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US 12,521,386 B2Granted
Small molecule inhibitors of the androgen receptor activity and/or expression and uses thereof
AssigneeArizona Board of Regents on Behalf of the University of Arizona
InventorsChristopher Hulme, Yeng-Jeng Shaw, Vijay Gokhale
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Abstract
This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a piperazine (or similar) structure which function as antagonists of androgen receptor activity, and their use as therapeutics for the treatment of cancer (e.g., castration-resistant prostate cancer) and other conditions characterized with androgen receptor activity and/or androgen receptor expression.
Claims4
A compound described by Formula I:
- including pharmaceutically acceptable salts, solvates, and/or prodrugs thereof;
- wherein X is Nitrogen rendering the resulting compound encompassed within Formula II:
- or wherein X is C—H rendering the resulting compound encompassed within Formula III:
- wherein R1 is selected from
- wherein R2 is selected from hydrogen, methyl,
- wherein R3 is selected from hydrogen, methyl,
- and
- wherein R4 is selected from hydrogen and methyl.
5 more elements
Dependencies are inferred from the claim text.