Patent classifications
C07J41/0061
Tetrazole derivatives of bile acids as FXR/TGR5 agonists and methods of use thereof
The present invention provides compounds of Formula I: ##STR00001##
pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated by FXR and/or TGR5.
FARNESOID X RECEPTOR MODULATORS
The present invention provides a compound of formula (I):
##STR00001##
or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.6 are as described herein. The present invention relates generally to selective FXR agonists and to methods of making and using them.
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.
STEROL ANALOGS AND USES THEREOF
The invention relates to compositions and methods for the preparation, manufacture, and therapeutic use of compositions comprising mRNA and a lipid nanoparticle comprising a compound of the invention and an ionizable lipid.
Fluorinated bile acid derivatives
The invention relates to compounds of general formula (I): ##STR00001##
wherein R.sup.2a, R.sup.2b, R.sup.3a, R.sup.3b, R.sup.5, Y and R.sup.7 are as defined herein are selective agonists at the FXR receptor and are useful for the treatment or prevention of diseases and conditions including nonalcoholic steatohepatitis (NASH); primary biliary cirrhosis; primary sclerosing cholangitis; biliary atresia; cholestatic liver disease; hepatitis C infection; alcoholic liver disease; fibrosis; and liver damage arising from fibrosis.
ISOTOPICALLY LABELED BILE ACID DERIVATIVES
The present application relates to isotopically labeled compounds of Formula I and methods of preparation and use thereof
##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.
Isotopically labeled bile acid derivatives
The present application relates to isotopically labeled compounds of Formula I and methods of preparation and use thereof. ##STR00001##
NANOPARTICLES COMPRISING DRUG DIMERS, AND USE THEREOF
The present invention relates to a nanoparticle comprising a drug dimer and a use thereof. The nanoparticle comprising a drug dimer of the present invention can increase the drug content and improve the dispersibility of the drug. In addition, the nanoparticle has increased targeting efficiency. Therefore, an effective pharmacological effect can be obtained by using a drug in a less amount, and thus the nanoparticle has excellent commercial applicability.
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.