C07J9/005

POLYMERIC BILE ACID DERIVATIVES INHIBIT HEPATITIS B AND D VIRUS AND NTCP TRANSPORT

The invention provides for treating HBV or HDV infection or inhibiting human sodium taurocholate co-transporting polypeptide (hNTCP) with a polymeric bile acid or salt thereof, and pharmaceutical compositions comprising a polymeric bile acid or salt thereof, and a second HBV or HDV medicament.

COMPOUND FOR TREATING CLOSTRIDIUM DIFFICILE

The invention relates to compounds, compositions and polymers comprising a first component adapted to promote germination of Clostridium difficile (C.diff) and a second component which acts as an antimicrobial agent. Said compounds, compositions and polymers are useful for destroying C.diff where conventional antimicrobial agents are unsuccessful. The compositions can be formulated as coating or materials which actively destroy C.diff which come into contact with it. The germination promotion is induced by bile salts. The invention also relates to the use of such materials as a treatment for C.diff associated diseases and toxic megacolon.

5.BETA.-6-ALKYL-7-HYDROXY-3-ONE STEROIDS AS INTERMEDIATES FOR THE PRODUCTION OF STEROIDAL FXR MODULATORS

The invention relates to compounds of formula (I): wherein R.sub.1, R.sub.2, Y, R.sub.4 and R.sub.5 are as defined herein. The compounds are intermediates in the synthesis of synthetic bile acids.

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BILE SALT HYDROLASE PROBE AND METHOD OF MAKING AND USING THE SAME

Probe embodiments for targeting, identifying, and isolating enzymes exhibiting BSH activity as well as devices and kits that use the probes are described herein. Methods of making and using the probes, devices, and kits are also described. In some embodiments, probes, devices, and kits for targeting, identifying, and isolating enzymes in a biological sample are disclosed. In some embodiments, compositions and methods of treatment using the probes, devices, and kits disclosed herein are described.

COMBINATION OF A POLYHYDROXYLATED BILE ACID AND A FARNESOID X RECEPTOR AGONIST
20220227804 · 2022-07-21 ·

The present invention relates to, in part, a combination therapy of a polyhydroxylated bile acid and a farnesoid X receptor agonist. The present invention also provides, in part, a pharmaceutical composition comprising a farnesoid X receptor agonist and a polyhydroxylated bile acid in the preparation of a medicament for treating a biliary disorder or a gastrointestinal disorder.

PREPARATION AND USES OF OBETICHOLIC ACID

The present invention relates to obeticholic acid:

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or a pharmaceutically acceptable salt, solvate or amino acid conjugate thereof. Obeticholic acid is useful for the treatment or prevention of a FXR mediated disease or condition, cardiovascular disease or cholestatic liver disease, and for reducing HDL cholesterol, for lowering triglycerides in a mammal, or for inhibition of fibrosis. The present invention also relates to processes for the synthesis of obeticholic acid.

Preparation Method of Vascular Leakage Blockers With a High Yield

The present invention relates to a preparation method of a novel vascular leakage blocker with a high yield. The preparation method is easy to react and more productive and economical than the conventional method by using an intermediate that can easily remove impurities generated during the reaction. In addition, the preparation method can produce a novel vascular leakage blocker with a high yield by using a new reagent that has not been previously used in the step of generating an isomer, and is very advantageous in producing a high-quality active pharmaceutical ingredient.

METHODS, COMPOUNDS, COMPOSITIONS AND VEHICLES FOR DELIVERING 3-AMINO-1-PROPANESULFONIC ACID

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease

SMALL MOLECULE MODULATORS OF GUT BACTERIAL BILE ACID METABOLISM

Described herein are methods and compositions related to inhibiting bile salt hydrolase (BSH) and uses thereof. Provided herein is a method for treating a metabolic disorder (e.g., diabetes, obesity), gastrointestinal disease (e.g., a gastrointestinal infection; inflammatory bowel disease (IBD); appendicitis; Crohn's disease (CD); ulcerative colitis (UC); gastritis; enteritis; esophagitis; pancreatitis; diabetes; hepatitis; liver diseases (e.g., Non-alcoholic Fatty Liver Disease (NAFLD); non-alcoholic steatohepatitis (NASH); hepatitis A; hepatitis B; hepatitis C; autoimmune hepatitis; and cirrhosis of the liver) gastroesophageal reflux disease (GERD); celiac disease; diverticulitis; food intolerance; ulcer; infectious colitis; irritable bowel syndrome; leaky gut; and cancer), cancer (e.g., cancer of the digestive system, liver cancer), or an inflammatory disease (e.g., Crohn's disease, inflammatory bowel disease, ulcerative colitis, pancreatitis, hepatitis, appendicitis, gastritis, diverticulitis, celiac disease, food intolerance, enteritis, ulcer, gastroesophageal reflux disease (GERD), psoriatic arthritis, psoriasis, and rheumatoid arthritis) in a subject in need thereof comprising administering to a subject a compound of Formulae (I)-(XVIII).

(17-)-3-oxoandrost-4-en-17-yl dodecanoate compositions and methods of preparation and use

Disclosed are bioavailable solid state (17-β)-3-Oxoandrost-4-en-17-yl dodecanoate compositions and methods of use in administration to mammals in need of thereof. The (17-β)-3-Oxoandrost-4-en-17-yl dodecanoate is preferably provided in a solid state crystalline form having a plurality of peaks corresponding to the peaks shown in FIG. 2, a plurality of crystallites ranging in size from about 40 nm to about 60 nm based as identified via powder x-ray diffraction spectra, and a melting point in the range of about 51° C. to about 63° C. The compositions may be provided in oral or injectable administration form for the treatment of conditions such as in need of testosterone therapy. An exemplary chemical structure of a (17-β)-3-Oxoandrost-4-en-17-yl dodecanoate composition disclosed herein is as follows: ##STR00001##