21 results about "Pteridine" patented technology

The invention discloses a multifunctional nano-carrier with drug resistance, biotin receptor targeting and hypoxia / low pH dual responsiveness and a preparation method and application thereof, and belongs to the technical field of biomedical polymer materials. The AGT inhibitor conjugate with biotin receptor targeting and low oxygen and low pH dual response provided by the invention comprises a hydrophobic 2-amino-O4-benzyl pteridine group (BD), a low oxygen response group azobenzene (AZO) and a hydrophilic high polymer material modified by biotin (Bio). According to the system, hydrophobic chemotherapeutic drugs can be loaded in a drug carrying system through intermolecular acting force, target biotin receptors on tumor cells and are enriched in tumor tissues by utilizing high permeability and long-term effectiveness of the hydrophobic chemotherapeutic drugs; the tumor microenvironment characterized by low oxygen and low pH can induce azo bond breakage and pH response on the nano-carrier to release BD with AGT activity inhibition and an alkylating agent with anti-tumor activity, so that the drug resistance and anti-tumor activity of the drug are improved, and the targeting property is increased.

The invention relates to a method for detecting related substances in sapropterin hydrochloride tablets. The related substances are selected from biological pterin, pterin, neopterin, pteridine and S-isomer. High performance liquid chromatography is adopted for detection, and a filling material of a stationary phase of a chromatographic column is octadecylsilane chemically bonded silica; a ghost peak trapping small column is arranged between the position behind the converging outlet of the pump and the sample injector; the mobile phase A is a phosphate buffer solution with the concentration of 10-30 mmol / L, and the pH value of the mobile phase A is 2.75-2.80; a mobile phase B is methanol; dissolving a to-be-detected sample with a diluent, and fixing the volume to form a sample injection solution; the diluent is a phosphate buffer solution containing ascorbic acid, the concentration of the phosphate buffer solution is 10-30 mmol / L, the pH value is 2.0-2.5, and the concentration of the ascorbic acid is 1-2 g / L.

A method for preparing 3,6-diaminopyrazine-2,5-dicarboxylic acid and its synthetic intermediates, the method comprising the step of preparing pyrimidino[4,5-g]pteridine-2,4,7,9(1H,3H,6H,8H)-tetraone or its disalt (pteridine) from 5-aminouracil or its monosalt.

The invention discloses flavonolignan glycoside and pharmaceutically acceptable salts thereof. The flavonolignan glycoside is shown as a structural formula I, the invention also discloses a preparation method of the flavonolignan glycoside and an application of the flavonolignan glycoside in preparation of a pteridine reductase-1 inhibitor. The flavonolignan glycoside provided by the invention can effectively inhibit the activity of pteridine reductase-1, and can be used for preparing medicines for relieving leishmaniasis.

The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer).

The present disclosure relates to a bicyclic fused-ring (for example, pteridine, pyridopyrimidine, pyridopyrazine, quinazoline, naphthyridine, or quinoxaline) derivative or a pharmaceutically acceptable salt thereof inducing activation of a triggering receptor expressed on myeloid cells 2 (TREM2), a pharmaceutical composition including the same, and a use thereof. The bicyclic fused-ring derivative or a pharmaceutically acceptable salt thereof may be useful in treatment and prevention of TREM2-mediated neurodegenerative diseases such as Alzheimer's disease (AD), frontotemporal lobar degeneration (FTLD), FTLD-like syndrome, Parkinson's disease, Huntington's disease and Nasu-Hakola disease.

The invention discloses a tetrahydropteridinone derivative as a Plk1 kinase selective covalent inhibitor, the derivative is shown as a general formula (I), and the definition of substituent groups is shown in the specification. According to the present invention, the high Plk1 inhibition activity is maintained while the selectivity on the same family kinase is improved so as to improve the Plk1 kinase targeting property, such that the effect of the drug on other targets is reduced while the drug effect is performed at the action site, and the occurrence of adverse reaction events is reduced. Meanwhile, compared with a reported Plk1 kinase inhibitor, the Plk1 inhibitor provided by the invention has different binding mechanisms, and forms a covalent bond with Plk1. The new mechanism can effectively overcome the drug resistance of the existing Plk1 inhibitor caused by target binding site mutation. Meanwhile, the compound has the advantages of higher selectivity, longer drug effect duration and the like. # imgabs0 #

The invention discloses a preparation method of a methotrexate drug intermediate, which comprises the following steps: by taking 2, 4, 5, 6-tetraaminopyrimidine as a raw material and tert-butyl hydroperoxide (TBHP) as an oxidant, carrying out cyclization reaction on the raw material and 1, 3-dihydroxyacetone in the presence of a catalyst, a buffering agent and a solvent, and carrying out post-treatment to obtain free alkali or acid salt of the free alkali of the methotrexate drug intermediate. The method has the advantages of simple reaction operation, mild reaction conditions, environment-friendly reaction process and high product purity and yield, and is suitable for industrial production.

Described herein are pyrido-pyrimidinone and pteridinone compounds or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods treating cancer, alone and in combination with other therapeutic agents.

The present invention discloses a pteridine compound or a salt thereof, wherein the pteridine compound is a compound of formula I. The present invention enriches and prepares a reference substance for a characteristic pteridine compound from leeches by column chromatography, performs purity testing by HPLC, and identifies the structure using mass spectrometry and nuclear magnetic resonance data, resulting in SZ-1. This compound is a characteristic chemical component of leeches and a hallmark component for distinguishing leeches from leeches and their closely related counterfeits. Platelet aggregation assay results show that SZ-1 promotes platelet aggregation, providing a candidate standard substance for identifying different leech origin varieties and authenticity. Currently, there are no reports on the isolation and identification of SZ-1 from leeches as described in the present invention. #imgabs0#

The invention relates to the technical field of medicines, in particular to a substituted pyrrolo pteridinone ubiquitin specific protease 1 (USP1) inhibitor compound, a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, a pharmaceutical composition containing the compound, the pharmaceutically acceptable salt thereof, or the stereoisomer thereof, and a preparation containing the compound, the pharmaceutically acceptable salt thereof, or the stereoisomer thereof. The invention relates to a compound, a pharmaceutically acceptable salt or a stereoisomer thereof, a method for preparing the compound, the pharmaceutically acceptable salt or the stereoisomer thereof, and application of the compound, the pharmaceutically acceptable salt or the stereoisomer thereof in preparation of drugs for treating and / or preventing USPl-mediated diseases and related diseases.

The invention provides a pteridinone compound and application thereof. The structure of the pteridinone compound is as shown in formula I in the specification. The pteridinone compound provided by the invention can effectively inhibit mTOR kinase, has an excellent anti-tumor effect, and is low in toxicity, small in harm to organs, safe and efficient.

The invention relates to the technical field of tumor treatment, in particular to a VEGFR-2 / BRD4 double-target inhibitor and application thereof. The structural general formula of the VEGFR-2 / BRD4 double-target inhibitor is as shown in a formula I in the specification. The tetrahydropteridine compound containing the aryl amide or aryl urea structure, disclosed by the invention, has relatively strong inhibitory activity on VEGFR-2 / BRD4 activity; according to the present invention, the VEGFR-2 / BRD4 double-target inhibitor has good anti-proliferative activity on tumor cells, the compound I-5 shows the optimal activity, and the activity is far superior to the positive control Sorafenib, ReGrafenib and JQ-1, the effect of the ReGrafenib and the effect of the combination of the Sorafenib and the JQ-1 respectively, and the target treatment drug for leukemia, gastrointestinal stromal tumor, liver cancer, kidney cancer, thyroid cancer, non-small cell lung cancer, colorectal cancer and the like can be prepared, and the compound I-5 can be used for the preparation of the target treatment drug for treating leukemia, gastrointestinal stromal tumor, liver cancer, kidney cancer, thyroid cancer, non-small cell lung cancer, colorectal cancer and the like.

The invention belongs to the technical field of organic synthesis and medicinal chemistry, and discloses a chiral or racemic tetrahydropteridine compound, a preparation method thereof and application of the chiral or racemic tetrahydropteridine compound in preparation of antitumor drugs and lead compounds thereof. The novel tetrahydropteridine compound is synthesized with high efficiency, high regioselectivity and high enantioselectivity. A CCK-8 method is used for carrying out preliminary in-vitro tumor inhibition activity evaluation on the synthesized compound, and the result shows that the tetrahydropteridine compound or the pharmaceutically acceptable salt thereof has good in-vitro tumor inhibition activity on various tumor cells such as colon cancer cells, liver cancer cells and cervical cancer cells; the compound has broad-spectrum activity on tumor tissue specific expression targets, and can be applied to preparation of anti-tumor drugs and lead compounds thereof. According to the invention, the application range of allylation reaction substrates is widened, and a novel heterocyclic structure and a novel method for efficiently constructing chiral heterocyclic molecules are provided for research and development of new drugs.

This invention provides a furosemide-triamterene compound thermosensitive hydrogel oral formulation, its preparation method, detection method, and application, belonging to the field of veterinary formulation technology. The formulation, by mass percentage, comprises furosemide 0.2%-2.0%, triamterene 0.2%-2.0%, an adhesion thickener 0.5%-2.0%, a thermosensitive hydrogel matrix 15%-30%, and moisturizing stabilizers, flavoring agents, and preservatives. The gelation temperature is 28-32℃, the maximum adhesion force to the gastric mucosa is 0.15N-0.35N, and the adhesion work is 5mJ-15mJ. This invention employs a cold-dissolution method, a process free of organic solvents, and simultaneously determines the content of two drugs using HPLC. The formulation flows at 2-8°C and rapidly gels and adheres at 37°C, achieving synergistic diuresis and potassium balance maintenance. It features precise dosage, good palatability, and stable blood drug concentrations, making it suitable for preparing veterinary drugs for canine and feline diuresis, swelling reduction, and potassium balance maintenance. This invention solves the problems of inaccurate dosage, poor compliance, and lack of quality control in existing pet diuretic preparations, ensuring stable and controllable quality and suitability for large-scale production.

The present application relates to pyrimidopyridone and pteridinone compounds of formula I, processes for their preparation and compositions comprising them. More particularly, the present application relates to compounds of formula I having activity as inhibitors of GCN2 kinase and their use in the treatment of diseases, disorders or conditions treatable by inhibition of GCN2 kinase, such as cancer and neuronal diseases. (I).

A method for preparing pyrimido[4,5-g]pteridine-2,4,7,9-tetrol or a salt thereof is provided. A method for preparing 3,6-diaminopyrazine-2,5-dicarboxylic acid or a salt thereof from pyrimido[4,5-g]pteridine-2,4,7,9-tetrol or a salt thereof is also provided. A method for preparing a substituted pteridine compound or a salt thereof is also provided. A method for preparing N-substituted 3,6-diaminopyrazine-2,5-dicarboxylic acid from a substituted pteridine compound or a salt thereof is also provided.

The present application relates to the technical field of medicine, specifically relates to substituted pyrrolo-pteridinone ubiquitin specific protease 1 (USP1) inhibitor compounds, pharmaceutically acceptable salts or stereoisomers thereof, pharmaceutical compositions and preparations containing the compounds, pharmaceutically acceptable salts or stereoisomers thereof, a method for preparing the compounds, pharmaceutically acceptable salts or stereoisomers thereof, and the use of the compounds, pharmaceutically acceptable salts or stereoisomers thereof in the preparation of drugs for treating and / or preventing diseases mediated by USP1 and related diseases.

The invention discloses a pteridine compound or a salt thereof. The pteridine compound is a compound as shown in a formula I in the specification. One characteristic pteridine compound in the leech is subjected to enrichment and preparation of a reference substance in a column chromatography mode, purity detection is performed through HPLC, and the structure is identified by adopting mass spectrum and nuclear magnetic data and is SZ-1. The compound is a leech characteristic chemical component and is a symbolic component for distinguishing leeches, leeches and related adulterants of leeches and leeches, platelet aggregation experiment results show that SZ-1 has the effect of promoting platelet aggregation, and a candidate standard substance is provided for different original varieties and authenticity identification of leech medicinal materials. No related reports for separating and identifying the SZ-1 from the leeches involved in the invention are found at present. # imgabs0 #