Patent classifications
C07J31/006
CRYSTALLINE AND LIQUID CRYSTALLINE 25-HYDROXY-CHOLEST-5-EN-3-SULFATE SODIUM AND METHODS FOR PREPARING SAME
Crystalline and liquid crystalline forms of 25HC3S sodium are described herein. The disclosure includes Forms I, II, III, V, IX, XI, and XIII of 25HC3S sodium and combinations thereof. Pharmaceutical formulations of said forms, or combinations thereof, and methods of treating or preventing disease such as hypercholesterolemia, hypertriglyceridemia, and conditions related to fat accumulation and inflammation (e.g., non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), alcoholic hepatitis, acute kidney injury (AKI), psoriasis, and atherosclerosis) are further disclosed herein. Methods for preparing 25HC3S are also provided
OXYSTEROLS AND METHODS OF USE THEREOF
Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.8 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
##STR00001##
COMPOSITIONS COMPRISING 5-CHOLESTEN-3, 25-DIOL, 3-SULFATE (25HC3S) OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF AND AT LEAST ONE CYCLIC OLIGOSACCHARIDE
Compositions comprising 5-cholesten-3, 25-diol, 3-sulfate (25HC3S) or pharmaceutically acceptable salt thereof and at least one cyclic oligosaccharide, e.g., a cyclodextrin (CD), are provided. The compositions may be used to prevent and/or treat a variety of diseases and conditions, including organ failure (e.g. acute liver failure), high cholesterol/high lipids, and various inflammatory diseases and conditions.
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.
METHODS FOR MODULATION OF LIPOPROTEIN LIPASE AND APOLIPOPROTEIN C2 EXPRESSION AND/OR ACTIVITY IN THE TREATMENT OF PERIPHERAL AND CENTRAL NERVOUS SYSTEM TISSUE DISEASE STATES
Methods for modulating lipoprotein lipase (LPL) and Apoliprotein C2 (ApoC2) expression and/or activity in the treatment of peripheral and central nervous system tissue disease states with C-6 substituted estradiol derivatives are presented herein.
CONJUGATED NEUROACTIVE STEROID COMPOSITIONS AND METHODS OF USE
The present disclosure provides modified neuroactive steroids. The modified neuroactive steroids may comprise, consist of, or consist essentially of a therapeutic agent and/or a modifying moiety. The modified neuroactive steroid can have modified characteristics as compared to native neuroactive steroids that do not include a modifying moiety and/or therapeutic agent. The modified neuroactive steroid may be, for example, modified pregnenolone, pregnenolone metabolites, allopregnanolone, and/or allopregnanolone metabolites. The modified neuroactive steroids can be used to treat, prevent and/or ameliorating a phenotypic state of interest in a subject.
Radiation-sensitive resin composition and resist pattern-forming method
A radiation-sensitive resin composition includes a polymer including a phenolic hydroxyl group, a compound represented by formula (1-1) or formula (1-2), and a compound represented by formula (2). In the formula (1-1), a sum of a, b, and c is no less than 1; at least one of R.sup.1, R.sup.2, and R.sup.3 represents a fluorine atom or the like; and R.sup.4 and R.sup.5 each independently represent a hydrogen atom, a fluorine atom, or the like. In the formula (1-2), in a case in which d is 1, R.sup.6 represents a fluorine atom or the like, and in a case in which d is no less than 2, at least one of the plurality of R.sup.6s represents a fluorine atom or the like; and R.sup.8 represents a single bond or a divalent organic group having 1 to 20 carbon atoms. ##STR00001##
Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid
The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I): ##STR00001##
wherein: , R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and Y are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS
Provided herein is a compound of Formula (1-I): or a pharmaceutically acceptable salt thereof, wherein R.sup.2a, R.sup.2b, R.sup.3, R.sup.4a, R.sup.4b, R.sup.5, R.sup.6a, R.sup.6b, R.sup.11a, R.sup.11b, R.sup.16a, R.sup.16b, R.sup.19, R.sup.18, X, q, r, s, t, u, and n are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (1-I) and methods of using the compounds, e.g, in the treatment of CNS-related disorders.
##STR00001##
ACTINIC-RAY-SENSITIVE OR RADIATION-SENSITIVE RESIN COMPOSITION, ACTINIC-RAY-SENSITIVE OR RADIATION-SENSITIVE FILM, METHOD FOR FORMING PATTERN, AND METHOD FOR PRODUCING ELECTRONIC DEVICE
The present invention provides an actinic ray-sensitive or radiation-sensitive resin composition containing (A) a resin having a polarity that increases by an action of an acid, and (B) a compound that generates an acid upon irradiation with actinic rays or radiation, represented by a specific general formula, is which the resin (A) includes a repeating unit represented by a specific general formula; and an actinic ray-sensitive or radiation-sensitive film formed of the actinic ray-sensitive or radiation-sensitive resin composition, a pattern forming method, and a method for manufacturing an electronic device.