The present invention provides compounds of Formula I: ##STR00001##
pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.

The present disclosure provides a purification method of progesterone. In this method, aldehyde impurities in a progesterone crude product react with a sulfurated nucleophile to yield highly polar hydroxysulfonates and progesterone to realize solubility differentiation, and highly pure progesterone with a content higher than 99.5% and a total aldehyde impurities content lower than 0.2% is obtained through elutriation, filtration, washing a filter cake with water, and drying. The purification method provided by the present disclosure avoids the technical bottleneck of progesterone purification in the prior art, and all reagents and raw materials used during the reaction are inexpensive and easily available, with low equipment requirement and cost input; the purification process is mild and safe, conditions are easy to control, and the purification and recovery rate of the product is high; reagents used cause little environmental pollution, and particularly highly polluting chromium-containing reagents are not used.

The present invention provides a compound of formula (I):

##STR00001##

or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are as described herein. The present invention relates generally to selective FXR agonists and to methods of making and using them.

Disclosed herein are monomeric and oligomeric compound embodiments for use as contraceptive agents. Monomeric compound embodiments disclosed herein comprise substituents that facilitate the ability of the compounds to exhibit progestogenic, androgenic, and estrogenic activity, which can prevent or inhibit bone density loss in subjects. Oligomeric compound embodiments disclosed herein provide the ability to control receptor activation and/or treatment by incorporating a tunable linker group which couples steroidal-based compounds to one another or with therapeutic agents and facilitates selective cleavage of the monomeric components of the oligomeric compound.

The present disclosure relates to polycyclic (e.g., tetracyclic) glucocorticoid receptor (GR) modulators, synthetic methods for preparing such GR modulators, and methods of using such GR modulators to treat a glucocorticoid-dependent condition, such as cancer or hypercortisolism. Exemplary compounds have quaternary centers at C9 and C13 in which the quaternary center at C9 projects a substituent on the opposite face of the tetracycle as the substituent at C13.

The invention relates to compositions and methods for the preparation, manufacture, and therapeutic use of compositions comprising mRNA and a lipid nanoparticle comprising a compound of the invention and an ionizable lipid.

N-methyl-d-aspartate receptors (NMDAR) and/or potentiating y-aminobutyric acid receptors (GABAAR) agents and uses thereof are described. Uses of these agents include methods of treating or preventing various psychiatric diseases, disorders, or conditions and methods of treating or preventing alcohol use disorder in a subject in need thereof.

The present invention discloses novel method for synthesizing vegan cholesterol and vitamin D3 from inexpensive crude phytosterol.

Disclosed is a method for preparing β-carbonyl sulfones. The method comprises: by taking an α-carbonyl diazo compound and sodium arylsulfinate as reaction substrates, cheap silver nitrate as an optimal catalyst, 1,10-phenanthroline as a ligand, and potassium persulfate as an oxidant, carrying out coupling reaction in a mixed solvent of acetonitrile and water to obtain a β-carbonyl sulfones compound. Compared with the prior art, the method has the following advantages: a wide range of reaction substrates, short reaction time, a relatively high reaction yield, a mild reaction condition, etc. In the present invention, non-toxic and harmless reagents are used as reaction raw materials, so that it has no harm to the environment and satisfies the requirements of contemporary green chemistry development. Post-reaction treatment is relatively simple, and is convenient for separation and purification. In addition, the reaction can achieve gram-scale synthesis, and lays a foundation for actual applications.

In one aspect, the disclosure relates to a facile strategy to introduce electron-deficient aryl sulfate diesters to silylated hydroxyl groups of carbohydrates and amino acids, among other substrates, wherein selective hydrolysis and the removal of an electron-deficient aromatic group allows for the efficient generation of sulfated carbohydrates, peptides, and other compounds. The incorporation of electron-deficient aryl sulfate diesters in the early stage of the synthesis of glycans, peptides, and the like, disclosed herein avoids time-consuming protecting group manipulations, simplifies the purification of sulfated products, and improves the overall yield and efficiency. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.