Pyrazoles are organic compounds of the general formula C3H3N2H. It is a five-membered heterocycle consisting of three carbon atoms and two adjacent nitrogen atoms. As an H-bond-donating heterocycle, pyrazole has been used as a more lipophilic and metabolically more stable bioisomer of phenol. Pyrazoles have attracted more and more attention due to their broad spectrum of action and strong efficacy.
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Boronic acids and boronate esters are commonly used reagents in Suzuki–Miyaura coupling chemistry. Organoboron derivatives are common reagents for C–C bond formation, either through classical palladium-mediated transformations or through other newer coupling methods. Boronic esters and acids are potential intermediates in the manufacture of many active pharmaceutical ingredients (API).
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Cyclopropane is the smallest cyclic compound with unique structural features and physicochemical properties, which is widely used in the design of small molecule drugs. In drug design, it is often used to increase activity, fix conformation and improve PK and water solubility. The introduction of cyclopropyl groups into drugs can change various properties of molecules, such as improving metabolic stability; increasing biological activity; enhancing drug efficacy; limiting polypeptide conformation and slowing down its hydrolysis; reducing plasma clearance; improving drug dissociation and many more. Cyclopropane rings are widely found in marketed drugs, including cardiovascular drugs, central nervous system (CNS) drugs, anticancer drugs, autoimmune and anti-inflammatory 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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