2808 results about "Pyrimidine" patented technology

Provided are compounds of Formula I:nucleosides, nucleoside phosphates and prodrugs thereof, wherein R6 is CN, ethenyl, 2-haloethen-1-yl, or (C2-C8)-alkyn-1-yl. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections.

Provided are a pyrimidine polycyclic derivative inhibitor, a preparation method therefor and the use thereof. In particular, provided are a compound as shown in the general formula, a preparation method therefor, a pharmaceutical composition comprising the compound, and the use thereof in the treatment of cancers and other related diseases.

The present disclosure relates generally to methods for treating or preventing central nervous system (CNS) metastases with a KRAS inhibitor, and more specifically to treating CNS metastases with a pyridopyrimidine derivative.

The present invention relates to a KRASG12D inhibitor and the use thereof. Specifically, provided in the present invention is a compound as shown in formula (I), and the definition of each substituent in the formula is as described in the description. In addition, the present invention further relates to a composition containing the inhibitor and the use thereof. The compound of the present invention has good tumor growth inhibitory activity, and has good safety.

The present invention belongs to the technical field of medicinal chemistry, and particularly relates to a pyrimidine macrocyclic compound. The compound has a good inhibitory effect on KRAS mutations, has a good inhibitory effect on the G12V mutation and other types of mutations of the KRAS gene, can be used as a general KRAS inhibitor, and can be used for the treatment of tumors driven by KRASG12V and other types of gene mutations.

Provided are a crystal form of a pyridopyrimidine derivative, a preparation method therefor, a pharmaceutical composition thereof and the use thereof. Specifically disclosed are a crystal form of a compound of formula (I), a preparation method therefor, a pharmaceutical composition thereof and the use thereof.

The present disclosure relates generally to methods for treating cancer with a KRAS inhibitor in combination with an immune checkpoint inhibitor, and more specifically to treating cancer with a pyridopyrimidine derivative in combination with a PD-1 or PD-L1 inhibitor.

Methods for treating prostate cancer, including advanced prostate cancer, in a subject in need thereof, include administering once-daily to the subject, at least 80 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof. Another method includes: administering once-daily to the subject in need thereof, an oral load dose formulation having from 240 mg to 480 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof, and thereafter administering once-daily to the subject, an oral maintenance dose formulation having 80 mg to 160 mg of N-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-N′-methoxyurea, or a corresponding amount of a pharmaceutically acceptable salt thereof.

The present disclosure relates generally to polymorphic forms of a KRAS inhibitor, and more specifically to polymorphic forms of a pyridopyrimidine derivative, and uses thereof.

The invention provides a pyrimidino heterocyclic compound as well as a pharmaceutical composition and application thereof. The invention provides a pyrimidino heterocyclic compound as shown in a formula I, and a stereoisomer, a tautomer, an atropisomer or a pharmaceutically acceptable salt of the pyrimidino heterocyclic compound. The compound disclosed by the invention has good proliferation inhibition activity on NCI-H358 cells, AsPC-1 cells and Capan-1 cells containing KRAS mutation, and has relatively weak proliferation inhibition activity on PC-9 cells wild in KRAS. # imgabs0 #

The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

The invention relates to a pyrimidine-containing polybasic ring derivative inhibitor as well as a preparation method and application thereof. In particular, the invention relates to a pyrimidine-containing multi-element fused ring compound or a stereoisomer thereof, a preparation method thereof, a pharmaceutical composition containing the compound, and an application of the compound or the stereoisomer thereof in preparation of drugs for treating cancers and other related diseases.

The invention belongs to the technical field of pesticides, and particularly relates to a mesoionic pyrimidinium compound, and an N-oxide or salt and application thereof. The compound is shown as a general formula I: # imgabs0 #, wherein X represents a cyano group, a cyano alkyl group, an aryl group or a heterocyclic group; q1 and Q2 independently represent O or S respectively; m1, M2, M3, M4 and M5 respectively and independently represent CR9 or N, and at least two of the M1, M2, M3, M4 and M5 are N; r1, R2, R3, R4, R5, R6, R7, R8 and R9 independently represent hydrogen, nitro, amino, cyano, halogen and the like respectively. The compound has excellent prevention and control effects on pests such as chilo suppressalis, spodoptera frugiperda, armyworm, prodenia litura, peanut aphid and rice planthopper, and is safe to bees.

The present disclosure relates generally to polymorphic forms of a KRAS inhibitor, and more specifically to polymorphic forms of a pyridopyrimidine derivative, and uses thereof.

Provided is a method for treating and / or preventing of cancer using Compound A or a pharmaceutically acceptable salt thereof.

The invention provides a dihydropyrimidinase mutant, a related product of the dihydropyrimidinase mutant and application of the dihydropyrimidinase mutant in production of a medical intermediate (R)-3-(carbamylmethyl)-5-methylhexanoic acid or an analogue of the (R)-3-(carbamylmethyl)-5-methylhexanoic acid. It is found for the first time that wild type dihydropyrimidinase shown in SEQ ID NO: 1 and a dihydropyrimidinase mutant modified by the wild type dihydropyrimidinase can effectively catalyze a substrate to generate a medical intermediate (R)-3-(carbamylmethyl)-5-methylhexanoic acid; particularly, compared with wild type dihydropyrimidinase, the dihydropyrimidinase mutant has the advantages that the dihydropyrimidinase activity is remarkably improved, the organic solvent tolerance and the high-temperature tolerance are relatively high, and the stereoselectivity of a product obtained by catalysis of the dihydropyrimidinase mutant is relatively high; therefore, the (R)-3-(carbamylmethyl)-5-methylhexanoic acid or the analogue thereof can be produced at lower cost and higher efficiency, and the method has higher industrial value.

The invention belongs to the technical field of pesticides, and particularly relates to a pyridyl alkoxy pyrimidine compound and application thereof. The compound is shown as a formula I: # imgabs0 #, wherein X and Y respectively and independently represent hydrogen, hydroxyl, alkyl, alkoxy, alkenyloxy, alkynyloxy and the like; z represents hydrogen, halogen, a cyano group, an amino group, a nitro group, a formyl group, a cyano alkyl group, a hydroxyalkyl group, an alkyl group, an alkenyl group, an alkynyl group and the like. The compound or the salt thereof has an excellent effect as an agricultural and horticultural insecticide.

The invention provides a preparation method of a high-adhesion transparent self-healing super-smooth coating. Polydimethylsiloxane is taken as a matrix, a three-arm type dynamic hydrogen bond network structure is constructed, and 2-ureido-4-pyrimidone (UPy unit) is taken as a crosslinking node to be connected with a siloxane main chain, so that the crosslinking density and the interface binding energy are remarkably improved. According to the invention, a UPy unit is innovatively introduced into a main chain or a side chain to construct two topological structures of (SUP) 2TD or (MUP) 2TD. Compared with (MUP) 2TD, the (SUP) 2TD shows excellent tensile property and self-healing property in both air and underwater environments. The enhancement of this performance is attributed to the improvement of chain displacement capability in (SUP) 2TD. Through interface dynamics, a UPy unit is guided to an interface and interacts with an interface group, and a very strong adhesion effect is obtained. In addition, the coating shows excellent self-healing performance.

Provided herein is a process for preparing compound A comprising (a) admixing 2-isopropyl-4-methylpyridin-3-amine (Compound B), or a salt thereof, a first base, and a reactive compound comprising phosgene or a phosgene equivalent in an organic solvent to form 3-isocyanato-2-isopropyl-4-methylpyridine (Compound C); (b) admixing Compound C and 2,6-dichloro-5-fluoronicotinamide (Compound D) to form 2,6-dichloro-5-fluoro-N-((2-isopropyl-4-methylpyridin-3-yl)carbamoyl)nicotinamide (Compound E); and (c) admixing Compound E and a second base to form a product mixture comprising Compound A and the second base. Also provided herein is a process for synthesizing AMG 510 comprising using Compound A prepared according to the disclosed processes

The invention discloses collagen polypeptide firming and anti-wrinkle freeze-dried powder, and relates to the technical field of cosmetics. The invention relates to a biological preservative which is prepared from water, butanediol, a bacillus / soybean fermentation product extract, soluble collagen, acetyl hexapeptide-8, panthenol, 1, 2, 4-trimethyl-1, 3-pentanediol and a proper amount of water. The cosmetic is prepared from 1, 2-hexanediol, tetrahydromethylpyrimidine carboxylic acid, hydroxypropyl tetrahydropyrantriol, tremella polysaccharide, saccharide isomeride, a bifidus yeast fermentation product lysate, sodium hyaluronate, DNA sodium, a radix gentianae extract, mannitol, palmitoyl tripeptide-1, palmitoyl tetrapeptide-7, oligopeptide-1, decapeptide-4, oligopeptide-3, hydrolyzed royal jelly protein, folic acid and disodium hydrogen phosphate. The additive is composed of sodium dihydrogen phosphate, citric acid and sodium citrate. The mask can provide rich nutrients for skin, deeply care the skin, moisturize and relieve the skin, tighten the skin, resist wrinkles and make the skin moisturized, glossy, elastic and tight, and is high in use safety and wide in application prospect.

The invention belongs to the technical field of pesticides, and particularly relates to a mesoionic pyrimidinium compound, and an N-oxide or salt and application thereof. The compound is shown as a general formula I, wherein X1 and X2 respectively and independently represent hydrogen, halogen, cyano, hydroxyl, amino, alkyl or halogenated alkyl; y1, Y2, and Y3 each independently represent hydrogen, halogen, or the like; q1 and Q2 respectively and independently represent CH2, O or S, and at least one of Q1 and Q2 is O; r1 and R2 respectively and independently represent halogen. The compound has an excellent prevention and treatment effect on pests such as spodoptera frugiperda and armyworm.

The invention belongs to the technical field of pyrimidine [1, 2-b] indazole derivative synthesis, and particularly relates to a fluoro pyrimidine [1, 2-b] indazole compound and a preparation method thereof. The preparation method specifically comprises the following steps: by taking an enamine compound as shown in a formula 1, heteroarylamine as shown in a formula 2 and polyfluoroalkyl halide as shown in a formula 3 as reaction substrates, mixing the reaction substrates, a catalyst and a solvent, and carrying out cyclization reaction in a protective gas atmosphere and under blue light irradiation to obtain the fluoropyrimidine [1, 2-b] indazole compound. The fluorine atom substituted or multi-fluoroalkyl substituted pyrimidine [1, 2-b] indazole derivative can be selectively constructed in the same reaction system, the diversity of the structure is obviously expanded, and the reaction conditions are mild and green and environment-friendly.

The invention relates to the technical field of membrane separation, in particular to a preparation method of a pH-step-by-step thermocuring regulation sodium-magnesium separation nanofiltration membrane. The method comprises the following steps: (1) pre-treating a base membrane; (2) preparation and treatment of an aqueous phase solution: S1, preparing the aqueous phase solution according to mass fraction: sequentially adding 1.2%-1.6% of piperazine, 0.10%-0.14% of triaminopyrimidine and 0.14%-0.18% of polyethylene glycol into deionized water, and stirring until the piperazine, the triaminopyrimidine and the polyethylene glycol are completely dissolved to form the aqueous phase solution; s2, adjusting the pH value of the water-phase solution to 10-11 by using hydrochloric acid; s3, pouring the water-phase solution of which the pH is adjusted on the surface of the pretreated base membrane, standing, and blow-drying to form a uniform water-phase layer; (3) interfacial polymerization reaction: S1, preparing an oil phase solution: adding 0.10-0.14% of trimesoyl chloride into n-hexane, and performing ultrasonic treatment until the trimesoyl chloride is completely dissolved; s2, pouring the oil-phase solution on the surface of the base membrane subjected to water-phase treatment, and after reaction, pouring out redundant solution to form a polyamide separation layer, so as to obtain a membrane sheet; (4) performing a step-by-step thermocuring process; and (5) cleaning and storing.

The invention belongs to the technical field of pesticides, and particularly relates to a mesoionic pyrimidinium compound, and an N-oxide or salt and application thereof. The compound is shown as a general formula I, wherein Q1 and Q2 respectively and independently represent O or S; x represents a cyano group, a cyano alkyl group, an aryl group or a heterocyclic group; y1 is halogen; y2 and Y3 each independently represent hydrogen, halogen, alkyl, or the like; and Z1, Z2, R1, R2, R3, R4, R5, R6, R7 and R8 independently represent hydrogen, halogen, cyano, nitro, alkyl and the like. The compound has an excellent prevention and treatment effect on pests such as spodoptera frugiperda, armyworm and prodenia litura.

The invention provides a perovskite solar cell, a preparation method thereof and a photovoltaic module. The perovskite solar cell comprises a first electrode, a hole transport layer, a perovskite layer, an electron transport layer and a second electrode which are stacked in sequence. The material of the hole transport layer comprises a biomolecular material which is fixed on a self-assembly monomolecular layer material through an intermolecular force, and the biomolecular material comprises one or more of guanine, adenine, thymine, uracil, cytosine, hydroxymethylcytosine, xanthine, hypoxanthine, 6-mercaptopurine and corrin. According to the perovskite cell provided by the invention, the biomolecular material with a plurality of nitrogen heterocyclic structures and amino groups is added to generate multipoint hydrogen-bond interaction and pi-pi accumulation with the tail end of the SAM, so that the orderliness of molecular arrangement is improved, and the dipole direction and strength of the whole interface are regulated and controlled; and a coordination bond or hydrogen bond network is formed by the coordination compound and uncoordinated cations or anions in perovskite, so that interface defects are effectively passivated, and the thermal stability and the humid and hot life of a device are enhanced.

Disclosed are a pyrrolopyrimidine compound and a use thereof in preparing a medicine for diseases related to a BTK protein kinase inhibitor. Specially, disclosed are a compound as shown in formula (III) and a pharmaceutically acceptable salt thereof.

The invention relates to a pyrimidyl full-conjugated structure covalent organic framework material, a catalyst containing the pyrimidyl full-conjugated structure covalent organic framework material and a preparation method and application thereof. The preparation method of the pyrimidyl full-conjugated structure covalent organic framework material comprises the following steps: (1) dissolving an aldehyde precursor and a methyl precursor containing a bipyrimidine structure in an organic mixed solvent, fully dispersing, and adding a catalyst to obtain a mixed solution; the organic mixed solvent is composed of mesitylene, 1, 4-dioxane and acetonitrile, and the catalyst is trifluoroacetic acid; (2) sequentially carrying out liquid nitrogen freezing-vacuumizing-unfreezing cyclic operation, vacuum sealing and secondary unfreezing on the obtained mixed solution to room temperature, and reacting at the temperature of 120-150 DEG C to obtain a crude product; and (3) deblocking the reaction system of the obtained crude product, and then carrying out solid-liquid separation, washing, Soxhlet extraction and drying to obtain the pyrimidyl covalent organic framework material with the fully conjugated structure.

The invention provides a uracil production strain and a construction method and application thereof.According to the strain, on an E.coli UR14 genome by means of a CRIPSR / Cas9 gene editing technology, firstly, psuG genes, preTA genes, rutA genes and upp genes are knocked out, so that decomposition of uracil is blocked; then, a uridine phosphorylase gene udp and a pyrimidine-5 '-nucleotide nucleotidase gene ppnN are subjected to overexpression, and synthesis and accumulation of uracil are synergistically enhanced; and finally, overexpression of the ribose phosphate mutase gene pgm further enhances the conversion of a by-product ribose phosphate 1-precursor 5-ribose phosphate 1-pyrophosphate and improves the carbon utilization rate, and the obtained strain has good genetic stability and high fermentation yield, can stably produce uracil, and has wide application prospects.