44 results about "Quinazoline derivatives" patented technology

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 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).

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 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).

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.

The present disclosure relates to tetrahydroquinazoline derivatives of formula (I) and their use for selectively killing GAG-POL expressing cells infected by HIV without accompanying cytotoxicity on HIV primordial cells, and for treating or preventing HIV infection, or for treating, preventing or delaying the onset or progression of AIDS or AIDS-related syndrome (ARC). (I).

The present disclosure relates to methods of treating or preventing cancer (e.g., advanced solid cancer) using Compound Number 1: (Compound Number 1) or a pharmaceutically acceptable salt thereof. The disclosure also relates to pharmaceutical compositions and pharmaceutical kits suitable for treatment or prevention. (Compound Number 1)

The invention belongs to the technical field of antitumor drug development, and particularly relates to a novel 4-aniline quinazoline derivative, a synthesis method and a drug for treating cancer. According to the invention, 2-amino-4-nitrobenzoic acid is used as an initial raw material, and a series of novel 4-aniline quinazoline derivatives containing cinnamic acid are synthesized through multi-step reactions such as trifluoroacetylation, ring closing, chlorination, aromatic amine substitution, reduction and cinnamic acylation. In-vitro antitumor activity research shows that part of the compounds show remarkable inhibitory activity on multiple tumor cells such as MDA-MB-231, A549 and SMMC-7721, can induce cell apoptosis and inhibit cell migration, and shows excellent antitumor drug development prospects. In addition, the structure-function relationship of the series of compounds is further deeply studied, and reference significance is provided for further development and research of novel antitumor drugs.

The present invention relates to a compound represented by chemical formula 1 or a pharmaceutically acceptable salt thereof. The compound according to the present invention can be effectively used for preventing or treating cancer or tumors. [Chemical formula 1] In chemical formula 1, R1 to R3, A, L and a are as defined in the specification.

The invention discloses a preparation method of a 2-substituted quinazoline derivative, which comprises the following step: heating and stirring three components, namely an ammonium salt, a benzyl alcohol compound and a 2, 1-benzisoxazole compound in an organic solvent to obtain the 2-substituted quinazoline derivative. According to the method, ammonium iodide which is low in price and easy to obtain is used as a nitrogen source and an oxidizing agent, benzyl alcohol is used as a carbon source, and efficient construction from a 2, 1-benzisoxazole skeleton to a 2-substituted quinazoline skeleton is achieved through a carbon-nitrogen diatom inserted ring expansion reaction under the mild conditions of no metal and no additive. The synthetic method developed by the invention has a good application prospect in the industrial fields of biological medicines, pesticides and the like, and is particularly suitable for efficiently preparing the quinazoline compound with biological activity under simple and convenient conditions. The synthetic method developed by the invention has a good application prospect in the industrial fields of biological medicines, pesticides and the like, and a theoretical basis is provided for commercialized application of the derivatives in the field of medicines.

The application belongs to the technical field of anti-infective drugs, and discloses 7H-pyrrolo[3,2-f]quinazoline derivatives and anti-infective applications thereof. Specifically, it relates to 1,3-diamino-7H-pyrrolo[3,2-f]quinazoline heterocyclic compounds, a preparation method of the compounds and the use of the compounds in the preparation of anti-infective drugs. The compounds contain an aromatic fused ring structure, and are connected to the 1,3-diamino-7H-pyrrolo[3,2-f]quinazoline skeleton through different carbon chains. Compared with existing dihydrofolate reductase inhibitors, the compounds have better antibacterial activity and can be used as anti-infective drugs.

The present disclosure relates generally to compounds and compositions thereof for inhibition of ErbB2, including mutant forms of ErbB2, particularly those harboring an Exon 20 mutation, methods of preparing said compounds and compositions, and their use in the treatment or prophylaxis of various cancers, such as lung, glioma, skin, head neck, salivary gland, breast, esophageal, liver, stomach (gastric), uterine, cervical, biliary tract, pancreatic, colorectal, renal, bladder or prostate 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] TIFF2026516541000123.tif46141