7 results about "Pteridine" patented technology

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 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 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).