Abstract: This invention is in the area of pyrimidine-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.

Abstract: Disclosed are compounds having formulae I and II or pharmaceutically acceptable salts or hydrates thereof, a preparation method thereof and pharmaceutical compositions thereof. The compounds having formulae I and II possesses an isocitrate dehydrogenase 2 (IDH2) inhibitory activity and are capable of treating IDH2 mutation-induced cancers.

Abstract: Disclosed are compounds of formula (I), pharmaceutical compositions comprising such compounds and methods/uses of using the same, for example, for treating a JAK-related disorder, such as cancer, cancer cachexia or an immune disorder: wherein R1 is methyl or ethyl; R2 is selected from methyl, ethyl, methoxy and ethoxy; R3 is selected from hydrogen, chlorine, fluorine, bromine and methyl; R4 is selected from methyl, ethyl and —CH2OCH3; R5 and R6 are each individually methyl or hydrogen; and R7 is selected from methyl, ethyl, —(CH2)2OH and —(CH2)2OCH3, or a pharmaceutically acceptable salt thereof.

Abstract: A method of preparing a tuned metal complex including the use of band gap tuning to change the light absorbing or light emitting properties of a metal complex. In one aspect, band gap tuning includes changing the energy gap between the conduction band and the valence band of a metal complex with a guest molecule.

Abstract: This invention provides heterocyclic compounds that bind to E3 Ubiquitin Ligase (typically through cereblon) (“Degrons”), which can be used as is or linked to a Targeting Ligand for a selected Target Protein for therapeutic purposes and methods of use and compositions thereof as well as methods for their preparation.

Abstract: A method of preparing Compound (1) or a pharmaceutically acceptable salt thereof: comprises: (a) reacting Compound (X): or a pharmaceutically acceptable salt thereof with Compound (Y): in the presence of a palladium catalyst and a carbonate or phosphate base to form compound (Z): or a pharmaceutically acceptable salt thereof; and (b) deprotecting the Ts group of Compound (Z) to form Compound (1) or a pharmaceutically acceptable salt thereof.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in the treatment of autoimmune diseases and inflammatory conditions.

Abstract: The present invention relates to a synthesis process of suvorexant, novel compounds represented by formulas II, III, IV or V, or salts thereof for preparing suvorexant, and a method for preparing the intermediates. The preparation method uses a chiral starting material to synthesize chiral compounds represented by formulas II, III, IV or V, the compounds obtained being used for synthesizing the suvorexant. The preparation method has the advantages of simple operation, low cost, mild reaction conditions, simple post-treatment, easy to purify, high yield, high ee value for the product, and easy to industrialize. In the reaction route shown, R represents benzyl, allyl or 1-phenethyl, or optionally substituted benzyl at the 2 position to 6 position, such as 4-methoxybenzyl, 4-nitrobenzyl, 2-methylbenzyl, 4-chlorobenzyl or 3-fluorobenzyl.

Abstract: The present invention relates to a process for preparing C4-C15 lactams, in which a C1-C10-alkyl nitrite is reacted with a C4-C15-cycloalkane and is illuminated with a light-emitting diode during the reaction. This forms a C4-C15-cyclohexanone oxime which is then converted further to a C4-C15 lactam; the C1-C10 alcohol formed is recycled into the preparation of the C1-C10-alkyl nitrite.

Abstract: Deuterated diaminopyrimidine compounds, and intermediates thereof are described. In particular, disclosed are deuterated diaminopyrimidine compounds of formula (I), and pharmaceutical compositions containing such compounds or crystal forms, pharmaceutically acceptable salt, hydrates or solvates thereof. The disclosed deuterated diaminopyrimidine compounds can be used for treating and/or preventing protein kinase-associated diseases, such as cell proliferative disease, cancer, immune disease and the like.

Abstract: Disclosed are a series of hydroxyl purine compounds and the use thereof as PDE2 or TNF? inhibitors, in particular, the compounds as shown in formula (I), or tautomers or pharmaceutically acceptable salts thereof.

Abstract: The invention relates to compounds having the structure of formula (I) which can be used for the treatment of or against influenza infections.

Abstract: The present invention provides a process for the manufacture of a compound of formula VIIIa and salts forms of VIIIa where Rc is an aryl sulfonic acid

Abstract: Disclosed are salts of obeticholic acid, solid state forms thereof, processes for preparation thereof, and use thereof in the preparation of pharmaceutical compositions or the preparation of a different solid state form of obeticholic acid or salt thereof, and use in methods of treating liver diseases, e.g. primary biliary cirrhosis (PBC) and nonalcoholic steatohepatitis (NASH).

Abstract: The present invention relates to compounds of formulae I, or pharmaceutically acceptable salts or esters thereof, wherein: R1 is selected from H and CO—NR8R9, wherein R8 and R9 are each independently selected from H, alkyl, cycloalkyl and mono or bicyclic heterocycloalkyl, wherein said alkyl group is optionally substituted by one or more R12 groups, and said heterocycloalkyl is optionally substituted by R10 or R12; or R8 and R9 are linked, together with the nitrogen to which they are attached, to form a heterocycloalkyl group optionally containing one or more additional heteroatoms, and optionally substituted by one or more groups select from R10 and (CH2)mR12; R2 is selected from H and alkyl, wherein said alkyl group is optionally substituted by one or more R12 groups; R3 is selected from alkyl, cycloalkyl and heterocycloalkyl, each of which may be optionally substituted by halo, OH or alkoxy; Z1, Z2, Z3 and Z4 are all C; R4, R5, R6 and R7 are each independently selected from H, alkyl, CN, NO2, OH, alkoxy, N

Abstract: Provided is a compound of Formula (I) below, or a pharmaceutically acceptable salt, metabolite, or prodrug thereof: wherein: A1 is CR4 or N; A2 is CR5R6 or NR7; A3 is CR5?R6? or NR7?; each of R1, R2, R2?, R3, R3?, R4, R5, R5?, R6, R6?, R7, and R7?, independently, is hydrogen, deuterium, halogen, cyano, hydroxyl, carboxyl, amino, formyl, nitro, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 alkoxy, C2-6 alkenyloxy, C1-6 alkylcarbonyl, C1-6 alkyloxycarbonyl, C1-6 alkylamine, C3-20 carbocyclyl, or C3-20 heterocyclyl; or R5 and R6, R5? and R6?, or R5 and R5?, together with the adjacent atom to which they are each attached, form C3-10 carbocyclyl or C3-10 heterocyclyl. Further provided are a method of using the above-described compound, or the pharmaceutically acceptable salt, metabolite, or prodrug thereof for treating influenza and a pharmaceutical composition containing same.

Abstract: The present invention relates to the field of biomedicine, and discloses a class of selenium-containing inhibitors that bind to the allosteric site of glutaminase, and/or inhibit glutamate dehydrogenase, which has a long carbon chain or similar derivative structure linked with the N atom of benzoisoselenazole 3-ketone. The advantages of this invention are that compounds have novel binding activity with glutaminase and potent inhibitory activity of glutaminase. Moreover, some novel dual KGA/GDH inhibitors demonstrated good in vivo efficacy in inhibiting the tumor growth in mice by blocking glutaminolysis. At the meantime, compounds of this invention play an important part in the protection of survival, growth and differentiation of nerve cells under the condition of hypoxia-ischemia.

Abstract: A process for preparing compounds of formula (I), or a salt or solvate thereof, including Brexpiprazole, which process comprises cyclization of a compound of formula (II) or (III), or a salt or solvate thereof. The invention also refers to intermediates of said process.

Abstract: Compounds of the general formula: processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.

Abstract: The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.