C07D213/73

Heteroaryl compounds as kinase inhibitor

Provided herein are compounds of formula (I) having activity on a receptor protein tyrosine kinase, wherein R.sup.1, R.sup.2, R.sup.3, A, Q, Z, X and W are set forth in the description, as well as solvates, hydrates, tautomers or pharmaceutically acceptable salts thereof. ##STR00001##

ENZYME AND RECEPTOR MODULATION

Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.

ENZYME AND RECEPTOR MODULATION

Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid, leads to accumulation of the carboxylic acid hydrolysis product in the cell and enables improved or more prolonged enzyme or receptor modulation relative to the unconjugated modulator.

Pyridylpyridone compounds

The invention provides novel pyridylpyridone compounds of formula (I), pharmaceutical compositions containing such compounds, and methods for using such compounds in treatment of diseases including cancer, type II diabetes, inflammatory disease, autoimmune diseases, neurodegenerative disorders, cardiovascular disorders and viral infections; wherein R.sup.1, R.sup.2, R.sup.3 and X are as defined in the specification. ##STR00001##

Compounds and Methods of Use

This disclosure provides compounds and compositions and methods of using those compounds and compositions to treat diseases and disorders associated with excessive transforming growth factor-beta (TGFβ) activity. This disclosure also provides methods of using the compounds in combination with one or more cancer immunotherapies.

AMINOPYRIDINE COMPOUNDS AND METHODS FOR THE PREPARATION AND USE THEREOF

The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A/B (Rgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I and Formula III, as described herein, and pharmaceutically acceptable salts thereof.

AMINOPYRIDINE COMPOUNDS AND METHODS FOR THE PREPARATION AND USE THEREOF

The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its proteases arginine gingipain A/B (Rgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I and Formula III, as described herein, and pharmaceutically acceptable salts thereof.

NOVEL IONIZABLE LIPID AND LIPID NANOPARTICLE COMPOSITION USING SAME
20250230131 · 2025-07-17 · ·

The present invention relates to a novel ionizable lipid and a lipid nanoparticle composition using same, wherein it has been identified that the lipid nanoparticle composed of the novel ionizable lipid exhibits an excellent rate of gene encapsulation efficiency and of gene delivery efficacy in in vitro/in vivo system and, simultaneously, exhibits an excellent rate of gene delivery efficacy even in serum-free environments, and thus the present invention can be effectively used as a composition for drug delivery.