1001185-45-0Relevant articles and documents
Discovery and pharmacological evaluation of a novel series of adamantyl cyanoguanidines as P2X7 receptor antagonists
O'Brien-Brown, James,Jackson, Alexander,Reekie, Tristan A.,Barron, Melissa L.,Werry, Eryn L.,Schiavini, Paolo,McDonnell, Michelle,Munoz, Lenka,Wilkinson, Shane,Noll, Benjamin,Wang, Shudong,Kassiou, Michael
, p. 433 - 439 (2017)
Here we report adamantyl cyanoguanidine compounds based on hybrids of the adamantyl amide scaffold reported by AstraZeneca and cyanoguanidine scaffold reported by Abbott Laboratories. Compound 27 displayed five-fold greater inhibitory potency than the lea
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.
KINASE INHIBITORS, COMPOSITIONS COMPRISING THEM, AND METHODS OF THEIR USE
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Page/Page column 10, (2009/03/07)
Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use
