Abstract: The invention relates to modulators of Embryonic Ectoderm Development (EED) and/or Polycomb Repressive Complex 2 (PRC2) useful in the treatment of disorders and diseases associated with EEC and PRC2, being macrocyclic azolopyridine derivatives and compositions thereof of Formula I: or a pharmaceutically acceptable salt, prodrug, solvate, hydrate, enantiomer, isomer, or tautomer thereof, wherein X1, X2, X3, A1, A2, Y, R1, R2, R3, and R4 are as described herein.

Abstract: The present disclosure provides tricyclic compounds of formula (I) that are histone methyltransferases G9a and/or GLP inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of G9a and/or GLP such as cancers and hemoglobinopathies (e.g., beta-thalassemia and sickle cell disease). Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.

Abstract: Provided herein are novel bioavailable dual inhibitors capable of inhibiting both soluble epoxide hydrolase (sEH) and phosphodiesterase 4 (PDE4), and methods of using the same.

Abstract: The present invention aims to provide a compound that may be useful for the prophylaxis or treatment of constipation and the like. The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the specification, salt thereof.

Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the beta-3 adrenergic receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a beta-3 adrenergic receptor-mediated disorder, such as, heart failure; cardiac performance in heart failure; mortality, reinfarction, and/or hospitalization in connection with heart failure; acute heart failure; acute decompensated heart failure; congestive heart failure; severe congestive heart failure; organ damage associated with heart failure (e.g.

Abstract: The present invention provides crystalline forms of (E)-6-(4-Phenylcyclohexyl)-5-(3-trifluoromethylbenzyl)-1H-pyrimidine-2,4-dione, and methods of making and using the same.

Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.

Abstract: 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.

Abstract: Substituted analogs of dextromethorphan (DM) are disclosed, which are shown to have substantial binding affinity at both NMDA and sigma-1 receptors, and which are degraded by human liver enzymes more slowly than dextromethorphan. The analogs are useful as alternatives to dextromethorphan, and can provide the same benefits without requiring co-administration of a cytochrome P-450 enzyme inhibitor.

Abstract: Provided are: a composition for an organic light emitting diode comprising an indole-based photocurable monomer, a non-indole-based photocurable monomer, and an initiator, and an organic light emitting display manufactured therefrom.

Abstract: Provided herein are compounds comprising compounds of formula I and/or salts thereof; wherein at least one of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 is fluorine, and the remainder are independently chosen from hydrogen and fluorine; and R14, R15, R16, R17, R18, R19, R20, R21, R22, and R23 are independently chosen from hydrogen and deuterium; with the proviso that when R1, R2, and R3 are fluorine, then at least one of R4, R5, R6, R7, R8, R9, R10, R11, R12, and R13 is fluorine or at least one of R14, R15, R16, R17, R18, R19, R20, R21, R22, and R23 is deuterium. Also provided are medicaments comprising these compounds and methods for treating central nervous system disorders with the compounds and medicaments described herein.

Abstract: The present invention relates to an organometal-complex luminescent material which has a structural formula (I), wherein A, B and C refer to substituted or unsubstituted C, N, O and S atoms independently; a dashed ring for linkage between A and B atoms refers to a substituted or unsubstituted conjugated ring structure; L1, L2, L3 and L4 are single bonds or double bonds independently, wherein L3 and L4 are part of the conjugated ring structure for linkage between A and B atoms; X, X1, Y and Y1 are C, N, O and S atoms independently; Ar1 and Ar2 are substituted or unsubstituted conjugated ring structures independently; M refers to Pt, W and Au atoms. An organometal complex in the luminescent material is high in fluorescence quantum efficiency and heat stability and low in quenching constant and can be used for manufacturing high-efficiency and low-efficiency roll-off red-light OLEDs.

Abstract: This invention relates to a novel process for making alkyl 7-amino-5-methyl-[1,2,5]-oxadiazolo[3,4-b]pyridine-carboxylate.

Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.

Abstract: Described herein are heterocycle substituted pyridine derivative antifungal agents and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of fungal diseases and infections.

Abstract: The present disclosure provides tetrahydroquinoline derivatives of Formula (I) wherein X1 and X2 each, independently, are oxygen or sulphur; R1 is a lower alkoxy, or an optionally substituted aryl group; R2 is selected from a group consisting of hydrogen, lower alkyl, haloalkyl, or an amino group; R3 and R4 each, independently, are hydrogen, or lower alkyl groups; and R5 and R6 are optionally substituted aryl groups. The present disclosure also provides a method for making the compound of Formula (I).

Abstract: The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, U, W1, W2, W3, R1-R6, and R9 are described herein.

Abstract: Disclosed is a compound of Formula I, including N-oxides, and salts thereof, wherein R1, R2 and R3 are defined as set forth in the disclosure. Also disclosed is a process for preparing a compound of Formula I. A compound of Formula I can also be used as a synthetic intermediate to prepare pyridazinone-based herbicides.

Abstract: Provided herein are lipids that can be used in combination with other lipid components, such as neutral lipids, cholesterol and polymer conjugated lipids, to form lipid nanoparticles for delivery of therapeutic agents (e.g., nucleic acid molecules) for therapeutic or prophylactic purposes, including vaccination.

Abstract: The present invention relates to a method for preparing mesaconine and related intermediaries. Specifically, in the method for preparing mesaconine of the present invention, aconitine extracted from the Aconitum soongaricum Stapf. of aconitum plant is used as a raw material and subjected to alkalization, acetylation, N-de-ethylation, N-methylation, and hydrolysis to obtain mesaconine. The method for preparing mesaconine in the present invention is simple in operation, high in yield, environmentally friendly and pollution-free, and suitable for industrial production.