Patent · US Expired

Compounds and methods for modulation of estrogen receptors

US6331562A · kind A · utility

33Cited by
1References
63Claims
0Family size

Assignee

Inventors

Key dates

Filing dateJul 6, 2000
Grant dateDec 18, 2001
Priority date
Expiry dateJul 6, 2020

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D311/18
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

Compounds that modulate gene expression through the estrogen receptor (ER) are disclosed having the following structure, as well as pharmaceutical compositions containing the same: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, n and p are as defined here. In a specific embodiment, the compounds are selective modulators for Er-.beta. over ER-.alpha.. Methods are also disclosed for modulating ER-.beta. in cells and/or tissues expressing the same, including cells and/or tissues that preferentially express ER-.beta.. More generally, methods for treating estrogen-related conditions are also disclosed, including conditions such as is breast cancer, testicular cancer, osteoporosis, endometriosis, cardiovascular disease, hypercholesterolemia, prostatic hypertrophy, prostatic carcinomas, obesity, hot flashes, skin effects, mood swings, memory loss, urinary incontinence, hairloss, cataracts, natural hormonal imbalances, and adverse reproductive effects associated with exposure to environmental chemicals.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.