Patent · US Expired

Triarylethylene carboxylic acids with estrogenic activity

US5189212A · kind A · utility

91Cited by
3References
29Claims
0Family size

Assignee

Inventor

Key dates

Filing dateSep 7, 1990
Grant dateFeb 23, 1993
Priority date
Expiry dateSep 7, 2010

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07C65/19
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

Nonsteroidal estrogenic triarylethylene carboxylic acids of the formula ##STR1## wherein R is (CH.sub.2).sub.m O or (CH.sub.2).sub.n, where m is an integer from 1 to 4 and n is an integer from 0 to 4, X is hydrogen or hydroxyl, Y is methyl, ethyl, chlorine, or bromine, and wherein the RCOOH and X moieties are either meta or para to the phenyl ethylene linkage. Examples of active compounds include 4-hydroxytamoxifen acid, 3-hydroxytamoxifen acid, 4-[1-(p-hydroxyphenyl)-2-phenyl-1-butenyl]benzoic acid and 4-[1-(p-hydroxyphenyl)-2-phenyl-1-butenyl]phenylacetic acid. Compositions containing these triarylethylene carboxylic acids can be administered to patients to alleviate medical conditions associated with a deficiency of estrogen, including osteoporosis, premenstrual syndrome, vasomotor symptoms associated with menopause, atrophic vaginitis, Kraurosis vulvae, female hypogonadism, primary ovarian failure, excessive hair growth and pr The U.S. Government has certain rights in this invention by virtue of grants from the National Institutes of Health.

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