Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds for inhibiting three prime repair exonuclease 1 (“TREX1”).

The present invention relates to certain compounds of formula (I) wherein—Ar is (Ar1) or (Ar2) and to their uses as antibacterial agents. The invention further relates to methods of treatment of bacterial infection with such compounds, optionally in combination with other antimicrobials and to compositions and pharmaceutical formulations containing such compounds. The invention additionally relates to coatings containing such compounds and to items having such coatings. ##STR00001##

The present application relates to a benzo five-membered nitrogen heterocyclic compound and an application thereof. The benzo five-membered nitrogen heterocyclic compound has the structure represented by formula I. The compound can be used as a compound of RORγ receptor inhibitor. The compound can effectively inhibit RORγ proteins and have good selectivity to other nuclear receptor family proteins. The benzo five-membered nitrogen heterocyclic compound or a pharmaceutical composition thereof provided by the present application can be used for preparing a drug for treating, preventing or ameliorating diseases such as inflammations, autoimmune diseases, cell proliferative disorder diseases, sepsis, cancer, neurodegeneration diseases or viral infections, has a good inhibitory effect on the treatment of tumors, especially the treatment of prostate cancer, and also has an amelioration effect on the treatment of other diseases.

The present application relates to a benzo five-membered nitrogen heterocyclic compound and an application thereof. The benzo five-membered nitrogen heterocyclic compound has the structure represented by formula I. The compound can be used as a compound of RORγ receptor inhibitor. The compound can effectively inhibit RORγ proteins and have good selectivity to other nuclear receptor family proteins. The benzo five-membered nitrogen heterocyclic compound or a pharmaceutical composition thereof provided by the present application can be used for preparing a drug for treating, preventing or ameliorating diseases such as inflammations, autoimmune diseases, cell proliferative disorder diseases, sepsis, cancer, neurodegeneration diseases or viral infections, has a good inhibitory effect on the treatment of tumors, especially the treatment of prostate cancer, and also has an amelioration effect on the treatment of other diseases.

The present disclosure describes, in part, compositions and methods for treating pathologic pains associated with malignant growth disorders by administering a therapeutically effective amount of K+/Cl-cotransporter (Kcc2/KCC2) gene expression enhancer to a subject in need.

A method of oxygenating a benzylic C—H bond is provided. The method comprises light induced activation of an initiator and subsequent reaction with oxygen, resulting in the formation of free radicals. Subsequently, free radicals catalyze the reaction of the benzylic C—H bond with oxygen, thereby forming an oxygenated compound.

Described herein are compounds of formula (I), and pharmaceutically acceptable salts, solvates, hydrates, isotopically labeled derivatives and radiolabeled derivative thereof, and pharmaceutical compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for detecting and imaging Tau aggregates in the brain for detection of Alzheimer's disease (AD) in a subject.

A composition for imaging a biological tissue or fluid comprising a compound of formula (A) and a biologically acceptable diluent or carrier, (A) wherein X represents one of a nitrogen atom, an oxygen atom, a sulphur atom, a phosphorus atom, or a selenium atom; R represents an aromatic group and/or an aliphatic group; p is an integer of 1 to 2; q and s are independently integers of 1, 2, 3, or 4; Y.sup.1, Y.sup.2, and Y.sup.3 independently represent a hydrogen atom, a deuterium atom, a fluorine atom, a chlorine atom, a bromine atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, a polyglycol group, an oxygen atom, a nitrogen atom, a cyano group, a nitro group; and/or wherein two or more of Y.sup.1, Y.sup.2, and Y.sup.3 may combine together to form a condensed ring.

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Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. ##STR00001##

Disclosed are compounds of Formula (I′), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. ##STR00001##