1160185-08-9Relevant academic research and scientific papers
Renin inhibitors for the treatment of hypertension: Design and optimization of a novel series of tertiary alcohol-bearing piperidines
Chen, Austin,Cauchon, Elizabeth,Chefson, Amandine,Dolman, Sarah,Ducharme, Yves,Dube, Daniel,Falgueyret, Jean-Pierre,Fournier, Pierre-Andre,Gagne, Sebastien,Gallant, Michel,Grimm, Erich,Han, Yongxin,Houle, Robert,Huang, Jing-Qi,Hughes, Gregory,Juteau, Helene,Lacombe, Patrick,Lauzon, Sophie,Levesque, Jean-Francois,Liu, Susana,MacDonald, Dwight,MacKay, Bruce,McKay, Dan,Percival, M. David,St-Jacques, Rene,Toulmond, Sylvie
, p. 3976 - 3981 (2011)
The design and optimization of a novel series of renin inhibitor is described herein. Strategically, by committing the necessary resources to the development of synthetic sequences and scaffolds that were most amenable for late stage structural diversification, even as the focus of the SAR campaign moved from one end of the molecule to another, highly potent renin inhibitors could be rapidly identified and profiled.
RENIN INHIBITORS
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Page/Page column 36-37, (2011/04/13)
Renin inhibitors, which are spirocyclic piperidine amides, of structural formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency, wherein n, for each instance in which it occurs, is independently 0, 1, or 2; R1 is hydrogen, C1-6 -alkyl or C3-6 -cycloalkyl, wherein said C1-6 -alkyl or C3-6 -cycloalkyl group can be independently substituted with 1-3 halogens; A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to another five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is a bond or -(C=O)-, -CH(OH)-, -CH2- or =CH-; U is a bond or -CH2-, or for the case when V is =CH-, U is -CH=; X is =CH-, =CF-, =C(OR3)-, or -C=O-; and Y is =CH-, =CF-, =N-, or for the case when X is -C=O-, Y is -N(R3)-.
3,4 - SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS
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Page/Page column 30, (2010/06/22)
The present invention relates to 3,4-substituted piperidinyl - based renin inhibitor compounds bearing at 4-position oxopyridine or lsoquinolone and having the formula (I): wherein., S is Formula (IIa) or Formula (IIb). The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency.
RENIN INHIBITORS
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Page/Page column 23, (2009/07/17)
The present invention relates to piperidinyl-based renin inhibitor compounds having the formula containing amino-terminal groups, and their use in treating cardiovascular events and renal insufficiency.
