Estratriene compound comprising heterocyclic bioisostere for the phenolic A ring

Abstract

The present invention is directed to novel pyrazolo-estrien and triazolo-estrien compound pharmaceutical composition containing them and its use in the treatment or prevention of disorders and diseases mediated by an estrogen receptor such as hot flashes, vaginal dryness, osteopenia, osteoporosis, hyperlipidemia, loss of cognitive function, degenerative brain diseases, cardiovascular diseases, cerebrovascular diseases, hormone sensitive cancers and hyperplasia (in tissues including breast, endometrium, and cervix in women and prostate in men), endometriosis, uterine fibroids, osteoarthritis; and as contraceptive agents either alone or in combination with a progestogen or progestogen antagonist. The compound: of the invention is selective estrogen receptor modulators