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. (C) 2009 Elsevier Ltd. All rights reserved.
DOI:
10.1016/j.bmcl.2009.12.012
作为产物:
描述:
2-氯吡嗪 、 C.I.酸性橙108 以
methanol-dichloromethane 为溶剂,
以to give the title compound (1.21 g, 8.70 mmol, yield: 99%) of yellow liquid form的产率得到2,2'-Hydroxyethylaminopyrazin
The present invention relates to a fused heterocyclic compound having the Formula 1, which is useful as a platelet aggregation inhibitor, a method for preparing the same, and a pharmaceutical composition for inhibiting platelet aggregation comprising the same.
Aminopyrazine analogs for treating glaucoma and other rho kinase-mediated diseases and conditions
申请人:Hellberg R. Mark
公开号:US20060142307A1
公开(公告)日:2006-06-29
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.
AMINOPYRAZINE ANALOGS FOR TREATING GLAUCOMA AND OTHER RHO KINASE-MEDIATED DISEASES AND CONDITIONS
申请人:Hellberg Mark
公开号:US20080269249A2
公开(公告)日:2008-10-30
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.