419 results about "Quinazoline" patented technology

Disclosed in the present invention are a quinazoline compound, and a pharmaceutical composition thereof and the use thereof. Provided in the present invention is a compound as represented by formula I, a stereoisomer thereof or a pharmaceutically acceptable salt thereof. The compounds of the present invention have a good degradation effect on the KRAS protein with a G12D mutation, have a good inhibitory activity against the proliferation of tumor cells with a KRAS G12D mutation, and exhibit good pharmacokinetic properties.

The invention relates to a quinazoline compound as well as a preparation method and application thereof. Specifically, the invention relates to a compound as shown in a formula (I) or pharmaceutically acceptable salt, stereoisomer, tautomer, polymorphic substance, solvate, N-oxide, isotope labeled compound, metabolite or prodrug thereof, and a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt, the stereoisomer, the tautomer, the polymorphic substance, the solvate, the N-oxide, the isotope labeled compound, the metabolite or the prodrug thereof. The invention also relates to a preparation method of the compound and application of the compound in preparation of drugs for preventing or treating KRAS G12D-mediated related diseases. # imgabs0 #

The invention discloses a preparation method of an optical OCA (Optical Clear Adhesive) and application of the optical OCA in a mobile phone folding screen, and relates to the technical field of optical cement, the optical OCA is prepared from the following raw materials in parts by weight: 50 parts of acrylate prepolymers, 2-4 parts of 3-allyl-2-mercapto-3H-quinazoline-4-ketone, 1-3 parts of diallyl disulfide, 1-3 parts of 3-[N, N-dimethyl formamide], 1-3 parts of 2, 3, 5-trimethyl-1, 3-pentanediol monoisobutyronitrile, 1-3 parts of 2, 3, 5-trimethyl-1, 3, 5-trimethyl-1, 3, 5-trimethyl-1, 3 The preparation method comprises the following steps: adding 3-5 parts of N, N-dimethyl-[2-(2-methylpropane-2-enoyloxy) ethyl] ammonium] propane-1-sulfonic acid inner salt, 1-3 parts of allyl succinimido carbonate, 2-4 parts of dicyclopentene methacrylate, 1-3 parts of 1, 3, 5-triacryloyl hexahydro-1, 3, 5-trimethyl-1, 3, 5-trimethyl-1, 3, 5-trimethyl-1, 3, 5-trimethyl-1, 3, 5-trimethyl-1, 3, 5-trimethyl-1, 3, 5-trimethyl-1, 3, 5- The invention relates to a graphene quantum dot photoinitiator which is prepared from the following components in parts by weight: 1-3 parts of 1, 3, 5-triazine, 0.8-1.2 parts of a photoinitiator, 1-3 parts of an aziridine cross-linking agent, 1-3 parts of graphene quantum dots, 0.8-1.2 parts of a coupling agent and 40-50 parts of a diluent. The optical OCA adhesive is high in light transmittance and bonding strength, good in weather resistance and excellent in folding resistance.

The present invention relates to compounds of the Formula I, and pharmaceutically salts thereof: I wherein RS, R1, R2, R3, R4 and X are each as defined herein. The compounds of the present invention inhibit WRN. The novel therapeutic compounds are therefore useful for the treatment and / or prevention of diseases and conditions in which WRN activity is implicated, such as, for example but not limited to, the treatment and / or prevention of cancer. The present invention also relates to pharmaceutical compositions comprising the novel therapeutic compounds defined herein, to processes for synthesising these compounds and to their use for the treatment of diseases and / or conditions in which WRN activity is implicated.

The invention discloses a quinazolinone compound as well as a preparation method, a pharmaceutical composition and application thereof, and relates to the technical field of pharmaceutical chemistry. In particular to a quinazolinone compound as shown in a formula I or pharmaceutically acceptable salt, prodrug, stereoisomer, diastereoisomer, enantiomer, tautomer, solvate, salt of solvate, polymorphic substance and isotope labeled compound of the quinazolinone compound. The quinazolinone compound designed and synthesized by the invention can effectively inhibit TAK1 protein activity, achieves an excellent curative effect at a molecular level, and can be applied to preparation of medicines for treating and / or preventing inflammation, chronic fibrosis diseases, hyperproliferative diseases and cardiovascular diseases.

The present disclosure relates to compounds of Formula (I′):and pharmaceutically acceptable salts and stereoisomers thereof. The present disclosure also relates to methods of preparation these compounds, compositions comprising these compounds, and methods of using them in the prevention or treatment of abnormal cell growth in mammals, especially humans.

The present disclosure relates to a dihydrofuro[3,4-f]quinazoline compound, a preparation method therefor and a use thereof in medicine. Specifically, the present disclosure relates to a dihydrofuro[3,4-f]quinazoline compound represented by formula (1), a preparation method therefor, a pharmaceutical composition containing the compound, and a use of the compound as a therapeutic agent, particularly a use of the compound in preparation of a drug for inhibiting KRAS amplification and / or mutant activity.

The invention relates to the technical field of plant disease control, in particular to application of a quinazoline carboxylic acid compound in plant virus resistance. The invention discovers that 1, 5-dioxo-2, 3, 4, 5-tetrahydropyrrolo [1, 2-a] quinazoline-3a (1H)-carboxylic acid (DHCA) has the effect of resisting plant viruses for the first time. In the specific embodiment of the invention, the 1, 5-dioxo-2, 3, 4, 5-tetrahydropyrrolo [1, 2-a] quinazoline-3a (1H)-carboxylic acid is used for preventing and treating the cucumber virus disease and the pepper virus disease, and the result shows that the 1, 5-dioxo-2, 3, 4, 5-tetrahydropyrrolo [1, 2-a] quinazoline-3a (1H)-carboxylic acid and the 1, 5-dioxo-2, 3, 4, 5-tetrahydropyrrolo [1, 2-a] quinazoline-3a (1H)-carboxylic acid are used for preventing and treating the cucumber virus disease and the pepper virus disease. And the composition has a good control effect by combining the 2, 2-a] quinazoline-3a (1H)-carboxylic acid with wuyiencin.

The presently disclosed subject matter relates to compositions comprising Ubiquitin-Specific Protease 1 (USP1) inhibitors and methods of using the same.

The invention belongs to the technical field of biological medicines, and particularly discloses a quinazoline derivative as well as a preparation method and application thereof. The structure of the quinazoline derivative is shown as a formula I. The invention provides a novel quinazoline derivative capable of efficiently inhibiting LSD1 activity, the preparation process is simple and easy to implement, a good effect of resisting colorectal cancer cell proliferation is shown on the animal level, and safe and effective candidate drug molecules are provided for targeted therapy of colorectal cancer.

Disclosed is a method of treating a disease or condition comprising administering to a subject in need thereof a therapeutically effective amount of a compound having the structure of Formula (I), or a pharmaceutically acceptable salt or solvate thereof, in combination with one or more additional therapeutic agents or therapies, wherein Formula (I) is: (I) wherein R1, R2, R3, R4, R5, R6, R7 are as described in the specification.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a 2, 4-disubstituted quinazoline derivative as well as a preparation method and application thereof. According to the invention, a series of 2, 4-disubstituted quinazoline derivative micromolecular ligands capable of acting on telomere G4 are developed on the basis of a quinazoline skeleton. The 2, 4-disubstituted quinazoline derivative disclosed by the invention has certain telomere G4 stability and telomere G4 binding capacity, better anti-tumor cell proliferation activity, low toxicity, higher cell membrane permeability and certain oral bioavailability, in addition, the 2, 4-disubstituted quinazoline derivative disclosed by the invention can activate congenital immune response of tumor cells, and can be used for preparing anti-tumor drugs. The compound has a wide prospect when being applied to preparation of anti-tumor drugs.

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 pharmaceutical composition including a nucleoside analogue loaded into liposomes of a liposomal delivery system, wherein the nucleoside analogue is a purine analogue chosen from {[2-(6-amino-9H-purin-9-yl)quinazolin-4-yl]oxy}phosphonic acid or 2-(6-amino-9H-purin-9-yl) quinazolin-4-ol, or a pyrimidine analogue chosen from 4-amino-1-(4-hydroxyquinazolin-2-yl)-1,2-dihydropyrimidin-2-one or N-[1-(4-hydroxyquinazolin-2-yl)-2-oxo-1,2-dihydropyrimidin-4-yl]acetamide.

The invention relates to the field of organic chemical synthesis, in particular to a quinazolinone compound synthesized by carbon dioxide and a preparation method of the quinazolinone compound. According to the preparation method for synthesizing the quinazolinone compound from carbon dioxide, carbon dioxide, a 2-aminobenzamide compound and aryl halide are taken as raw materials, and are subjected to a heating reaction in the presence of a palladium metal catalyst, a ligand, a reducing agent, alkali and an organic solvent to generate the quinazolinone compound. The mechanism is as follows: carbon dioxide forms an intermediate A under the conditions of alkali and a reducing agent, aryl halide and the intermediate A form a carbonyl metal compound B under the action of a palladium metal catalyst, and then the carbonyl metal compound B reacts with a 2-aminobenzamide compound under the action of the alkali and the reducing agent to obtain the quinazolinone compound. The catalyst system has universality to various types of 2-aminobenzamide and derivatives and aryl halides thereof, the raw materials are wide in source, cheap and easy to obtain, and the reaction process is simple and controllable.

The application discloses a crystal form of a quinazoline compound and a preparation method of the crystal form, and particularly discloses a crystal form of a compound of formula (I) and a preparation method and application of the crystal form.

A quinazoline compound and a pharmaceutically acceptable salt thereof, in particular a compound of formula (II) and a pharmaceutically acceptable salt thereof.

Described herein are inhibitors of EGFR exon 20 insertion mutants and methods of treating cancer comprising the administration of said inhibitors.

Quinazoline dione compounds are provided for treating cardiac indications such as hypertrophic cardiomyopathy and diastolic dysfunction. Diseases treated by the methods described herein include, but are not limited to, cardiomyopathy, hypertrophic cardiomyopathy (HCM), abnormal heart rhythms, aortic disease, Marfan syndrome, coronary artery disease, heart attack, heart failure, rheumatic heart disease, peripheral vascular disease, stroke, deep vein thrombosis, and pulmonary embolism.

There is provided herein compounds of formula (I), (XXI), (XXII) and (XXIII) as defined herein, and salts thereof, for use in the treatment of colorectal and / or lung cancer.

Provided are a series of 5,6-dihydrothieno[3,4-h]quinazoline compounds as represented by formula (P) and pharmaceutically acceptable salts thereof, and the use of the compounds or pharmaceutically acceptable salts thereof in the preparation of solid tumor drugs, such as solid tumor drugs associated with selective PLK1 inhibitors.

The present invention described herein relates to a compound having Structure I for treating diseases and disorders for which inhibition or modulation of the Ubiquitin Ligase COP1 enzyme produces a physiologically beneficial response, in particular for the treatment of Non-Alcoholic Fatty Liver Disease (NAFLD). These compounds having Structure I are capable of increasing the level of adipose triglyceride lipase (ATGL). Also provided is the process of preparing compounds having Structure I.

Ophthalmic compositions comprising 4 - (7-hydroxy-2-isopropyl-4-oxo - 4H - quinazolin-3-yl) - benzonitrile (Compound I) are provided.SOLUTION: The present invention provides crystalline Form E of 4 - (7-hydroxy-2-isopropyl-4-oxo - 4H - quinazolin-3-yl) - benzonitrile (Compound I). Further provided are methods of preparing crystalline Form E of Compound I comprising heating a hydrate form of Compound I to a temperature greater than 250 °C. or 260 °C. to provide Compound I as crystalline Form E. Further provided are ophthalmic compositions comprising crystalline Form E of Compound I.SELECTED DRAWING: None

The invention belongs to the field of biological medicines, and particularly relates to 4-quinazolinone compounds serving as thyroid hormone beta receptor agonists and application of the 4-quinazolinone compounds. The invention discloses a thyroid hormone beta receptor agonist as shown in a formula (I), relates to a 4-quinazolinone compound and a preparation method thereof, and further relates to a pharmaceutical composition containing the compound and application. The compound or the pharmaceutical composition provided by the invention can be used for preventing, treating or relieving diseases regulated by thyroid hormone beta receptors, especially for treating non-alcoholic fatty liver diseases.

The application relates to quinoline and quinazoline carboxamide derivatives of the general formula (I) that have activity as cluster of differentiation 38 (CD38) inhibitors, and to pharmaceutical compositions comprising such compounds. The compounds are useful for preventing or treating diseases and disorders such as, for example, diseases and disorders of metabolism.

The present invention provides formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4H-quinazolin-3-yl)-benzonitrile (compound I) and methods for treating ocular surface pain by administering such formulations. The present invention also provides methods for treating dry eye disease and ocular hyperemia by administering formulations of 4-(7-hydroxy-2-isopropyl-4-oxo-4 H-quinazolin-3-yl)-benzonitrile.

The application provides a preparation method of a dihydroquinazoline compound and belongs to the technical field of organic synthesis. 1 comprises hydrogen, methyl, tert-butyl, methoxy or halogen; R 2 comprises phenyl; R 3 comprises phenyl; R 4 comprises phenyl, p-tolyl, p-methoxyphenyl, o-tolyl, p-fluorophenyl, p-chlorophenyl, naphthyl, pyridyl or thienyl; Ar comprises phenyl, naphthyl or pyridyl; R 5 comprises phenyl, cyclopropyl, cyclohexyl or [1,1'-biphenyl]-4-yl. The preparation method provided by the application has the advantages of short reaction route, no need to add a transition metal catalyst, good functional group compatibility, high yield, high production efficiency and green environmental protection.