2008 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.

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 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.

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 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 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.

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.

The present invention relates to compounds that inhibit at least one of KRas wild type, KRas G12A, KRas G12C, KRas G12D, KRas G12R, KRas G12S, KRas G12V, KRas G13D and KRas Q61H, pharmaceutical compositions comprising the compounds and methods of use therefor.

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, Y2, Y3, Z1, Z2, R1, R2, R3, R4, R5, R6, R7, and R8 independently represent hydrogen, halogen, a cyano group, a nitro group, an alkyl group, etc. The compound has an excellent prevention and treatment effect on pests such as spodoptera frugiperda, armyworm and prodenia litura.

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 X and Z respectively and independently represent hydrogen, alkyl, alkenyl, alkynyl, naphthenic base and the like; y represents chlorine or bromine. The compound has an excellent prevention and treatment effect on pests such as spodoptera frugiperda, armyworm and prodenia litura.

Provided herein are inhibitors of KRAS, pharmaceutical compositions comprising the inhibitory compounds, and methods for using the KRAS inhibitory compounds for the treatment of diseases or disorders.

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; y represents hydrogen, an alkyl group, an alkenyl group, an alkynyl group 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 present invention belongs to the technical field of pesticides and specifically relates to a substituted pyrazole compound containing pyrimidine and a use thereof. The compound is represented by general formula I: where Q represents an aryl group or a heterocyclic group; Y1 and Y2 each independently represent hydrogen, alkyl, or the like; R1 and R2 each independently represent hydrogen, halogen, nitro, or the like; R3 represents hydrogen, alkyl, or the like; R4, R5, R6, and R7 each independently represent hydrogen, alkyl, or halogenated alkyl; and R8 and R9 each independently represent hydrogen, halogen, cyano, alkyl, or the like. The described compound exhibits good control activity against fungi, etc.

Described herein is a topical formulation. The topical formulation includes a thymine-thymine compound including Formula (1) and a solvent system. The topical formulation includes about 0.01 wt% to about 10 wt% of the thymine-thymine compound, based on total weight of the formulation. A method of preparing the topical formulation is also provided.

The invention discloses a preparation method of alplsutentan and an alplsutentan intermediate, alplsutentan is obtained by taking a compound SM1 as a raw material through a one-step method or a multi-step method, and the multi-step method comprises the following steps: reacting the compound SM1 with a compound SM2 to obtain an intermediate I; reacting the intermediate I with 2-[(5-bromo-2-pyrimidinyl) oxy] ethanol to obtain an intermediate II, or reacting the intermediate I with ethylene glycol to obtain an intermediate I-b, and then reacting with 5-bromo-2-chloropyrimidine or 5-fluoro-2-chloropyrimidine to obtain the intermediate II; and finally, removing a protecting group from the intermediate II to obtain alpoxivan. The one-step method comprises the following steps: when X in a compound SM1 is a fluorine atom, the compound SM1 is 5-(4-bromophenyl)-4, 6-difluoropyrimidine, and the compound SM1 reacts with sulfonamide and 2-[(5-bromo-2-pyrimidinyl) oxy] ethanol to directly obtain alpoxivan. The synthesis route is short, and the reaction conditions are mild.

The invention provides an anti-hair-loss and hair-growing product containing plant extract components and a preparation method thereof, and relates to the field of wash supplies, the anti-hair-loss and hair-growing product is prepared from the following raw materials by weight: 50-80 parts of water, 5-10 parts of propylene glycol, 1-5 parts of 1, 3-propylene glycol, 1-5 parts of 1, 3-propylene glycol, and 1-5 parts of 1, 3-propylene glycol. The composition is prepared from the following components in parts by weight: 0.1 to 1 part of 1, 2-pentanediol, 0.1 to 1 part of pyrrolidinyl diaminopyrimidine oxide, 0.1 to 0.5 part of diaminopyrimidine oxide, 0.01 to 0.02 part of caffeine, 0.01 to 0.1 part of adenosine, 0.05 to 0.2 part of vitamin B6, 0.01 to 0.5 part of biotin tripeptide-1, 0.1 to 1 part of dipotassium glycyrrhizinate, 0.02 to 0.05 part of ethylenediamine tetraacetic acid, 0.1 to 1 part of D panthenol, 0.2 to 1 part of p-hydroxyacetophenone, 0.01 to 1 part of 1, 2-pentanediol, 0.1 to 1 part of 1, 2-pentanediol, 0.1 to 1 part of 2, 2-pentanediol, 0.1 to 1 part of 2, 2-pentanediol, 0.1 to 1 part of 2, 2- The composition comprises the following components in parts by weight: 1-2 parts of 1, 2-hexanediol, 0.1-0.5 part of citric acid, 1-2 parts of 1, 3-butanediol, 0.01-1 part of NMN and 3-5 parts of a plant extract. According to the present invention, the extraction method of the plant extract in the raw materials is specifically adjusted so as to significantly reduce the content of the pigment and the odor substance in the extract, such that the obtained hair growing liquid has characteristics of good hair growing effect, light color and light drug taste, can be easily accepted by consumers, and is suitable for large-scale promotion and application.

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.

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 invention relates to a pyrrolo [2, 3-d] pyrimidine-4-amine derivative and application thereof in medicine, in particular to a compound shown in a formula (I) or a stereoisomer, a tautomer, a deuterated compound, a solvate, a prodrug, a metabolite, pharmaceutically acceptable salt or eutectic of the compound, and application of the compound in preparation of medicines for treating sGC-related diseases.

The invention belongs to the technical field of biological medicines, and particularly discloses an alkynyl pyrimidine derivative as well as a preparation method and application thereof. The structure of the alkynyl pyrimidine derivative is shown as a formula I. The novel alkynyl pyrimidine derivative capable of efficiently inhibiting the LSD1 activity is provided, the preparation process is simple and easy to implement, the good effect of resisting colorectal cancer cell proliferation is shown on the animal level, and safe and effective candidate drug molecules are provided for targeted therapy of colorectal cancer.

The invention relates to a specific PET molecular probe of a targeted KRASG12D mutant as well as a preparation method and application of the specific PET molecular probe. Pyridopyrimidine compounds and R5 are subjected to cooling reaction under the action of N, N-diisopropylethylamine to generate a compound 2; the compound 2 and (2-fluorotetrahydro-1H-pyrrolizine-7A (5H)-yl) methanol are subjected to a heating reaction under the action of N, N-diisopropylethylamine, and a compound 3 is generated; carrying out heating reaction on the compound 3 and biphenyl boronic acid pinacol ester under the action of N, N-diisopropylethylamine and tetrakis (triphenylphosphine) palladium to generate a compound 4; carrying out heating reaction on the compound 4 and 1, 2-bis (tolyloxy) alkane under the action of potassium carbonate to generate a compound 5; the compound 5, radioisotope < 18 > F and an anion complexing agent are subjected to a heating reaction under the action of potassium carbonate to generate the trisubstituted pyridopyrimidine < 18 > F labeled PET molecular probe. Compared with the prior art, the kit has a positioning diagnosis effect on KRASG12D mutant tumors, and image typing of mutant and non-mutant tumors and pathological evaluation after tumor treatment are realized at the same time.

The present disclosure relates to pyrrolo-pyrimidine compounds, or pharmaceutically acceptable salts thereof, of Formula (I"): Compounds of the disclosure are useful for degrading cyclin-dependent kinase 4 (CDK4), and methods of making the same are provided.

The invention discloses a low-foam acidic zinc plating additive and a preparation process thereof, and belongs to the technical field of electroplating additives, the additive comprises a low-foam softening agent and a water-based brightener, and the low-foam softening agent comprises the following raw materials in percentage by mass: 0.8-1.2% of polyethyleneimine, 0.03-0.06% of monododecyl phosphate potassium, 0.2-0.6% of water-soluble polyether amine and the balance of water. The water-based brightener is prepared from the following raw materials: 0.6 to 1.2 percent of 5-hydroxymethylfurfural, 0.2 to 0.4 percent of L-cysteine salt, 0.1 to 0.15 percent of 4-amino-2 (1H) pyrimidone, 0.05 to 0.1 percent of sodium salicylate, 1 to 1.5 percent of citric acid, 0.3 to 0.5 percent of alpha-ketoglutaric acid, 0.2 to 0.4 percent of erythorbic acid and the balance of water. The water-based formula is prepared by optimizing the components in the additive, the components are uniformly dispersed, the foam amount is low, and the plating quality is good.

The invention discloses a synthesis method of 2 '-fluoro-2'-deoxyguanosine. According to the method, thymine nucleoside phosphorylase and purine nucleoside phosphorylase are used as biocatalysts, and 2 '-fluoro-2'-deoxyuridine and guanine are used as substrates to synthesize the 2 '-fluoro-2'-deoxyguanosine. Compared with a chemical method, the production cost is greatly reduced; meanwhile, the synthesis method can effectively solve the problem that the product is difficult to separate.

This disclosure provides redox cyclable molecules for energy storage. These molecules belong to either the 4H-pyran-4-ylidene family or include a six-membered aromatic ring with one nitrogen atom at position 1 (pyridinium family) or two nitrogen atoms at positions 1 and 4 (pyrazinium family) or at positions 1 and 3 (pyrimidinium family). Molecules in these families are used as analytes in redox flow batteries.

The present invention relates to organic electroluminescent materials and devices. Novel ligands for metal complexes containing a five-membered ring fused on a pyridine or pyrimidine ring, combined with partially fluorinated side chains, which exhibit improved external quantum efficiency and lifetime are disclosed.