1307795-85-2Relevant academic research and scientific papers
3,4-Diarylpiperidines as potent renin inhibitors
Lacombe, Patrick,Arbour, Mélissa,Aspiotis, Renée,Cauchon, Elizabeth,Chen, Austin,Dubé, Daniel,Falgueyret, Jean-Pierre,Fournier, Pierre-André,Gallant, Michel,Grimm, Erich,Han, Yongxin,Juteau, Hélne,Liu, Suzanna,Mellon, Christophe,Ramtohul, Yeeman,Simard, Daniel,St-Jacques, René,Tsui, Gavin Chit
, p. 1953 - 1957 (2012/04/04)
The discovery and SAR of a series of potent renin inhibitors possessing a novel 3,4-diarylpiperidine scaffold are described herein. The resulting compound 38 exhibit low nanomolar plasma renin IC50, had a clean CYP 3A4 profile and displayed mic
SPIROCYCLIC PIPERIDINE DERIVATIVES USEFUL AS RENIN INHIBITORS
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Page/Page column 43, (2011/06/16)
Renin inhibitors which are spirocyclic piperidine derivatives, of formula (I) and pharmaceutical compositions thereof useful in the treatment of cardiovascular diseases and renal insufficiency. or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable salt of the stereoisomer thereof, wherein: n, for each instance in which it occurs, is independently 0, 1, or 2; W is a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring, A is (i) a five- or six-membered saturated or unsaturated heterocyclic or carbocyclic monocyclic ring or (ii) a first five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring which is fused to a second five- or six-membered saturated or unsaturated heterocyclic or carbocyclic ring, V is -(C=O)-, -CH2- or =CH-; U is a bond or -CH2-, or, 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)-.
