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2,3-Diaminopyrazines as rho kinase inhibitors
Alan J. Henderson ,
Mark Hadden ,
Cheng Guo ,
Neema Douglas ,
Helene Decornez ,
Mark R. Hellberg ,
Andrew Rusinko ,
Marsha McLaughlin ,
Naj Sharif ,
Colene Drace ,
Raj Patil
February 2010
February 2010
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Abstract
Inhibition of rho kinase (ROCK) has been recognized as an important target for a number
of diseases, including glaucoma. Herein we report SAR development around two hits
from a kinase library that led to the discovery of the ROCK inhibitor compound 38.
In vitro and in vivo analysis of this compound, including its effects in a monkey
model of glaucoma will be discussed.
Copyright (c) 2009 Elsevier Ltd. All rights reserved.