The present invention relates to treatment of neurological diseases such as multiple sclerosis (MS) and Alzheimer's disease, using an estrogen receptor beta (ER) ligand.

The present invention relates to treatment of neurological diseases such as multiple sclerosis (MS) and Alzheimer's disease, using an estrogen receptor beta (ER) ligand.

This disclosure relates to modulators of liver receptor homologue 1 (LRH-1) and methods of managing disease and conditions related thereto. In certain embodiments, modulators are derivatives of hexahydropentalene. In certain embodiments, this disclosure relates to methods of treating or preventing cancer, diabetes, or cardiovascular disease by administering an effective amount of a hexahydropentalene derivative disclosed herein.

Provided are compounds of formulae provided herein. The compounds may include pathway-preferential estrogens (PaPEs) derivatives with tissue-selective activities. Also provided are pharmaceutical compositions comprising the compounds, as well as methods of treating a disease or condition including administering the compounds. The disease or condition may include postmenopausal symptoms, cardiovascular disease, stroke, vascular disease, bone disease, metabolic disease, arthritis, osteoporosis, obesity, vasomotor/hot flush, cognitive decline, cancer including breast cancer.

Provided are compounds of formulae provided herein. The compounds may include pathway-preferential estrogens (PaPEs) derivatives with tissue-selective activities. Also provided are pharmaceutical compositions comprising the compounds, as well as methods of treating a disease or condition including administering the compounds. The disease or condition may include postmenopausal symptoms, cardiovascular disease, stroke, vascular disease, bone disease, metabolic disease, arthritis, osteoporosis, obesity, vasomotor/hot flush, cognitive decline, cancer including breast cancer.

The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof:

##STR00001##

wherein each symbol is as defined in the specification.

The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy, myocardial ischemia, brain ischemia, cerebral apoplexy, pulmonary hypertension, hyperlactacidemia, mitochondrial disease, mitochondrial encephalomyopathy or cancer, namely, a PDHK inhibitor and the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof:

##STR00001##

wherein each symbol is as defined in the specification.

The present invention is directed to a method of treating a subject for a disease or disorder associated with Trpv2 activity. The present invention also relates to a compound having the following structure:

##STR00001## where substituents A and R.sup.1-R.sup.5 are as defined herein. Also disclosed is a composition and a method of increasing Trpv2 activity in a cell or tissue.

The present invention is directed to a method of treating a subject for a disease or disorder associated with Trpv2 activity. The present invention also relates to a compound having the following structure:

##STR00001## where substituents A and R.sup.1-R.sup.5 are as defined herein. Also disclosed is a composition and a method of increasing Trpv2 activity in a cell or tissue.

Provided are: a method for producing fluorenylidene diallylphenols represented by formula (1), the method including a reaction step for reacting fluorenones represented by formula (2) and allylphenols represented by formula (3) in the presence of an acid catalyst, excluding compounds having mercapto groups, the amount of acid catalyst being 0.001-20 mol per mol of compound represented by formula (2); and fluorenylidene diallylphenols represented by formula (4).

##STR00001##