14 results about "Pyrimidifen" patented technology

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 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 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 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.

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.

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 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 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.

To provide an inhibitor of complement system.SOLUTION: Compounds of Formula (I), and pharmaceutically acceptable salts thereof, are disclosed. Also provided are pharmaceutical compositions comprising such compounds, and methods of using the compounds and compositions in the treatment or prevention of diseases or conditions characterized by aberrant complement system activity.SELECTED DRAWING: None

This invention discloses a D-A type pyrimidine-based covalent organic framework material of Formula I, its preparation method, and its applications. The material is obtained by a Schiff base condensation reaction of an electron-rich monomer 1,3,5-trimethoxy-2,4,6-tricarboxyphenyl and an electron-deficient monomer 5,5',5''-(1,3,5-phenyltriyl)tris(2-pyrimidineamine). This invention synthesizes a covalent organic framework rich in pyrimidine groups linked by imine bonds through a Schiff base reaction between electron-rich and electron-deficient monomers. This enhances the light absorption capacity of the COF material, effectively modulates the band structure, reduces carrier migration resistance, and improves photocatalytic activity, significantly increasing the efficiency of photocatalytic hydrogen peroxide production in a short time. In oxygen-saturated deionized water, the photocatalytic hydrogen peroxide production rate of the COF material of this invention is 5287 µmol / h. ‑1 g ‑1 I

The present invention relates to a crystalline form of N-(4-(4-amino-6-ethynyl-5-(quinolin-3-yl)-7H-pyrrolo [2, 3-d] pyrimidin-7-yl) bicyclo [2.2. 1] heptane-1-yl)-5-methylpyrazine-2-carboxamide (TAS3351), a compound having an EGFR inhibitory effect, and an acid. The crystalline form has superior physical properties, including stability, hygroscopicity, and oral absorbability. The crystal form has a peak at a specific diffraction angle (2 [theta] + / -0.2 DEG) in a powder X-ray diffraction spectrum.

The invention discloses a 4-(2-(methylamino) thiazole-5-yl) pyrimidine-2-amine derivative and application thereof, the structural formula of the 4-(2-(methylamino) thiazole-5-yl) pyrimidine-2-amine derivative is shown in the specification, in the formula, R1 is hydrogen or methyl; r2 is a substituted benzoyl group, a substituted phenylacetyl group, and a substituted or unsubstituted benzene propionyl group; and R3 is a substituted phenyl group, a 5-nitrofuran-2-yl group or a 1H-imidazole-2-yl group. As a novel CDK9 inhibitor, the ESCC inhibitor fills the blank of special medicines for ESCC; pharmaceutical salts and compositions can be prepared, and development of oral or injection preparations is facilitated; the compound is suitable for esophageal cancer single-drug treatment or is combined with other targeting / immune / chemotherapeutic drugs to improve the curative effect and reduce the drug resistance risk; meanwhile, other CDK9 related tumors such as lung cancer and breast cancer can be expanded.

The invention belongs to the technical field of medicine synthesis, and particularly relates to a synthesis method of a tofacitinib key intermediate. According to the method, N-((3R, 4R)-1-benzyl-4-methylpiperidine-3-yl)-N-methyl-7H-pyrrolo [2, 3-d] pyrimidine-4-amine is taken as a starting material, under the action of N, N-diisopropylethylamine and 1-chloroethyl chloroformate, debenzylation is carried out through a one-pot method, conditions are mild, aftertreatment purification is simple and easy to operate, energy consumption is low, working hours are short, and the method is suitable for large-scale production.