216099-46-6Relevant articles and documents
Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account
Wu, Frank,Büttner, Frank H.,Chen, Rhonda,Hickey, Eugene,Jakes, Scott,Kaplita, Paul,Kashem, Mohammed A.,Kerr, Steven,Kugler, Stanley,Paw, Zofia,Prokopowicz, Anthony,Shih, Cheng-Kon,Snow, Roger,Young, Erick,Cywin, Charles L.
scheme or table, p. 3235 - 3239 (2010/08/22)
Two closely related scaffolds were identified through an uHTS campaign as desirable starting points for the development of Rho-Kinase (ROCK) inhibitors. Here, we describe our hit-to-lead evaluation process which culminated in the rapid discovery of potent leads such as 22 which successfully demonstrated an early in vivo proof of concept for anti-hypertensive activity.
RHO KINASE INHIBITORS
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Page/Page column 43, (2008/12/06)
Disclosed are novel substituted 2H-isoquinolin-1-one and 3H-quinazolin-4-one derivatives useful as inhibitors of Rho kinase and for treating a variety of diseases and disorders that are mediated or sustained through the activity of Rho kinase, including c
