884512-56-5Relevant academic research and scientific papers
Discovery of VTP-27999, an alkyl amine renin inhibitor with potential for clinical utility
Jia, Lanqi,Simpson, Robert D.,Yuan, Jing,Xu, Zhenrong,Zhao, Wei,Cacatian, Salvacion,Tice, Colin M.,Guo, Joan,Ishchenko, Alexey,Singh, Suresh B.,Wu, Zhongren,McKeever, Brian M.,Bukhtiyarov, Yuri,Johnson, Judith A.,Doe, Christopher P.,Harrison, Richard K.,McGeehan, Gerard M.,Dillard, Lawrence W.,Baldwin, John J.,Claremon, David A.
, p. 747 - 751 (2011/12/01)
Structure guided optimization of a series of nonpeptidic alkyl amine renin inhibitors allowed the rational incorporation of additional polar functionality. Replacement of the cyclohexylmethyl group occupying the S1 pocket with a (R)-(tetrahydropyran-3-yl)
RENIN INHIBITORS
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Page/Page column 28, (2010/08/07)
Disclosed are aspartic protease inhibitors represented by the following structural formula: and pharmaceutically acceptable salts thereof. These compounds are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the t
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
PIPERIDINE AND MORPHOLINE RENIN INHIBITORS
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, (2008/06/13)
Described are compounds which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with renin activity. Also described are methods of use of these compounds for treating or ameliorating a renin mediated disorder in a subject.
DIAMINOPROPANOL RENIN INHIBITORS
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, (2008/06/13)
Described are diaminopropanols of which are orally active and bind to renin to inhibit its activity. They are useful in the treatment or amelioration of diseases associated with elevated levels of renin activity or in the treatment of aspartic protease me
ASPARTIC PROTEASE INHIBITORS
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Page/Page column 129, (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.
