Abstract: A pharmaceutical formulation of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide (compound 1), in particular methanesulfonic acid salt thereof, and methods of using the pharmaceutical formulation for the treatment or prevention of diseases or medical conditions mediated through mutated forms of epidermal growth factor receptor (EGFR), such as various cancers, are disclosed.

Abstract: The invention relates to HPK1 inhibitors useful in the treatment of cancers, and other serine-threonine kinase mediated diseases, having the Formula: where A, R1, R2, R3, R4, R5, R6, R16, R17, X1, X2, X3, X4, m, and n are described herein.

Abstract: Compounds and compositions that can modulate mitochondrial function in neuronal cells are provided herein, as are methods for using the compounds and compositions to treat or prevent conditions such as Alzheimer's disease. For example, compounds of Formula I, compositions containing the compounds, and methods for using the compounds and compositions are provided herein: wherein X is absent, CH2, or C(O); R1 is H, OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino; R2 is H or C1-6 alkyl; R3 is H, C1-6 alkyl, —C(O)(C1-3 alkyl), or —C(O)O(C1-3 alkyl); R4 is C3-10 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, or 5-10 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 independently selected R5 groups; and R5 is OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, or di(C1-3 alkyl)amino.

Abstract: Bifunctional compounds that increase uric acid excretion and reduce uric acid production, and monofunctional compounds that either increase uric acid excretion or reduce uric acid production. Methods of using these compounds for reducing uric acid levels in blood or serum, for treating disorders of uric acid metabolism, and for maintaining normal uric acid levels in blood or serum are also provided. Pharmaceutical compositions comprising the bifunctional and monofunctional compounds are also provided.

Abstract: The present invention provides compounds of Formula I?: wherein , W, X, Y, Z, Z1, Z2, R1, R2, R3, R4 and R5 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the STING protein and thus can be used as medicaments for treating or preventing disorders affected by the agonism of STING.

Abstract: New N-(2,6-diethylphenyl)-8-({4-[4-(dimethyl amino)piperidin-1-yl]-2-methoxyphenyl}amino)-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide phosphate of formula (II): Medicaments.

Abstract: The present application provides bifunctional compounds of Formula (I): which act as protein degradation inducing moieties for EGFR and/or a mutant thereof. The present application also describes methods for the targeted degradation of EGFR and/or a mutant thereof through the use of the bifunctional compounds that link a ubiquitin ligase-binding moiety to a ligand that is capable of binding to EGFR and/or a mutant thereof which can be utilized in the treatment of disorders modulated by EGFR or a mutant thereof.

Abstract: Provided are a p-type organic semiconductor represented by Chemical Formula (1), which has improved thermal resistance and may detect near-infrared light, and a photoelectric conversion film, a photoelectric conversion device, and an image sensor including the same: In Chemical Formula (1), R1 and R2 are independently a substituted or unsubstituted C1 to C30 alkyl group, and R3 to R26 are independently a hydrogen atom, a deuterium atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted aryloxy group, a substituted or unsubstituted arylthio group, an oxy group substituted with a substituted or unsubstituted heterocyclic group, a thio group substituted with a substituted or unsubstituted heterocyclic group, or a substituted or unsubstituted amino group.

Abstract: The invention provides photodynamic therapeutic compounds and photodynamic methods of treatment. The photodynamic therapeutic compounds may be activated by long wavelength light. The photo-activation by long wavelength light may allow improved tissue penetration. The compounds are selected from the group consisting of compounds of formula (i), or a pharmaceutically acceptable salt thereof: formula (i) wherein PDC is a photodynamic core and wherein R1; R2; R3; and R4 are H, phenyl, pyridine-4-yl, methylpyridinium, N-methylpyridinium-3-yl; 2-phenyl-N-methylpyridinium-4-yl, 3-phenyl-N-methylpyridinium-4-yl, 4-phenyl-N-methylpyridinium-4-yl, 2-phenyl-N-methylpyridinium-3-yl, 3-phenyl-N-methylpyridinium-3-yl or 4-phenyl-N-methylpyridinium-3-yl; and wherein any one or more of R1, R2, R3 and R4 may be optionally substituted.

Abstract: The present invention discloses a compound shown in formula I or a stereoisomer, pharmaceutically acceptable salt, crystal form, solvate or isotopologue thereof. The compound of the present invention shows excellent inhibition activity against histone deacetylases, has remarkable inhibition effects on cancer cells, and provides a new choice of drugs used for the clinic treatment and diseases related to the abnormal activity of histone deacetylases.

Abstract: The invention provides novel chemical compounds useful for treating cancer, or a related disease or disorder thereof, and pharmaceutical composition and methods of preparation and use thereof.

Abstract: There are provided compounds of formula (I) as defined in the specification which are p38 MAP kinase inhibitors for use as medicaments for the treatment inter alia of inflammatory diseases.

Abstract: Disclosed are an amino alcohol-boron-binol complex as an intermediate, including Complex 3-1-1 shown below, and a method for preparing an optically active amino alcohol by using the same, wherein a racemic amino alcohol is resolved in an enationselective manner using a boron compound and a (R)- or (S)-binol, whereby an amino alcohol derivative with high optical purity can be prepared at high yield.

Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: The present invention discloses deuterated thienopiperidine derivatives, a manufacturing method and an application thereof. The deuterated thienopiperidine derivatives in the present invention are of a structure of the following formula (I). The present invention also comprises the application of the deuterated thienopiperidine derivatives as a drug for treating and preventing cardiovascular and cerebrovascular diseases.

Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula I for treating metabolic conditions, such as type 2 diabetes mellitus, heart failure, diabetic kidney disease, and non-alcoholic steatohepatitis.

Abstract: Provided herein are dUTPase inhibitors of Formula (I), compositions comprising such compounds and methods of using such compounds and compositions

Abstract: The present invention provides compounds of Formula A: or a pharmaceutically acceptable salt, tautomer, or stereoisomer, thereof, wherein the variables are as defined herein. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating, preventing, inhibiting, ameliorating, or eradicating the pathology and/or symptomology of a disease caused by a parasite, such as leishmaniasis, human African trypanosomiasis and Chagas disease.

Abstract: The disclosure provides compounds with warheads and their use in treating medical diseases or disorders, such as viral infections. Pharmaceutical compositions and methods of making various compounds with warheads are provided. The compounds are contemplated to inhibit proteases, such as the 3C, CL- or 3CL-like protease.

Abstract: The present invention provides a compound of Formula (I) wherein X is selected from the group consisting of (CH2)2— and CH2—CH(CH3)—; Q is selected from the group consisting of C(CH3)2 and Formula (a); or a pharmaceutically acceptable salt thereof; compositions, methods to treat liver disease and NASH.