C07J31/00

19-NOR NEUROACTIVE STEROIDS AND METHODS OF USE THEREOF

Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (1): and pharmaceutical compositions thereof. 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, 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, tinnitus, and status epilepticus.

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SELECTIVE PROGESTERONE RECEPTOR MODULATOR (SPRM) REGIMEN
20190211053 · 2019-07-11 ·

The invention is directed to a pharmaceutical composition comprising a progesterone receptor antagonist namely (11,17)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethyl)estra-4,9-dien-3-one for the treatment and/or prophylaxis of Uterine Fibroids (myomas, uterine leiomyoma) that is administered to a patient diagnosed with Uterine Fibroids following a specific regimen. Additionally, the invention is directed to a method for treating Uterine Fibroids (myomas, uterine leiomyoma) and/or for reducing Uterine Fibroids (myomas, uterine leiomyoma) size and symptoms related to Uterine Fibroids following a specific regimen as well as treatment of Heavy Menstrual Bleeding (HMB).

METHODS FOR THE PREPARATION OF OBETICHOLIC ACID AND DERIVATIVES THEREOF
20190211052 · 2019-07-11 ·

The present application relates to a method of preparing a bile acid derivative, or a pharmaceutical acceptable salt, solvate, or amino acid conjugate thereof, comprising reacting Compound 2 with paraldehyde to form Compound 3:

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Pharmaceutical composition for prevention, treatment or delay of Alzheimer's disease or dementia containing G protein-coupled receptor 19 agent as active ingredient

The present invention relates to a pharmaceutical composition for preventing, treating or delaying an Alzheimer's disease (AD) or dementia including a G protein-coupled receptor19 (GPCR19) agonist or its pharmaceutically acceptable salt as an active ingredient and a food composition for preventing, treating or delaying an Alzheimer's disease or dementia. The GPCR19 agonist according to the present invention has an effect of improving cognitive and behavioral disorders without harming the health of objects when administrated to the objects and has an effect of preventing the Alzheimer's disease or dementia or delaying or treating the progression of the disease in the objects with the disease by suppressing apoptosis of the brain tissue, enhancing immunity, and reducing formation of an amyloid (A) plague.

RESIST COMPOSITION, METHOD OF FORMING RESIST PATTERN, AND COMPOUND
20190204739 · 2019-07-04 ·

A resist composition containing a compound (B1) represented by Formula (b1) in which R.sup.b1 represents a monovalent hydrocarbon group which has a steroid skeleton and 17 to 50 carbon atoms, Y.sup.b1 and Y.sup.b2 each independently represent a divalent linking group having a hetero atom, V.sup.b1 represents a divalent linking group containing a cyclic aliphatic hydrocarbon group, V.sup.b2 represents an alkylene group, a fluorinated alkylene group, or a single bond, R.sup.f1 represents a hydrogen atom, a fluorine atom, or a fluorinated alkyl group having 1 to 5 carbon atoms, m represents an integer of 1 or greater, and M.sup.m+ represents an m-valent organic cation

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Tandem facial amphiphiles

The invention provides tandem facial amphiphiles for biochemical manipulations and characterization of membrane proteins, such as intrinsic membrane proteins. Members of this new family display favorable behavior with several membrane proteins. These amphiphiles can form relatively small micelles, and small changes in amphiphile chemical structures can result in large changes in their physical properties. The tandem facial amphiphiles can be used to aid the solubilization, isolation, purification, stabilization, crystallization, and/or structural determination of membrane proteins.

Chemical compounds and use thereof for improving muscular quality

Chemical compounds and the therapeutic use thereof, in particular for improving muscular quality in mammals. More particularly, a method of improving muscular quality in sarcopenic mammals and treating and/or preventing sarcopenia using the chemical compounds and, in particular, sarcopenic obesity and the associated complications and/or pathologies thereof, such as loss of strength, muscle mass, performance and of physical and movement capacity. Also, a method of improving muscle quality in obese mammals and treating and/or preventing of obesity and associated complications and/or pathologies, advantageously type 2 diabetes and metabolic syndrome, using the chemical compounds.

PREPARATIONS OF HYDROPHOBIC THERAPEUTIC AGENTS, METHODS OF MANUFACTURE AND USE THEREOF

The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic agent such as fluticasone or triamcinolone, pharmaceutical compositions (e.g., topical or intranasal compositions) thereof and methods for treating and/or preventing the signs and/or symptoms of disorders such as blepharitis, meibomian gland dysfunction or skin inflammation or a respiratory disease (e.g., asthma).

Nuclear Sulfated Oxysterol, Potent Regulator of Lipid Homeostasis, for Therapy of Hypercholesterolemia, Hypertriglycerides, Fatty Liver Diseases, and Atherosclerosis
20190169225 · 2019-06-06 ·

The sulfated oxysterol 5-cholesten-3, 25-diol 3-sulphate, a nuclear cholesterol metabolite that decreases lipid biosynthesis and increases cholesterol secretion and degradation, is provided as an agent to lower intracellular and serum cholesterol and/or triglycerides, and to prevent or treat lipid accumulation-associated inflammation and conditions associated with such inflammation. Methods which involve the use of this sulfated oxysterol to treat conditions associated with high cholesterol and/or high triglycerides and/or inflammation (e.g. hypercholesterolemia, hypertriglyceridemia, non-alcoholic fatty liver diseases, atherosclerosis, etc.) are also provided.

S1PR2 ANTAGONISTS AND USES THEREFOR
20190169187 · 2019-06-06 ·

Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) through the administration of a therapeutically effective amount of a sphingosine-1-phosphate receptor type 2 (S1PR2) antagonist. Also provided herein are (Z)-3-((2,6-dichloropyridin-4-yl)amino)-3-(((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)amino)acrylonitrile and analogs thereof, and their use in treating retinopathies and diseases characterized by insufficient angiogenesis.