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US 12,319,681 B2Granted
Tripartite androgen receptor eliminators, methods and uses thereof
AssigneeSPG Therapeutics, Inc.
InventorZory Shaposhnik
Life of this patent
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Abstract
The present specification discloses tripartite androgen receptor eliminators (AREs), pharmaceutical compositions and medicaments comprising such AREs, methods and uses for such AREs and compositions and medicaments, and methods and uses for AREs and compositions and medicaments for treating an androgen receptor signaling-mediated condition, disease or disorder.
Claims19
A compound of formula (I),
- ARA-L-EE (I)
- wherein
- ARA is an androgen receptor (AR) antagonist that is spironolactone
- having the following structure:
- L is a linker molecule of formula (III), (IV), (V), (VI), (VII), (VIII), (IX) or (X):
- wherein each n is independently any integer from 0 to 10;
- and
- EE is an E3 ligase-recruiting moiety selected from the group consisting of a nutlin moiety, a bestatin moiety, a phthalimide moiety, and a moiety according to formula (XII):
- wherein R8 is OH, COOH, NH2, a halogen, R9OH, R9COOH, ROC(O) NH2 or R6C(O) R10,
- wherein R9 is C1-10 alkyl, C2-10 alkenyl, or C2-10 alkynyl, and R10 is a halogen;
- wherein ARA is conjugated to EE via the linker molecule, and wherein the linker molecule is covalently attached to each of ARA and EE.
8 more elements
A compound of formula (I),
- ARA-L-EE (I)
- wherein
- ARA is an androgen receptor (AR) antagonist that is ketoconazole having the following structure:
- L is a linker molecule of formula (III), (IV), (V), (VI), (VII), (VIII), (IX) or (X):
- wherein each n is independently any integer from 0 to 10;
- and
- EE is an E3 ligase-recruiting moiety selected from the group consisting of a nutlin moiety, a bestatin moiety, a phthalimide moiety, and a moiety according to formula (XII):
- wherein R8 is OH, COOH, NH2, a halogen, R9OH, R9COOH, R6C(O) NH2 or R6C(O) R10, wherein R9 is C1-10 alkyl, C2-10 alkenyl, or C2-10 alkynyl, and R10 is a halogen;
- wherein ARA is conjugated to EE via the linker molecule, and wherein the linker molecule is covalently attached to each of ARA and EE.
6 more elements
Dependencies are inferred from the claim text.