Glycyrrhetinic acid derivatives
AssigneesThe Texas A&M University System, Wellington Laboratories Inc.
InventorsStephen H. Safe, Sudhakar Chintharlapalli, Alan McAlees, Robert McCrindle
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Abstract
The present invention relates to novel derivatives of glycyrrhetinic acid, compositions comprising said derivatives and their use in the treatment of conditions or diseases that benefits from an upregulation of PPARγ and/or a downregulation of the expression or activity of one or more specificity (Sp) proteins, such as cancer, diabetes and Huntington's disease.
Claims19
A method of treating a condition or disease that benefits from an upregulation of PPARγ and/or a downregulation of the expression or activity of one or more specificity (Sp) proteins, comprising administering an effective amount of a compound of Formula (I):
- wherein
- R1 is selected from CN, halo, NO2, CO2R3, C1-6alkyl, fluoro-substituted C1-6alkyl, C2-6alkenyl, C2-6alkynyl, OR3, SR3, SOR3, SO2R3, NR3R4, C(O)NR3R4, C(O)R3, OC(O)R3, NHC(O)R3, P(O)R3R4, —C≡C—R3, —CR3═CR4R5, aryl and heteroaryl;
- R2 is selected from OC1-6alkyl, fluoro-substituted OC1-6alkyl, NH2, NHC1-6alkyl, N(C1-6alkyl)(C1-6alkyl), SH and SC1-6alkyl;
- R3, R4 and R5 are independently selected from H, C1-6alkyl, fluoro-substituted C1-6alkyl, aryl and heteroaryl;
- and
- one of X and Y is C═O while the other is CH2, and if X is C═O then adjacent to X represents a single bond and adjacent to Y represents a double bond and if Y is C═O then adjacent to Y represents a single bond and adjacent to X represents a double bond;
- and pharmaceutically acceptable salts, solvates and prodrugs thereof,
- to a subject in need thereof.
Dependencies are inferred from the claim text.