Back to results
US 2023/0092979 A1Published application
Tripartite Androgen Receptor Eliminators, Methods and Uses Thereof
AssigneeSPG Therapeutics, Inc.
InventorZory Shaposhnik
Life of this patent
Estimating the term…
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 AR antagonist that is apalutamide, bicalutamide, canrenone, chlormadinone acetate, cimetidine, cyproterone acetate, drospirenone, enzalutamide, flutamide, ketoconazole, megestrol acetate, nilutamide, RU58841, spironolactone, topilutamide (fluridil),
- L is a linker molecule of formula II
- wherein R1 and R2 are each independently H, OH, COOH, NH2, R3OH, R3COOH, OR3OH, OR3COOH, R3NH(CO)R4, R3NH(CO)R4OH, R3NH(CO)R4COOH;
- R3 and R4 are each independently C1-10 alkyl, C2-10 alkenyl, or C2-10 alkynyl;
- and n any integer from 0 to 10;
- and
- EE is an AR elimination promoter or elimination enhancer element that is a hydrophobic tag or an E3 ligase-recruiting moiety.
6 more elements
Dependencies are inferred from the claim text.