7 results about "New chemical entity" patented technology

The invention belongs to the technical field of natural pharmaceutical chemistry and medicine, and relates to a sesquiterpene compound and a separation method thereof, and application of the sesquiterpene compound in blood sugar reduction. According to the 14-acetylated 1-indanone type sesquiterpene glucoside compound disclosed by the invention, a new 14-acetylated 1-indanone type sesquiterpene glucoside compound, namely 14-acetyl-(2S, 3S)-Pterosine C-3-O-D glucoside, is separated and identified from pteris multifida poir for the first time. According to the compound, a new chemical entity is added for a natural product library, and valuable candidate molecules are provided for drug research and development. The sesquiterpene compound disclosed by the invention shows excellent alpha-glucosidase inhibitory activity; an in-vitro enzyme activity experiment shows that the sesquiterpene compound has a remarkable inhibition effect on alpha-glucosidase from yeast (the inhibition rate reaches 52.1% under the concentration of 10 mg / mL).

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.

The invention relates to a chalcone derivative, a preparation method thereof and application of the chalcone derivative in preparation of an anti-angiogenesis medicine. The molecular structure of the chalcone derivative is shown as a formula I. The chalcone derivative disclosed by the invention can obviously inhibit angiogenesis in a vascular endothelial cell HMEC-1 and a zebra fish body at a relatively low concentration, and can be used as a new chemical entity for preparing a novel anti-angiogenesis medicine.

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 invention relates to the technical field of cosmetics, and discloses bakuchiol salicylate and application thereof. The structural formula of the bakuchiol salicylate is as shown in formula I in the specification. According to the bakuchiol salicylate disclosed by the invention, two active molecules are integrated into a brand new chemical entity through a covalent ester bond, so that an easily oxidized phenolic hydroxyl group of bakuchiol and a strongly acidic carboxyl group of salicylic acid are effectively masked, the chemical stability is improved, the bakuchiol salicylate is difficult to oxidize and degrade, the skin irritation is greatly reduced, the lipophilicity is improved, and the skin care effect is good. Compared with simple physical compounding of bakuchiol and salicylic acid in the prior art, by means of the innovative prodrug design, the synergistic breakthrough of stability, safety and efficacy is successfully achieved, and the obvious synergistic effect is shown in the aspects of stability, oxidation resistance, inflammation resistance, whitening, aging resistance and the like.

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.

The invention belongs to the technical field of medicinal chemistry, and discloses a targeted PARP11 small-molecule inhibitor and application thereof in preparation of antitumor drugs, and the novel PARP11 inhibitor with high efficiency, strong selectivity and high safety is obtained through systematic optimization of an ITK7 skeleton structure. The compound can effectively activate an IFN-gamma / STAT1 signal channel, inhibit AKT signal activation, improve a tumor immune microenvironment and significantly inhibit tumor growth and metastasis, and a new chemical entity and a treatment strategy are provided for development of novel immunoregulation type antitumor drugs.