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US 12,180,159 B2Granted
Activators of the unfolded protein response
AssigneeThe Board of Trustees of the University of Illinois
InventorsDavid J. Shapiro, Paul J. Hergenrother, Matthew W. Boudreau
Life of this patent
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Abstract
A set of small molecules ERα biomodulators that kill therapy-resistant ERα positive breast, ovarian, and endometrial cancer cells. These small molecules have increased therapeutic potential because of an increased ability to kill therapy-resistant breast cancer cells compared to BHPI and other conventional therapies (endocrine therapies, tamoxifen and fulvestrant/ICI). The new compounds do not only inhibit proliferation of the cancer cells but actually kills them, which prevents reactivation of tumors years later.
Claims24
A compound of Formula I:
- or a salt or solvate thereof;
- wherein
- R1 is —ORA, —SRA, —N(RA)2, alkyl, cycloalkyl, or aryl;
- R2, R3 and R4 are each independently H, halo, —ORA, —SRA, —N(RA)2, alkyl, cycloalkyl, or aryl;
- A1, A2, A3 and A4 are each independently H, halo, or alkyl;
- G1 is —ORB wherein RB is CF3, CHF2, CH2CF3, CF2CH3, or CF2CF3;
- G2 is halo, —ORC, —SRC, —S(═O)2RC, or alkyl;
- X and Z are each independently O, S, or —NRD;
- and
- RA, R′ and RD are each independently H or alkyl;
- wherein each alkyl, cycloalkyl, or aryl is optionally substituted with one or more halo substituents.
8 more elements
Dependencies are inferred from the claim text.