Patent classifications
C07J31/00
Nuclear sulfated oxysterol, potent regulator of lipid homeostasis, for therapy of hypercholesterolemia, hypertriglycerides, fatty liver diseases, and atherosclerosis
The sulfated oxysterol 5-cholesten-3β, 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.
METHODS OF MAKING CHOLIC ACID DERIVATIVES AND STARTING MATERIALS THEREFOR
Methods of making cholic acid derivatives, particularly ursodeoxycholic acid, tauroursodeoxycholic acid, 7-ketolithocholic acid, obeticholic acid, their carboxylate salts and carboxylate esters, and starting materials and intermediates therefor.
PROCESS FOR THE PREPARATION OF FULVESTRANT
The present invention relates to a process for the preparation of Fulvestrant which includes recovering the by-products deriving from the oxidation of the corresponding sulfide and then subjecting the by-products to a reduction reaction in the presence of specific reducing agents.
C7 SUBSTITUTED OXYSTEROLS AND METHODS OF USE THEREOF
Compounds are provided according to Formula (A):
##STR00001##
and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1A, R.sup.1B, n, R.sup.2A, R.sup.2B, R.sup.3, and R.sup.4 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
POSITIVE RESIST COMPOSITION AND PATTERNING PROCESS
A positive resist composition is provided comprising (A) an acid generator in the form of a sulfonium salt consisting of a fluorine-containing sulfonate anion and a fluorine-containing sulfonium cation, (B) a quencher in the form of a sulfonium salt containing at least two fluorine atoms in its cation or containing at least 5 fluorine atoms in its anion and cation, and (C) a base polymer comprising repeat units (a1) having a carboxy group whose hydrogen is substituted by an acid labile group and/or repeat units (a2) having a phenolic hydroxy group whose hydrogen is substituted by an acid labile group. The resist composition exhibits a high sensitivity, high resolution and improved LWR or CDU.
FLUORINATED BILE ACIDS
Compounds of general formula (1):
##STR00001##
wherein R.sup.1, R.sup.2 and R.sup.3 are as defined herein;
are of use in the treatment and prevention of neurodegenerative disorders including Alzheimer's disease and Parkinson's disease.
C7 substituted oxysterols and methods of use thereof
Compounds are provided according to Formula (A): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1A, R.sup.1b, n, R.sup.2A, R.sup.2b, R.sup.3, and R.sup.4 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions. ##STR00001##
PREPARATIONS OF HYDROPHOBIC THERAPEUTIC AGENTS, METHODS OF MANUFACTURE AND USE THEREOF
The present invention further provides method of preparing nanocrystals of a hydrophobic therapeutic gent 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 dysfuntion or skin inflammatiom or a respiratory disease (e.g., asthma).
TGR5 MODULATORS AND METHODS OF USE THEREOF
The invention relates to compounds of Formula A:
##STR00001##
or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, liver disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
TGR5 MODULATORS AND METHODS OF USE THEREOF
The invention relates to compounds of Formula A:
##STR00001##
or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, liver disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.