279 results about "Pyrimidone" patented technology

The invention relates to a self-repairing high-mechanical-property film and a preparation method and application thereof, and the preparation method comprises the following steps: adding ureido pyrimidone and a chain extender into a solvent to obtain a mixed solution, adding the mixed solution into a polyurethane prepolymer, reacting, and drying to obtain the self-repairing high-mechanical-property film. UPy containing hydrogen bonds is introduced into the polymer to prepare the self-repairing high-mechanical-property film, and the hydrogen bond density can be adjusted by adjusting the UPy content of ureido pyrimidone, so that the composite material has excellent self-healing property; and density hydrogen bonds are introduced to construct a physical cross-linked network, so that the mechanical properties of the composite material can be remarkably improved.

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.

An advantageous isolated morphic form of trilaciclib which is 2′-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7′,8′-dihydro-6′H-spiro[cyclohexane-1,9′-pyrazino[1′,2′:1,5]pyrrolo[2,3-d]pyrimidin]-6′-one, for example in the form of a dihydrochloride salt or a dihydrochloride, dihydrate.

The present disclosure provides crystalline and amorphous forms of 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(2-propanyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(2-propenoyl)-1-piperazinyl)pyrido[2,3-d]pyrimidin-2(1H)-one, including several anhydrous, hydrate and solvate forms, and solid state forms thereof, pharmaceutical compositions, and methods of treating a disease mediated by KRAS G12C inhibition.

An advantageous isolated morphic form of trilaciclib which is 2′-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7′,8′-dihydro-6′H-spiro[cyclohexane-1,9′-pyrazino[1′,2′:1,5]pyrrolo[2,3-d]pyrimidin]-6′-one, for example in the form of a dihydrochloride salt or a dihydrochloride, dihydrate.

An advantageous isolated morphic form of trilaciclib which is 2′-((5-(4-methylpiperazin-1-yl)pyridin-2-yl)amino)-7′,8′-dihydro-6′H-spiro[cyclohexane-1,9′-pyrazino[1′,2′:1,5]pyrrolo[2,3-d]pyrimidin]-6′-one, for example in the form of a dihydrochloride salt or a dihydrochloride, dihydrate.

The invention discloses a novel PARP / CK2 double-target kinase inhibitor small molecule as well as a pharmaceutical composition and application thereof, the small molecule takes benzofuran pyrimidone as a parent drug effect ring and a benzene ring as a connector in drug design, and is coupled with a 1-amino-2-methylisothiourea group, so that the novel PARP / CK2 double-target kinase inhibitor is obtained. The compound has good inhibitory activity on exogenous PARP enzyme, exogenous CK2 alpha enzyme and proliferation activity of various cancer cells, and can be used for preparing antitumor drugs. # imgabs0 #

Disclosed in the present application are a pyridopyrimidinone compound, and a preparation method therefor and the use thereof, wherein the pyridopyrimidinone compound, or a racemate, R-isomer, S-isomer, pharmaceutically acceptable salt thereof or a mixture thereof has a structure as shown in formula (I). The pyridopyrimidinone compound provided by the present application has an agonistic effect on an HsClpP protease, and can be used for treating diseases related to HsClpP receptor activation.

The invention discloses a warp-resistant mineral reinforced PC / PBT alloy material with dimensional stability and a preparation method thereof, and relates to the technical field of polymer composite materials. The preparation method comprises the following steps: weighing polycarbonate, polybutylene terephthalate, ureido pyrimidone-polydimethylsiloxane, epoxy polyhedral oligomeric silsesquioxane, polyimide coated halloysite nanotubes, magnesium-aluminum hydrotalcite, perfluoroalkyl modified boron nitride nanosheets, liquid crystal polymer microfibers, modified PVA (Polyvinyl Alcohol) fibers and a silane coupling agent KH550 according to a ratio; the preparation method comprises the following steps: pre-mixing polycarbodiimide and a composite antioxidant to obtain a mixture, mixing, adding into a double-screw extruder, extruding and granulating, drying, carrying out injection molding, and standing at constant temperature and constant humidity to obtain the composite material. The invention has the significance of providing the PBT / PC alloy material with dimensional stability, warping resistance, low shrinkage rate, low hygroscopicity, creep resistance, impact resistance, arc resistance and chemical corrosion resistance for consumer-grade and industrial-grade underwater plastic parts.

The present disclosure provides crystalline and amorphous forms of 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(2-propanyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(2-propenoyl)-1-piperazinyl)pyrido[2,3-d]pyrimidin-2 (1H)-one, including several anhydrous, hydrate and solvate forms, and solid state forms thereof, pharmaceutical compositions, and methods of treating a disease mediated by KRAS G12C inhibition.

The present disclosure provides crystalline and amorphous forms of 6-fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-(2-propanyl)-3-pyridinyl)-4-((2S)-2-methyl-4-(2-propenoyl)-1-piperazinyl)pyrido[2,3-d]pyrimidin-2(1H)-one, including several anhydrous, hydrate and solvate forms, and solid state forms thereof, pharmaceutical compositions, and methods of treating a disease mediated by KRAS G12C inhibition.

The invention provides a monomer and a preparation method thereof, a gel electrolyte precursor, a gel electrolyte, a battery and electric equipment. The monomer disclosed by the invention has a structure of a formula 1 # imgabs0 #, the monomer disclosed by the invention has an acrylate fragment and a ureido pyrimidone fragment, unsaturated carbon-carbon double bonds in the acrylate fragment can be subjected to in-situ polymerization to form a polymer network structure, and flowing electrolyte is bound in the network; and the ureido pyrimidone can realize physical cross-linking and perform self-healing repair on the gel network through multi-hydrogen-bond interaction, so that the liquid retention reliability of the battery is effectively improved, the liquid leakage risk is reduced, and the safety performance of the battery is enhanced.

The invention relates to the technical field of functional materials, in particular to a supramolecular aggregate modified vinyl resin material and a preparation method thereof. The supramolecular aggregate modified vinyl resin material is prepared from the following raw materials in parts by weight: 1.3 to 4.6 parts of aliphatic isocyanate monomer, 5 to 15 parts of micromolecular polyol, 0.8 to 2.9 parts of ureido pyrimidone monomer, 1 to 3 parts of curing agent, 50 to 100 parts of vinyl resin and 0.5 to 2.3 parts of accelerant, so that the modified vinyl resin material has reversible dynamic mechanical property; good damping vibration attenuation performance can be provided; and the material has good mechanical properties and excellent impact toughness, and can be widely applied to various fields as a high-performance functional material.

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 invention provides polyurethane serving as a hot melt adhesive and alcosol water as well as a preparation method and application thereof, and relates to the technical field of polyurethane binders. The preparation method comprises the following steps: mixing polydihydric alcohol, diisocyanate, an organic solvent and a catalyst to carry out polymerization reaction, and then mixing with chain extenders (dihydric alcohol containing 2-ureido-4-pyrimidone groups and dihydric alcohol containing bipyridine groups) to carry out chain extension reaction to obtain polyurethane. According to the invention, 2-ureido-4-pyrimidone and dipyridyl groups are introduced into a macromolecular chain of polyurethane, and a formed hydrogen bond can provide strong intermolecular cohesion in the adhesive, so that the strength of the material is improved, and the adhesive force with the surface of a base material can be enhanced; the bipyridine group can form a chelating structure with metal ions on the surface of a metal substrate, so that the bonding strength with the metal substrate is enhanced. According to the invention, a single polyurethane material has dual functions of hot-melt bonding and normal-temperature green solvent bonding, and has excellent bonding performance and milder bonding conditions.

The use of a combination of a pyrido[2,3-d]pyrimidin-2(1H)-one derivative and an anti-PD-1 or anti-PD-L1 antibody and / or a chemotherapeutic drug in the preparation of a drug for preventing or treating a tumor disease.

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 invention discloses an application of a tetrahydropyridopyrimidinone compound with a structural characteristic shown in a formula (I) or pharmaceutically acceptable salt, hydrate or crystal form thereof in treatment of human casein lyase (HsClpP) mediated diseases, and belongs to the field of chemical medicines. The technical problem to be solved by the invention is to provide the tetrahydropyridinopyrimidinone compound. The imidazolidine derivative is characterized by having a tetrahydropyridinopyrimidinone skeleton structure, and nitrogen atoms on an imidazolidine ring are connected with other substituent groups. The compounds have obvious activity of regulating and controlling HsClpP, and can be used for treating HsClpP-mediated related diseases.

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.

A fungicidal composition containing a fungicidally effective amount of the compound of Formula I:5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide to provide synergistic control of selected fungi wherein the at least one fungicide is a multi-site inhibitor or a strobilurin inhibitor.

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.

Process for preparing an enantiomerically enriched form of 2-[2-(2-chlorothiazol-5-yl)-2-hydroxy- ethyl]sulfanyl-6-hydroxy-3-methyl-5-phenyl-pyrimidin-4-one (compound (I)) or a tautomer thereof which comprises reducing 2-[2-(2-chlorothiazol-5-yl)-2-oxo-ethyl]sulfanyl-6-hydroxy-3-methyl-5- phenyl-pyrimidin-4-one (compound (II)) with a silane compound in the presence of a chiral zinc compound.

The invention relates to a solid dispersion of a triazolopyrimidine derivative with tankyrase inhibitory activity and a preparation method of the solid dispersion. The solid dispersion of the triazolopyrimidone derivative represented by chemical formula I according to the present invention has high solubility and excellent bioavailability, and thus can be usefully used as a pharmaceutical raw material.

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 specifically, this application relates to pyrazolo[3,4-d]pyrimidinone compounds for use in the treatment and prevention of chronic heart failure.

The application provides a preparation method of 2-aminopyridopyrimidinone compounds, which comprises the following steps: reacting 2-bromo-N-phenyl nicotinamide compounds and monocyanoamine in an organic solvent in the presence of alkali to obtain 2-aminopyridopyrimidinone compounds. The method has the advantages of no metal catalysis, mild reaction conditions, high atom economy, wide substrate applicability and simple operation, and has important application value in the fields of medicinal chemistry and organic synthesis.

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 discloses application of benzofuran pyrimidone or benzothiophene pyrimidone compounds, and belongs to the technical field of medicinal chemistry. The compound provided by the invention can be used as a PARP-1 and / or CK2 alpha double-target inhibitor. The compound is obtained by taking benzofuran pyrimidinone or benzothiophene pyrimidinone as a mother nucleus and taking a benzene ring or pyridine as a connecting body and coupling 1-amino-2-methyl isothiourea groups, can effectively inhibit PARP-1 enzyme activity, CK2 alpha enzyme activity and proliferation of various cancer cells, and has good potential of being developed into anti-tumor drugs.