229 results about "Pyrimidinones" patented technology

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 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 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

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.

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 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 present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutically acceptable salts thereof, and pharmaceutical formulations containing them, and their uses, alone or in combination with one or more additional agents, for treating various diseases in which an increase in the concentration of nitric oxide (NO) and / or an increase in the concentration of cyclic guanosine monophosphate (cGMP), or both, or upregulation of the NO pathway, is desired. In some embodiments, the compound is of Formula I or a pharmaceutically acceptable salt thereof. (I) TIFF2025536343000075.tif3865

The invention discloses a pyrimidine compound as well as a preparation method and medical application thereof. Specifically, the invention discloses 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 as a ubiquitin specific protease 1 (USP1) inhibitor, especially application of the compound in treating or preventing cancers. The definition of each group in the general formula (I) is the same as that in the specification.

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 invention provides pyrimidine compounds and their uses. Specifically, the present invention provides a novel compound that effectively inhibits ATX, which is a compound represented by the following formula, or a tautomer, stereoisomer, hydrate, solvate, pharmaceutically acceptable salt or prodrug of the compound represented by the following formula: #imgabs0#