3876 results about "Medicinal chemistry" patented technology

This invention belongs to the field of pharmaceutical technology, specifically relating to a quinazoline-azaindole compound, its preparation method, and its application in treating Alzheimer's disease. The quinazoline-azaindole compound of this invention regulates NF-κB by inhibiting DYRK1A. k B. A series of signaling pathways, including PI3k-Akt, achieve anti-neuroinflammatory effects; quinazoline-azaindole compounds can reduce the expression of inflammatory factor-related genes in an LPS-induced BV2 microglial inflammation model, thereby reducing the levels of inflammatory factors in the hippocampus and cortex, alleviating neuronal pathological damage caused by neuroinflammation, and improving cognitive impairment caused by neuroinflammation; in summary, quinazoline compounds inhibit DYRK1A and downregulate NF-κB signaling pathways. k It can reduce the expression and release of inflammatory factors, improve brain tissue pathology, and alleviate cognitive impairment through signaling pathways such as B, and has significant clinical application value.

A compound of formula (I) or a pharmaceutically acceptable salt thereof is provided, which is useful as a pharmaceutical ingredient having S1P3 receptor antagonistic activity in the prevention and / or treatment an S1P3-mediated disease, wherein all symbols represent the same meaning as the symbols described in the specification. A drug is also provided, which containing, as an active ingredient, a compound having S1P3 receptor antagonistic activity in the prevention and / or treatment an S1P3-mediated disease.

Disclosed in the present invention are a crystalline form of a compound, a preparation method therefor, an active pharmaceutical ingredient or composition comprising same, and a use thereof in the preparation of an extracellular histone inhibitor. The crystalline form of the compound of the present application has high crystallinity, good solid properties and high stability, crystallization conditions are mild, the operation is simple, the process is stable, the cost is low, and the crystalline form of the compound is adapted to be stored as an active pharmaceutical ingredient and produce a formulation product.

The present disclosure relates to a pharmaceutically acceptable salt (formula 1) and a crystal form of a 1,4-dihydro-1,6-naphthyridine amide compound, and a preparation method therefor. Specifically, provided in the present disclosure are a pharmaceutically acceptable salt and crystal form of (S)-4-(3-acetyl-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-4-yl)-3-(methoxy-d3)benzonitrile, and a preparation method therefor. The corresponding crystal form has good stability and can be better used for clinical treatment.

The application relates to the technical field of fine chemicals, and discloses a method for preparing secondary alcohol by catalyzing alpha-olefin hydration. The method comprises the following steps: under the catalysis of a catalyst, performing an aldehyde amine condensation reaction on 1,3,5-tri-(p-formylphenyl) benzene and o-sulfonic acid p-phenylenediamine in a first organic solvent in an air-isolated condition, then sequentially performing washing and drying on the obtained reaction product to obtain a COF-HSO3 catalyst, and then under the catalysis of the COF-HSO3 catalyst, performing a hydration reaction on alpha-olefin in a second organic solvent and water. The method for preparing secondary alcohol by catalyzing alpha-olefin hydration has high alpha-olefin conversion rate and secondary alcohol yield.

Provided herein are isotopologues of MC4R agonist, processes for the preparation of the compounds, pharmaceutical compositions comprising the compounds, and methods of treating, managing, or preventing certain conditions, diseases, or disorders using the compounds or pharmaceutical compositions described herein.

The application relates to a preparation method of a BTK inhibitor intermediate. In particular, the application relates to a preparation method of a compound as shown in formula (A'K), which comprises the following steps: a step of preparing a compound as shown in formula (IIK) from a compound as shown in formula (IIIK), and a step of preparing a compound as shown in formula (A'K) from a compound as shown in formula (IIK). The method has high yield and mild reaction conditions, and is suitable for industrial production.

This invention relates to the field of cyclohexanone ammoniation to produce cyclohexanone oxime, and discloses a method and system for cyclohexanone ammoniation to produce cyclohexanone oxime. The method includes: mixing cyclohexanone, ammonia, and a circulating catalyst slurry, and then reacting the mixture with hydrogen peroxide to obtain a reaction slurry containing cyclohexanone oxime, ammonia, water, and a catalyst; wherein the feed cyclohexanone accounts for 2-6% of the total mass of cyclohexanone and the circulating catalyst slurry; mixing a portion of the reaction slurry with an organic solvent and then separating the two phases to obtain an organic phase containing cyclohexanone oxime and the organic solvent, and an aqueous phase containing the catalyst; wherein the mass ratio of the organic solvent to the cyclohexanone oxime in this portion of the reaction slurry is 0.5-5:1; reheating the remaining portion of the reaction slurry and recycling it to the reaction; and membrane filtering the aqueous phase containing the catalyst to obtain a clear liquid and a catalyst-rich stream. This method improves the selectivity of cyclohexanone oxime while effectively extending the service life of the catalyst.

This invention relates to a compound containing trifluoromethyloxadiazole and a spirocyclic structure, or a pesticide-acceptable salt, hydrate, or solvate thereof, characterized in that the structure of the compound containing trifluoromethyloxadiazole and a spirocyclic structure is shown in general formula I. Compared with the prior art, the compound provided by this invention can be used to prepare histone deacetylase inhibitors, effectively inhibiting the growth and reproduction of various rust fungal spores, with effects comparable to fluopyram.

The invention relates to a liquid detergent containing, based on the total weight thereof, a) 22 to 50 wt.% anionic surfactant; b) 0.1 to 8 wt.% gluconic acid salt; c) 0 to 2 wt.% antioxidant; d) 5 to 25 wt.% organic solvent; e) 0.1 to 15 wt.% water; f) less than 0.1 wt.% organic phosphonate, and g) 0.01 to 5 wt.% perfume composition.

The present application relates to the field of medicinal chemistry and pharmacotherapy, and in particular to a class of bazedoxifene and its preparation method and application. The bazedoxifene derivative is used for gp130 small molecule inhibitor, the compound is a compound shown in formula (I), or a pharmaceutically acceptable salt or ester thereof, and relates to the application of tumor-related activity and the like, in particular the application in preparing drugs for preventing and / or treating diseases related to tumors, especially colorectal cancer.

The present invention is directed to a method for acidulation of tall oil soap in an alcohol selected from methanol, ethanol and / or iso-propanol. In the method according to the present invention, a mixture comprising sodium salts of fatty acids and rosin acids and an alcohol selected from methanol, ethanol and / or iso-propanol is acidulated using carbon dioxide.

This invention discloses a synthetic process for 3-chloro-5,5-disubstituted-4,5-dihydroisoxazole. The process comprises the following steps: S1: Under acid catalysis, compound III undergoes a cyclization reaction with hydroxylamine and / or hydroxylamine salt to obtain compound V; S2: In a solvent, compound V undergoes a chlorination reaction with a chlorinating agent to obtain compound VI. This invention provides an economical, environmentally friendly synthetic process that improves the selectivity of 3-chloro-5,5-dimethyl-4,5-dihydroisoxazole, and has significant industrial application value.

This application belongs to the field of biomedicine, specifically relating to a method for preparing an antitumor composition for pets, aiming to solve the technical problems of low bioavailability, poor stability, and poor drug administration compliance of poorly soluble active ingredients in antitumor drugs for pets. The method includes: a raw material pretreatment step, in which curcumin, resveratrol, quercetin, green tea polyphenols, and astragalus polysaccharides are pulverized and sieved separately; an organic phase preparation step, in which egg yolk lecithin and solid lipids are dissolved in an ethanol-acetone mixed solvent, and curcumin and resveratrol are added and dissolved by stirring in a water bath; an aqueous phase preparation step, in which poloxamer F68 is dissolved in purified water and dissolved in a water bath; a high-pressure homogenization step, in which a nanoemulsion containing a solid lipid core is prepared; a moderately polar component encapsulation step, in which quercetin and green tea polyphenols are ultrasonically dispersed and then added dropwise to the nanoemulsion; a freeze-drying step, in which a nano-lyophilized powder is obtained; and an outer hydrophilic component coating step, in which astragalus polysaccharides are sprayed or adsorbed onto the surface of the freeze-dried powder. The composition obtained by this method is a core-shell multilayer nanoparticle with a core consisting of curcumin and resveratrol encapsulated by solid lipids, a middle shell adsorbing quercetin and green tea polyphenols, and an outer shell coated with astragalus polysaccharides. This application utilizes the above-mentioned layered encapsulation technology to achieve stable co-encapsulation of multiple antitumor active ingredients, improve the bioavailability of poorly soluble components, optimize drug stability, and enhance antitumor effects through multi-target synergistic effects. Simultaneously, it endows the composition with immunomodulatory functions and sustained-release properties. The composition can be formulated into a nano-lyophilized powder form, making it easy to add to pet food or formulate into a paste for administration, improving pet drug compliance. Figure 2 is a schematic diagram of the three-layer core-shell nanoparticle structure of the composition of this invention.

This invention belongs to the field of organic synthetic chemistry technology, specifically relating to a selenium-based indoloquinazoline derivative, its preparation method, and its application, comprising: in an organic solvent, using aromatic amine compounds, malononitrile, and diselenoether as raw materials, in the presence of a palladium catalyst and an organic base, at 90°C... o The reaction was carried out under C conditions with stirring to obtain a selenyl indoline quinazoline derivative. This method features mild reaction conditions, simple operation, high yield, and good functional group compatibility, conforming to the principles of green chemistry. Furthermore, the selenyl indoline quinazoline derivative provided by this invention exhibits good inhibitory activity against Plasmodium, providing a drug lead compound for the development of novel antimalarial drugs and holding significant importance for the prevention and / or treatment of malaria.

The present invention encompasses compounds of formula (I), the compounds of formula (I) for use as inhibitors of KRAS mutated in position 12, preferrably G12D, pharmaceutical compositions and preparations containing such compounds and the compounds of formula (I) for use as medicaments / medical uses, especially as agents for treatment and / or prevention of oncological diseases.

This invention relates to the use of a natural terpene compound in pharmaceuticals, said natural terpene compound having the structure shown in formula (I), and having the function of preparing a compound for the prevention or treatment of hypoxia-inducible factor-1. α Use in medicines for diseases associated with abnormally elevated activity. This invention has discovered that the compound possesses hypoxia-inducible factor-1. α It exhibits inhibitory activity, effectively suppressing macrophage inflammatory responses and hepatocyte damage. It also demonstrates significant protective function against lipopolysaccharide / galactosamine-induced acute liver injury in mice, and can be used as a lead compound for the preparation of new drugs or drugs for the prevention and treatment of acute liver injury.

The application belongs to the technical field of biological medicine, and relates to a bipyridine compound, a preparation method thereof and application of the bipyridine compound in preparation of an AChE inhibitor. A chemical structural formula of the bipyridine compound is provided. The bipyridine compound provided by the application has AChE inhibitory activity, and the AChE inhibitory activity of the bipyridine compound is significantly higher than that of an existing clinical drug (such as galantamine), thereby providing a drug with better effect for treatment of Alzheimer's disease.

In particular, this disclosure provides technologies, including I-66 formulations, compositions, and methods, for treating various cancers. This disclosure provides technologies, such as formulations, dosages, and drug regimens, for treating conditions, disorders, or diseases, in particular certain types of cancer. In some embodiments, this disclosure provides high-purity I-66 active pharmaceutical ingredients. In some embodiments, this disclosure provides I-66 pharmaceutical products. In some embodiments, this disclosure provides I-66 formulations, which are liquid compositions in which I-66 has sufficiently high solubility and stability for clinical application.

The present invention encompasses compounds of formula (I) wherein POI is a moiety of formula (IV) as degraders of KRAS for use in the treatment and / or prevention of oncological diseases.

The application provides a composition containing Omega 3, which comprises a conjugate formed by connecting Omega 3 and a PEDF-derived peptide. The PEDF-derived peptide is obtained by truncation on the basis of a full-length PEDF protein, and the amino acid sequence is shown as SEQ ID No. 1. The Omega 3 is EPA, and the conjugate is obtained by connecting the Omega 3 and the PEDF-derived peptide through a click chemistry method. The composition can promote eye health repair, especially the treatment and improvement of dry eye, and has a clinical application prospect.

A lipidoid compound having the structure of Formula I or a pharmaceutically acceptable salt thereof is disclosed: [Chemical Formula I] (In the above formula, gi is as defined in the present application). Additionally, a nanoparticle composition comprising a lipidoid of the present invention capable of delivering a therapeutic agent is disclosed. The present application also discloses a pharmaceutical composition comprising a lipidoid composition of the present invention.

The present invention relates to a benzene-containing polycyclic derivative modulator, a preparation method therefor and the use thereof. In particular, the present invention relates to a compound as shown in general formula (I-1), a preparation method therefor, a pharmaceutical composition containing the compound, and the use thereof as a modulator in the preparation of a drug for treating diabetes, obesity, NASH, renal diseases and diseases associated therewith, wherein each substituent in general formula (I-1) is the same as that defined in the specification.

A method for measuring the content of hydrazine in a carbidopa-containing drug, comprising the following steps: (1) in a solvent, under the action of acid, mixing a sample under test with an aldehydes substance, said sample being a carbidopa-containing drug, and hydrazine in said sample and the aldehydes substance being derivatized to obtain a test solution; and (2) measuring the content of the hydrazine in the test solution. Compared with the prior art, the method for measuring the content of hydrazine in a carbidopa-containing drug does not require pretreatment to remove carbidopa, introduces negligible hydrazine during measurement, is easy to operate, does not need to accurately control derivatization time and sample introduction time, and exhibits good repeatability and accurate measurements.

1. Name of the designed product: pendant (Qiji-Yuanbao pony). 2. Use of the designed product: ornaments for wearing. 3. Design points of the designed product: combination of shape and pattern. 4. Picture or photo best indicating the design points: perspective view.

The present disclosure provides compounds, and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis. The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL- 2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.

This invention belongs to the field of analytical detection technology, and specifically relates to a Schiff base compound, its preparation method, and its application. The Schiff base compound of this invention is a Schiff base fluorescent probe with a 2-furanoylhydrazine core, capable of dual-response quenching-type recognition of Cu. 2+ and Fe 3+ It exhibits a clear color change under fluorescent light and shows fluorescence quenching under 365 nm ultraviolet light, providing a simple and reliable new method for rapid visual detection of dual ions.