Small-molecule inhibitors of the androgen receptor
AssigneeThe Regents of the University of California
InventorsMarc I. Diamond, Jeremy O. Jones, Adam R. Renslo
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Abstract
The present invention provides tetrahydropyrvinium (THP), derivatives thereof, benzoxazole compounds, and derivatives thereof. The present invention provides a method of using tetrahydropyrvinium (THP), derivatives thereof, benzoxazole compounds, and derivatives thereof.
Claims20
-21. (canceled)
The method of claim 42, wherein the compound is selected from the group consisting of
The method of claim 42, wherein the salt forms comprise a counterion selected from the group consisting of pamoate, chloride, bromide, succinate, maleate and acetate.
The method of claim 42, wherein the salt forms comprise a counterion selected from the group consisting of pamoate, chloride, bromide, succinate, maleate and acetate.
The method of claim 42, wherein the method of inhibiting treats or prevents a disease selected from the group consisting of prostate cancer, ovarian cancer, hepatocellular carcinoma, acne vulgaris, endometriosis, acanthosis nigricans, hypertrichosis, breast cancer, precocious puberty, polycystic ovary syndrome, benign prostatic hyperplasia, alopecia, hirsutism and hypersexuality/paraphilia.
The method of claim 42, wherein the compound of Formula I is administered with a course of hormonal therapy, wherein the compound for hormonal therapy is selected from the group consisting of an anti-androgen and a LnRH agonist.
-41. (canceled)
A method of inhibiting the androgen receptor, the method comprising:
- administering to a patient in need thereof, a therapeutically effective amount of a compound of Formula I:
- wherein
- each R1 is independently selected from the group consisting of hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, —SR4, —NR4R5, cycloalkyl, heterocycloalkyl, aryl and heteroaryl;
- R2 is selected from the group consisting of hydrogen, C1-6 alkyl, C1-6 alkyl-OH, C2-6 alkenyl and C2-6 alkynyl;
- R3 is aryl, optionally substituted with from 1 to 3 R6 groups;
- R4 and R5 are each independently selected from the group consisting of hydrogen, C1-6 alkyl, C2-6 alkenyl and C2-6 alkynyl;
- or R4 and R5 are combined with the nitrogen to which they are attached to form a heterocyclic ring having from 5 to 7 ring members and from 1 to 3 heteroatoms each independently selected from the group consisting of N, O and S;
- each R6 is independently selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl and C1-6 alkoxy;
- L is a linker selected from the group consisting of C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene and C3-6 cycloalkylene;
- X is a heteroaryl ring having from 5 to 6 ring members and from 1 to 3 heteroatoms each independently selected from the group consisting of N, O and S, optionally substituted with from 1 to 3 R8 groups;
- each R8 is independently selected from the group consisting of H, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl and C1-6 alkoxy;
- and salts, hydrates and prodrugs thereof, thereby inhibiting the androgen receptor.
Dependencies are inferred from the claim text.