Abstract: Described herein are compounds of Formula (XIV) that are TYK2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of TYK2 activity.

Abstract: The present invention relates to novel fused imidazo pyrazole derivatives of formula (I), and formula (II), and methods for preparation thereof, in the presence of a chitosan-Al2O3 nanocomposite film. The invention also relates to pharmaceutical compositions comprising compounds of the invention as active ingredients as well as the use of compounds of the invention for antimicrobial action.

Abstract: The disclosure includes compounds of Formula (I) wherein Q1, Q2, Q3, W, X, Y, Z1, m, n, Warhead, R1, R2, R3, R4, and R5, are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compounds.

Abstract: Described herein are compounds of Formula (XIII) that are TYK2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of TYK2 activity.

Abstract: Compounds are of the structure of Formula (II) wherein: each X is —C(?O)—; R1 is a C1-C18 alkyl polyol; R2 is a saccharide group of formula (G)p; G is a monosaccharide residue, where (i) at least one of the —OH groups in (G)p is substituted by a halogen atom, and (ii) the saccharide group of formula (G)p is linked to —O— through a —CH2 group; p is 1 or 2; and m is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10. The compounds are effective in treating hepatotoxicity and fatty liver diseases.

Abstract: Provided herein are KRAS G12C inhibitors, such as composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

Abstract: The present invention provides compositions containing efinaconazole, butylated hydroxytoluene, a salt of ethylenediaminetetraacetic acid, and optional citric acid. The compositions exhibit stable color profiles and are useful in the treatment of fungal infections.

Abstract: Disclosed herein are heterocyclic compounds that inhibit the binding of menin and MLL or MLL fusion proteins. Also described are specific irreversible inhibitors of menin-MLL interaction. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the menin-MLL irreversible inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, leukemia and other diseases or conditions dependent on menin-MLL interaction.

Abstract: The present invention provides compounds of formula I, compositions thereof, and methods of using the same for the inhibition of HPK1, and the treatment of HPK1-mediated disorders.

Abstract: Disclosed are compounds including phosphate and N-oxide prodrugs of the NK1 antagonist netupitant, useful in the prevention and/or treatment of diseases including emesis induced by chemotherapy. Also disclosed are methods of making a di-tert-butyl (chloromethyl) phosphate useful in the manufacture of such prodrugs by reacting a dialkylphosphate salt with an acid to obtain the corresponding ester of phosphoric acid, reacting the ester with a quaternary ammonium hydroxide base to form a monobasic salt, and reacting the monobasic salt with chloroiodomethane to form the corresponding chloromethyl dialkyl phosphate.

Abstract: The present invention relates to heteroaryl heterocyclic compounds, e.g., the compound of the formula shown below, pharmaceutical compositions comprising same, methods for preparing same, and uses thereof.

Abstract: Provided herein are substituted tetrazolo[1,5-a]pyrazines and tetrazolo[1,5-c]pyrimidines useful for the treatment of diseases and disorders associated with the adenosine receptor, such as cancer. Also provided herein are pharmaceutical compositions, methods of inhibiting the activity of an adenosine receptor, and methods of treating disease and disorders using these compounds.

Abstract: The disclosure provides substituted pyrrolo[2,3-d]pyrimidine compounds of Chemical Formula 1 and compositions and uses thereof, wherein R1-R7, X, Y, Cy, m and n are defined in the disclosure. The compounds are useful for inhibiting ENPP1, activating the STING pathway, and treating cancer.

Abstract: Described herein are compounds, for example, 1,2,4-triazole-substituted N-heteroaryl amines, that are useful in treating a TYK2-mediated disorder. In some embodiments, the TYK2-mediated disorder is an autoimmune disorder, an inflammatory disorder, a proliferative disorder, an endocrine disorder, a neurological disorder, or a disorder associated with transplantation.

Abstract: The disclosure is directed to substituted dibenzo[b,f]azepines of the formula (II): wherein the variables n, X3, R1, R2, R4, and R5 are defined herein, and uses of such compounds to treat conditions including neurodegenerative diseases and cancers.

Abstract: Compounds are provided that are modulators of the CCR2 receptor. The compounds have the general formula (Ia1?): and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of CCR2 receptors.

Abstract: The present invention describes substituted benzo[f]imidazo[1,5-a][1,4]diazepines of the formula (I): wherein R1, R2, R2?, R3, and X are as disclosed herein. These compounds target alpha-4 and alpha-5 GABAa receptors and are useful for the treatment of airway hyperresponsiveness and inflammation in asthma.

Abstract: The invention relates to substituted amidrazones represented by Formula (IIA): or a salt thereof, and their use in novel methods for preparing 3-substituted 1,2,4-triazole compounds.

Abstract: Provided herein are novel heterocyclic compounds, for example, compounds of Formula (IV-C). Also provided herein are pharmaceutical compositions comprising the compounds and methods of using the same, for example, in inhibiting aldehyde dehydrogenases, retinoid pathway activation, and/or for treating various cancers, cancer metastasis, type 2 diabetes, pulmonary arterial hypertension (PAH) or neointimal hyperplasia (NIH) or as a male contraceptive.

Abstract: Disclosed are heterocyclic heteroaromatic macrocyclic ether compounds of Formula (I): pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof. The disclosure further relates to methods of treating or preventing cancer using the heterocyclic heteroaromatic macrocyclic ether compounds, pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof.