Back to results
US 10,703,747 B2Granted
Benzothiophene-based selective mixed estrogen receptor downregulators
AssigneeThe Board of Directors of the University of Illinois
InventorsGregory R. Thatcher, Rui Xiong, Yunlong Lu, Jiong Zhao, Debra A. Tonetti
Life of this patent
Estimating the term…
Abstract
This invention is benzothiophene-based selective mixed estrogen receptor downregulators and their compositions and uses to treat estrogen-related disorders.
Claims30
A compound of Formula (I), or a pharmaceutically acceptable salt thereof:
- wherein:
- m is 0, 1, 2, 3, or 4;
- n is 0, 1, 2, 3, or 4;
- X is —C(O)—;
- Ring B is phenyl, or naphthyl;
- Ring C is phenyl, or C3-C6cycloalkyl;
- R1 is selected from hydroxyl, hydrogen, halogen, —O(C1-C6alkyl), —OC(O)(C1-C6alkyl), —OC(O)C6H5, —OC(O)O(C1-C6alkyl), —OC(O)OC6H5, and —OSO2(C2-C6alkyl);
- R2 is selected from —OCH═CHCOOH, —NHC(O)COOH, —COOH, —C2-C6alkylene-COOH, and —C2-C6alkynylene-COOH;
- and
- R3 and R4 are independently selected at each occurrence from hydrogen, halogen, hydroxyl, —NO2, C1-C6alkyl, C1-C6fluoroalkyl, —CN, —O(C1-C6alkyl), and —O(C1-C6fluoroalkyl).
7 more elements
A compound of Formula (V), or a pharmaceutically acceptable salt thereof:
- wherein:
- m is 0, 1, 2, 3, or 4;
- n is 0, 1, 2, 3, or 4;
- X is —C(O)—;
- Ring B is phenyl, or naphthyl;
- Ring C is phenyl, or C3-C6cycloalkyl;
- Ring D is C3-C6cycloalkyl;
- R1 is selected from hydroxyl, hydrogen, halogen, —O(C1-C6alkyl), —OC(O)(C1-C6alkyl), —OC(O)C6H5, —OC(O)O(C1-C6alkyl), —OC(O)OC6H5, and —OSO2(C2-C6alkyl);
- R2a is selected from —OH, —NH(CO)NHOH, —CH═CHCOOH, —NH(CO)COOH, —COOH, —NH2, —C2-C6alkylene-COOH, and —C2-C6alkynylene-COOH;
- and
- R3 and R4 are independently selected at each occurrence from hydrogen, halogen, hydroxyl, —NO2, C1-C6alkyl, C1-C6fluoroalkyl, —CN, —O(C1-C6alkyl), and —O(C1-C6fluoroalkyl).
8 more elements
A compound of Formula (VII), or a pharmaceutically acceptable salt thereof:
- wherein:
- m is 0, 1, 2, 3, or 4;
- n is 0, 1, 2, 3, or 4;
- Ring D1 is selected from
- R2b is selected from —OH, —NH2, and —COOH;
- and
- R3 and R4 are independently selected at each occurrence from hydrogen, halogen, hydroxyl, —NO2, C1-C6alkyl, C1-C6fluoroalkyl, —CN, —O(C1-C6alkyl), and —O(C1-C6fluoroalkyl).
4 more elements
Dependencies are inferred from the claim text.