C07J5/00

Process for the preparation of 17-desoxy-corticosteroids

The present invention provides an improved process for the preparation of 17-desoxy corticosteroid derivatives in a single chemical step by reacting the 17-hydroxy starting material with an excess of Trimethylsilyl Iodide. The present invention is specifically advantageous in preparing 17-desoxy corticosteroid derivatives having one or more halogen groups at positions 2, 6, 7 or 9 of the corticosteroid such as Clocortolone of Desoximetasone.

Polymorphic forms of a steroid-like compound and methods for the preparation and use thereof

Provided herein are multiple solid forms of a defined steroid-like compound, and methods for the preparation and use thereof. In one aspect, there is provided a crystalline form of said steroid-like compound, and methods for the preparation and use thereof. In another aspect, there is provided a substantially amorphous form of said steroid-like compound, and methods for the preparation and use thereof. In yet another aspect, there are provided compositions containing compounds according to the present invention. In certain aspects, such compositions are suitable for delivery of active agents according to the present invention to a subject in need thereof. In another aspect of the invention, there are provided methods for the treatment of a variety of indications, including glaucoma, ocular hypertension, and the like. In still another aspect of the present invention, there are provided kits containing compounds according to the present invention and/or compositions containing same.

CRYSTALLINE SOLVATE FORMS OF A PHARMACEUTICAL

Described herein are solid state 17-ethynylandrost-5-ene-3,7,17-triol including amorphous and crystalline forms and specific polymorphic forms thereof, and use of solid state 17-ethynylandrost-5-ene-3,7,17-triol in treating numerous diseases and disorders, including hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions, and neurodegenerative conditions in subjects or human patients.

STABLE ISOQUINOLINE-CORTICOSTEROID CONJUGATES AND USES THEREOF

Provided herein are compounds and pharmaceutical compositions useful in modulating kinase activity, and related diseases. These compounds are conjugates of glucocorticoids with rho-kinase inhibitors. Also provided herein are methods of treating an eye disease or disorder in a subject. Also provided herein are methods of reducing intraocular pressure in a subject. Also provided herein are methods of modulating kinase activity in a cell. Also provided herein are methods of making the compounds provided herein, and compounds useful for the preparation of the compounds provided herein.

Non-hormonal steroid modulators of NF-?B for treatment of disease

The present invention relates to compounds and methods which may be useful as treatments of neuromuscular diseases such as muscular dystrophy, and as inhibitors of NF-?B for the treatment or prevention of muscular wasting disease, including muscular dystrophy.

PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF 4-PREGENEN-11BETA-17-21-TRIOL-3,20-DIONE DERIVATIVES
20180147217 · 2018-05-31 ·

The present invention relates to pharmaceutical compositions comprising 4-pregenen-11?-17-21-triol-3,20-dione derivatives, and their use as pharmaceuticals as modulators of the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR). The invention relates specifically to the use of these compounds and their pharmaceutical compositions to treat ocular conditions associated with the glucocorticoid receptors (GR) and/or the mineralocorticoid receptors (MR).

A METHOD FOR SCREENING REGULATOR OF MITOCHONDRIAL FISSION

The present invention is directed to a method for screening a regulator of mitochondrial fission using a cell treated to a protopanaxadiol (PPD)-type ginsenoside compound, a composition therefor, and a kit comprising the composition. As the use of the method for screening the regulator of mitochondrial fission of the present invention enables effective discovery of a formulation capable of preventing, improving, or treating a mitochondria-related disease, the method will be widely used for the development of a therapeutic agent for the mitochondria-related disease.

17alpha, 21-dihydroxypregnene esters as antiandrogenic agents
09895379 · 2018-02-20 · ·

The present application provides 17 and/or 21 esters of 17,21-Dihydroxypregna-4,9(11)-diene-3,20-dione and 17,21-dihydroxypregna-4-ene-3,20-dione having remarkable antiandrogenic activity, methods of using these compounds, and processes for their preparation.

Treatment methods using pharmaceutical solid state forms

The invention provides and describes solid state 17-ethynyl-androst-5-ene-3, 7,17-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17-ethynyl-androst-5-ene-3, 7,17-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17-ethynyl-androst-5-ene-3,7,17-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17-ethynyl-androst-5-ene-3, 7,17-triol and uses of such formulations in treating the described conditions.

Treatment methods using pharmaceutical solid state forms

The invention provides and describes solid state 17-ethynyl-androst-5-ene-3, 7,17-triol including amorphous and crystalline forms and specific polymorphic forms thereof. Anhydrates and solvates of 17-ethynyl-androst-5-ene-3, 7,17-triol include Form I anhydrate and Form IV and Form V solvates. The invention further relates to solid and suspension formulations containing 17-ethynyl-androst-5-ene-3,7,17-triol in a described solid state form and use of the formulations to treat hyperglycemic conditions, such as type 2 diabetes and metabolic syndrome, and autoimmune conditions, such as rheumatoid arthritis, ulcerative colitis and type 1 diabetes, among other inflammation related conditions in subjects or human patients. The invention also relates to methods to make liquid formulations from solid state forms of 17-ethynyl-androst-5-ene-3, 7,17-triol and uses of such formulations in treating the described conditions.