161 results about "Pyrimidinones" patented technology

The application discloses an indole-linked pyrimidine compound, an intermediate thereof, a preparation method and application thereof. The application provides an indole-linked pyrimidine compound shown as formula I or a pharmaceutically acceptable salt thereof, which has a good inhibiting effect on EGFR Del19 / T790M / C797S mutation, and is expected to treat and / or prevent various diseases mediated by EGFR.

The invention discloses a 2-amino-4-(5-cyano-1-isopropyl-1H-indole-3-yl) pyrimidine compound and application thereof, the compound has the following structural general formula: in the formula, substituent R is substituted phenyl, the number of substituent groups on the benzene ring of the substituted phenyl is 1-2, and the substituent groups on the benzene ring of the substituted phenyl are 1-2. Substituent groups are respectively and independently selected from nitro, cyano, halogen, carbamoyl, furyl or pyridyl. The 2-amino-4-(5-cyano-1-isopropyl-1H-indole-3-yl) pyrimidine compound designed and synthesized by the invention is a novel efficient NF-kappa B induced kinase (NIK) inhibitor, and is suitable for drug development taking NF-kappa B induced kinase (NIK) as a target spot, and the obtained drug can be used for treating malignant tumors such as leukemia, multiple myeloma and the like.

The invention discloses a novel pyrimidine KRAS-G12C inhibitor as well as a preparation method and application of the novel pyrimidine KRAS-G12C inhibitor. The pyrimidine compound disclosed by the invention has a remarkable inhibition effect on non-small cell lung cancer cells (NCI-H23 and NCI-H358) with high expression of KRAS-G12C, is particularly used as a medicine for treating and / or preventing the non-small cell lung cancer, is simple and efficient in preparation route, and has a good antitumor medicine development and application prospect.

The invention relates to the technical field of compound synthesis, in particular to an aminopyrimidine compound, a pharmaceutical composition, application of the aminopyrimidine compound and an intermediate compound. The structural formula of the aminopyrimidine compound is shown as a formula (I), and the aminopyrimidine compound can effectively inhibit the activity of NUAKs kinase, and especially has a good inhibition effect on the activity of NUAK1 kinase and the activity of NNUAK2 kinase. Formula (I).

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.

Compounds according to formula I are useful as agonists of Toll-like receptor 7 (TLR7). Such compounds can be used in cancer treatment, especially in combination with an anti-cancer immunotherapy agent, or as a vaccine adjuvant.

The invention discloses a stabilizer for a transparent PVC (Polyvinyl Chloride) product with good gamma-ray irradiation resistance. Comprising the following components in parts by weight: 10-20 parts of benzoic acid organic calcium salt, 10-20 parts of benzoic acid organic zinc salt, 10-20 parts of benzoic acid organic magnesium salt, 10-20 parts of benzoic acid organic aluminum salt, 20-30 parts of hydrotalcite, 5-10 parts of borate, 3-10 parts of a pyrimidine auxiliary color retention agent, 3-10 parts of a hindered amine light stabilizer and 5-10 parts of a thioester antioxidant. The hindered amine light stabilizer is a light stabilizer with a hindered amine methyl piperidine structure. The transparent PVC product added with the stabilizer has excellent gamma-ray irradiation resistance, and after the irradiation dose is 25kGy, the yellowness index YI of the transparent PVC product is less than 5.0, which indicates that the transparent PVC product added with the stabilizer does not change color in later application and storage processes after gamma-ray irradiation; the transparency is kept well, the light transmittance after irradiation is greater than 85%, and the transparency requirements of medical and food packaging are met; the mechanical property is well maintained, and the tensile strength retention rate after irradiation is greater than 90%.

The present application relates to the technical field of chemical medicines, in particular to a pyrimidine compound containing nitrogen methoxy benzamide and a preparation method and application thereof.The present application provides a brand-new pyrimidine compound containing nitrogen methoxy benzamide, which is a brand-new compound newly synthesized.The pyrimidine compound containing nitrogen methoxy benzamide is novel in structure, has good water solubility, has a strong inhibitory effect on tumor cells, and has a good application prospect in the preparation of antitumor drugs.

The invention belongs to the technical field of medicines, and particularly relates to pyrrolo [2, 3-d] pyrimidine compounds of aryl fragments and piperidine fragments as well as a preparation method and application of the pyrrolo [2, 3-d] pyrimidine compounds. The pyrrolo [2, 3-d] pyrimidine compound containing the aryl fragment and the piperidine fragment is an HIV-1 reverse transcriptase inhibitor, and the pyrrolo [2, 3-d] pyrimidine compound further comprises pharmaceutical salt, hydrate and solvate of the pyrrolo [2, 3-d] pyrimidine compound, polycrystal or eutectic of the pyrrolo [2, 3-d] pyrimidine compound, and precursors and derivatives with the same biological functions of the pyrrolo [2, 3-d] pyrimidine compound. The invention also relates to a preparation method of the compound and application of a composition containing one or more of the compounds in related medicines for treating AIDS and the like. The result of an in-vitro cellular level anti-HIV-1 activity experiment shows that the micromolecule has relatively strong anti-HIV-1 biological activity, can remarkably inhibit virus replication in MT-4 cells infected by HIV-1 viruses, and has relatively low cytotoxicity.

The invention provides an aminomethylation reaction method based on a pyrazolo [1, 5-a] pyrimidine nitrogen-containing fused heterocycle substrate, a product and application, and belongs to the technical field of chemistry. Pyrazolo [1, 5-a] pyrimidine nitrogen-containing fused heterocycle, secondary amine and glyoxylic acid are used as raw materials, an aminomethylation reaction is achieved at the C3 site of pyrazolo [1, 5-a] pyrimidine through heating for the first time, a transition metal catalyst or a chemical oxidizing agent is not needed, the drug purification problem caused by metal residues and oxidation byproduct pollution are avoided, and the purity of the product is improved. The method is a novel efficient, simple, convenient and environment-friendly nitrogen-containing fused heterocyclic aromatic hydrocarbon functionalization strategy, the reaction can be directly carried out at the temperature of 100-120 DEG C, shielding gas does not need to be filled, and compared with some reactions needing high-temperature or high-pressure conditions, the mild reaction conditions are easier to control, side reactions are reduced, and the yield of the target product is increased. Meanwhile, the reaction conditions are also beneficial to reducing energy consumption, and conform to the concept of green chemistry.

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.

This invention discloses a polycyclic pyrimidine compound and its uses. The invention provides a polycyclic pyrimidine compound of formula (I), its solvate, a pharmaceutically acceptable salt thereof, a solvate of its pharmaceutically acceptable salt, its tautomer, or its stereoisomer. The compound provided by this invention exhibits good degradation activity against CDK9 and good inhibitory activity against neuroblastoma.

The application belongs to the technical field of medicines, and relates to a pyrimidine compound and application thereof in medicines, in particular, application of the pyrimidine compound in preparation of medicines for treating and / or preventing diseases or symptoms caused by a novel coronavirus (SARS-CoV-2). Specifically, the application relates to a compound shown in a general formula (I) or a stereoisomer, a tautomer, a nitroxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, a pharmaceutical composition containing the compound, and application of the compound and the pharmaceutical composition in preparation of medicines for preventing and / or treating diseases or symptoms caused by a coronavirus, in particular, application of the compound and the pharmaceutical composition in preparation of medicines for treating and / or preventing diseases or symptoms caused by SARS-CoV-2, wherein each variable in the formula (I) is as defined in the specification.

The application belongs to the technical field of pharmaceutical chemistry, and particularly relates to a pyrimidine and thienopyrimidine derivative, a preparation method and application thereof. The pyrimidine derivative in the application is a compound with the structure of formula I, and the thienopyrimidine derivative is a compound with the structure of formula II. The pyrimidine and thienopyrimidine derivative can be used as an AcrB efflux pump inhibitor, and can significantly enhance the antibacterial activity when combined with an antibacterial drug. The Nile red experiment shows that the compound 64c can completely inhibit the AcrB-mediated efflux at a concentration of 50 μM, and the effect is better than that of the positive control PA beta N. The compound in the application has novel structure and excellent activity, and can be used for preparing an AcrB efflux pump inhibitor for reversing bacterial drug resistance and an antibacterial sensitizing drug.

A pyrrolopyrimidine or pyrrolopyridine derivative and its medical use. Specifically, the compound has the structure shown in formula I, has good inhibitory effect on focal adhesion kinase (FAK), and can inhibit its related signal pathways, and can be prepared for treating or preventing diseases related to cancer, pulmonary arterial hypertension, pathological angiogenesis, etc., and can be particularly used for treating diseases caused by excessive or abnormal cell proliferation, such as tumors or cancers.

A chlorine-resistant nanofiltration membrane and a preparation method therefor. The preparation method comprises: preparing a base membrane; making the base membrane be sequentially contact with an aqueous phase solution comprising an amine monomer and an organic phase solution comprising an acid chloride monomer, wherein the amine monomer includes a piperazine substance and a pyrimidine substance having two or more amino groups, and the acid chloride monomer includes an acid chloride monomer having three or more acid chloride groups; placing the base membrane that has completed contact in an environment having a temperature of 10-30°C, and spraying an aqueous solution containing a dialdehyde crosslinking agent; placing the base membrane in an environment having a temperature of 40-80°C for treatment; and carrying out work-up to obtain a chlorine-resistant nanofiltration membrane.

The invention relates to a pyrrolopyrimidine compound, a preparation method thereof and application of the pyrrolopyrimidine compound in medicine. Specifically, the invention relates to a pyrrolopyrimidine compound as shown in a general formula (I), a preparation method thereof, a pharmaceutical composition containing the pyrrolopyrimidine compound and application of the pyrrolopyrimidine compound as a therapeutic agent, the invention also relates to a use thereof, in particular as a BTK inhibitor or degradation agent and in the preparation of a medicament for the treatment and / or prevention of BTK-mediated or dependent diseases or conditions. Wherein each group in the general formula (I) is defined in the specification.

The invention discloses a 2-amino-4-anilino pyrimidine compound as well as a preparation method and application of the 2-amino-4-anilino pyrimidine compound. The compound has a strong inhibition effect on EGFR (epidermal growth factor receptor) gene mutation targets and c-MET and has a strong inhibition effect on osimertinib drug-resistant cells; and the compound can inhibit proliferation of various tumor cells, and provides excellent application prospects for treatment of EGFR gene mutation and MET amplified malignant tumors.

The application discloses a pyridopyrimidine compound containing a morpholine structure and a preparation method and application thereof, and belongs to the technical field of medicines. The pyridopyrimidine compound containing the morpholine structure has a strong ability of inhibiting PI3K alpha kinase, and thus can be used as an active ingredient for preparing a therapeutic drug for diseases caused by abnormal activation of PI3K alpha kinase, and shows potential application value in preparation of a drug for treating and / or preventing proliferative diseases and cancers. The application provides important technical support for development of an anticancer drug with high efficiency and better selectivity.

The present disclosure describes novel dihydropyrimidopyrimidines which are useful as proteinase 3 (PR3) and / or human neutrophil elastase (HNE) inhibitors. The dihydropyrimidopyrimidine compounds of the disclosure can be fused with another heteroaromatic ring. The compounds are believed to be useful for treatment of inflammatory diseases, including chronic obstructive pulmonary disease.

The application discloses a crystallization method of an isoxazoline uracil compound, which comprises the following steps: preparing the isoxazoline uracil compound, washing an organic layer with water, and filtering; adding a certain amount of a solvent C to dissolve, and then adding a solvent B; fully mixing after heating, and crystallizing after cooling to obtain slurry, and then performing solid-liquid separation and drying to obtain a powdery solid. The application is characterized in that the mass ratio of the amount of the solvent B to the amount of the solvent C is 5:1-1:5 by optimizing the amount of the solvent C, the content of the solvent in the oily product is reduced, the saturation of the target product in the solution is improved, and the further crystallization and purification are facilitated. Moreover, the crystal form of the isoxazoline uracil compound can be changed, the isoxazoline uracil compound is changed from an oily substance into a bundle-shaped crystal form or a crystal block, and the isoxazoline uracil compound is changed from an oily substance into a powdery substance, the transfer of the production process of the isoxazoline uracil compound, the storage of the material and the usability of the product are improved, and the application range of the product is expanded.

Relates to a dihydrothienopyrimidine compound as well as a preparation method and application thereof, and belongs to the field of biological medicines. Specifically, the invention relates to a compound shown in a general formula (I), a preparation method of the compound, a pharmaceutical composition containing the compound, and application of the compound in preparation of drugs for treating inflammatory diseases, autoimmune diseases, metabolic diseases, nervous system diseases and related diseases.

The subject matter described herein is directed to ferroportin inhibitor compounds of Formula (I) and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and methods of administering the compounds for prophylaxis and / or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, particularly iron overload states, such as thalassemia, sickle cell disease and hemochromatosis, and also kidney injuries.

The invention discloses a compound represented by a formula I, a stereoisomer thereof, a nitrogen oxide compound or a salt thereof, and R1, R2, R3, R4, R5, R6 and G are defined in the specification. The compound provided by the invention is high in herbicidal activity, low in toxicity, small in dosage and small in environmental pollution, and has a good application prospect.

The present disclosure belongs to the technical field of medicines, and relates to the use of an isothiazolo[5,4-d]pyrimidine compound in treating inflammatory diseases, in particular to the use of a compound shown as formula (I) or pharmaceutically acceptable salts thereof in treating rheumatoid arthritis. The compound of formula (I) or the pharmaceutically acceptable salts or pharmaceutical compositions thereof of the present disclosure can achieve good safety while achieving good therapeutic effects, including but not limited to a relatively low incidence of adverse reactions.

The utility model relates to pyrimidine compound production technical field, specifically disclose a kind of extraction device of pyrimidine compound production, including the support mechanism that provides space support to pyrimidine compound extraction, support mechanism is provided with filter material subassembly and raffinate pipe, further include the agitating mechanism for mixing agitation of the compound original solution and extractant for being added in setting on support mechanism, and agitating mechanism includes first agitating subassembly and second agitating subassembly. Through the setting of first agitating subassembly, second agitating subassembly and power transmission component of agitating mechanism, make power piece work drive central shaft, first cross bar and first agitating blade rotation, simultaneously through power transmission component drive rotating sleeve, second cross bar and second agitating blade reverse rotation, first agitating blade and second agitating blade are rotated to each other in the raw material in mixing barrel and carry out mutual cross mixing, accelerate the contact of original solution and extractant, improve mixing effect.

The present invention provides a bovine sex-sorted sperm sorting solution mediated by a small molecule compound and its application. The sperm sorting solution comprises a sperm sorting protection solution and a sex control functional component. The sperm sorting protection solution contains sodium chloride, potassium chloride, calcium chloride dihydrate, sodium dihydrogen phosphate, glucose, sodium pyruvate, sodium bicarbonate, penicillin-streptomycin, and phenol red. The sex control functional component includes creatine and a 24e drug. The concentration of creatine is 450 μM-550 μM, and the concentration of the 24e drug is 0.27 μM-0.33 μM. The 24e drug is a pyrido [3,2-d]pyrimidine-based TLR7&8 dual agonist. The present invention can meet the large demand for sex-sorted semen in production. Moreover, the sorting process is carried out under the suitable conditions for sperm and does not require complex treatment of sperm. It takes less time for sorting and causes less damage to sperm.

The present application relates to a kind of 7-difluoromethyl-5-aryl pyrazolopyrimidine compound and preparation and application, the structural general formula of the compound is as shown in formula a, it is a kind of compound with inhibiting HIF-2 alpha activity, can block HIF-2 alpha / ARNT dimerization and play the role of HIF-2 transcription inhibition.The present application is proved by multiple experiments, the synthesized compound all has excellent HIF-2 transcription inhibition effect, in human renal clear cell carcinoma cell strain 786-O, show good VEGF protein inhibitory activity.The compound described in the present application can be applied in the preparation of hypoxia-inducible factor-2 alpha (HIF-2 alpha) inhibitor for treating VHL deletion or / and HIF-2 alpha abnormal expression disease.This kind of compound can inhibit the overexpression and activation of HIF-2 alpha, to achieve the treatment and prevention of target disease, such as VHL deletion or / and HIF-2 alpha abnormal expression disease.

The present disclosure relates to pyrrolone pyrimidine compounds, methods for preparing the same and their use in medicine. In particular, the present disclosure relates to a pyrrolone pyrimidine compound of general formula (I), methods for preparing the same, pharmaceutical compositions containing the same and their use as therapeutic agents, in particular as DNA-PK inhibitors and in the manufacture of a medicament for the treatment and / or prevention of cancer. Wherein the groups in general formula (I) are as defined in the specification.

The invention relates to an application of a pyrimidine-based additive in a perovskite solar cell. A pyrimidine derivative with moderate Lewis alkalinity is selected as the additive and forms a moderate and stable coordination intermediate with a lead iodide precursor, so that nucleation of alpha-phase formamidine lead iodide can be accelerated and defect generation can be inhibited; the method is suitable for planar formal and trans-structure devices, the photoelectric conversion efficiency of 25% or above is achieved in the formal structure and the trans-structure, and excellent stability is kept under the long-time operation and storage conditions. The invention provides an additive design principle based on pyrimidine molecules, and provides a theoretical basis and a technical path for development of high-performance and long-life perovskite photovoltaic devices.