2,3-Diaminopyrazines as rho kinase inhibitors |
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| Authors: | Alan J Henderson Mark Hadden Cheng Guo Neema Douglas Helene Decornez Mark R Hellberg Andrew Rusinko Marsha McLaughlin Naj Sharif Colene Drace Raj Patil |
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| Institution: | 1. AMRI, 26 Corporate Circle, PO Box 15098, Albany, NY 12212-5098, USA;2. Alcon Laboratories Inc., 6201 South Freeway, Fort Worth, TX 76134-2099, USA |
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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. |
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