Abstract: The present invention provides bicyclic heterocyclyl kinase enzyme inhibitor compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors. wherein A, Y, Z, X1, X2, X3, R1, R3, ‘m’, ‘n’ and ‘p’ have the meanings given in the specification and pharmaceutically acceptable salt or stereoisomer thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical composition comprising at least one of the compounds of compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.

Abstract: Substituted benzoxazole and benzofuran chemical entities of Formula (I): wherein, V, W, X, Y, Z, and m have any of the values described herein and compositions comprising such chemical entities; processes for making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques; radioactive treatments; and the treatment of one or more disorders, including neurological, cognitive, immunological, and inflammatory disorders, as well as other conditions and diseases involving PDE7 or cyclic nucleotide signaling.

Abstract: A cyclic compound formed by a Friedel-Crafts reaction at positions 1 and 3 of carbazole and a preparation method thereof are disclosed. The compound is formed by connecting an achiral type I di-(tertiary alcohol) synthon constructed from fluorenyl and benzene or a derivative thereof, at position 9 of fluorenyl with positions 1 and 3 of carbazole, forming a closed ring structure with a clear and durable shape, having clear side lengths and vertices on the nanometer scale.

Abstract: Described herein are compounds that disrupt the interaction between Fbxo48 and phosphorylated-AMPK.

Abstract: The present disclosure provides certain tetrazole derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing the same.

Abstract: The present disclosure provides certain tetrazole derivatives that are inhibitors of transient receptor potential ankyrin 1 (TRPA1), and are therefore useful for the treatment of diseases treatable by inhibition of TRPA1. Also provided are pharmaceutical compositions containing the same, and processes for preparing the same.

Abstract: The present invention is directed to processes for making an anhydrous form of relugolix, designated herein as Form T of anhydrous relugolix. The processes of making Form T of anhydrous relugolix are from the following: (i) Form A of the DMF solvate of relugolix; (ii) Form B of anhydrous relugolix; or (iii) amorphous relugolix.

Abstract: The disclosure relates to compounds of Formula (I) as allosteric chromenone inhibitors of phosphoinositide 3-kinase (PI3K) useful in the treatment of diseases or disorders associated with PI3K modulation, Formula (I): or a prodrug, solvate, enantiomer, stereoisomer, tautomer, or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, W, X, Y, s, and Ring A are as described herein.

Abstract: Provided is a cyclopropylamine compound as lysine-specific demethylase 1 (LSD1) inhibitor, and a use thereof in preparation of drug for treating diseases associated with LSD1. The cyclopropylamine compound is a compound represented by formula (I), an isomer thereof, and a pharmaceutically acceptable salt thereof.

Abstract: Compounds of Formula I and methods of use as Janus kinase inhibitors are described herein.

Abstract: The present disclosure discloses a method for synthesizing a diaza-bridged compound and a diaza-bridged compound, belonging to the field of organic synthesis. The present disclosure includes the following reaction: in the formula, R is aryl, substituted aryl, alkyl or haloalkyl, Ra is any one of H, 2-nitrobenzenesulfonyl, 4-nitrobenzenesulfonyl or 2,4-dinitrobenzenesulfonyl, n=1 or 2. Since compound 2 and NH3 are used as raw materials, the present disclosure can not only effectively shorten the process flow and save process costs, but also improve the reaction yield to a certain extent. The present disclosure also provides a diaza-bridged compound, where the structural formula thereof is in the formula, Ra is any one of 2-nitrobenzenesulfonyl, 4-nitrobenzenesulfonyl or 2,4-dinitrobenzenesulfonyl.

Abstract: Provided is a process for synthesizing a functionalized cyclic dithiocarbamate.

Abstract: The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.

Abstract: Syntheses of compounds of Formula III from compounds of Formula I via compounds of Formula II are described, as well as particular compounds of Formula III, or pharmaceutically acceptable salts thereof, compositions comprising such compounds, and uses thereof. For example, certain of these compounds and compositions of Formula III have uses in the treatment of psychiatric or neurological disorders.

Abstract: Provided herein are compounds of Formula (I), or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, R9, X, Y, Z, W, and m are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof and a pharmaceutically acceptable excipient.

Abstract: Benzoxazine compounds, methods of making them, polymers made therefrom and methods of polymerizing the benzoxazines. These renewable benzoxazine monomers and polymers that utilize the variety of building blocks found in renewable plant biomass, demonstrate excellent processability and large temperature windows for processing of resin systems.

Abstract: This invention relates to the large-scale production of psilocybin for use in medicine. More particularly, it relates to a method of obtaining high purity crystalline psilocybin, particularly, in the form of Polymorph A. It further relates to a method for the manufacture of psilocybin and intermediates in the production thereof and formulations containing psilocybin.

Abstract: The present invention provides a novel process for preparing a diaminopyrimidine derivative or acid addition salt thereof having an activity as a 5-HT4 receptor agonist. And also, the present invention provides novel crystalline forms of a hydrochloride of the diaminopyrimidine derivative and processes for preparing the same.

Abstract: The invention relates to inhibitors of ROCK1 and/or ROCK2. Also provided are methods of inhibiting ROCK1 and/or ROCK2 that are useful for the treatment of disease.

Abstract: Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.