222 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.

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 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 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.

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 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.

5, 6, 7, 8-tetrahydro-1, 6-naphthyridines and derivatives thereof, which are substituted in the 6 position with 6, 7-dihydro-5H-pyrrolo [3, 4-b] pyridin-5-one, furo [3, 4-b] pyridin-5 (7H)-one, 6, 7-dihydro-5H-cyclopenta [b] pyridin-5-one, or [1, 2, 4] triazolo [4, 3-a] pyrimidine-3 (2H)-one, are positive allosteric modulators of muscarinic acetylcholine receptor M4 (mAChR M4), and can be used for treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction.

The present invention provides a method for obtaining a 5-fluoro-4-imino-3-methyl-1-(phenyl-4-sulfonyl)-3, 4-dihydro-1H-pyrimidin-2-one of the formula (I), which is characterized in that the 5-fluoro-4-imino-3-methyl-1-(phenyl-4-sulfonyl)-3, 4-dihydro-1H-pyrimidin-2-one has a general formula (I), wherein R is hydrogen, an alkyl group, an alkenyl group, an alkynyl group, an alkoxy group, a halogenated alkyl group, a halogenated alkoxy group, an alkylthio group, a halogenated alkylthio group, an amino group, an alkylamino group, a dialkylamino group, an alkoxycarbonyl group, an alkylcarbonyl group, a hydroxyalkyl group, an ester, a haloid acid,-SH,-OH,-NH2,-NO2,-CN or CF3.

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.