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US 10,377,735 B2Granted
Benzothiophene-based selective estrogen receptor downregulators
AssigneeThe Board of Trustees of the University of Illinois
InventorsGregory R. Thatcher, Rui Xiong, Jiong Zhao, Debra A. Tonetti
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Abstract
This invention is benzothiophene-based estrogen receptor downregulators and their compositions and uses to treat estrogen-related medical disorders.
Claims43
A method of treating an estrogen-related disorder in a subject comprising administering to the subject in need thereof a therapeutically effective amount of a compound of Formula:
- or a pharmaceutically acceptable salt thereof;
- wherein:
- m is 0, 1, 2, 3, or 4;
- n is 0, 1, 2, 3, or 4;
- XA is —O—;
- Ring B is phenyl, naphthyl, quinolinyl, 5- or 6-membered monocyclic heteroaryl, or 7-, 8-, 9- or 10 membered bicyclic heterocyclyl;
- Ring C is phenyl, thiophenyl, 5- or 6-membered monocyclic heteroaryl, or 7-, 8-, 9-, or 10-membered bicyclic heterocyclyl;
- R1 is selected from hydroxyl, hydrogen, halogen, —O(C1-C6 alkyl), —OC(O)(C1-C6 alkyl), —OC(O)C6H5, —OC(O)O(C1-C6 alkyl), —OC(O)OC6H5, and —OSO2(C2-C6 alkyl);
- R2 is selected from —CH═CHCOOH, —NH(CO)COOH, —COOH, C2-C6alkenylene-COOH, and C2-C6alkynylene-COOH;
- R3 is independently selected at each occurrence from hydrogen, halogen, —CN, —NO2, C1-C6alkyl, and C1-C6fluoroalkyl;
- and
- R4 is independently selected at each occurrence from hydrogen, halogen, hydroxyl, C1-C6alkyl, C1-C6fluoroalkyl, —CN, —O(C1-C6 alkyl), and —O(C1-C6fluoroalkyl).
9 more elements
Dependencies are inferred from the claim text.