4results about How to "Has inhibitory activity" patented technology

This invention provides compounds useful as active ingredients in pharmaceutical compositions for the treatment of pancreatic cancer. The inventors studied compounds useful as active ingredients in pharmaceutical compositions for the treatment of pancreatic cancer and discovered that 4-aminoquinazoline compounds possess excellent G12D mutant KRAS inhibitory activity, making them suitable for use as therapeutic agents for pancreatic cancer, thus completing this invention. The 4-aminoquinazoline compound or its salt of this invention can be used as a therapeutic agent for pancreatic cancer.

The application discloses a donkey skin oligopeptide, and an application thereof. The amino acid sequence of the donkey skin oligopeptide is selected from Glu-Thr-Trp-Arg or Ala-Tyr-Phe-Pro-Lys. The donkey skin oligopeptide disclosed by the application has alpha-glucosidase and alpha-amylase inhibitory activity, can assist in reducing blood sugar, has very important significance for developing medicines with blood sugar reducing function, and can be used for preparing alpha-glucosidase, alpha-amylase inhibitors and anti-type 2 diabetes drugs.

This invention provides a benzothiadiazine 1,1-dioxide compound, its preparation method, and its applications. The general structural formula of the benzothiadiazine 1,1-dioxide compound is shown in Formula (I), or its isomers, or pharmaceutically acceptable salts, esters, or prodrugs thereof. The benzothiadiazine 1,1-dioxide compound of this invention has a novel structure, can selectively inhibit HDAC6 enzyme, has a strong protective effect on nerve cells, low toxicity, and low potential cardiotoxicity, and is expected to be used as a neuroprotective agent for the treatment of neurodegenerative diseases.

The application discloses antibacterial application of repaglinide, relates to the technical field of medicines, and comprises prediction of antibacterial activity of a compound and evaluation of structural novelty of the compound, and specifically comprises the following steps: step 1, collecting and collating high-throughput data of antibacterial activity to form antibacterial activity benchmark data; step 2, generating Daylight molecular fingerprint features of benchmark compounds by using Pybel and PyDPI and constructing an activity prediction model; step 3, predicting and evaluating antibacterial activity and structural novelty of a to-be-tested compound by using the model and fmcsR; and step 4, experimentally verifying repaglinide with high potential. The application can provide important ideas and guidance for research and development of novel antibacterial drugs, and more importantly, provides a novel antibacterial active compound repaglinide with low toxicity to cope with the increasingly serious crisis of bacterial drug resistance.