942142-91-8Relevant academic research and scientific papers
Optimization of orally bioavailable alkyl amine renin inhibitors
Xu, Zhenrong,Cacatian, Salvacion,Yuan, Jing,Simpson, Robert D.,Jia, Lanqi,Zhao, Wei,Tice, Colin M.,Flaherty, Patrick T.,Guo, Joan,Ishchenko, Alexey,Singh, Suresh B.,Wu, Zhongren,McKeever, Brian M.,Scott, Boyd B.,Bukhtiyarov, Yuri,Berbaum, Jennifer,Mason, Jennifer,Panemangalore, Reshma,Cappiello, Maria Grazia,Bentley, Ross,Doe, Christopher P.,Harrison, Richard K.,McGeehan, Gerard M.,Dillard, Lawrence W.,Baldwin, John J.,Claremon, David A.
scheme or table, p. 694 - 699 (2010/06/16)
Structure-guided drug design led to new alkylamine renin inhibitors with improved in vitro and in vivo potency. Lead compound 21a, has an IC50 of 0.83 nM for the inhibition of human renin in plasma (PRA). Oral administration of 21a at 10 mg/kg
Design and optimization of renin inhibitors: Orally bioavailable alkyl amines
Tice, Colin M.,Xu, Zhenrong,Yuan, Jing,Simpson, Robert D.,Cacatian, Salvacion T.,Flaherty, Patrick T.,Zhao, Wei,Guo, Joan,Ishchenko, Alexey,Singh, Suresh B.,Wu, Zhongren,Scott, Boyd B.,Bukhtiyarov, Yuri,Berbaum, Jennifer,Mason, Jennifer,Panemangalore, Reshma,Cappiello, Maria Grazia,Mueller, Dominik,Harrison, Richard K.,McGeehan, Gerard M.,Dillard, Lawrence W.,Baldwin, John J.,Claremon, David A.
scheme or table, p. 3541 - 3545 (2010/03/31)
Structure-based drug design led to the identification of a novel class of potent, low MW alkylamine renin inhibitors. Oral administration of lead compound 21l, with MW of 508 and IC50 of 0.47 nM, caused a sustained reduction in mean arterial bl
ASPARTIC PROTEASE INHIBITORS
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Page/Page column 145-146, (2010/11/27)
The present invention is directed to aspartic protease inhibitors. Certain aspartic protease inhibitors of the invention can be represented by the following structural formula or a pharmaceutically acceptable salt thereof. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.
