C07D473/08

Methods and compositions for treating pain

The present application relates to compounds and methods for treating pain, incontinence and other conditions.

Methods and compositions for treating pain

The present application relates to compounds and methods for treating pain, incontinence and other conditions.

Flagellar and needle complex (injectosome) loop as anti bacterial drug target

The present invention relates to a method for screening a compound that inhibits secretion of toxins into host-cell cytoplasm by virulent bacteria using a needle type III secretion system. The compound of the invention is selected by screening for a compound which interacts with a loop region of the cytoplasmic domain of the membrane protein FlhB from Salmonella typhimurium or a paralog thereof. Compositions including the compound of the invention, use of the compound, and methods of treating disorders caused by virulent bacteria are also provided.

Flagellar and needle complex (injectosome) loop as anti bacterial drug target

The present invention relates to a method for screening a compound that inhibits secretion of toxins into host-cell cytoplasm by virulent bacteria using a needle type III secretion system. The compound of the invention is selected by screening for a compound which interacts with a loop region of the cytoplasmic domain of the membrane protein FlhB from Salmonella typhimurium or a paralog thereof. Compositions including the compound of the invention, use of the compound, and methods of treating disorders caused by virulent bacteria are also provided.

Compounds for repressing cancer cell growth

The disclosure generally relates to compounds, compositions, and methods for the treatment of cancer by restoring the P53 pathway signaling to repress cancer cell growth. In particular, the compounds comprise Formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein: R.sub.1 is hydrogen or a haloalkyl group; and each R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 is, independently, hydrogen, halogen, hydroxyl, cyano, alkyl, alkenyl, alkoxy, substituted or unsubstituted aryl, heteroaryl, phosphate, phosphoramidate, amine, alkylamino, acylamino, aminoalkoxy, or alkylthio.

Compounds for repressing cancer cell growth

The disclosure generally relates to compounds, compositions, and methods for the treatment of cancer by restoring the P53 pathway signaling to repress cancer cell growth. In particular, the compounds comprise Formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein: R.sub.1 is hydrogen or a haloalkyl group; and each R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, and R.sub.7 is, independently, hydrogen, halogen, hydroxyl, cyano, alkyl, alkenyl, alkoxy, substituted or unsubstituted aryl, heteroaryl, phosphate, phosphoramidate, amine, alkylamino, acylamino, aminoalkoxy, or alkylthio.

SPECIFICALLY-SHAPED CRYSTAL OF COMPOUND AND METHOD FOR PRODUCING SAME

The present invention provides a method for obtaining a specifically-shaped crystal (specifically, spherocrystal) of a compound with good reproducibility. This method for producing a specifically-shaped crystal (specifically spherocrystal) of a compound comprises: (1) a step for preparing a supersaturated solution of a compound having a degree of supersaturation equal to or higher than a critical degree of supersaturation; and (2) a step for precipitating a specifically-shaped crystal (specifically spherocrystal) of a compound from the supersaturated solution.

SPECIFICALLY-SHAPED CRYSTAL OF COMPOUND AND METHOD FOR PRODUCING SAME

The present invention provides a method for obtaining a specifically-shaped crystal (specifically, spherocrystal) of a compound with good reproducibility. This method for producing a specifically-shaped crystal (specifically spherocrystal) of a compound comprises: (1) a step for preparing a supersaturated solution of a compound having a degree of supersaturation equal to or higher than a critical degree of supersaturation; and (2) a step for precipitating a specifically-shaped crystal (specifically spherocrystal) of a compound from the supersaturated solution.

SMALL MOLECULE PARG INHIBITORS AND METHODS OF USE THEREOF

The present disclosure provides methods of inhibiting PARG in cancer cells, including methods comprising administering a PARG inhibitor that modulates position Tyr795 in PARG. Also provided herein are methods of treating and/or preventing cancer comprising administering a PARG inhibitor. In some embodiments, the PARG inhibitors are of the formula: wherein the variables are defined herein.

##STR00001##

2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(6-(2-hydroxyphenyl)pyridazin-3-yl)acetamide as a Wnt pathway modulator

The application relates to a 2,6-dioxo-purine derivative, 2-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)-N-(6-(2-hydroxyphenyl)pyridazin-3-yl)acetamide, and the use of this compound in the modulation of the Wnt pathway, and treating a disease or condition associated with Wnt pathway activity, such as cancer, a fibrotic disease, a degenerative disease or a metabolic disease.