Androgen receptor (AR) plays a critical role in the function of several organs including primary and accessory sexual organs, skeletal muscle, and bone, making it a desirable therapeutic target. Selective androgen receptor modulators (SARMs) bind to the AR and demonstrate osteo- and myo-anabolic activity; however, unlike testosterone and other anabolic steroids, these nonsteroidal agents produce less of a growth effect on prostate and other secondary sexual organs. SARMs provide therapeutic opportunities in a variety of diseases, including muscle wasting associated with burns, cancer, or end-stage renal disease, osteoporosis, frailty, and hypogonadism. This review summarizes the current standing of research and development of SARMs, crystallography of AR with SARMs, plausible mechanisms for their action and the potential therapeutic indications for this emerging class of drugs.

https://journals.sagepub.com/doi/pdf/10.1621/nrs.06010

Selective androgen receptor modulators in preclinical and clinical development

The present invention relates to: a novel compound having an excellent light-emitting ability; and an organic electroluminescent element having improved characteristics such as light-emitting efficiency, driving voltage, and lifespan since at least one organic layer thereof contains the compound.

Organic compound and organic electroluminescent element comprising same

A compound having the general structure of Formula (I): Formula (I) or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, wherein: Q is selected from the group consisting of: Formula (a), (b), (c), (d) and (e); and L is selected from the group consisting of: Formula (f), (g), (h), and (i); or a pharmaceutically acceptable salt, solvate, ester, or tautomer thereof, are useful in treating diseases, disorders, or conditions such as metabolic syndrome and dyslipidemia.

Heterocycles as nicotinic acid receptor agonists for the treatment of dyslipidemia

Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.

Compounds for treating spinal muscular atrophy

Introduction: The role of estrogens is mostly mediated by two nuclear receptors (ERα and ERβ) and a membrane-associated G-protein (GPR30 or GPER), and it is not limited to reproduction, but it extends to the skeletal, cardiovascular and central nervous systems Various pathologies such as cancer, inflammatory, neurodegenerative and metabolic diseases are often associated with dysfunctions of the estrogenic system Therapeutic interventions by agents that affect the estrogenic signaling pathway might be useful in the treatment of many dissimilar diseases Areas covered: The massive chemodiversity of ER ligands, limited to patented small molecules, is herein reviewed The reported compounds are classified on the basis of their chemical structures Non-steroidal derivatives, which mostly consist of diphenolic compounds, are further segregated into chemical classes based on their central scaffold Expert opinion: Estrogens have been used for almost a century and their earlier applications have concerned inter

Estrogen receptor ligands: a patent review update

The present invention is directed to novel benzopyran derivatives of formula (I), pharmaceutical compositions containing them and their use in the treatment of disorders related to potassium channel.

Novel benzopyran derivatives as potassium channel openers

The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.

Novel tetracyclic heteroatom containing derivatives useful as sex steroid hormone receptor modulators

The present invention is directed to novel heterocyclic benzo[c]chromene derivatives of Formula (I), pharmaceutical compositions containing them and their use in the treatment of disorders mediated by one or more estrogen receptors. The compounds of the invention are useful in the treatment of disorders associated with the depletion of estrogen such as hot flashes, vaginal dryness, osteopenia and osteoporosis; hormone sensitive cancers and hyperplasia of the breast, endometrium, cervix and prostate; endometriosis, uterine fibroids, osteoarthritis and as contraceptive agents, alone or in combination with a progestogen or progestogen antagonist.

Novel heterocyclic benzo[c]chromene derivatives useful as modulators of the estrogen receptors

The present invention is directed to novel heterocycle derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.

Novel heterocycle derivatives useful as selective androgen receptor modulators (sarms)

The present invention is directed to novel benzopyran derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to potassium channel.

Zhihua Sui

Papers

Novel benzopyran derivatives as potassium channel openers

Novel tetracyclic heteroatom containing derivatives useful as sex steroid hormone receptor modulators

Novel heterocyclic benzo[c]chromene derivatives useful as modulators of the estrogen receptors

Novel heterocycle derivatives useful as selective androgen receptor modulators (sarms)

Benzopyran derivatives as potassium channel openers