Patent classifications
C07J9/005
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.
METHOD FOR SYNTHESIZING URSODEOXYCHOLIC ACID USING BA AS RAW MATERIAL
The present invention discloses a synthesis method of ursodeoxycholic acid by using the plant-derived compound BA as a raw material to synthesize ursodeoxycholic acid through the steps of ethylene glycol or neopentyl glycol protection, oxidation, Wittig reaction, deprotection, reduction and hydrolysis, etc. The raw materials used for the synthesis of ursodeoxycholic acid in the present invention are cheap and easy to get, the synthesis steps are easy to operate, the yield is high, the reaction is environmentally friendly, and the industrial production is convenient.
Tetrazolones as a Carboxylic Acid Bioisosteres
The present disclosure provides compounds that include a tetrazolone derivative of a carboxyl group of an active agent. This disclosure also relates to pharmaceutical compositions that include these compounds, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
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.
DEXAMETHASONE PRODRUG COMPOSITIONS AND USES THEREOF
The disclosure features pharmaceutical compositions formed from prodrug dimers for the extended delivery of a drug and for the treatment of a disease or condition.
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.
PHARMACEUTICAL COMPOSITION FOR TREATING FATTY LIVER DISEASE
Provided is a pharmaceutical composition for treating and/or preventing fatty liver disease, particularly nonalcoholic fatty liver disease, the pharmaceutical composition having an excellent ACC2-selective inhibitory action and having no side effects such as an increase in plasma triglyceride or a decrease in platelet concentration.
A pharmaceutical composition for treating and/or preventing fatty liver disease, the pharmaceutical composition comprising a compound represented by Formula (I):
##STR00001## wherein R.sup.1 is haloalkyl or non-aromatic carbocyclyl, R.sup.2 is a hydrogen atom or halogen, R.sup.3 is halogen, ring A is a group represented by the formula:
##STR00002## -L.sup.1- is —O—(CH.sub.2)—, —(CH.sub.2).sub.2—, or the like, R.sup.4 is alkyl or haloalkyl, and R.sup.5 is alkylcarbonyl or carbamoyl, or a pharmaceutically acceptable salt thereof.
BILE ACID DERIVATIVES AS FXR/TGR5 AGONISTS AND METHODS OF USE THEREOF
The present invention provides compounds represented by Formula I, or pharmaceutically acceptable salts, stereoisomers, solvates, hydrates or combination thereof,
##STR00001##
The invention also provides pharmaceutical compositions comprising these compounds and methods of using this compounds for treating FXR-mediated or TGR5-mediated diseases or conditions.
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.
NMDAR INHIBITING AGENTS AND GABAAR POTENTIATING AGENTS AND USES THEREOF
N-methyl-d-aspartate receptors (NMDAR) and/or potentiating y-aminobutyric acid receptors (GABAAR) agents and uses thereof are described. Uses of these agents include methods of treating or preventing various psychiatric diseases, disorders, or conditions and methods of treating or preventing alcohol use disorder in a subject in need thereof.