11 results about "New chemical entity" patented technology

The invention discloses a novel amide compound with a substituted diphenyl ether structure as well as a preparation method and application of the novel amide compound. The compound comprises a structure as shown in a general formula (I) or a general formula (II), and is characterized in that a benzo five-membered aromatic heterocycle (including but not limited to benzofuran, benzothiophene, indole and the like) is connected with a substituted diphenyl ether group through an amido bond to form a unique molecular skeleton. Diversified substituent groups R1 such as halogen, alkyl and heterocyclic rings can be introduced into a benzene ring, substituent groups R2 such as alkyl and alkoxy (n is an integer from 0 to 2) are introduced into an intermediate connecting chain, and therefore diversity optimization of the molecular structure is achieved. A biological activity test shows that the compound has remarkable proliferation inhibition activity on SK-N-AS neuroblastoma cells, and shows potential treatment value on malignant tumors such as neuroblastoma. Through systematic molecular design, a substituted diphenyl ether structure compound with a novel structure is constructed, and a brand new chemical entity is provided for developing new anti-cancer drugs.

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 application provides a compound, a preparation method and application in preparation of a medicine for treating tumors, and relates to the technical field of chemical synthesis. The compound can stably induce cells to produce pyroptosis characteristic cell membrane large bubbles, simultaneously induce intracellular formation of a large vacuole-like structure similar to the characteristics of vacuole death and paraptosis, and has significant tumor cell proliferation inhibition activity, thereby providing a new chemical entity and research idea for research and development of a new type of anti-tumor medicine and research of new cell death mechanisms such as pyroptosis, vacuole death and paraptosis.

The invention discloses a phenylbutazone metformin salt as well as a preparation method, a composition and application of the phenylbutazone metformin salt. Specifically, the invention discloses a new chemical entity taking the phenylbutazone metformin salt as the active pharmaceutical ingredient. A process for the preparation of a phenylbutazone metformin salt; the invention relates to an application of a phenylbutazone metformin salt as an active pharmaceutical ingredient in preparation of a non-steroidal anti-inflammatory analgesic drug, and belongs to the technical field of medicines.

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.

The invention discloses ketoprofen metformin salt as well as a preparation method, a composition and application thereof. Specifically, the invention discloses a novel chemical entity taking ketoprofen metformin salt as a pharmaceutical active ingredient. A process for the preparation of ketoprofen metformin salts; the invention relates to application of ketoprofen metformin salt as an active pharmaceutical ingredient in preparation of non-steroidal antipyretic, analgesic and anti-inflammatory drugs, and belongs to the technical field of medicines.

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.