207691-65-4Relevant articles and documents
Synthesis of 3-azabicyclo[3.3.1]Nonane-6,9-diones
Williams, Brian D.,Williams, Birute,Bernardoni, Francis,Finn, Robert C.,Zubieta, Jon
, p. 2199 - 2206 (2001)
A one pot synthesis of 3-azabicyclo[3.3.1]nonane-6,9-diones is described via the additibn of acryloyl chloride to enamines of N-carboxy-4 piperidones. Yields of bicycle were highest when additions were made to vigorously boiling solutions of morpholine en
BICYCLIC JAK INHIBITORS AND USES THEREOF
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Paragraph 000361; 000363, (2020/10/20)
Provided herein are compounds of Formulas (I), (II), (III), and (IV) and subformulas thereof, wherein the variables are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I), (II), (III), or (IV) and methods of using the compounds, e.g., in the treatment of immune disorders, inflammatory disorders, and cancer.
Synthesis and evaluation of tetrahydropyrazolopyridine inhibitors of anion exchange protein SLC26A4 (pendrin)
Zhu,Lu, Julia Y.,Tan, Joseph-Anthony,Rivera, Amber A.,Phuan, Puay-Wah,Shatskikh, Marina E.,Son, Jung-Ho,Haggie, Peter M.,Verkman, Alan S.,Kurth, Mark J.
supporting information, p. 2119 - 2123 (2019/07/09)
Pendrin is a transmembrane chloride/anion antiporter that is strongly upregulated in the airways in rhinoviral infection, asthma, cystic fibrosis and chronic rhinosinusitis. Based on its role in the regulation of airway surface liquid depth, pendrin inhibitors have potential indications for treatment of inflammatory airways diseases. Here, a completely regioselective route to tetrahydro-pyrazolopyridine pendrin inhibitors based on 1,3-diketone and substituted hydrazine condensation was been developed. Structure-activity relationships at the tetrahydropyridyl nitrogen were investigated using a focused library, establishing the privileged nature of N-phenyl ureas and improving inhibitor potency by greater than 2-fold.