Novel compounds possessing potent cAMP and cGMP phosphodiesterase inhibitory activity. Synthesis and cardiovascular effects of a series of imidazo[1,2-a]quinoxalinones and imidazo[1,5-a]quinoxalinones and their aza analogs
摘要:
A series of novel imidazoquinoxalinones and their aza analogues were prepared by the cyclization of o-amino(H-1-imidazol-1-yl)aryls and heteroaryls with carbonyldiimidazole. The compounds were screened for inhibition of Type I and Type IV phosphodiesterases (PDE's) and evaluated for their vasorelaxant and positive inotropic activities in vitro. In general, compounds having potent PDE inhibitory activity also possessed good inotropic and vasodilator activity, although linear correlations between these activities could not be established.
[EN] JAK1 SELECTIVE KINASE INHIBITOR<br/>[FR] INHIBITEUR SÉLECTIF DE KINASE JAK1
申请人:DIZAL JIANGSU PHARMACEUTICAL CO LTD
公开号:WO2020211839A1
公开(公告)日:2020-10-22
Disclosed herein are compounds of Formula (I), and pharmaceutically acceptable salts thereof, that are useful as JAK kinase inhibitors. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula (I), and methods of using such compounds or compositions to treat respiratory conditions (e.g., asthma or COPD).
Novel compounds possessing potent cAMP and cGMP phosphodiesterase inhibitory activity. Synthesis and cardiovascular effects of a series of imidazo[1,2-a]quinoxalinones and imidazo[1,5-a]quinoxalinones and their aza analogs
作者:David D. Davey、P. W. Erhardt、E. H. Cantor、S. S. Greenberg、W. R. Ingebretsen、J. Wiggins
DOI:10.1021/jm00113a002
日期:1991.9
A series of novel imidazoquinoxalinones and their aza analogues were prepared by the cyclization of o-amino(H-1-imidazol-1-yl)aryls and heteroaryls with carbonyldiimidazole. The compounds were screened for inhibition of Type I and Type IV phosphodiesterases (PDE's) and evaluated for their vasorelaxant and positive inotropic activities in vitro. In general, compounds having potent PDE inhibitory activity also possessed good inotropic and vasodilator activity, although linear correlations between these activities could not be established.
Lampe, John W.; Meo, Susan V. Di; Traina, Joseph A., Journal of Heterocyclic Chemistry, 1994, vol. 31, # 2, p. 287 - 292
作者:Lampe, John W.、Meo, Susan V. Di、Traina, Joseph A.