The author of 《Identification of 2-Imidazopyridine and 2-Aminopyridone Purinones as Potent Pan-Janus Kinase (JAK) Inhibitors for the Inhaled Treatment of Respiratory Diseases》 were Bach, Jordi; Eastwood, Paul; Gonzalez, Jacob; Gomez, Elena; Alonso, Juan Antonio; Fonquerna, Silvia; Lozoya, Estrella; Orellana, Adela; Maldonado, Monica; Calaf, Elena; Alberti, Joan; Perez, Juan; Andres, Ana; Prats, Neus; Carreno, Cristina; Calama, Elena; De Alba, Jorge; Calbet, Marta; Miralpeix, Montserrat; Ramis, Isabel. And the article was published in Journal of Medicinal Chemistry in 2019. Reference of trans-4-Aminocyclohexanol The author mentioned the following in the article:
Janus kinases (JAKs) have a key role in regulating the expression and function of relevant inflammatory cytokines involved in asthma and chronic obstructive pulmonary disease. Herein are described the design, synthesis, and pharmacol. evaluation of a series of novel purinone JAK inhibitors with profiles suitable for inhaled administration. Replacement of the imidazopyridine hinge binding motif present in the initial compounds of this series with a pyridone ring resulted in the mitigation of cell cytotoxicity. Further systematic structure-activity relationship (SAR) efforts driven by structural biol. studies led to the discovery of pyridone I, a potent pan-JAK inhibitor with good selectivity, long lung retention time, low oral bioavailability, and proven efficacy in the lipopolysaccharide-induced rat model of airway inflammation by the inhaled route. The experimental process involved the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9Reference of trans-4-Aminocyclohexanol)
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Reference of trans-4-Aminocyclohexanol
Referemce:
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