Patent classifications
A61K31/4453
COMPOUNDS AND METHODS FOR THE TREATMENT OF MICROBIAL INFECTIONS
Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (I):
##STR00001##
In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.
COMPOUNDS AND METHODS FOR THE TREATMENT OF MICROBIAL INFECTIONS
Provided herein are compounds, derivatives thereof, composition comprising one or more of said compounds and derivatives prevention and/or treatment of microbial infections and/or related diseases or conditions. The present compounds and/or derivatives thereof can be represented by Formula (I):
##STR00001##
In one embodiment, said microbial infections are bacterial infections. More specifically, said bacterial infections are staphylococcal infections.
OCT3 ACTIVITY INHIBITOR CONTAINING IMIDAZOPYRIDINE DERIVATIVE AS ACTIVE COMPONENT, AND OCT3 DETECTION AGENT
To provide an OCT3 activity inhibitor having a different basic skeleton than that of conventional OCT3 activity inhibitors. This inhibitor of organic cation transporter 3 (OCT3) contains, as an active component, an imidazo[1,2-a]pyridine derivative, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof.
OCT3 ACTIVITY INHIBITOR CONTAINING IMIDAZOPYRIDINE DERIVATIVE AS ACTIVE COMPONENT, AND OCT3 DETECTION AGENT
To provide an OCT3 activity inhibitor having a different basic skeleton than that of conventional OCT3 activity inhibitors. This inhibitor of organic cation transporter 3 (OCT3) contains, as an active component, an imidazo[1,2-a]pyridine derivative, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate thereof.
Extended release compositions comprising trihexyphenidyl
The present disclosure provides extended release trihexyphenidyl compositions suitable for once- or twice-daily administration. The compositions comprise a core comprising organic acid that is coated with at least one drug layer comprising trihexyphenidyl hydrochloride, and a functional coat over the drug-layered core. The extended release compositions of the disclosure provide extended release of trihexyphenidyl hydrochloride, with reduced C.sub.max, and a C.sub.min:C.sub.max ratio of ≥0.4, while maintaining a therapeutically effective concentration for a period of at least about 16 hours. The compositions of the disclosure improve solubility of trihexyphenidyl hydrochloride, at a pH of greater than or equal to 5, to maintain its minimum effective concentration at such pH. In certain embodiments, the compositions of the disclosure comprise an IR drug layer to provide extended release with a minimal lag time, while maintaining a therapeutically effective concentration of trihexyphenidyl hydrochloride for a period of at least about 16 hours.
Extended release compositions comprising trihexyphenidyl
The present disclosure provides extended release trihexyphenidyl compositions suitable for once- or twice-daily administration. The compositions comprise a core comprising organic acid that is coated with at least one drug layer comprising trihexyphenidyl hydrochloride, and a functional coat over the drug-layered core. The extended release compositions of the disclosure provide extended release of trihexyphenidyl hydrochloride, with reduced C.sub.max, and a C.sub.min:C.sub.max ratio of ≥0.4, while maintaining a therapeutically effective concentration for a period of at least about 16 hours. The compositions of the disclosure improve solubility of trihexyphenidyl hydrochloride, at a pH of greater than or equal to 5, to maintain its minimum effective concentration at such pH. In certain embodiments, the compositions of the disclosure comprise an IR drug layer to provide extended release with a minimal lag time, while maintaining a therapeutically effective concentration of trihexyphenidyl hydrochloride for a period of at least about 16 hours.
PEPTIDES, COMPOUNDS, COMPOSITIONS AND METHODS FOR INHIBITING SOX9
The present application provides SOX9 inhibitor compounds and compositions and methods of use thereof. In certain aspects, the SOX9 inhibitor is a peptide comprising a portion of the SOX9 dimerization motif. In other aspects, the SOX9 inhibitor is a compound of the general formula I
##STR00001##
where one A is H and the other is:
##STR00002##
and the remaining substituents are as defined in the application.
METHOD OF USING HUMAN SPHEROIDS FOR DRUG DISCOVERY
The present invention discloses, in one embodiment, a method of using human induced pluripotent stem cells to generate three-dimensional human organ tissue for therapeutic drug toxicity and discovery⋅. In one embodiment, a high throughput microtiter plate is loaded with both wild type and Rett disease 3D spheroids and exposed to a drug library, and activity is measured and analyzed for disease rescue to wild type cell behavior.
METHOD OF USING HUMAN SPHEROIDS FOR DRUG DISCOVERY
The present invention discloses, in one embodiment, a method of using human induced pluripotent stem cells to generate three-dimensional human organ tissue for therapeutic drug toxicity and discovery⋅. In one embodiment, a high throughput microtiter plate is loaded with both wild type and Rett disease 3D spheroids and exposed to a drug library, and activity is measured and analyzed for disease rescue to wild type cell behavior.
BILE ACID RECYCLING INHIBITORS FOR TREATMENT OF HYPERCHOLEMIA AND CHOLESTATIC LIVER DISEASE
Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.