Compounds which activate estrogen receptors and compositions and methods of using the same
AssigneesThe Board of Trustees of the University of Illinois, Board of Regents, The University of Texas System
InventorsJohn A. Katzenellenbogen, Benita Katzenellenbogen, Sung Hoon Kim, Zeynep Madak-Erdogan, Philip Shaul
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Abstract
Provided are compounds of formulae provided herein. The compounds may include pathway-preferential estrogens (PaPEs) derivatives with tissue-selective activities. Also provided are pharmaceutical compositions comprising the compounds, as well as methods of treating a disease or condition including administering the compounds. The disease or condition may include postmenopausal symptoms, cardiovascular disease, stroke, vascular disease, bone disease, metabolic disease, arthritis, osteoporosis, obesity, vasomotor/hot flush, cognitive decline, cancer including breast cancer.
Claims21
A compound of formula (i):
- or stereoisomers, or pharmaceutically acceptable salts thereof;
- wherein
- n is an integer from 0 to 4;
- m is an integer from 0 to 4;
- X is hydroxy or C1-4 alkoxy;
- R1 and R2 are independently H, hydroxy, C1-4 alkyl, C1-4 alkoxy, —S—C1-4 alkyl, or halo;
- R3 is H, hydroxy, cyano, halo, C1-4 alkyl, or C1-4 alkoxy;
- each R4 is independently hydrogen, hydroxy, oxo, halo, C1-4 alkyl, or C1-4 alkoxy;
- R5 is H or C1-4 alkynyl;
- and
- --- is an optional double bond;
- wherein a C1-4 alkyl or C1-4 alkoxy is optionally substituted with one or more of halo, cyano, amino, hydroxy, and C1-4 alkoxy.
A compound selected from the group consisting of:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.