Substituted benzothiophene analogs as selective estrogen receptor degraders
AssigneeThe Board of Trustees of the University of Illinois
InventorsGregory R Thatcher, Rui Xiong, Jiong Zhao, Yunlong Lu, Lauren Gutgesell, Carlo Ivan Rosales, Yangfeng Li
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Abstract
In one aspect, the disclosure relates to relates to substituted benzothiophene analogs which are useful as selective degraders of estrogen receptor, methods of making same, pharmaceutical compositions comprising same, and methods of treating one or more clinical conditions associated with estrogen receptor, such as a cancer, including breast cancer, or osteoporosis. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
Claims15
A method for the treatment of breast cancer in a mammal comprising the step of administering to the mammal a therapeutically effective amount of a compound having a structure represented by a formula:
- wherein m is selected from 0 and 1;
- wherein p is selected from 0, 1, and 2;
- wherein q is selected from 0, 1, and 2;
- wherein each of Z1 and Z2 is independently selected from —CH— or —N—;
- provided Z1 and Z2 are not simultaneously —CH— or —N—;
- and provided when Z1 is —CH— and m is 1, that p and q are not both 0;
- wherein Z10 is selected from —O— or —NH;
- wherein Z11 is, when present, —CH2CH2;
- wherein Z40 is —(CH2)n—, wherein n is selected from 1, 2, 3, or 4;
- wherein each of R10a and R10b are independently selected from hydrogen, deuterium, halogen, and C1-C3 methyl;
- wherein R is C1-C6 alkyl, C1-C6 haloalkyl, halogen, or hydroxy;
- and
- r is 0, 1, 2, 3, or 4;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.