrogen, hydroxyl, or amino;
- R1, R2, and R3 are hydrogen;
- R4 and R5 are independently hydrogen, C1-C6 alkyl, C3-C10 cycloalkyl, or aryl, wherein the aryl is unsubstituted or substituted one, two, or three times with C1-C6 alkoxy;
- and
- provided that R4 and R5 are not both hydrogen.
A method of treating a disease in a subject, comprising administering to a subject an amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof:
- wherein:
- Rx is hydrogen, hydroxyl, or amino;
- R1, R2, and R3 are hydrogen;
- R4 and R5 are independently hydrogen, C1-C6 alkyl, C3-C10 cycloalkyl, or aryl, wherein the aryl is unsubstituted or substituted one, two, or three times with C1-C6 alkoxy;
- provided that R4 and R5 are not both hydrogen.
Dependencies are inferred from the claim text.