853763-68-5Relevant academic research and scientific papers
KINASE INHIBITORS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE
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Page/Page column 9, (2009/03/07)
Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use
Novel class of LIM-kinase 2 inhibitors for the treatment of ocular hypertension and associated glaucoma
Harrison, Bryce A.,Whitlock, N. Andrew,Voronkov, Michael V.,Almstead, Zheng Y.,Gu, Kun-Jian,Mabon, Ross,Gardyan, Michael,Hamman, Brian D.,Allen, Jason,Gopinathan, Suma,McKnight, Beth,Crist, Mike,Zhang, Yulian,Liu, Ying,Courtney, Lawrence F.,Key, Billie,Zhou, Julia,Patel, Nita,Yates, Phil W.,Liu, Qingyun,Wilson, Alan G. E.,Kimball, S. David,Crosson, Craig E.,Rice, Dennis S.,Rawlins, David B.
supporting information; experimental part, p. 6515 - 6518 (2010/03/31)
The discovery of a pyrrolopyrimidine class of LIM-kinase 2 (LIMK2) inhibitors is reported. These LIMK2 inhibitors show good potency in enzymatic and cellular assays and good selectivity against ROCK. After topical dosing to the eye in a steroid induced mouse model of ocular hypertension, the compounds reduce intraocular pressure to baseline levels. The compounds also increase outflow facility in a pig eye perfusion assay. These results suggest LIMK2 may be an effective target for treating ocular hypertension and associated glaucoma.
