185 results about "Quinazolinone" patented technology

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.

Disclosed is a compound of formula (I), its pharmaceutically acceptable salt or pro-drug thereof, where R1, R2, X, L1, L2, L3, L4, L5, and R are as disclosed herein. The compounds disclosed herein can have poly[ADP-Ribose) polymerase 1 (PARP- 1) inhibitory activity. As such, the compounds and compositions containing the compounds, as disclosed herein, can have use for treatment of diseases associated with PARP-1.

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 invention provides a quinazolinone-fused five-membered heterocyclic derivative with a structure represented by formula (I-A). Experimental results show that the compound provided by the present invention has good inhibitory activity against MAT2A, has inhibitory activity against the proliferation of cancer cells with an MTAP deletion mutation, and can be used for treating and / or preventing MAT2A-related cancer diseases.

Provided herein are quinazolinone compounds for modulating muscle myosin to treat obesity and related disorders such as cardiovascular diseases, type 2 diabetes, obstructive sleep apnea, cancer, and osteoarthritis.

The invention relates to a quinazolinone derivative as shown in a formula (I) as well as a preparation method and application of the quinazolinone derivative. The quinazolinone derivative shown in the formula (I) has PARP14 inhibiting activity and can be used for preventing and / or treating cancers and inflammatory diseases. # imgabs0 #

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.

Small molecule inhibitors of Nav1.8 voltage-gated sodium ion channel, including compounds of formula (I), (II), (III), (IV), and (V) are described. Also described are pharmaceutical compositions containing a compound of formula (I), (II), (III), (IV), and (V) and uses of the compounds and pharmaceutical compositions for inhibiting Nav1.8 voltage-gated sodium channels and treating Nav1.8 mediated diseases, such as pain and pain-associated diseases and cardiovascular diseases, such as atrial fibrillation.

The invention discloses an in-situ synthesis method and application of a dysprosium complex of quinazolinone Schiff base. The complex is prepared by a low-temperature solvothermal method in a methanol solvent using N'-(3-ethoxysalicylidene)-2-(3-ethoxysalicylideneimine) benzohydrazide and dysprosium nitrate as reaction raw materials. During the reaction process, part of the initial ligand is in-situ transformed into 3-(3-ethoxysalicylideneimine) quinazolinone. The initial ligand and the in-situ generated quinazolinone Schiff base ligand jointly construct an unprecedented dysprosium-based pentanuclear cluster structure formed by the sharing of edges of {Dy4} tetrahedral units and {Dy3} triangular units. Under zero external field, the complex exhibits obvious single-molecule magnet behavior characteristics and has application potential in the field of new molecular-based magnetic materials.

A quinazolinone catalyst with both N-N and C-C axis chirality and its synthesis method and application, its chemical structural formula is shown in Formula 4; Synthesis method: using indole-derived o-aminobenzamide and 1-naphthaldehyde derivative as raw materials, using molecular sieve as dehydrating agent, bromobenzene as reaction solvent, stirring for 4h under the catalysis of chiral phosphoric acid and 10°C, then adding ethyl acetate, 2,3-dichloro-5,6-dicyano-1,4-benzoquinone, stirring for 10h under room temperature, TLC tracking reaction to complete formula 3 compound; using formula 3 compound, phenylsilane, trifluoromethanesulfonic acid as raw materials, adding toluene, stirring reaction under 100°C, TLC tracking reaction to end to obtain formula 4 compound. The catalyst prepared by the present invention can be used as a chiral ligand in transition metal-catalyzed asymmetric allylation reaction, with excellent stereoselectivity control effect; the method has mild reaction conditions, low cost and high enantioselectivity.

The application discloses a dihydroquinazolinone-containing N-hydroxy amide compound and a preparation method and application thereof, relates to the technical field of medicinal chemistry, and utilizes the splicing principle to design and synthesize dihydroquinazolinone-containing N-hydroxy amide compounds with novel structures, and the compounds are tested in terms of HDAC6 protein affinity and anti-proliferation activity of cervical cancer cell Siha, and the results show that the compounds E1-E5 have better affinity to the HDAC6 protein, the IC 50 values are 4.1-85.4 nM, wherein the affinity of the compound E4 to the HDAC6 protein is higher than that of a positive control SAHA; and the compounds E1-E5 can better inhibit the proliferation of the cervical cancer cell Siha, the IC 50 values are 2.4-9.3 muM, wherein the activity of the compound E4 is the strongest.

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 present invention discloses a compound represented by formula I, its stereoisomers, deuterides or pharmaceutically acceptable salts, or a pharmaceutical composition containing them, and their use as BRAF regulators in the manufacture of drugs for treating related diseases, and each group represented by formula (I) is as defined in the specification. [Chemical formula 1] TIFF2025523998000103.tif38156

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 invention discloses 9-phenyl-10-aryloxy evodiamine quinazolinone with a structural formula shown as a formula 3, wherein Ar is selected from benzyl and substituted benzyl. The invention further discloses a preparation method of the 9-phenyl-10-aryloxy evodiamine quinazolinone. The 9-phenyl-10-aryloxy evodiamine quinazolinone derivative as shown in the formula 3 is prepared by the following steps: (1) taking 10-hydroxyevodiamine (A) as a raw material, and reacting with an arylation reagent (ArX) in the presence of a proper alkali catalyst under proper conditions to obtain 10-aryloxy evodiamine 1; (2) reacting the compound 1 with a bromination reagent under proper conditions to obtain 9-bromo-10-aryloxy evodiamine 2; and (3) reacting the compound 2 with an arylboronic acid reagent under proper conditions to obtain the 9-phenyl-10-aryloxy evodiamine quinazolinone derivative 3. The 9-phenyl-10-aryloxy evodiamine quinazolinone derivative 3 synthesized by the preparation method disclosed by the invention is used for treating liver cancer cells in vitro; the neuroblastoma cells show good anti-cancer activity and can be applied to preparation of corresponding anti-tumor drugs.

The present invention relates to quinazolinones and related compounds which degrade PARP14 and are useful, for example, in the treatment of cancer and inflammatory diseases.

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 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 invention provides a trifluoromethyl-containing quinazolinone derivative as well as a preparation method and application thereof, and belongs to the technical field of organic synthetic chemistry. A quinazolinone compound 1 and a trifluoromethyl-containing alkynone compound 2 are taken as raw materials, a catalyst is added, synthesis of the novel trifluoromethyl quinazolinone compound is realized in a solvent in one step, and a series of trifluoromethyl-containing quinazolinone compounds with novel structures are synthesized. The reaction does not need inert gas protection, the operation is simple, the condition is mild, the functional group tolerance is strong, the atom utilization rate is 100%, only a catalytic amount of [Ru (p-cymene) Cl2] 2 needs to be added in the reaction, the used solvent is a green solvent, and the method has high step economy and atom economy. The obtained product has a wide industrial application prospect, and meanwhile, a new thought and a new method are provided for the field of synthesis of medicines and natural products.

The present invention relates to a new process for the preparation of (3R)—N-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide, as well as to a novel intermediate useful for the synthesis of said compound at large scale.

A 2,3-fused quinazolinone derivative, its preparation method, and application are disclosed. A 2,3-quinazolinone derivative was synthesized using a simple method with high yield and low production cost. At a concentration of 5 µM and an LPS concentration of 1 µg / mL, compounds 1e and 1f exhibited superior NO release inhibition compared to the anti-inflammatory drugs indomethacin and evodiamine, while compounds 1g and 1q were comparable to indomethacin, and compounds 1w and 1m were comparable to evodiamine. Compounds 1e, 1f, 1g, 1q, and 1m, which exhibited strong NO release inhibition, exhibited less cytotoxicity against RAW264.7 cells than the anti-inflammatory drugs indomethacin and evodiamine. The derivative exhibited significant anti-inflammatory effects and low toxicity. The derivative can be formulated into various dosage forms of anti-inflammatory drugs, possessing high medical value and broad market prospects.

The present invention relates to quinazolinones and related compounds that degrade PARP14 and are useful, for example, in the treatment of cancer and inflammatory diseases.

The present invention relates to dihydroquinazolinone compound, a preparation method therefor, and a use thereof. The dihydroquinazolinone compound has an excellent inhibitory effect on GLUT9, can effectively inhibit GLUT9 activity so as to promote uric acid excretion, thereby achieving a uric acid lowering effect, and can be used for treating diseases related to GLUT9 activity or expression. The dihydroquinazolinone compound or a pharmaceutically acceptable salt thereof has no obvious toxicity to organs, can significantly reduce kidney damage caused by hyperuricemia, and alleviates gout symptoms.

This invention discloses a method for preparing a bis(trifluoromethyl)quinazolinone amide derivative, comprising the following steps: under nitrogen protection, intermediate A is activated using an alkaline reagent, and then an acylation reagent is added to react and obtain the target compound. By innovatively utilizing a precise ratio system of bis(trimethyl)silylamine lithium (LiHMDS) and acetic anhydride, and conducting the reaction under low-temperature conditions, the acylation step can be completed in only 1-5 minutes, significantly shortening the overall process cycle compared to traditional methods and greatly improving production efficiency.

The invention relates to an application of a Ru-Pt alloy catalyst in catalyzing acceptor-free dehydrogenation of alcohol to synthesize quinazolinone compounds. The Ru-Pt alloy catalyst comprises a carbon black carrier and active components ruthenium and platinum loaded on the carbon black carrier. In the method for synthesizing the quinazolinone compound through acceptor-free dehydrogenation of alcohol, the Ru-Pt alloy catalyst can efficiently catalyze an aminobenzamide compound to react with low-equivalent alcohol under the condition that additives such as an acid-base additive, an oxidizing agent or a hydrogen acceptor are not added, so that the yield of the quinazolinone compound is increased, and the yield of the quinazolinone compound is increased. The yield of the quinazolinone compound reaches a relatively high level; moreover, the Ru-Pt alloy catalyst can achieve good cycle performance only through simple washing and drying treatment without activation treatment such as oxidation or reduction.

The invention discloses a synthesis method of a 2-position amide substituted quinazolinone derivative, which is characterized in that anthranilamide and pyruvoamide are used as raw materials, under the condition that N, N-dimethylformamide is used as a solvent, iodine is used as a catalyst, and various amide-containing quinazolinone derivatives with different substituent groups are conveniently and quickly prepared. The method is wide in substrate compatibility, mild in reaction condition, easy to operate, simple in post-treatment and suitable for industrial production.

The present disclosure relates to novel compounds, to said 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 said diseases comprising the use of the novel compounds. The present disclosure furthermore relates to pharmaceutical compositions or combination preparations of the novel compounds as well as to said 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 said compounds.

A compound of general formula (I) and also the stereoisomeric forms, mixtures of stereoisomeric forms or pharmaceutically acceptable salts thereof, and also to the use thereof for the prevention and / or treatment of disorders caused by intracellularly acting toxins using retrograde transport, or by viruses or bacteria using retrograde and / or syntaxin 5-dependent transport to infect cells.

Dihydroquinazolinone and azadihydroquinazolinone compounds are provided for use in the treatment of cardiac indications, such as hypertrophic cardiomyopathy and diastolic dysfunction.