Patent classifications
C07J41/0061
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, and R.sup.3 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions. ##STR00001##
FUNCTIONALIZED BILE ACIDS FOR THERAPEUTIC AND MATERIAL APPLICATIONS
The subject disclosure is directed to functionalized bile acids, preparation thereof, and usage thereof for therapeutic and material applications. In one embodiment, a method of generating functionalized bile acid materials can comprise directly activating a carboxylic acid of a bile acid compound using a coupling agent comprising an amide or ester compound, thereby generating an intermediate bile acid derivative material. The method can further comprise attaching a functional group material to the intermediate bile acid derivative material by reacting the functional group material and the intermediate bile acid derivative material, thereby generating a functionalized bile acid material.
CATIONIC STEROIDAL ANTIMICROBIAL COMPOUNDS WITH URETHANE LINKAGES
Cationic steroidal antimicrobial (CSA) compounds having a structure of Formula I, II or III, or salt thereof, wherein at least one of at least one of R.sub.1-R.sub.18, (e.g., R.sub.3, R.sub.7 and R.sub.12) is linked to the steroidal backbone by a urethane group:
##STR00001##
At least one of R.sub.1-R.sub.18, (e.g., R.sub.3, R.sub.7 and R.sub.12) has the following urethanyl structure:
—O—(C═O)—NR.sub.19R.sub.20
where R.sub.19 and R.sub.20 are independently hydrogen, alkyl, alkenyl, alkynyl, aryl, aminoalkyl, aminoalkenyl, aminoalkynyl, or aminoaryl, provided that at least one of R.sub.19 or R.sub.20 includes an amino group (e.g., R.sub.19 is hydrogen and R.sub.20 is (C.sub.2-C.sub.6)aminoalkyl).
R.sub.18 can have the following structure:
—R.sub.21—(C═O)—NR.sub.22R.sub.23
where R.sub.21 is omitted or alkyl, alkenyl, alkynyl, or aryl, and R.sub.22 and R.sub.23 are hydrogen, alkyl, alkenyl, alkynyl, or aryl, provided that at least one of R.sub.22 or R.sub.23 is not hydrogen.
FLUORINATED AND ALKYLATED BILE ACIDS
The present invention relates to fluorinated and alkylated bile acids.
Composition for adjusting biological tissue size, and method for adjusting size of biological tissue using said composition
The present invention provides a composition for adjusting biological tissue size and a method for adjusting the size of biological tissue using the said composition. The composition for adjusting the size of biological tissue according to the present invention can adjust the size of biological tissue according to the specifications of a microscope and the needs of a researcher, and can be used as a mounting solution to easily acquire an image of the biological tissue. Therefore, the composition can be usefully used to reveal the causes of and find treatment methods for various disorders.
Functionalized bile acids for therapeutic and material applications
The subject disclosure is directed to functionalized bile acids, preparation thereof, and usage thereof for therapeutic and material applications. In one embodiment, a method of generating functionalized bile acid materials can comprise directly activating a carboxylic acid of a bile acid compound using a coupling agent comprising an amide or ester compound, thereby generating an intermediate bile acid derivative material. The method can further comprise attaching a functional group material to the intermediate bile acid derivative material by reacting the functional group material and the intermediate bile acid derivative material, thereby generating a functionalized bile acid material.
METHOD FOR MASS-PRODUCING SODIUM TAURODEOXYCHOLATE
The present invention relates to a mass production method of sodium taurodeoxycholate having low impurity and few by-products, in which the procedure of process is simplified since isopropyl alcohol is used and separation and purification is performed through batch washing for commercial production of sodium taurodeoxycholate.
TGR5 modulators and methods of use thereof
The application relates to compounds of formula A: ##STR00001##
or a salt, solvate, ester, tautomer, amino acide conjugate, or metabolite thereof. The compounds of formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
STEROIDAL COMPOSITIONS AND METHODS OF TREATING LIPOGENIC CANCERS
The invention describes novel steroidal compounds, compositions containing the same, and methods of using the same as SREBP inhibitors, as LXR agonists, or as dual modulators of SREBP and LXR, to treat SREBP and/or LXR mediated diseases.
BILE ACID DERIVATIVE, COMPOSITION AND APPLICATION THEREOF
Provided are a novel bile acid derivative for treating fatty liver disease, a pharmaceutical composition thereof, and a use in the preparation of a medicine for treating and improving diseases and symptoms mediated or caused by FXR or TGR5. The bile acid derivative of the present invention inhibits or delays the metabolism of bile acid by bacterial BSH/7α dehydroxylase in the intestine and greatly prolongs the effective survival time of bile acid in the intestine. The bile acid derivative and the pharmaceutical composition thereof can significantly stimulate bile acid membrane receptor TGR5, promote the secretion of glucagon-like peptide 1 from enteroendocrine cells, reduce liver fat accumulation, significantly improve liver function and increase glucose tolerance, thereby having an excellent effect on the treatment of fatty liver disease.