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US 2026/0103461 A1Published application
Estrogen receptor modulators and uses thereof
AssigneeOlema Pharmaceuticals, Inc.
InventorsBrian R. Hearn, David C. Myles, Dirk A. Heerding
Life of this patent
Estimating the term…
Abstract
The present disclosure provides compounds that are estrogen receptor modulators (e.g., estrogen receptor agonists, estrogen receptor antagonists, and/or complete estrogen receptor antagonists), and uses thereof.
Claims84
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- A is selected from optionally substituted 5-membered heteroaryl comprising 1-3 heteroatoms selected from N, O, and S, wherein at least 1 heteroatom is S or O, optionally substituted 7- to 10-membered bicyclic heteroaryl comprising 1-4 heteroatoms selected from N, O, and S, and optionally substituted 3- to 6-membered heterocyclyl comprising 1-3 heteroatoms selected from N, O, and S;
- L is a covalent bond or an optionally substituted bivalent group selected from —O—C0-C5 aliphatic- and —C1-C5 aliphatic-O—;
- B is selected from 3- to 12-membered heterocyclyl comprising 1-3 heteroatoms selected from N, O, and S and C3-C6 cycloaliphatic;
- R1 is selected from hydrogen and optionally substituted C1-C6 aliphatic;
- R2 is selected from hydrogen and optionally substituted C1-C6 aliphatic;
- R3 is selected from hydrogen, halogen, —CN, —ORa, —C(O)Ra, —C(O)ORa, —OC(O)Ra, —C(O)N(Ra)2, —OC(O)N(Ra)2, —NO2, —N(Ra)2, —N(Ra)C(O)Ra, —N(Ra)C(O)ORa, —N(Ra)S(O)2Ra, —SRa, —S(O)2Ra, —S(O)N(Ra)2, —S(O)2N(Ra)2, and an optionally substituted C1-6 aliphatic group;
- each R4 is independently halogen, —CN, —ORa, —N(Ra)2, —C(O)Ra, —OC(O)Ra, —C(O)ORa, —C(O)N(Ra)2, —N(Ra)C(O)Ra, or an optionally substituted group selected from C1-C6 aliphatic and 3- to 12-membered heterocyclyl comprising 1 to 3 heteroatoms selected from N, O, and S;
- each Ra is independently selected from hydrogen and optionally substituted C1-C6 aliphatic;
- and
- n is 0 to 5.
8 more elements
A compound selected from Table 1, or a pharmaceutically acceptable salt thereof.
A compound selected from Table 3, or a pharmaceutically acceptable salt thereof.
A compound selected from Table 4, or a pharmaceutically acceptable salt thereof.
A compound selected from Table 5, or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.