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.
Henderson, Alan J.,Hadden, Mark,Guo, Cheng,Douglas, Neema,Decornez, Helene,Hellberg, Mark R.,Rusinko, Andrew,McLaughlin, Marsha,Sharif, Naj,Drace, Colene,Patil, Raj
scheme or table
p. 1137 - 1140
(2010/06/15)
Aminopyrazine analogs for treating glaucoma and other rho kinase-mediated diseases and conditions
Methods for using aminopyrazine analogs to treat rho kinase-mediated diseases or rho kinase-mediated conditions, including controlling intraocular pressure and treating glaucoma, are disclosed. Ophthalmic pharmaceutical compositions useful in the treatment of eye diseases such as glaucoma, and additionally useful for controlling intraocular pressure, the compositions comprising an effective amount of aminopyrazine analogs, are also disclosed.
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Page/Page column 5-6
(2008/06/13)
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