Patent classifications
C07F9/6518
Method to treat lipid dysregulation by modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9) protein activity with small molecule ligands
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.
Method to treat lipid dysregulation by modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9) protein activity with small molecule ligands
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.
REAGENTS BASED ON A TERTIARY AMINE BACKBONE TO INTRODUCE CHEMICAL FUNCTIONALITY IN NUCLEIC ACIDS AND SEQUENCE-CONTROLLED POLYMERS
It is provided an achiral, non-nucleosidic backbone for phosphoramidites that can be inserted with high yields in nucleic acid strands and sequence-controlled oligo(phosphodiester)s through solid phase synthesis (SPS) using a DNA synthesizer. From this backbone, platforms with useful chemical handles were synthesized, further functionalized, transformed into phosphoramidites and attached to nucleic acid strands and sequence-controlled oligo(phosphodiester)s. The backbone is based on a tertiary amine with a 3-6 carbon spacer between the central nitrogen and the two external hydroxyls. The spacer has been optimized to increase coupling yields and stability.
Human helicase DDX3 inhibitors as therapeutic agents
The present invention refers to compounds endowed with RNA helicase DDX3 inhibitory activity of formula I and II and their therapeutic use, in particular for the treatment of viral diseases.
Human helicase DDX3 inhibitors as therapeutic agents
The present invention refers to compounds endowed with RNA helicase DDX3 inhibitory activity of formula I and II and their therapeutic use, in particular for the treatment of viral diseases.
Application of click chemistry for signal amplification in IHC and ISH assays
Applicants have developed an amplification system and methodology for IHC and ISH staining that utilizes click chemistry to covalently bind reporter molecules to tissue.
Application of click chemistry for signal amplification in IHC and ISH assays
Applicants have developed an amplification system and methodology for IHC and ISH staining that utilizes click chemistry to covalently bind reporter molecules to tissue.
Benzotriazole derivative, preparation process and the use thereof
The present invention relates to a benzotriazole derivative, a preparation process thereof and the use thereof in preparation of the lubricating oil composition. The structure of the benzotriazole derivative of the present invention is shown by general formula (I). The benzotriazole derivative of the present invention, as the anti-wear additive for lubricating oil, not only has an excellent extreme pressure anti-wear property, but also has one or more excellent properties of thermal oxidation stability, corrosion resistance, rust resistance and anti-friction performance. ##STR00001## In the general formula (I), each of the group(s) and the number(s) are defined as in the description.
Benzotriazole derivative, preparation process and the use thereof
The present invention relates to a benzotriazole derivative, a preparation process thereof and the use thereof in preparation of the lubricating oil composition. The structure of the benzotriazole derivative of the present invention is shown by general formula (I). The benzotriazole derivative of the present invention, as the anti-wear additive for lubricating oil, not only has an excellent extreme pressure anti-wear property, but also has one or more excellent properties of thermal oxidation stability, corrosion resistance, rust resistance and anti-friction performance. ##STR00001## In the general formula (I), each of the group(s) and the number(s) are defined as in the description.
POLYCATENAR LIGANDS AND HYBRID NANOPARTICLES MADE THEREFROM
Described herein are polycatenar ligand compounds and their use in the production of hybrid nanoparticles, typically nanocrystals. The present disclosure also relates to films containing the hybrid nanoparticles described herein and their use.