40 results about "Pyrimidifen" patented technology

The invention relates to preparation and application of a trifluoroethyl thiophenylpyrimidinamine derivative. Specifically, the invention relates to a compound as shown in a formula (I), or an isotope labeled compound thereof, or an optical isomer, a geometric isomer, a tautomer or an isomer mixture thereof, or a pharmaceutically acceptable salt thereof, and application of the compound in preparation of insecticides for pest control. The compound can achieve a better pest control effect at a lower dosage, especially for pests such as tetranychidae, microcosaridae, acaridae, tarsonidae, aleuridae and root-knot nematode, and can be used for controlling pests such as tetranychidae, microcosaridae, gall mite, tarsonidae, aleuridae and the like. # imgabs0 #

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 present application provides a pyrimidineamine compound, characterized in that the pyrimidineamine compound is a compound represented by Formula I, or its stereoisomer, tautomer, isotope derivative, hydrate, solvate, prodrug, and pharmaceutically acceptable salt. The pyrimidineamine compound described in the present application has excellent NUAK1 / NUAK2 kinase inhibitory activity and can be used for preventing or treating the following diseases by inhibiting NUAK1 / NUAK2: neuropsychiatric diseases, metabolic diseases, tumors, visceral fibrosis diseases, and skin fibrosis diseases. #imgabs0#

The present application provides a pyrimidineamine compound, characterized in that the pyrimidineamine compound is a compound represented by Formula I, or its stereoisomers, tautomers, isotopic derivatives, hydrates, solvates, prodrugs, and pharmaceutically acceptable salts. The pyrimidineamine compound described herein has excellent NUAK1 / NUAK2 kinase inhibitory activity and can be used to prevent or treat the following diseases by inhibiting NUAK1 / NUAK2: neuropsychiatric diseases, metabolic diseases, tumors, visceral fibrosis, and skin fibrosis. #imgabs0#

The present invention relates to the crystalline form of bipyrimidine compounds, as well as methods for preparing the same and their use. In particular, the present invention relates to crystalline form I of 4'-cyclopropyl-5,6'-dimethoxy-N-((4-(1-methyl-4-(trifluoromethyl)-1H-imidazole-2-yl)bicyclo[2.2.2]octan-1-yl)methyl)-[2,5'-bipyrimidine]-4-amine, wherein the X-ray powder diffraction pattern of crystalline form I includes characteristic peaks at diffraction angles (2θ) of 6.378±0.2°, 9.521±0.2°, 15.721±0.2°, 16.379±0.2°, 16.981±0.2°, 17.560±0.2°, 19.080±0.2° and 22.200±0.2°. Crystal form I possesses high stability, high solubility, high plasma concentration, high bioavailability, and excellent pharmacological activity, making it suitable for pharmaceutical preparations.

The present invention relates to a pyrido[2,3-d]pyrimidine-4-amine compound of general formula (I): wherein R 1 、R 2 、R 3 , A, x and y are as defined herein; methods for preparing the compounds; intermediate compounds used to prepare the compounds; pharmaceutical compositions and combinations comprising the compounds; and the use of the compounds as a single agent or in combination with other active ingredients for the preparation of pharmaceutical compositions for treating or preventing diseases, particularly hyperproliferative diseases.

The invention belongs to the technical field of organic synthesis, and particularly relates to a preparation method of a pyrrolopyrimidine-4-amine derivative, which selects methanol, ammonium formate and formic acid as a reaction system to carry out directional reaction, avoids the use of high-pressure hydrogen and a high-pressure kettle, avoids the safety risk caused by high-pressure operation, and improves the yield of the pyrrolopyrimidine-4-amine derivative. And the alcoholic solution solves the problems of low solubility and obvious amplification effect of a starting material when water is used as a solvent in the prior art, and realizes homogeneous reaction. By adopting the fixed bed reaction unit, the problem of pipeline blockage caused by sublimation of ammonium formate is solved, the potential safety hazard in large-scale production is eliminated, the fixed bed reaction unit is used for continuous catalytic reaction to replace the traditional staged reaction, the production period is remarkably shortened, the production efficiency is improved, and the method is suitable for large-scale industrial production.

The invention relates to a preparation method of 4-chloro-5H-pyrrolo [3, 2-D] pyrimidine-2-amine, which comprises the following steps: step 1, synthesizing a compound B from a compound A; 2, synthesizing a compound C from the compound B; 3, synthesizing a compound D from the compound C; wherein the structures of the compound A, the compound B, the compound C and the compound D are respectively as follows: # imgabs0 #. Compared with the prior art, the preparation method disclosed by the invention has the advantages that the process is simple, only three-step reaction is needed, and complicated post-treatment is not needed; the cost is controllable, raw materials are easy to obtain, reagents are cheap, and the prepared compound is a key intermediate of kinase inhibitor drugs, has important application value in research and development of anti-cancer and anti-inflammatory drugs and has high potential economic benefits; the method has no harsh reaction conditions, is simple to operate and is suitable for large-scale production.

The application discloses a ceramic paint for metal doors and a preparation method thereof, and relates to the technical field of paints. The ceramic paint prepared by the application contains sodium silicate, methyltrimethoxysilane, modified polyacrylate emulsion, modified silicon dioxide, glass powder, sodium fluorosilicate, dispersant, leveling agent and pure water. The modified polyacrylate emulsion is obtained by polymerizing phosphorus-containing monomers and vinyl monomers to generate polyacrylate, reacting the polyacrylate with 5-chloromethyl-2-pyrimidine amine after sulfonyl chlorination, and then emulsifying. The silicon dioxide is obtained by polymerizing aniline on the surface of pretreated silicon dioxide, reacting with 1-benzothiophene-5-carbonyl chloride, then salifying with diphenyl iodonium triflate and copper acetate, and then reacting with bis(2-ethynylphenyl) sulfane. The ceramic paint prepared by the application has good corrosion resistance, antibacterial property and anti-aging property, and greatly improves the performance of the metal door.

The present application relates to a kind of porous coordination polymers with interpenetrating framework, preparation method and application in ethane / ethylene high temperature separation, belong to coordination chemistry material technical field.Porous coordination polymers are Cu-based coordination polymers, its chemical formula is [Cu2 (BDC) 2L2] n (solvent) x , belong to C2 / c space group, L2 is 4,6-di (1H-1,2,4-triazole-1-yl) pyrimidine-2-amine, NH2 Group is again with adjacent framework forms single hydrogen bond;It is obtained by adding regulating ligand during solvothermal reaction of ligand and metal salt.The present application proposes a new method to regulate temperature-dependent dynamic characteristics in hydrogen-bonded interpenetrating framework, with the weakening of hydrogen bond, porous coordination polymers with one-dimensional narrow-neck channel exhibit promising structural response to ethane / ethylene at high temperature, so that it shows significant ability to directly obtain polymerization grade ethylene.

The invention relates to a crystal form of a bipyrimidine compound as well as a preparation method and application thereof. In particular, the present invention relates to a crystalline form I of 4 '-cyclopropyl-5, 6'-dimethoxy-N-((4-(1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl) bicyclo [2.2. 2] oct-1-yl) methyl)-[2, 5 '-bipyrimidinyl]-4-amine, a crystalline form II of 4'-cyclopropyl-5, 6 '-dimethoxy-N-((4-(1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl) bicyclo [2.2. 2] oct-1-yl) methyl)-[2 An X-ray powder diffraction pattern of the compound comprises characteristic peaks at diffraction angles (2 theta) of 6.378 + / -0.2 degrees, 9.521 + / -0.2 degrees, 15.721 + / -0.2 degrees, 16.379 + / -0.2 degrees, 16.981 + / -0.2 degrees, 17.560 + / -0.2 degrees, 19.080 + / -0.2 degrees and 22.200 + / -0.2 degrees. The crystal form I is high in stability, high in solubility, high in blood concentration, high in bioavailability and excellent in pharmacological action, so that the crystal form I is suitable for pharmaceutical preparations.

The present application provides a pyrimidineamine compound, which is characterized in that the pyrimidineamine compound is a compound represented by Formula I, or its stereoisomer, tautomer, isotope derivative, hydrate, solvate, prodrug and pharmaceutically acceptable salt. The pyrimidineamine compound described in the present application has excellent NUAK1 / NUAK2 kinase inhibitory activity and can be used for preventing or treating the following diseases by inhibiting NUAK1 or NUAK2: neuropsychiatric diseases, metabolic diseases, tumors, visceral fibrosis diseases, and skin fibrosis diseases.

The present application provides imidazolyl pyrimidinylamine inhibitors of cyclin-dependent kinase 2 (CDK2), as well as pharmaceutical compositions thereof, and methods of treating cancer using the same.

Disclosed in the present invention are 6-arylquinazolin-4-amine and 6-arylpyridopyrimidin-4-amine derivatives, and the use thereof as PI3Kδ covalent inhibitors. Said derivatives disclosed by the present invention are compounds capable of being used as PI3Kδ inhibitors. PI3Kδ kinase activity and PI3K selectivity tests verify that the compounds disclosed in the present invention exhibit an obvious inhibition effect on PI3Kδ kinase activity and have obvious selectivity on the activity of PI3Kδ. In-vitro cell anti-proliferative activity tests by means of using various blood tumor cell lines exhibit that the compounds disclosed in the present invention have different inhibition effects on various blood tumor cells.

The invention belongs to the technical field of oil and gas development, and particularly relates to a sterilization defoaming agent for foam drainage and a preparation method thereof. The cleaning agent is prepared from the following components: alkynediol polyether modified silicone oil, polyoxyethylene polyoxypropylene pentaerythritol ether, modified nano silicon dioxide, an emulsifier, a mutual solvent, a benzyl quaternary ammonium salt disinfectant, a pyrilamine bactericide and water. The preparation method comprises the following steps: heating and stirring the alkynediol polyether modified silicone oil, adding the modified nano silicon dioxide, stirring, cooling, reducing the stirring speed, adding the polyoxyethylene polyoxypropylene pentaerythritol ether, and continuously stirring to obtain an intermediate product A; adding water into another reaction kettle, heating and stirring, then adding an emulsifier, a mutual solvent, a benzyl quaternary ammonium salt disinfectant and a pyrilamine bactericide, stirring to obtain an intermediate product B, and then heating; and adding the intermediate product A into the intermediate product B, and stirring. The sterilizing and defoaming agent for foam drainage has multiple functions of sterilizing and defoaming, and realizes multiple effects by one agent.

The invention belongs to the technical field of medicine detection, and particularly relates to a method for detecting related impurities of an imatinib mesylate intermediate. In particular to a method for detecting related substances in N-(2-methyl-5-nitrophenyl)-4-(pyridine-3-yl) pyrimidine-2-amine. The related substances in N-(2-methyl-5-nitrophenyl)-4-(pyridine-3-yl) pyrimidine-2-amine are detected by high performance liquid chromatography, and the content of each impurity in N-(2-methyl-5-nitrophenyl)-4-(pyridine-3-yl) pyrimidine-2-amine is calculated by a main component external standard method with correction factors. The methodology verification shows that the detection method provided by the invention is good in specificity and high in accuracy and sensitivity, and can be used for quality control of related substances in N-(2-methyl-5-nitrophenyl)-4-(pyridine-3-yl) pyrimidine-2-amine, so that the product quality is effectively controlled, and the medication safety of imatinib mesylate is improved.

Crystalline and amorphous forms of N-(5-((4-ethylpiperazin-1-yl)methyl)pyridin-2-yl-5-fluoro-4-(3-iso-propyl-2-methyl-2H-indazol-5-yl)pyrimidin-2-amine (Compound 1) and various salts thereof, preparation methods of these crystalline and amorphous forms, pharmaceutical compositions containing these crystalline or amorphous forms, and use of these crystalline and amorphous forms, or pharmaceutical compositions thereof, for treatment of diseases or disorders associated with cyclin-dependent kinase (CDK), especially CDK4 and CDK6, activities, such as various cancers, are disclosed.

The present invention generally relates to compounds of formula (I) inhibiting 3- phosphoglycerate dehydrogenase (PHGDH) activity; particularly, the invention relates to compounds that are thienopyrimidylamine derivatives, including pharmaceutically acceptable salts thereof, methods of preparing such compounds, and therapeutic use thereof. The compounds of the invention may be useful for instance in the treatment of many disorders associated with PHGDH, for instance in the treatment of many disorders associated with fibrosis, such as idiopathic pulmonary fibrosis (IPF).

Provided herein are solid dispersions of 5-chloro-N-(3-cyclopropyl-5-{[(3R, 5S)-dimethylpiperazine-1-yl] methyl} phenyl)-4-(6-methyl-1H-indol-3-yl) pyrimidine-2-amine and methods for preparing the solid dispersions. The solid dispersions of 5-chloro-N-(3-cyclopropyl-5-{[(3R, 5S)-dimethylpiperazine-1-yl] methyl} phenyl)-4-(6-methyl-1H-indol-3-yl) pyrimidine-2 Also provided herein is a pharmaceutical composition comprising a solid dispersion of 5-chloro-N-(3-cyclopropyl-5-{[(3R, 5S)-dimethylpiperazin-1-yl] methyl} phenyl)-4-(6-methyl-1H-indol-3-yl) pyrimidine-2-amine, and a use thereof. The invention also provides a pharmaceutical composition comprising a solid dispersion of 5-chloro-N-(3-cyclopropyl-5-{[(3R, 5S)-dimethylpiperazin-1-yl] methyl} phenyl)-4-(6-methyl-1H-indol-3-yl) pyrimidine-2-amine.

The application discloses a one-pot method for preparing a medicine building block 5-bromo-4-fluoropyrimidine-2-amine, and relates to the field of organic chemical synthesis.The specific steps of the synthesis route are as follows: step one, 2-amino-4-chloropyrimidine and a bromination reagent are added into a solvent, and stirring reaction is carried out;step two, a fluorination reagent is added into the reaction solution, and heat preservation reaction is carried out;step three, water is added to precipitate, and the filter cake is dried and filtered.The 5-bromo-4-fluoropyrimidine-2-amine is prepared by the one-pot method, and the problems of low yield, complex operation, much waste, existence of isomers, and difficult purification in the existing synthesis preparation route of the 5-bromo-4-fluoropyrimidine-2-amine are solved successfully, and the method does not cause environmental pollution, and is beneficial to the green and environment-friendly industrial production of the 5-bromo-4-fluoropyrimidine-2-amine.

The present invention belongs to the technical field of oil and gas development, and particularly relates to a bactericidal defoaming agent for foam drainage and a preparation method thereof. Its components include: alkynediol polyether modified silicone oil, polyoxyethylene polyoxypropylene pentaerythritol ether, modified nano-silica, emulsifier, co-solvent, benzyl quaternary ammonium salt disinfectant, pyrimidineamine bactericide and water. The preparation method includes: heating and stirring the alkynediol polyether modified silicone oil, adding the modified nano-silica and stirring, cooling and reducing the stirring speed, adding the polyoxyethylene polyoxypropylene pentaerythritol ether, and continuing to stir to obtain intermediate product A; adding water to another reaction kettle, heating and stirring, then adding the emulsifier, co-solvent, benzyl quaternary ammonium salt disinfectant, pyrimidineamine bactericide, stirring to obtain intermediate product B and then heating up; adding intermediate product A to intermediate product B and stirring to obtain the product. This bactericidal defoaming agent for foam drainage has multiple functions of sterilization and defoaming, achieving multiple effects with one agent.

Provided in the present invention are an oxazolone-substituted pyrimidinamine compound, a preparation method therefor, a pharmaceutical composition thereof and the use thereof. Specifically, provided in the present invention are a compound having a structure as shown in general formula (I), and a racemate, R-isomer, S-isomer, pharmaceutically acceptable salt thereof, or a mixture thereof. The compound has good IDH1 inhibitory activity, and therefore can be used for treating, preventing and relieving diseases related to IDH1 enzyme, especially for treating malignant tumors or other related diseases caused by IDH1 enzyme mutation.

The present application relates to a synergistic composition containing a biologically effective amount of compound A and component B, wherein the component B is one of thiazide ketone, avermectin, spirotetramat, pyridalyl, emamectin benzoate, azamethiphos, azocyclotin, pyridaben, quimacryd thiocyl, pyrimidifen, tebufenpyrad, flufenoxuron, chlorfenapyr, cyromazine, and halofenozide, and a method thereof for controlling pests in agronomic and non-agronomic environments. The compound A has a synergistic effect with the component B, which can improve the pest control effect, reduce the application amount, reduce the use frequency, and reduce the use cost.

The invention belongs to the technical field of organic chemistry, and particularly relates to a nitration method of 5-phenylpyrazolo [1, 5-a] pyrimidine-7-amine, which comprises the following steps: adding 5-phenylpyrazolo [1, 5-a] pyrimidine-7-amine and Fe (NO3) 3.9 H2O into a reaction tube, adding a solvent, and after the reaction is completed, separating and purifying the reaction liquid to obtain the final product 3-nitro-5-phenylpyrazolo [1, 5-a] pyrimidine-7-amine. The invention relates to a pyrimidine-7-amine compound. The efficient selective C3 nitration method of 5-phenylpyrazolo [1, 5-a] pyrimidine-7-amine and iron nitrate nonahydrate is realized at room temperature under the action of a solvent by taking non-toxic, cheap and easily available Fe (NO3) 3.9 H2O as a nitro source without additionally adding a metal catalyst, an organic ligand and alkali, a corresponding nitration product is obtained, and the highest yield can reach 94%.

The invention relates to pyrazolopyrimidine-5-amine compounds as well as a preparation method and application thereof, and belongs to the technical field of compounds and medicines. The preparation method comprises the following steps: protecting 5 # amino of pyrazolo [1, 5-a] pyrimidine-5-amine by adopting butyric acid methyl ester amide with large steric hindrance, enabling an electrophilic reagent (such as a halogenating agent) to highly selectively attack a 7 # site with small steric hindrance by utilizing a space shielding effect so as to obtain a key 7 # halogenated intermediate, and modifying the 5 # amino by virtue of a hydrolysis reaction, so that the pyrazolo [1, 5-a] pyrimidine-5-amine is obtained. According to the pyrazolo [1, 5-a] pyrimidine compound, the 5 # site and the 7 # site of the pyrazolo [1, 5-a] pyrimidine are accurately substituted, the 5 # site amino substituted pyrazolo [1, 5-a] pyrimidine compound is obtained, and the compound has better anti-tumor activity, provides a new drug choice for tumor treatment and enriches an anti-tumor drug library.

The invention belongs to the field of medical chemistry, and particularly relates to a phenyl ether linked cyclohexylpyrimidinamine CDK12 / 13 inhibitor as shown in a formula I or an isomer, a pharmaceutically acceptable salt and a preparation method thereof, and a pharmaceutical composition containing the phenyl ether linked cyclohexylpyrimidinamine CDK12 / 13 inhibitor or the isomer and the pharmaceutically acceptable salt of the phenyl ether linked cyclohexylpyrimidinamine CDK12 / 13 inhibitor. According to the present invention, the compound of the formula I has the ether cyclohexyl amine linking chain group, such that the affinity of the compound with the CDK12 / 13 protein is increased, the selectivity on the CDK12 / 13 kinase is improved, the synthesis difficulty is reduced, the druggability is substantially improved, and the application prospect is broad.

The present invention provides a pyrimidineamine compound represented by formula (I), or a stereoisomer, tautomer, N-oxide, solvate, or pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the compound, as well as the use of the compound and its pharmaceutical composition in the preparation of a drug for preventing, treating, and / or alleviating a disease, disorder, and / or condition associated with abnormal PI3-kinase, or inhibiting PI3-kinase activity. The compound provided by the present invention exhibits excellent inhibitory activity and kinase selectivity against PI3-kinase.

The invention provides an oxazolone-substituted pyrimidinamine compound as well as a preparation method, a pharmaceutical composition and application thereof, and particularly provides a compound with a structure as shown in a general formula I, and a racemate, an R-isomer, an S-isomer, a pharmaceutically acceptable salt or a mixture of the racemate, the R-isomer, the S-isomer and the pharmaceutically acceptable salt thereof. The compound has good IDH1 inhibitory activity, so that the compound can be used for treating, preventing and relieving diseases related to IDH1 enzyme, especially malignant tumors or other related diseases caused by IDH1 enzyme mutation. # imgabs0 #

The present application provides a pyrimidineamine compound, which is characterized in that the pyrimidineamine compound is a compound represented by Formula I, or its stereoisomer, tautomer, isotope derivative, hydrate, solvate, prodrug, and pharmaceutically acceptable salt. The pyrimidineamine compound of the present application has excellent NUAK1 / NUAK2 kinase inhibitory activity and can be used for preventing or treating the following diseases by inhibiting NUAK1 or NUAK2: neuropsychiatric diseases, metabolic diseases, tumors, visceral fibrosis diseases, and skin fibrosis diseases.

Disclosed are compounds that bind to embryonic ectoderm development (EED) protein and proteolysis-targeting chimeric (PROTAC) derivatives thereof that induce degradation of EED. The disclosed compounds may be characterized as substituted [1,2,4]triazolo[4,3-c]pyrimidin-5-amine compounds having the Formula I:where R1 is as disclosed herein. The disclosed PROTAC derivatives thereof typically include a first targeting moiety that binds to BED (MEED) which may be derived from the disclosed [1,2,4]triazolo[4,3-c]pyrimidin-5-amine compounds having the Formula I that bind to EED. The first targeting moiety typically is linked via a bond or a linker (L) to a second targeting moiety that binds to an E3 ubiquitin ligase (ME3). As such, the disclosed PROTACS may be described as having a formula MEED-L-ME3 or ME3-L-MEED.