140 results about "Pyrimidone" patented technology

The invention relates to the field of organic chemical synthesis, in particular to a synthetic method and application of pyrimidone compounds. The invention provides a synthesis method, reactants are o-amino heterocyclic formamide and triethyl orthoformate respectively, a solvent system is a hexafluoroisopropanol solvent, and a product is a heterocyclic pyrimidone compound. The reaction does not need strong acid or strong alkali conditions, does not need additional reducing agents or oxidizing agents, does not need transition metal catalysis, is economical and practical, the reaction conditions are relatively mild, and the synthesized pyrimidone compound has a good antibacterial effect.

The invention provides a water-borne epoxy resin silicon steel sheet rapid curing self-adhesion coating, and relates to the technical field of curing coatings. The coating is prepared from water-borne epoxy resin emulsion, ureido pyrimidone modified epoxy resin, gold nanorod and silicon dioxide core-shell particles, silane modified carbon nanohorns, a cationic photoinitiator, a microencapsulated diaminodiphenylmethane curing agent, deionized water, propylene glycol methyl ether acetate and auxiliaries. The ureido pyrimidone modified epoxy resin, the gold nanorod and silicon dioxide core-shell particles, the silane modified carbon nanohorns and the microencapsulated diaminodiphenylmethane curing agent are added into the coating, so that the curing time of the coating is prolonged, meanwhile, a multi-layer stacked structure is formed after the coating is cured, and the adhesive force between the coating and a base material is improved.

The application relates to fused pyrimidinone derivatives of the general formula (I) which act as agonists of Triggering Receptor Expressed on Myeloid cells 2 (TREM2) useful for the treatment of Parkinson's disease, rheumatoid arthritis, Alzheimer's disease, amyotrophic lateral sclerosis, Nasu-Hakola disease, frontotemporal dementia, multiple sclerosis, prion disease, and stroke.

The present invention relates to a solid dispersion of a triazolopyrimidinone derivative having tankyrase inhibitory activity and a method for producing the same. The solid dispersion of the triazolopyrimidinone derivative represented by formula I according to the present invention has high solubility and excellent bioavailability, and can be usefully used as a pharmaceutical raw material.

The invention relates to the technical field of electrochemistry, in particular to a phosphorus-containing ureido pyrimidone monomer and a preparation method thereof, a gel electrolyte and a lithium battery. The phosphorus-containing ureido pyrimidone monomer is prepared by the following steps: reacting a phosphorus-containing hydroxyl compound with a diisocyanate compound to generate a phosphorus-containing isocyanate intermediate, reacting the phosphorus-containing isocyanate intermediate with a 2-amino-4-hydroxypyrimidine derivative to generate a urea intermediate, and reacting the urea intermediate with an acrylic anhydride compound. According to the phosphorus-containing ureido pyrimidone monomer, a dynamic self-repairing unit and a flame-retardant unit are integrated into the monomer from a molecular source, so that the monomer molecule has a flame-retardant function and a self-repairing function. The raw materials of the gel electrolyte comprise the phosphorus-containing ureido pyrimidone monomer, the gel electrolyte is prepared in the lithium battery through constant-temperature gradient boosting curing, the lithium battery is obtained, the gel electrolyte has good flame retardance and self-repairing performance, and the lithium battery has good conductivity, cycle performance and safety.

The invention discloses application of a thiophene pyrimidone derivative in preparation of a medicine for treating Alzheimer's disease, and belongs to the technical field of medicines, and the thiophene pyrimidone derivative is 2-[(4-methylpiperidine-1-yl) methyl]-3-(tetrahydrofuran-2-yl methyl)-5-(thiophene-2-yl) thieno [2, 3-d] pyrimidine-4-ketone. According to the application of the thiophene pyrimidinone derivative in preparation of the medicine for treating the Alzheimer's disease, 2-[(4-methylpiperidine-1-yl) methyl]-3-(tetrahydrofuran-2-yl methyl)-5-(thiophen-2-yl) thieno [2, 3-d] pyrimidin-4-one has an efficient inhibition effect on BChE, can remarkably improve the cognitive function defect of an AD model, and can be used for preparing the medicine for treating the Alzheimer's disease. A novel efficient BChE targeting candidate inhibitor is provided for the field of AD treatment.

This invention relates to pyrimidin-4(3H)-one derivatives of formula (I),that act as modulators of the TRPV4 receptor. The present invention also relates to processes for the preparation of novel pyrimidin-4(3H)-one derivatives of formula (I) and to their use in the treatment of a wide range of diseases, syndromes, and disorders, in particular, for the treatment of inflammation, pain, and urological diseases or disorders.

The present application is concerned with tricyclic pyrimidinones as inhibitors of WRN, as well as pharmaceutical compositions and methods of use related thereto. The compounds are useful in treating, preventing, or ameliorating diseases or disorders such as cancer or infections.

The invention relates to the technical field of medicine synthesis, in particular to a synthesis method and application of a 4H-pyrido [1, 2-a] pyrimidine-4-one-1, 3, 5-triazine derivative. The structure of the target compound is shown as a formula I. The preparation method of the 4H-pyrido [1, 2-a] pyrimidine-4-ketone-1, 3, 5-triazine derivative comprises the following step: reacting a compound shown in a formula I with a compound shown in a formula II in the presence of acetonitrile, secondary amine and anhydrous potassium carbonate to obtain the 4H-pyrido [1, 2-a] pyrimidine-4-ketone-1, 3, 5-triazine derivative. The 4H-pyrido [1, 2-a] pyrimidine-4-ketone-1, 3, 5-triazine derivative disclosed by the invention has a relatively good anti-tumor effect, and is characterized by relatively strong tumor cell growth inhibition activity.

To provide pyridopyrimidinone derivatives as AHR antagonists.SOLUTION: The present disclosure relates to compounds of formula (Ia) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, methods of preparing the same, intermediate compounds useful for preparing the same, and methods for treating or prophylaxis of diseases, in particular cancer or conditions with dysregulated immune responses or other disorders associated with aberrant AHR signaling. These compounds may also be useful in treating cancer when administered in combination with at least one additional therapy.SELECTED DRAWING: None

The present application belongs to the technical field of scale inhibitors, and particularly relates to a phosphorus-free composite scale inhibitor and a preparation method thereof. The phosphorus-free composite scale inhibitor comprises, in terms of mass fraction, 4.5-9.5 parts of beta-CD grafted hyperbranched polyglycidyl ether, 8-20 parts of AA / AMPS copolymer, 15-30 parts of PESA, 18-30 parts of CETSA, 6.5-10.5 parts of 2,4,6-trithiol-1,3,5-triazine, 3-6 parts of sodium molybdate dihydrate, 5-12 parts of sodium polyacrylate, 2-6 parts of N-octadecyl-D-glucosamide, 1.2-3 parts of ureido pyrimidone derivative containing isocyanate groups, 0.5-1.2 parts of 2,6-pyridine dicarboxamide, and 65-85 parts of water. The preparation method comprises the following steps: stirring raw materials such as beta-CD grafted hyperbranched polyglycidyl ether and water, adjusting pH, and keeping warm, then adding ureido pyrimidone derivative containing isocyanate groups and 2,6-pyridine dicarboxamide, and mixing uniformly to obtain the phosphorus-free composite scale inhibitor. The present application solves the problem of poor scale inhibition and corrosion inhibition effect of the phosphorus-free scale inhibitor in sewage containing high concentrations of calcium silicate and magnesium silicate components by reasonable compounding.

This application relates to a series of novel compounds that are selective inhibitors of phosphodiesterase type 9 ("PDE9") for the treatment of chronic heart failure. More particularly, the application relates to pyrazolo[3,4-d]pyrimidinone compounds for use in the treatment and prevention of chronic heart failure.

Provided is a type I crystal of a free base of 4-(4-(3-((2-(tert-butylamino)ethyl)amino)-6-(5-(trifluoromethyl)-1,3,4-oxadiazol-2-yl)pyridin-2-yl)piperidin-1-yl)-5,5-dimethyl-5H-pyrrolo[2,3-d]pyrimidin-6(7H)-one, which has peaks at, at least, 2 diffraction angles (2θ±0.2°) selected from the following (a), and at, at least, 2 diffraction angles (2θ±0.2°) selected from the following (b), in a powder X-ray diffraction spectrum (CuKα):(a) 6.2°, 9.3°, 9.7°, 11.1°, 15.4° and 25.1°; and(b) 6.7°, 8.3°, 8.7°, 13.0°, 13.7°, 16.3°, 16.9°, 17.7°, 18.7°, 19.4°, 20.3°, 25.9° and 26.5°.

This invention relates to the field of chemical synthesis, specifically to a malonate dithioester compound, its preparation method, and its uses. The structural formula of the malonate dithioester derivative of this invention is shown in Formula I. The malonate dithioester compound of this invention is more stable than malonyl chloride and has the advantage of higher reactivity than ordinary malonate ester derivatives, and can be used as an excellent intermediate for the synthesis of pyrido[1,2-α]pyrimidinone mesoionic compounds.

The present invention relates to compounds useful for modulating Triggering Receptor Expressed on Myeloid Cells-2 ("TREM2"). The invention also relates to the compounds for use in treatment of conditions related to loss of function of TREM2, such as neurodegenerative diseases, and to pharmaceutical compositions comprising the compounds.

The present invention provides a pyrimidinone-containing compound, a pharmaceutical composition thereof, and a use thereof. Specifically, disclosed is a compound as shown in formula (I) or a pharmaceutically acceptable salt thereof. The compound of the present invention has strong inhibitory activity against hNE, and the compound or the pharmaceutical composition thereof can be used for treating related diseases caused by an abnormal increase in neutrophil elastase.

The invention relates to the technical field of polymer composite materials, and discloses a composition for a polyurethane composite adhesive, the polyurethane composite adhesive and application of the polyurethane composite adhesive. The composition contains a component A and a component B, on the basis of the total mass of a raw material composition A forming the component A, the raw material composition A contains polyether polyol I, polyester polyol I and polyisocyanate; on the basis of the total mass of the raw material composition B forming the component B, the raw material composition B contains polyether polyol II, polyester polyol II, a chain extender and an auxiliary agent; the chain extender is a combination of a main chain UPy chain extender capable of enabling the main chain of the polymer to contain a ureido pyrimidone group and a side chain UPy chain extender capable of enabling the side chain of the polymer to contain a ureido pyrimidone group. The polyurethane composite adhesive provided by the invention is applied to a composite membrane for an asphalt waterproof coiled material, and can effectively prevent oxygen permeation, reduce the oxygen permeation rate and isolate oxygen.

The invention relates to the technical field of medicines, in particular to a substituted pyrimidinone compound or pharmaceutically acceptable salt thereof as well as a preparation method and application of the substituted pyrimidinone compound. The structure of the substituted pyrimidinone compound is shown as a formula (I) or a formula (II). The substituted pyrimidone compound provided by the invention shows a good inhibition effect on phosphodiesterase, can be applied as a phosphodiesterase type 1 inhibitor, and has an important medicinal value and a wide application prospect. In addition, the preparation method of the substituted pyrimidinone compound is simple and suitable for large-scale industrial production and application.

The application discloses a luminescent intelligent detection self-repairing supramolecular polyethylene fishing line coating and a preparation method thereof, and relates to the fields of fishing line functional coating and intelligent sensing technology.The coating core component comprises, by weight, 10-15 parts of a supramolecular matrix resin, 3-6 parts of a luminescent-sensing composite functional unit, 1-3 parts of an interface modifier, 0.5-2 parts of an auxiliary additive, and 60-80 parts of a solvent; the urea-based pyrimidone grafted polycaprolactone is used as the supramolecular matrix, and a rare earth complex and a long-afterglow material are used to construct the composite functional unit; and the coating adhesion is strengthened through plasma pretreatment and interface modification.The application synchronously realizes long-afterglow luminescence visualization, corrosion intelligent monitoring, efficient self-repairing and high wear resistance through multi-component cooperation and a step-by-step preparation process, solves the defects of single function, poor wear resistance and easy falling of traditional coatings, is suitable for night fishing, deep water fishing and other scenes, has simple and controllable process, and is suitable for large-scale production.

The application discloses a phenylpyridine salt derivative G, a room-temperature phosphorescent supramolecular gel and a preparation method and application thereof. The preparation method of the room-temperature phosphorescent supramolecular gel comprises the following steps: taking Cucurbit[8]uril (CB[8]) as a host, a phenylpyridine salt derivative containing a urea-based pyrimidone (UPy) quadruple hydrogen bond site as a guest, self-assembling a supramolecular assembly phosphorescent material in a 1:2 molar ratio in an aqueous solution; and introducing the assembly into a polyvinyl alcohol (PVA) matrix to obtain a humidity-responsive room-temperature phosphorescent supramolecular gel. The assembly and the supramolecular gel both present phosphorescent emission at room temperature. Under the dual constraints of macrocycle limitation and multiple hydrogen bonds on the phosphorescent molecules, the phosphorescent intensity and lifetime of the supramolecular gel are greatly enhanced compared with the assembly. Meanwhile, the phosphorescent intensity and the light-emitting color of the supramolecular gel change with the water content of the gel or the environmental humidity, realizing a visual response from green to blue, and the supramolecular gel can be applied to humidity sensing, anti-counterfeiting and information encryption.

The invention relates to the technical field of coating preparation, and particularly discloses a high-impermeability and high-strength water conservancy project coating and a preparation method thereof.The high-impermeability and high-strength water conservancy project coating is prepared from, by weight, 62-78 parts of epoxy resin prepolymer, 6-8 parts of diluent, 2.8-3.4 parts of flatting agent, 12-14 parts of modified filler, 1.6-2 parts of accelerant, 20-22 parts of curing agent and 0.8-1 part of photoinitiator; the epoxy resin prepolymer and the modified filler are added into the coating, and the epoxy resin prepolymer contains a ureido pyrimidone structure, a benzene ring and a pyrimidine ring, not only can participate in a curing reaction of epoxy resin, but also can be chemically bonded with the modified filler, so that the synergistic effect between the epoxy resin prepolymer and the modified filler can be brought into full play; the weather resistance, the anti-permeability and the mechanical property of the coating are obviously improved.

To provide a pyrimidone compound and a pharmaceutical composition thereof which can be used as Lp-PLA2 inhibitor for treating or preventing a diabetic complication, neuroinflammation-related disease, or atherosclerosis.SOLUTION: Disclosed herein are: a compound represented by general formula (I); a cis-trans isomer thereof, an enantiomer thereof, a diastereoisomer thereof, a racemate thereof, a solvate thereof, a hydrate thereof, or a pharmaceutically acceptable salt thereof, or a prodrug thereof; a preparation method therefor; a pharmaceutical composition comprising the compound; and the use of the compound as an Lp-PLA2 inhibitor.SELECTED DRAWING: None

The invention relates to application of a phenyl pyrimidone compound, in particular to application of the phenyl pyrimidone compound shown in a formula (I) or tautomers, pharmaceutically acceptable salts, solvates or isotope labels of the phenyl pyrimidone compound in preparation of drugs for improving or treating cognitive impairment and / or improving or treating brain vascular diseases. Through cell model and animal model test research, compared with a clinically available drug donepezil on the market and a clinically researched drug mironafil, the compound disclosed by the invention has remarkable treatment characteristics and substantive technical progress in the aspects of protecting nerve cells, improving cognitive impairment, improving brain vascular diseases, improving degenerative diseases such as Parkinson's disease and the like.

There are disclosed imidazolinopyrimidinone compounds that have activity to induce TRAIL gene expression in macrophages. There is further disclosed a method for treating various cancers comprising administering effective amounts of an imidazolinopyrimidinone having the structure of Formula I herein.

The present disclosure relates to 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-1,3,4,7-tetrahydro-2H-pyrrolo[3′,2′:5,6]pyrido[4,3-d]pyrimidin-2-one, solid forms and polymorphs thereof, methods of preparation thereof, and intermediates in the preparation thereof, which are useful in the treatment of the FGFR-associated or mediated diseases such as cancer.

The application belongs to the technical field of chemical medicine, and particularly relates to a kind of 2,3-dihydropyrimidino [4,5-d] pyrimidine-4 (1H) -ketone derivatives and preparation method and purposes thereof.The existing Wee1 small molecule inhibitors still have one or more defects in activity, safety or pharmacokinetic properties, and a new generation of Wee1 small molecule inhibitors with novel structure, low toxicity, high efficiency and excellent pharmacokinetic properties needs to be developed.The application provides a kind of 2,3-dihydropyrimidino [4,5-d] pyrimidine-4 (1H) -ketone derivatives, specifically including 95 new compounds, or pharmaceutically acceptable salt thereof, or stereoisomer thereof.Experiments show that the compound of formula (I) disclosed in the application has good inhibitory activity on Wee1, and therefore the compound of the application can be used for treating diseases caused by abnormal Wee1 activity.

The application belongs to the technical field of membrane separation, and particularly relates to an alkali-resistant membrane for paper pulp waste liquid treatment and a preparation method thereof. The alkali-resistant membrane for paper pulp waste liquid treatment is a nanofiltration membrane, which comprises a base film and a functional layer. The functional layer is obtained by polymerization reaction of a cationic urea-based pyrimidone monomer containing a double bond and 1-vinylimidazole. The alkali-resistant membrane for paper pulp waste liquid treatment provided by the application has high water flux, lignin retention rate and cellulose retention rate, and still has high water flux, lignin retention rate and cellulose retention rate after being soaked in paper pulp waste liquid with a pH of 14 for 3 months.