Boronic acid derivatives of resveratrol for activating deacetylase enzymes
AssigneeGeorgetown University
InventorsInsoo Bae, Yong Weon Yi, Hyo Jin Kang, Hee Jeong Kim
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Abstract
Disclosed herein are compounds, compositions and methods for the treatment of a disease or disorder related to activation of deacetylase enzymes. The compounds and methods are related to boronic acid derivatives of resveratrol. In some forms, the compound, compositions and methods relate to treatment of prostate cancer, colon cancer, or breast cancer, a cardiovascular disease, inflammation, obesity, diabetes, or a neurodegenerative disease.
Claims21
A method comprising administering a composition to a subject, wherein the composition comprises a compound, or a pharmaceutically acceptable salt, prodrug, clathrate, tautomer or solvate thereof, wherein the compound has the structure:
- wherein
- R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are independently hydrogen, hydroxyl, —B(OH)2, alkyl, alkenyl, alkynyl, halo, alkoxy, amino, alkylamino, dialkylamino, cyano, nitro, formyl, carboxyl, alkoxycarbonyl, alkoxydialkylamino, aminocarbonyl, alkylaminocarbonyl, dialkylamino carbonyl, haloalkyl, haloalkloxy, haloalkylamino, or di(haloalkyl)amino;
- R8 and R9 are optionally cyclized to form cycloalkyl, aryl, heteroaryl or heterocyclyl, optionally substituted with —B(OH)2, mild Lewis acid, strong acid, weak acid, alkyl, alkenyl, alkynyl, halo, alkoxy, amino, alkylamino, dialkylamino, cyano, nitro, formyl, carboxyl, alkoxycarbonyl, alkoxydialkylamino, aminocarbonyl, alkylaminocarbonyl, dialkylamino carbonyl, haloalkyl, haloalkloxy, haloalkylamino, di(haloalkyl)amino or sugars;
- L is
- or L is absent when R8 and R9 are cyclized;
- wherein at least one of R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 is or includes —B(OH)2, and at least one of R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 is or includes alkoxy, alkoxydialkylamino or hydroxyl,
- wherein the compound is a deacetylase activator, wherein the subject is in need of treatment of a disease or condition, wherein the disease or condition is associated with expression of a deacetylase enzyme, and wherein cells of the subject express mutant p53, under-express SIRT1, have low SIRT1 activity, or combinations thereof.
Dependencies are inferred from the claim text.