302 results about "Quinazoline" patented technology

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 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 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.

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.

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.

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 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.

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 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 invention provides compounds of formula (IA) and compounds of formula (IB) and pharmaceutically acceptable salts thereof; wherein A is selected from group (A1) and group (A2): wherein #1 is attached to the carbon atom forming the oxime moiety and wherein group (A1) is optionally substituted by one or two R10 and group (A2) is optionally substituted by one R10, and wherein R1, X, R2 and R10 are as defined in the claims, as well as methods of using the compounds to treat neoplastic diseases, in particular cancer.

The application discloses a preparation method of a key intermediate of dacomitinib, and comprises the following steps: (1) a cyclization reaction of compound 2 and compound 3 is generated under catalysis of a catalyst 1 to obtain compound 4; the catalyst 1 is CuI supported by modified mesoporous material MCM-41; (2) an amination reaction of compound 4 and 4-fluoro-3-chloroaniline is directly generated under the action of a catalyst 2, an oxidizing agent and DMF to obtain compound 5; the catalyst 2 is a copper compound, and the oxidizing agent is a peroxide; (3) a reduction reaction of compound 5, hydrazine hydrate and activated carbon is generated to obtain the target compound 1, i.e. 7-methoxy-6-amino-4-(3-chloro-4-fluoroanilino) quinazoline; the method uses cheap compound 2 and compound 3 as starting materials, and compound 1 is prepared through three steps, and the total yield can reach more than 76%; the reaction condition is mild, the catalyst can be recycled, the production cost is low, and the method is safe and environmentally friendly.

The invention relates to application of a PARP inhibitor in cancer treatment, in particular to application of the PARP inhibitor in ovarian cancer maintenance treatment. More specifically, the present invention provides a maintenance therapy for an ovarian cancer patient comprising administering an effective amount of 5-fluoro-1-(4-fluoro-3-(4-(pyrimidin-2-yl) piperazine-1-carbonyl) benzyl) quinazoline-2, 4 (1H, 3H)-dione, a hydrate or a pharmaceutically acceptable salt thereof, to an ovarian cancer patient who has undergone a first-line platinum-containing regimen treatment and achieves complete or partial remission, or a pharmaceutical composition containing 5-fluoro-1-(4-fluoro-3-(4-(pyrimidin-2-yl) piperazine-1-carbonyl) benzyl) quinazoline-2, 4 (1H, 3H)-dione, a hydrate thereof, or a pharmaceutically acceptable salt thereof, or a medicament containing the pharmaceutical composition.

This application relates to the field of organic chemical synthesis, specifically to a method for synthesizing quinazolinone compounds from carbon dioxide and its preparation. The method uses carbon dioxide, 2-aminobenzamide compounds, and aryl halides as raw materials, and reacts under heating in the presence of a palladium metal catalyst, a ligand, a reducing agent, a base, and an organic solvent to generate quinazolinone compounds. The mechanism is as follows: carbon dioxide forms intermediate A under alkaline and reducing conditions; the aryl halide reacts with intermediate A under the action of a palladium metal catalyst to form a carbonyl metal compound B, which then reacts with the 2-aminobenzamide compound under the action of an alkaline and reducing agent to obtain the quinazolinone compound. This catalyst system is universally applicable to various types of 2-aminobenzamides and their derivatives, as well as aryl halides; the raw materials are widely available, inexpensive, and readily available; and the reaction process is simple and controllable.

The present disclosure relates to formulations comprising Compound No. 1: or a pharmaceutically acceptable salt thereof. The present disclosure also relates to uses of the formulations, e.g., in treating or preventing cancer.

The invention discloses a quinazolinone 5-HT2A receptor antagonist or agonist compound as shown in a formula I, pharmaceutically acceptable salts of the quinazolinone 5-HT2A receptor antagonist or agonist compound as well as a preparation method and medical application of the quinazolinone 5-HT2A receptor antagonist or agonist compound and the pharmaceutically acceptable salts. The quinazolinone 5-HT2A receptor antagonist or agonist compound is a powerful 5-HT2A receptor antagonist and has potential anti-mental disease activity.

The invention discloses a crystal form of an alkynyl-substituted quinazoline compound as well as a preparation method and application thereof. Specifically disclosed are a monohydrate crystal form I, an N, N-dimethylformamide solvate crystal form II and an n-butanol solvate crystal form III of a compound represented by formula (I). The crystal form of the compound shown in the formula (I) disclosed by the invention can improve the physical and chemical properties of the compound shown in the formula (I) in the prior art, and has one or more of the following advantages: good stability, few impurities, good bioavailability and suitability for subsequent drug preparation.

The invention belongs to the technical field of preparation of quinazolinone. The invention provides a method for preparing butene substituted quinazoline-4 (3H)-ketone, which is characterized in that a spiro-2, 3-dihydroquinazoline-4 (1H)-ketone compound, sodium bicarbonate, 4DPAIPN and dimethyl sulfoxide are subjected to a reaction together. According to the method provided by the invention, additional addition of a metal catalyst, a ligand and an additional oxidant is not needed, reaction conditions are relatively mild, an operation process is relatively simple and convenient, post-treatment is relatively easy, side reactions possibly caused under high temperature and strong oxidation conditions can be reduced, and potential problems caused by metal residues and use of the oxidant are reduced.

The present invention is directed to dihydroquinazoline, -benzothiazine and -benzoxazine derivatives, advantageously for use in the prevention or treatment of neurological, psychiatric and sleep disorders and diseases in which central orexin neurotransmission is impaired or in which central and peripheral orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds for use in the prevention and / or treatment of neurological disorders and diseases. The present invention is also directed to dihydroquinazoline, -benzothiazine and -benzoxazine derivatives and the use of these compounds as medicaments.