Pyridine is a six-membered heterocyclic compound containing one nitrogen heteroatom. Pyridine and piperidine are the most frequently occurring heterocyclic building blocks in drug molecules. According to incomplete statistics, there are currently more than 180 drugs containing pyridine or piperidine structure that have been marketed, nearly 1/5 of the drugs approved for marketing in recent years contain these two structures.
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Pyridine is a basic heterocyclic organic compound with the chemical formula C5H5N. It is structurally related to benzene, with one methine group (=CH−) replaced by a nitrogen atom. It is a highly flammable, weakly alkaline, water-miscible liquid with a distinctive, unpleasant fish-like smell.
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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Diabetes Care, a peer-reviewed journal of the American Diabetes Association publishes the data from Lexicon’s RELIEF-DPN 1 phase 2 study of LX9211. Adaptor-Associated Kinase 1 (AAK1) is linked to clathrin-mediated endocytosis, and plays a critical role in neuropathic pain and various neurological disorders.
Lexicon’s LX9211 is a selective small molecule inhibitor of AAK1, that is developed as a novel non-opioid approach to neuropathic pain. LX9211 is designed to become an efficacious treatment for moderate-to-severe pain due to diabetic peripheral neuropathic pain (DPNP), which is difficult to manage with current approved medications.
LX9211 is in late-stage development, and the patient enrollment of Phase 2b study will be completed by 2024. Its top-line data is expected in Q2 2025. Lexicon received Fast Track Designation from the FDA for LX9211 in DPNP in 2020.
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