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.
PIPERAZINE DERIVATIVES FOR TREATMENT OF AD AND RELATED CONDITIONS
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Page/Page column 63, (2008/12/08)
Compounds of formula (I) selectively inhibitproduction of Aβ(1-42) and hence find use in treatment of Alzheimer's disease and other conditions associated with deposition ofA(β) in the brain.
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.
Synthesis and cytotoxicity evaluation of novel indolylpyrimidines and indolylpyrazines as potential antitumor agents
Jiang, Biao,Yang, Cai-Guang,Xiong, Wen-Nan,Wang, Jun
, p. 1149 - 1154 (2007/10/03)
Novel indolylpyrimidines and indolylpyrazines have been synthesized as potential antitumor agents. They were screened in a panel of 60 human tumor cell lines in vitro. Compounds 7, 9, 10, 15, 21 exhibited efficiently cytotoxic activities with GI50 values in the low micromolar range against a variety of human cancer cell lines. 2,4-Bis(3′-indolyl)pyrimidine 8 displayed selective cytotoxic activity against IGROV1 tumor cell line with the GI50 value below 0.01 μM.
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.