This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.

This invention pertains to the use of fused bicycle heterocyclic adducts of thiohydroxy pyridines or pyrimidines as diacylglycerol O-acyltransferase 1 (DGAT-1) inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.

The present application provides oxazoles-containing compounds, or a pharmaceutically acceptable salt thereof, that are 12/15-LOX inhibitors. Pharmaceutical compositions and methods of using these compounds for treating various conditions wherein 12/15-LOX is implicated (such as stroke) are also provided.

The present application provides oxazoles-containing compounds, or a pharmaceutically acceptable salt thereof, that are 12/15-LOX inhibitors. Pharmaceutical compositions and methods of using these compounds for treating various conditions wherein 12/15-LOX is implicated (such as stroke) are also provided.

The present invention relates electroluminescent devices, comprising a compound of the formula

##STR00001##

especially as host for phosphorescent compounds. The hosts may function with phosphorescent materials to provide improved efficiency, stability, manufacturability, or spectral characteristics of electroluminescent devices.

This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.

Disclosed are novel conjugates and methods for the preparation thereof. One of the methods for the preparation of a conjugate comprises a step of: acting a compound of formula (I), with a thiol-containing molecule of formula (II), wherein represents an amino acid, a peptide, a protein, an antibody, a nucleotide, an oligonucleotide, a saccharide, a polysaccharide, a polymer, a small molecule, an optionally substituted C.sub.1-C.sub.8-alkyl, an optionally substituted phenyl, or an optionally substituted aromatic 5- or 6-membered heterocyclic system; resulting in a compound of formula (III).

The present disclosure provides phosphonate-containing heterocycle compounds with TYK2 kinase inhibitory activity, pharmaceutical compositions comprising the same, and applications thereof. The present disclosure provides compounds of Formula (I), as inhibitors of TYK2 kinase. These compounds can be used for preventing and/or treating TYK2 kinase-related diseases and/or conditions.

##STR00001##

A heteroleptic binuclear copper(I) complex of the Cu.sub.2X.sub.2(E?N*)L.sub.2 form, having a structure of formula A: ##STR00001##
The copper(I) complex may be used in optoelectronic components, particularly for use in organic light emitting diodes (OLEDs).

In one aspect, the invention relates to compounds having the formula X: ##STR00001##
where R.sup.a, R.sup.b, R.sup.2, R.sup.7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.