18 results about "New chemical entity" patented technology

The invention discloses an indole styryl oxadiazole bridging compound with toxoplasma gondii resisting activity, which is formed by bridging three pharmacophores of 3-indoleacetonitrile, oxadiazole and cinnamic acid. The invention relates to the technical field of antiparasite, and has the beneficial effects that the compound provides a new chemical entity for development of toxoplasma gondii resistant drugs, opens up a new direction for design of the antiparasite drugs, has a wide application prospect, and is suitable for industrial production. Particularly, the gene has an important transformation value in the aspects of immunodeficiency patient treatment and toxoplasma gondii prevention and control in the livestock breeding industry.

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.

A solid film and an article having a surface are provided, the surface having discrete regions patterned with deposited low molecular weight organic compounds (such as pharmaceutically active substances and new chemical entities). The organic compounds can be present in one or more discrete regions at ≥ about 99 mass % and can be crystalline or amorphous. The deposited organic compounds can be deposited as a film having a high surface area. As a non-limiting example, the deposited organic compounds exhibit improved solubility and bioavailability. Also provided is a method for depositing such low molecular weight organic compounds by organic vapor jet printing in an inert gas stream.

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.

The present invention discloses an indole styryl oxadiazole bridged compound having anti-Toxoplasma activity, comprising a compound formed by bridging three pharmacophores: 3-indoleacetonitrile, oxadiazole, and cinnamic acid. The present invention relates to the field of antiparasitic technology and has the beneficial effects of providing a new chemical entity for the development of anti-Toxoplasma drugs and opening up new directions for the design of antiparasitic drugs. The compound has broad application prospects, particularly in the treatment of immunocompromised patients and the prevention and control of Toxoplasma gondii in the livestock and aquaculture industry.

In an aspect, the disclosure provides methods for making LC-PUFA and VLCFAs in a host organism. The LC-PUFA and VLCFAs can be new chemical entities, well-known LC-PUFA, and derivatives of LC-PUFA as well as VLCFAs. The host cells can be microalgae, fungi or other host cells. In a related aspect, the disclosure provides host cells engineered to have biochemical pathways for making LC-PUFA and VLCFAs.

Provided a technology platform for the delivery of nucleic acids, centered around a new chemical entity known as Fatty Acid Derivatives (FADS). FADS can covalently or non-covalently bind to nucleic acid substances, thereby enhancing their stability and effectiveness.

The invention discloses a cinnamyl polypeptide compound and a preparation method and application thereof, the structural formula of the cinnamyl polypeptide compound is as shown in formula (I): # imgabs0 #. According to the invention, two novel cinnamyl polypeptide compounds coprisamide E and F are separated from a liquid fermentation product of actinomycetes Streptomyces thermomolinestatus strain NAK03196 for the first time, the compounds have novel cinnamyl polypeptide skeletons, and the cinnamyl polypeptide skeletons can be used for preparing the cinnamyl polypeptide compound. A brand new chemical entity is provided for drug research and development.

Embodiments of this disclosure describe the synthesis of 4-amino-3 bromocarbohydroxymoyl-1,2,5-oxadiazole from a precursor solution in methanol. The synthesis uses 4-amino-3-aminocarbohydroxymoyl-1,2,5-oxadiazole as the starting material. The procedure involves the sequential treatment of the starting material in methanol with hydrobromic acid, cuprous bromide, and sodium nitrite. This treatment results in the precipitation of a new chemical entity, the bromo-oxime 4-amino-3-bromocarbohydroxymoyl-1,2,5-oxadiazole. Upon obtaining the bromo-oxime derivative, the method further facilitates the production of 3,4-bis(4-amino-1,2,5-oxadiazol-3-yl)-1,2,5-oxadiazole-N-oxide (furoxan derivative) through dimerization in a biphasic reaction medium consisting of ethyl acetate and water, with potassium carbonate serving as a key reactant. This innovative method offers a streamlined approach, enabling the direct use of the intermediate oxadiazole derivative without the need for additional purification, leading to the desired furoxan derivative. This synthesis method stands out for its efficiency, high-purity yield, and fewer steps, offering potential applications in various chemical industries.

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.