350 results about "Pyrimidinones" patented technology

The invention provides a pyridopyrimidine derivative as a small GTP enzyme KRAS mutation inhibitor, and particularly provides a pyridopyrimidine derivative with a structural formula as shown in a general formula (A) and pharmaceutically acceptable salts thereof, and the pyridopyrimidine derivative has inhibitory activity on mutants such as KRAS G12D and the like. The invention also provides a preparation method of the derivative, a pharmaceutical composition and a salifying compound of the derivative, and medical application of the derivative as a small GTP enzyme KRAS mutation inhibitor in treatment of different types of tumors.

The invention belongs to the technical field of medicines, and relates to tetrahydropyridopyrimidine compounds as well as a preparation method and application thereof, in particular to tetrahydropyridopyrimidine compounds or pharmaceutically acceptable salts thereof as well as a preparation method and application thereof in preparation of antitumor drugs. The structure of the tetrahydropyridopyrimidine compound or the pharmaceutically acceptable salt thereof is as shown in a general formula (I), and R1-R4 are as shown in the specification and claims. The compound provided by the invention can be used for preparing a KRAS G12C inhibitor, is used for inhibiting G12C mutation of KRAS, has an obvious inhibiting effect on lung cancer, pancreatic cancer or colon cancer, and can be used for preparing antitumor drugs. # imgabs0 #

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 invention discloses a novel isoxazolopyrimidine derivative with anti-new coronavirus activity as well as a preparation method and application of the novel isoxazolopyrimidine derivative. The isoxazolopyrimidine compound provided by the invention has a good inhibition effect on SARS-CoV-2, and relates to the compound shown in the general formula (I), and pharmaceutically acceptable salts and solvent compounds thereof have a good inhibition effect on new coronavirus, and can be used for preparing antiviral drugs related to the new coronavirus for prevention, treatment or adjuvant treatment. # imgabs0 #

The invention discloses a genetically engineered bacterium for producing pseudouridine and a construction method of the genetically engineered bacterium, escherichia coli W3110 is used as a starting strain, the supply of precursor substances including aspartic acid, carbamyl phosphoric acid, glutamine and 5 '-phosphoribosyl pyrophosphate prpp is enhanced, pyrimidine nucleoside synthesis operon from bacillus subtilis is introduced, and the pseudouridine is produced. The invention discloses a pseudouridine-5 '-phosphosidase gene psuG and a preparation method thereof, and relates to the field of microorganisms, the field of genetic engineering and the field of fermentation engineering. The pseudouridine-5'-phosphosidase gene psuG is expressed by using high-copy plasmids, and the application of the pseudouridine-5 '-phosphosidase gene psuG to preparation of the pseudouridine-5'-phosphosidase gene psuG is provided. The strain is fermented in a 50L fermentation tank for 60h, the yield of pseudouridine reaches 50.8 g / L, the conversion rate is 18%, which is the highest value reported at present, and the strain has high industrial production value.

The present disclosure relates to herbicidal combinations, compositions and methods for controlling weeds comprising the carbamate herbicide asulam and an additional herbicide selected from the group comprising cyclohexanedione oxime herbicides, pyrimidinylsulfonyhirea herbicides, triazolopyrimidine herbicides, imidazolinone herbicides, alkylazine herbicides, triketone herbicides, N-phenylimide herbicides or chloroacetamide herbicides. Specifically, the additional herbicide may be one of clethodim, chlorimuron, diclosulam, imazamox, imazethapyr, indaziflam, mesotrione, saflufenacil, tiafenacil or S-metolachlor.

A triazolopyrimidine derivative, a preparation method therefor and a use thereof. The present invention particularly relates to a compound represented by general formula (IC) or a stereoisomer thereof, a preparation method therefor, a pharmaceutical composition containing the compound, and a use of the compound in preparing a drug for treating diseases. The compound has a structure represented by formula (IC).

The invention belongs to the technical field of medicinal chemistry, and particularly relates to a 2-aminopyrimidine compound, application thereof and an antitumor drug. The 2-aminopyrimidine compound provided by the invention has a structure as shown in a formula (I). According to the invention, 2-aminopyrimidine is used as a mother nucleus structure, and a series of 2-aminopyrimidine compounds are successfully constructed by accurately introducing a biologically active imidazole, thiazole or oxazole nitrogen-containing heterocyclic ring fragment at the 5 # site of 2-aminopyrimidine; systematic in-vitro anti-tumor activity evaluation proves that the 2-aminopyrimidine compound with the structure as shown in the formula (I) provided by the invention shows remarkable inhibitory activity on various tumor cell lines, and the activity of part of the compound is even superior to that of a clinical control drug. The structural diversity of 2-aminopyrimidine compounds is enriched, valuable lead compounds are provided for developing novel efficient antitumor drugs, and the 2-aminopyrimidine compounds have important scientific significance and clinical transformation potential. # imgabs0 #

The invention discloses a sulfonyl-containing uracil compound and an application thereof. The structure of the compound is shown as a general formula I, wherein the definition of each substituent group in a # imgabs0 # formula is shown in the specification; also disclosed in the specification are their use as herbicides.

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 invention discloses a thiazole amido pyrimidine DYRK2 inhibitor as well as a preparation method and application thereof. The compound is shown as a formula P. The invention further discloses a preparation method of the thiazole amido pyrimidine DYRK2 inhibitor. The compound disclosed by the invention can inhibit proliferation of cancer cells and induce apoptosis of the cancer cells, is high in cancer inhibition activity and low in toxicity, and can be used for preparing medicine # imgabs0 # for treating cancers or tumor-related diseases

Disclosed are a pyrimidine compound, a preparation method therefor and a medical use thereof. Specifically, disclosed are a compound represented by the general formula (SI), a preparation method therefor, a pharmaceutical composition containing said compound, and a use thereof as a ubiquitin-specific protease 1 (USP1) inhibitor, particularly a use thereof for treating or preventing cancer. The definitions of the groups in the general formula (SI) are the same as those in the description.

The invention discloses a pyrimidine compound as well as a preparation method, a pharmaceutical composition and application thereof. The structure of the compound is shown in a formula I, and the compound further comprises enantiomers, diastereoisomers, racemes, cis-trans-isomers, deuterated compounds, metabolites, prodrugs, solvates, hydrates, pharmaceutically acceptable salts or co-crystals of the compound. The compound has high-efficiency and high-selectivity inhibitory activity on various mutants of EGFR single mutation, double mutation and triple mutation, has low activity and low toxicity on wild type EGFR, and has a good treatment effect on cancers; the problems that an existing EGFR inhibitor is poor in effect, low in selectivity, resistant to drugs and the like are solved. # imgabs0 #

The present invention relates to a pyrido[1,2-a]pyrimidine mesoionic derivative containing a 1,2,4-oxadiazole structure and a preparation method and use thereof. The compound has a structure of formula (I), has excellent insecticidal activity against bean aphids, white-backed plant hoppers, diamondback moths, fall armyworms, striped stem borers, armyworms, etc., and can be used to prepare drugs or medicaments for preventing and controlling pests such as aphids, rice plant hoppers, diamondback moths, fall armyworms, striped stem borers, armyworms, etc. The compound has a simple structure and preparation process, and has low production cost.

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 present invention relates to the field of pesticides, and in particular to a preparation method for a compound of formula (III). The compound of formula (III) can be used for preparing a novel highly efficient uracil herbicide. The present invention further provides an intermediate compound used in the method, a method for producing the intermediate compound, and a sterilization use of the intermediate compound. The present invention has a simple synthetic route, and wide prospects of application.

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.

A novel fused pyrimidine based sulfonamide derivative represented by Formula I, a solvate thereof, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition including the same as an active ingredient, and the uses thereof are disclosed. The novel fused pyrimidine based sulfonamide derivative can effectively suppress the growth of cancer cells and resistance to drugs, which are induced by mutations in the tyrosine kinase domain of epidermal growth factor receptors, or the growth of cancer cells having such resistance.

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 application relates to the field of medicine, and particularly relates to a kind of uracil compound containing formula (I) and its application in preparing bacterial virulence factor lasB inhibitor.The uracil compound involved in the present application is verified by in vitro drug efficacy, and most of the obtained compounds have excellent lasB inhibitory activity, can be used for preparing anti-toxicity agent, and has the potential to be developed as a new antibacterial drug.

The present invention belongs to the field of medicinal chemistry, relates to use of a pyrrolopyrimidine compound in the treatment of medium-risk or high-risk myelofibrosis, and specifically relates to use of a compound of formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising same in the treatment of medium-risk or high-risk myelofibrosis. The compound of formula I, the stereoisomer thereof, the pharmaceutically acceptable salt thereof, or the pharmaceutical composition thereof has a good therapeutic effect.

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.