C07J1/00

INHIBITORS OF GLUCOCORTICOID RECEPTOR

The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer and hypercortisolism.

ESTROGEN RECEPTOR BETA SELECTIVE LIGANDS
20200377546 · 2020-12-03 ·

An estrogen receptor selective ligand can be a compound according to Structure 1:

##STR00001##

wherein m is 0, 1, or 2 and R is H, a C.sub.1 to C.sub.5 alkyl group, vinyl, CF.sub.3, CH.sub.2CH.sub.2F, CH.sub.2CHF.sub.2, or CH.sub.2CF.sub.3. A composition (e.g., pharmaceutical or cosmetic composition) can include an effective amount of a compound according to Structure 1 and a physiologically acceptable carrier, diluent, or excipient, formulated for topical administration. A method (e.g., therapeutic or cosmetic method) can include administering to a subject in need thereof an effective amount of a compound according to Structure 1 or a composition including Structure 1. Administration can be topical (e.g., to skin, scalp or mucosa).

Process for the preparation of estetrol

The present invention relates to a process for the preparation of estra-1,3,5(10)-trien-3, 15a, 16a, 17-tetraol (estetr-01), via a silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10), 16-tetraene, wherein A is a protecting group and B is Si(R.sup.2).sub.3. The invention further relates to a process for the synthesis of 3-A-oxy-estra-1,3,5(10), 15-tetraen-17-one, in which A is a protecting group, via silyl enol ether derivative 17-B-oxy-3-A-oxy-estra-1,3,5(10),16-tetraene, and B is Si(R.sup.2).sub.3.

POLYSUBSTITUTED BENZENE, PREPARATION METHOD THEREOF, AND METHOD OF USING THE SAME
20200361893 · 2020-11-19 ·

A polysubstituted benzene compound, preparation method thereof, and method of using the same. The compound has a formula I or I, where X represents carbon, sulfur, or oxygen; R.sup.1 represents a C.sub.1-16 alkyl, C.sub.2-16 alkenyl, or C.sub.2-10 alkynyl; R.sup.2 represents hydrogen, halogen, C.sub.1-16 alkyl, C.sub.2-16 alkenyl, or C.sub.2-10 alkynyl; or an aryl group or a substituted aryl group by 1-5 groups selected from halogen, C.sub.1-26 alkyl, C.sub.1-3 halogenated alkyl, OC.sub.1-3 alkyl, hydroxyl, amino, nitro, cyano group, aldehyde group and ester group; or a heteroaryl group or a substituted heteroaryl group by 1-5 groups selected from halogen, C.sub.1-26 alkyl, C.sub.1-3 halogenated alkyl, OC.sub.1-3 alkyl, hydroxyl, amino, nitro, cyano group, aldehyde group and ester group; the heteroaryl group is a 3-10-membered heteroaryl group including N, S, O, or a combination thereof.

PREPARATION OF BILE ACIDS AND INTERMEDIATES THEREOF

Synthetic methods for preparing deoxycholic acid and intermediates thereof are provided.

PREPARATION OF BILE ACIDS AND INTERMEDIATES THEREOF

Synthetic methods for preparing deoxycholic acid and intermediates thereof are provided.

C19 SCAFFOLDS AND STEROIDS AND METHODS OF USE AND MANUFACTURE THEREOF
20240010670 · 2024-01-11 ·

The present disclosure relates to stereodefined polycyclic (e.g., tetracyclic) compounds that contain quaternary centers at one or multiple ring fusions, synthetic methods for preparing such compounds, and methods of using such compounds to treat a disease, such as a brain tumor and, particularly, a glioma.

STABLE ISOTOPE-LABELED COMPOUNDS
20200283469 · 2020-09-10 · ·

Provided are a novel internal standard useful in the measurement of androgens, a method capable of measuring the androgen in a highly selective and highly sensitive (accurate) manner using liquid chromatography mass spectrometry with simplified pretreatments, and a method for diagnosis of a disease using the androgen measurement method. The novel stable isotope-labeled compound is synthesized by performing reduction reaction in a specific solvent. An androgen is measured using this novel stable isotope-labeled compound as an IS.

Composition containing saponins of <i>Panax ginseng </i>as active ingredient

Disclosed are uses of ginseng saponin, which contains at least 90% of a compound K, Rd, F2, and Rg3 as a main ingredient and has effects in extending the lifespan of the cell, promoting the cell differentiation, increasing the number of red blood cells, and reducing the triglycerides by extracting, heat-treating, and enzyme-converting the ginseng saponin to prepare active saponins Rd, F2, and Rg3 including a compound K.

Neuroactive steroids, compositions, and uses thereof

Compounds are provided according to Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v): ##STR00002##
and wherein L.sup.1, L.sup.2, L.sup.3, X.sup.1, X.sup.2, Y, R.sup.Z4, R.sup.Z5, R.sup.Z6, n, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.14, R.sup.17, R.sup.19, R.sup.20, R.sup.23a, R.sup.23b, and R.sup.24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.