84539-07-1Relevant articles and documents
2,3-Diaminopyrazines as rho kinase inhibitors
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)
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.
Aminopyrazine analogs for treating glaucoma and other rho kinase-mediated diseases and conditions
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Page/Page column 4-5; 19, (2008/06/13)
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.
Bromination of Some Pyridine and Diazine N-Oxides
Paudler, William W.,Jovanovic, Misa V.
, p. 1064 - 1069 (2007/10/02)
Selected monosubstituted pyridines, pyrazines, pyrimidines, and their N-oxides, having an electron-donating substituent, were successfully brominated under very mild conditions.The N-oxide function itself is not sufficient to cause these ?-deficient systems to undergo electrophilic aromatic halogenation.Only strongly electron-donating substituents (amino groups) activate the heterocyclic nucleus toward bromination.These substituents direct the electrophilic substitution ortho/para to them with or without the N-oxide group present.Pyridine and diazines with moderately activating substituents such as alkoxy groups are brominated only when their ortho/para activation is augmented by the activation of the N-oxide funtion.Failure to brominate 5-methoxypyrimidine 1-oxide may well reflect the greater ? deficiency of the pyrimidine ring.