94 results about "Quinazoline derivatives" 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 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.

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.

A quinazoline derivative (represented by the formula (I)) salt's crystal form, a preparation method and application are provided; specifically, the hydrochloride crystal form A, B, C, D, F, H, I, Sulphate crystal form A, Maleate crystal form A, Succinate crystal form A, Adipate crystal form A, Glycolate crystal form A, Malate crystal form A, Fumarate Salt crystal form A, besylate crystal form A, B, C, benzoate crystal form A, hippurate crystal form A and oxalate crystal form A of the quinazoline derivative represented by formula (I). The salt crystal form provided by the present invention has good stability, which can be used in the treatment of non-small cell lung cancer brain metastasis, meningeal metastasis, primary brain cancer or glioma, etc., and has good bioavailability, which is of great significance for further research on the efficacy of such solid drugs.

To provide a type I receptor tyrosine kinase inhibitor.SOLUTION: Or a pharmaceutically acceptable salt thereof. Specific examples thereof include N - (4 - ([1,2,4] triazolo [1, 5-c] pyrimidin-7-yloxy) - 3-methylphenyl) - 5 - (3 - (dimethylamino) azetidin-1-yl) - 6-methoxyquinazolin-4-amine.SELECTED DRAWING: None

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 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 2-aminoquinazoline derivative as well as a preparation method and application thereof, and relates to the technical field of organic synthesis. The 2-aminoquinazoline derivative disclosed by the invention has a structure as shown in a formula I or a formula II. On the basis of a simple and efficient synthesis route, a plurality of 2-aminoquinazoline derivatives are rapidly constructed by using commercially available and low-cost raw materials and reagents through modular design; the 2-aminoquinazoline derivative has an obvious protective effect on cytopathy caused by viruses, shows down-regulation effect on virus RNA and protein level, lays a solid foundation for subsequent drug development and optimization, and has a wide application prospect.

The present application relates to compounds of formula (A) that inhibit the growth of cancers that express G12D mutant Ras proteins. The molecules of the specification are thus indicated for use in the treatment of cancer that express G12D mutant Ras protein.

Use of a quinazoline compound and a third-generation epidermal growth factor receptor (EGFR) inhibitor in a combined drug for treating non-small cell lung cancer. The quinazoline compound comprises at least one of a quinazoline derivative represented by formula (I), a salt thereof, a solvate thereof, a hydrate thereof, and a polymorph thereof.

The present application relates to the technical field of chemical pharmaceuticals, and provides a quinazoline derivative, a preparation method therefor, and a use thereof. The quinazoline derivative provided in the present application has a strong effect of targeted inhibition of DDR1 / 2 activity, with kinase inhibition activity against DDR1 / 2 reaching low nanomolar concentrations, and can inhibit the activity of DDR1 / 2 in a dose-dependent manner, some compounds achieving pM-level inhibitory activity against DDR1, and being usable in the preparation of a medicament for treating and / or preventing diseases caused by abnormal DDR1 / 2-related signaling pathways. Among the currently reported DDR-targeting compounds in the literature, the derivative is in a leading position and also has relatively good selectivity. The present application provides a preparation method for the quinazoline derivative having a short synthesis route, safe operation process, and feasibility for scaled-up production.

The present application relates to a quinazoline derivative of general formula (I) or stereoisomer, pharmaceutically acceptable salt, solvate, or tautomer, which can selectively inhibit CDK9 and / or TNIK, and has good enzymatic and cellular activity.

The present disclosure is directed to tetrahydroquinazoline derivatives of Formula I and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV naïve cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).

The application belongs to the field of chemical industry, and particularly relates to a synthesis method of a substituted pyrazoloquinazoline derivative. The method provided by the application comprises sequentially preparing 2-chloro-5,6,7,8-tetrahydroquinazoline, 2-chloro-6,7-dihydroquinazolin-8(5H)-ketoxime, 2-chloro-6,7-dihydroquinazolin-8(5H)-ketone, 2-(2-methoxy-8-oxo-5,6,7,8-tetrahydroquinazolin-7-yl)-2-oxoacetic acid methyl ester and 1-(2-hydroxyethyl)-8-methoxy-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxylic acid methyl ester, and finally obtaining 1-(2-hydroxyethyl)-8-((5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl)amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide. By using the method of the application, three reaction steps are reduced, the total yield is increased by nearly one time, and the method is far higher than the original process route; and the application of dangerous reagents such as hydrazine hydrate and iodine is avoided, and the method is easy to scale up.

The invention relates to the technical field of medicinal chemistry, in particular to a substituted quinazoline derivative and a preparation method and application thereof.The structure of the compound is shown in the formula I. Experiments prove that the compound has good in-vitro anti-tumor activity, and a foundation is laid for further research and development of anti-tumor drugs.

This invention discloses a quinazoline derivative containing a benzofuran structure and its applications, the general structural formula of which is shown in Figure I. This class of compounds exhibits significant inhibitory activity against VEGFR and HDAC, and can be used to treat VEGFR and HDAC-mediated diseases such as tumors.

To provide a polymorphic form of a quinazoline compound exhibiting type I receptor tyrosine kinase inhibitory activity.SOLUTION: Provided is a crystalline form of Compound (I) represented by the following structural formula: wherein the crystalline form is a complex of the free base and a pharmaceutically acceptable acid, or the free base.SELECTED DRAWING: None

The present application relates to quinazoline derivatives, salts thereof, and pharmaceutical compositions comprising the same as an effective ingredient, which can exhibit a preventive or therapeutic effect on cancer by inhibiting MASTL activity, and in particular, can exhibit an effective anticancer effect in cancer in which MASTL is overexpressed, such as breast cancer.

This application discloses trisubstituted quinazoline derivatives, their acid addition salts, pharmaceutical compositions thereof, and uses. Specifically, the trisubstituted quinazoline derivatives are (E)-4-(dimethylamino)-N-(4-((4-(4-fluoro-phenoxy)phenyl)amino)-7-ethoxyquinazoline-6-yl)but-2-enamides. This application also discloses (E)-4-(dimethylamino)-N-(4-((4-(4-fluoro-phenoxy)phenyl)amino)-7-ethoxyquinazoline-6-yl)but-2-enamide acid addition salts, their solvates or hydrates, or pharmaceutical compositions thereof. The substances disclosed in this application can be used for the prevention, inhibition, or treatment of cancer.

This disclosure relates to tetrahydroquinazoline derivatives represented by Formula I, and their use for selectively killing HIV-infected GAG-POL-expressing cells without cytotoxicity to HIV-naive cells, and for treating or preventing HIV infection, or for treating, preventing or delaying the onset or progression of AIDS or AIDS-related syndromes (ARC). [Formula 1] TIFF0007861226000129.tif46141

The invention relates to a preparation method of (R)-N-(4-([1, 2, 4] triazolo [1, 5-c] pyrimidin-7-yloxy)-3-methylphenyl)-5-((3, 4, 5-triazolo [1, 5-c] pyrimidin-7-yloxy)-3-methylphenyl The present invention relates to crystalline forms of 2, 3-difluoro-1-methylpiperidin-4-yl) oxy)-6-methoxyquinazolin-4-amine, to processes for their preparation, to pharmaceutical compositions comprising one or more of the crystalline forms as an active ingredient and to the use of said crystalline forms in the treatment of hyperproliferative diseases.

The invention belongs to the field of chemical pharmacy. Relates to 4-methylquinazoline derivatives, and a preparation method, a pharmaceutical composition and application thereof. The 4-methylquinazoline derivative is a compound shown in a formula (I) or a pharmaceutically acceptable salt thereof, is a PI3K inhibitor, and can be used for preventing and / or treating diseases related to PI3K activity, such as tumors, autoimmune diseases, kidney diseases, cardiovascular diseases, inflammation, metabolism / endocrine dysfunction or nerve diseases.

The invention relates to a crystal form of a quinazoline derivative and a preparation method thereof. Specifically, the invention provides an E crystal form, a D crystal form and an H crystal form of 1-(inner-3-((4-((4-([1, 2, 4] triazolo [1, 5-a] pyridine-7-yloxy)-2-fluoro-3-methylphenyl) amino) quinazoline-6-yl) oxy)-8-azabicyclo [3.2. 1] oct-8-yl) prop-2-en-1-one, and the E crystal form, the D crystal form and the H crystal form have good stability and can be better used for clinical treatment. Formula (I).

The present disclosure is directed to tetrahydroquinazoline derivatives of Formula (I) and their use for selectively killing HIV infected GAG-POL expressing cells without concomitant cytotoxicity to HIV naive cells, and for the treatment or prophylaxis of infection by HIV, or for the treatment, prophylaxis or delay in the onset or progression of AIDS or AIDS Related Complex (ARC).

The invention discloses a polyquinazoline derivative as well as a preparation method and application thereof, and relates to the technical field of organic high-molecular polymers. The invention provides a polyquinazoline derivative as shown in a formula I, wherein a is an integer from 1 to 200; r1 and R2 are respectively and independently an aryl group, an aryl derivative, an ester group, a bioactive fragment or an aliphatic substituent; the bioactive fragment comprises one of terpenoids, steroids, fatty alcohol and vitamins; r is NH or O. In the formula, R is an aryl group, an aryl derivative or a heteroaromatic ring group. The polyquinazoline derivative provided by the invention is novel in structure, the structural library of the polyquinazoline derivative is enriched, the molecular weight of the polyquinazoline derivative is high, the absolute weight-average molecular weight of the polyquinazoline derivative is 410,000-4064,000 g / mol, the polymer dispersion index (PDI) of the polyquinazoline derivative is 1.42-3.90, and the polyquinazoline derivative has excellent thermal stability, morphology stability and good solubility and has aggregation luminescence property or chiral optical property.

The present invention relates to an inhibitor having a quinazoline-containing structure for the treatment of cancer. Specifically, the present invention relates to a derivative as represented by formula (I) having a quinazoline-containing structure, and a pharmaceutically acceptable salt thereof. The compound or the salt thereof can simultaneously inhibit a plurality of mutation types of the KRAS proteins, including KRAS G12C, G12D and G12V mutant proteins, and can be used as a KRAS small-molecule inhibitor for treating various diseases caused by KRAS mutations. The present invention relates to the structure of an inhibitor derivative having a quinazoline-containing structure and a preparation method therefor. The present invention further relates to a pharmaceutical composition containing the compound or the salt thereof, and a method for treating diseases related to KRAS mutations by means of using the compound and the salt thereof.

Relates to a pharmaceutically acceptable salt of a quinazoline derivative, and a crystal form and application thereof. Specifically, the invention provides a medicinal salt, a crystal form and a preparation method of 1-(inner-3-((4-((4-([1, 2, 4] triazolo [1, 5-a] pyridine-7-yloxy)-2-fluoro-3-methylphenyl) amino) quinazoline-6-yl) oxy)-8-azabicyclo [3.2. 1] oct-8-yl) prop-2-en-1-one, and the corresponding salt has good stability and can be better used for clinical treatment.