Indazoles are a class of organic heterocyclic compounds, also known as 1,2-diazaindene and benzopyrazole. Indazole is a good bioisomer of phenol, which is more lipophilic than phenol and less prone to phase I and II metabolism. Indazole derivatives have a wide range of biological activities, and it has been confirmed that indazole compounds have anti-tumor, analgesic, anti-inflammatory and other drug activities. Anticancer is the most important application field of indazole drugs. Renal cell carcinoma, solid tumor, nausea and vomiting caused by chemotherapy and leukemia are the main indications of this structural backbone drug.
Fluorine is the most electronegative element in the periodic table, and the fluorine atom has a small atomic radius, so fluorine-containing organic compounds have many wonderful properties. For example, the introduction of fluorine atoms or fluorine-containing groups into drug molecules can improve the permeability to cell membranes, metabolic stability and bioavailability; in addition, the introduction of fluorine atoms will improve the lipid solubility of the compound and promote its absorption in the body. The speed of delivery changes the physiological effect. In the field of medicinal chemistry, the introduction of fluorine atoms into organic molecules is an important direction for the development of new anticancer drugs, antitumor drugs, antiviral agents, anti-inflammatory drugs, and central nervous system drugs.
Avistone announced that they received conditional approval from the National Medical Products Administration (NMPA) to commercialize Vebreltinib (Bozitinib) to treat patients with MET exon 14 skipping non-small cell lung cancer (NSCLC) in China. The conditional approval was based on results from a pivotal Phase II KUNPENG study with an objective response rate (ORR) of 75.0% and median progression-free survival (PFS) in patients with advanced METex14 mutations to 14.1 months with a good safety profile as was recently presented at the 2023 European Society for Clinical Oncology (ESMO) Congress in Madrid, Spain. Vebreltinib is a potent, small molecule, orally bioavailable and highly selective c-Met Tyrosine Kinase Inhibitor (TKI). Chemenu has been working to develop more compounds for drug discovery. Here are the building blocks we can provide.
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