The current invention is in the field of
molecular biology /
pharmacology and provides novel 3-oxabicyclo[3.3.1]
nonene compounds and derivatives that modulate the effects of the classical
estrogen receptors alpha and beta (ERalpha and ERbeta) with little to no biological or physiological effects on the
G protein-coupled
estrogen receptor GPER (also known as GPR30). These compounds may function as agonists and / or antagonists of one or more of the disclosed classical
estrogen receptors. Diseases that are mediated through one or more of these receptors include
cancer (including but not limited to breast (particularly endocrine or anti-
hormone resistant, and for the prevention / reduction of endocrine or anti-
hormone resistance), reproductive and other
hormone-dependent cancers,
leukemia, colon
cancer,
prostate cancer), reproductive (genito-urological) including
endometritis,
prostatitis, polycystic ovarian syndrome, bladder control, hormone-related disorders, hearing disorders, cardiovascular conditions including hot flashes and profuse sweating, hypertension,
stroke,
obesity,
osteoporosis, hematologic diseases, vascular diseases or conditions such as venous
thrombosis, atherosclerosis, among numerous others and disorders of the central and
peripheral nervous system, including depression,
insomnia,
anxiety,
multiple sclerosis, neuropathy, neurodegenerative disorders (such as Parkinson's
disease and Alzheimer's
disease), as well as
inflammatory bowel disease, Crohn's
disease, coeliac (celiac) disease and related disorders of the intestine, among numerous others as described herein. A contraceptive indication to prevent or reduce the likelihood of
pregnancy after intercourse is a further aspect of the present invention.