51 results about "Quinazoline" 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.

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.

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 application provides novel N-heterocyclic compounds, such as quinoline or isoquinoline compounds, preferably quinazoline compounds, as calcineurin inhibitors (CNIs,) that provide improved safety profiles, and the pharmaceutical composition and formulation thereof, as well as a method of using the N-heterocyclic compounds for the treatment of, inter alia, an inflammatory-related disease or disorder.

The application belongs to the technical field of chemical medicine raw materials, and particularly relates to a quinazoline compound and application thereof, a structure of the compound is shown as formula I. It is verified through experiments that the compound provided in the application has good in-vitro anti-tumor activity, and lays a foundation for further development of anti-tumor drugs. Formula I.

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 application relates to the technical field of medicines, and discloses a 4-methyl quinazoline PI3K-Tubulin dual-target inhibitor and a preparation method and application thereof. Specifically disclosed are a PI3K-Tubulin dual-target inhibitor compound or a pharmaceutically acceptable salt thereof, a pharmaceutical composition and preparation containing the compound or the pharmaceutically acceptable salt thereof, a method for preparing the compound or the pharmaceutically acceptable salt thereof, and application of the compound or the pharmaceutically acceptable salt thereof in preparing medicines for treating and / or preventing diseases mediated by PI3K-Tubulin and related diseases.

The present invention provides a solid form of (3R)-N-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxyphenyl]-3-fluoropyrrolidine-1-sulfonamide and its solvate, as well as its therapeutic use and pharmaceutical compositions containing the same.

The present disclosure relates to spiro-fused tetrahydroquinazoline compounds, to the compounds for use as a medicine, more in particular for the prevention or treatment of diseases mediated by activity of YAP / TAZ-TEAD transcription, yet more in particular for the prevention or treatment of cancer or fibrosis. The present disclosure also relates to a method for the prevention or treatment of diseases comprising the use of the compounds.The present disclosure furthermore relates to pharmaceutical compositions or combination preparations of the compounds as well as to compositions or preparations for use as a medicine, more preferably for the prevention or treatment of diseases mediated by activity of YAP / TAZ-TEAD transcription, yet more in particular for the prevention or treatment of cancer or fibrosis. The present disclosure also relates to processes for the preparation of compounds.

This invention relates to the field of medicinal chemistry, specifically disclosing 4-(2-fluoro-4-iodophenoxy)-6-methoxy-7-[3-(4-methylpiperazin-1-yl)propoxy]quinazoline, its preparation method, and its applications. A novel N-[4-(quinazoline-4-yl)oxyphenyl]biarylsulfonamide compound prepared from this intermediate is a dual inhibitor targeting EGFR and c-Met. The quinazoline core and sulfonamide biaryl side chain in its molecular structure can specifically recognize and bind to mutant EGFR and abnormally activated c-Met, significantly enhancing its selective killing effect on tumor cells. Pharmacodynamic studies show that it exhibits excellent inhibitory activity against the human lung cancer cell line (NCI-H1975) at the cellular level, with an IC50 of [missing information - likely an IC50 value] against p-EGFR. 50 A value of 1.56 nM for p-Met IC 50 The value is 1.8nM.

Provided are a salt of an arylaminoquinazoline-containing compound as shown in formula 2, a solvate or hydrate thereof, a preparation method therefor and the use thereof. The prepared salt has good crystallinity, and compared to a compound in a free form, the water solubility is significantly improved, and preferably, the salt form and crystal form can stably exist. Therefore, compared to a compound in a free form or other salts, the salt has better druggability.

The present disclosure provides CDK2 inhibitor compounds that can have a fused 6-6 bicyclic core, such as a naphthyridine, quinazoline, pyridopyrimidine or related isosteric core structure that is further substituted. Also provided herein are pharmaceutical compositions including the subject CDK2 inhibitor compounds, and methods for using compositions of the disclosure as anticancer therapeutics.

This invention relates to 2-amino-4-methylquinazoline compounds, their preparation methods, uses, and pharmaceutical compositions. Specifically, it provides a compound represented by Formula I, which is a phosphatidylinositol 3-kinase δ (PI3Kδ) inhibitor that can be used to prevent and / or treat diseases related to PI3Kδ activity, such as tumors, autoimmune diseases, immunodeficiency diseases, inflammation, kidney diseases, cardiovascular diseases, metabolic / endocrine disorders, or neurological diseases.

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.

The present disclosure relates to compounds of Formula (I') and pharmaceutically acceptable salts and stereoisomers thereof. The present disclosure also relates to methods of making these compounds, compositions comprising these compounds, and methods of using the same to prevent or treat abnormal cell growth in mammals, particularly humans.

Providing quinazolindione compounds and their uses. [Solution] 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.

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 application belongs to the technical field of biological medicine, and particularly relates to application of an imidazoquinazoline small-molecule compound or a pharmaceutically acceptable salt thereof shown in formula (I) in preparation of a drug for treating KRAS mutant gastrointestinal tumors, wherein R is as described in the claims and the specification. The imidazoquinazoline compound can selectively inhibit proliferation, migration and invasion of KRAS mutant gastrointestinal tumor cells, and induce cell cycle arrest and apoptosis. Specifically, the compound exerts an anti-tumor effect by inhibiting the binding of p-ERK2 and p53, restoring p53 transcriptional activity, and up-regulating the expression of a pro-apoptotic gene PUMA downstream of p53. The mechanism of action is different from that of traditional KRAS or MEK inhibitors, and provides a new treatment option for KRAS mutant gastrointestinal tumor patients.

This invention relates to the field of pharmaceutical technology, specifically to a 6-(6-methyl-1H-pyrrolo[2,3-b]pyridin-3-yl)quinazoline-4-amine derivative, its preparation method, and its applications. This invention utilizes a "conformation-locking" and "drug-likeness optimization" strategy to optimize the 4-position side chain of quinazoline into conformationally defined structures such as dihydroindanol and fluoropiperidine, thereby reducing P-gp recognition through conformational rigidity. Simultaneously, the introduction of groups such as cyclopropylformyl groups reduces off-target toxicity, thus broadening the therapeutic window. The 6-(1H-pyrrolo[2,3-b]pyridin-3-yl)quinazoline-4-amine derivative provided by this invention simultaneously achieves potent DYRK1A inhibition, high kinase selectivity, low microglial cytotoxicity, significant anti-neuroinflammatory effects, good blood-brain barrier permeability, and oral bioavailability. Furthermore, it is a novel small-molecule inhibitor that can be validated for cognitive improvement in AD animal models, possessing significant clinical value and urgent application needs.