Compounds for selective binding to estrogen receptors alpha/beta relative to GPER/GPR30 and methods of treating disease states and conditions mediated through these receptors

Abstract

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.

Dependencies are inferred from the claim text.