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US 2023/0039244 A1Published application
2-beta-naphthyl-acetic acid analogs as akr1c3 inhibitors and methods of using same
AssigneesThe Trustees of the University of Pennsylvania, Vanderbilt University
InventorsTrevor M. PENNING, Adegoke ADENIJI, Lawrence J. MARNETT
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Abstract
The invention includes 2-β-naphthyl-acetic acid derivatives, which are selective AKR1C3 inhibitors. In certain embodiments, the compounds of the invention are R-naproxen analogs. The invention further includes methods of treating cancer, such as prostate cancer and/or castration-resistant prostate cancer, using at least one compound of the invention.
Claims19
A compound of formula (I), or a salt, solvate, or stereoisomer thereof:
- wherein:
- R1 is selected from the group consisting of OH, —NHSO2(C1-C6 alkyl), C1-C6 alkoxy, and C3-C8 cycloalkoxy, wherein the alkyl, alkoxy or cycloalkoxy group is optionally substituted with at least one substituent selected from C1-C6 alkyl, C3-C8 cycloalkyl, optionally substituted aryl, OH, C1-C6 alkoxy, halogen, and —CN;
- R2 and R3 are independently selected from the group consisting of H, C1-C6 alkyl, and C3-C8 cycloalkyl, wherein the alkyl or cycloalkyl is optionally substituted with at least one selected from the group consisting of C1-C6 alkyl and C3-C8 cycloalkyl;
- R4 is selected from the group consisting of C1-C6 alkyl, C3-C8 cycloalkyl, C1-C6 alkoxy, C3-C8 cycloalkoxy, —S(C1-C6 alkyl), —S(C3-C8 cycloalkyl), —S(═O)(C1-C6 alkyl), —S(═O)(C3-C8 cycloalkyl), —S(═O)2(C1-C6 alkyl), and —S(═O)2(C3-C8 cycloalkyl);
- wherein the compound is not a compound wherein R1 is OH, one of R2 and R3 is methyl and the other is H, and R4 is methoxy.
2 more elements
Dependencies are inferred from the claim text.