In an article, author is Melot, Romain, once mentioned the application of 142-25-6, Safety of N1,N1,N2-Trimethylethane-1,2-diamine, Name is N1,N1,N2-Trimethylethane-1,2-diamine, molecular formula is C5H14N2, molecular weight is 102.18, MDL number is MFCD00014874, category is amides-buliding-blocks. Now introduce a scientific discovery about this category.
Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2
A search for structurally diversified Tyk2 JH2 ligands from 6 (BMS-986165), a pyridazine carboxamide-derived Tyk2 JH2 ligand as a clinical Tyk2 inhibitor currently in late development for the treatment of psoriasis, began with a survey of six-|membered heteroaryl groups in place of the N-methyl triazolyl moiety in 6. The X-ray co-crystal structure of an early lead (12) revealed a potential new binding pocket. Exploration of the new pocket resulted in two frontrunners for a clinical candidate. The potential hydrogen bonding interaction with ThrS99 in the pocket was achieved with a tertiary amide moiety, confirmed by the X-ray co-crystal structure of 29. When the diversity search was extended to nicotinamides, a single fluorine atom addition was found to significantly enhance the permeability, which directly led to the discovery of 7 (BMS-986202) as a clinical Tyk2 inhibitor that binds to Tyk2 JH2. The preclinical studies of 7, including efficacy studies in mouse models of IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus, will also be presented.
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