C07J5/00

NON-HORMONAL STEROID MODULATORS OF NF-kB FOR TREATMENT OF DISEASE
20180015104 · 2018-01-18 ·

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.

-ent-19-norprogesterone, compositions and uses thereof to treat traumatic brain injury (TBI), including concussions-
20240409576 · 2024-12-12 · ·

The present invention relates to ent-19-Norprogesterone, compositions and methods of use thereof to treat, minimize and/or prevent traumatic brain injury (TBI), including severe TBI, moderate TBI and mild TBI, including concussions.

19-nor C3,3-disubstituted C21-n-pyrazolyl steroids and methods of use thereof

Provided herein are 19-nor C3,3-disubstituted C21-pyrazolyl steroids of Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof; wherein custom character, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6, and R.sup.7 are as defined herein. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, convulsive disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain, traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, and tinnitus.

Crystalline solvate forms of a pharmaceutical

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.

Pharmaceutical compositions and methods of use of 4-pregenen-11β-17-21-triol-3,20-dione derivatives
09717743 · 2017-08-01 · ·

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).

Process for the production of 21-methoxy-11-beta-phenyl-19-nor-pregna-4,9-diene-3,20-dione derivatives

The present invention relates to a process for the synthesis of compounds of formula (I), ##STR00001##
wherein the meaning of R is dimethylamino or acetyl group, using the compound of formula (III) or (IV), wherein the meaning of R is dimethylamino or 2-methyl-1,3-dioxan-2-yl group, as starting material and methoxymethyl lithium as reagent. ##STR00002##

Neuroactive 19-alkoxy-17-substituted steroids, prodrugs thereof, and methods of treatment using same

The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Industrial process for the synthesis of ulipristal acetate and its 4′-acetyl analogue

The present invention relates to a new process for the synthesis of compounds of formula (I) (wherein the meaning of R is dimethylamino or acetyl group) using the compound of formula (II) (wherein the meaning of R is dimethylamino or 2-methyl-1,3-dioxolan-2-yl group) as starting material, as well as to the intermediate of the process. ##STR00001##

NEUROACTIVE 19-ALKOXY-17-SUBSTITUTED STEROIDS, PRODRUGS THEREOF, AND METHODS OF TREATMENT USING SAME
20170152282 · 2017-06-01 · ·

The present disclosure is generally directed to neuroactive 19-alkoxy-17-substituted steroids as referenced herein, and pharmaceutically acceptable salts thereof, for use as, for example, an anesthetic, and/or in the treatment of disorders relating to GABA function and activity. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

Crystalline solvate forms of a pharmaceutical

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.