3 results about "New chemical entity" patented technology

This invention provides the application of chlorogenic acid in the preparation of drugs for treating intranuclear inclusion body disease (NIID), belonging to the field of pharmaceutical technology. This invention utilizes widely available sources with abundant safety data. Compared to novel chemical entities, chlorogenic acid, with its lower development risk, is used as a raw material. It has been found that chlorogenic acid can enhance the interaction between polyG protein and the E3 ubiquitin ligase TRIM21, forming a stable TRIM21-chlorogenic acid-polyG ternary complex. This promotes polyG ubiquitination and proteasome-dependent degradation, thereby reducing intracellular inclusion body burden and alleviating NIID from its pathological root cause. This provides a safe, effective, and highly specific new targeted therapeutic strategy for NIID.

This invention discloses a copper dicyclopentyl dithiocarbamate compound and its applications, relating to the field of pharmaceutical chemistry, with the molecular formula C0. 22 H 36 CuN2S4, with a central copper ion and two dicyclopentyl dithiocarbamate ligands coordinated via sulfur atoms to form a four-coordinate planar square structure, or its pharmaceutically acceptable salts, solvates, crystal forms, or hydrates. This invention utilizes a novel chemical entity of dicyclopentyl-substituted copper dithiocarbamate, leveraging the greater steric hindrance and lipophilicity advantages of its cyclopentyl structure, as well as its selective response to the high-copper microenvironment of cholangiocarcinoma. Furthermore, it exhibits strong targeting, achieving high enrichment in liver and cholangiocarcinoma tissues, broadening the therapeutic index. Simultaneously, by avoiding the inhibition of systemic ALDH2 activity, it eliminates the alcohol-like toxicity caused by acetaldehyde accumulation. Moreover, it does not cross the blood-brain barrier, exhibits no significant neurotoxicity or cardiotoxicity, is patient-friendly for those with renal insufficiency, and demonstrates high safety.

The application belongs to the technical field of pharmaceutical chemistry, and discloses a small-molecule inhibitor targeting PARP11 and application thereof in preparation of an antitumor drug. Through systematic optimization of the skeleton structure of ITK7, a new type of PARP11 inhibitor with high efficiency, high selectivity and high safety is obtained. The compound can effectively activate the IFN-gamma / STAT1 signal pathway, inhibit AKT signal activation, improve the tumor immune microenvironment, and significantly inhibit tumor growth and metastasis, thereby providing a new chemical entity and treatment strategy for development of a new type of immunomodulatory antitumor drug.