1087347-11-2

Upstream product

• 199177-26-9 3-bromo-5-hydroxybenzaldehyde 
• 13949-93-4 (+/-)-ethyl trans-2-formyl-1-cyclopropanecarboxylate 
• 626-41-5 3,5-dibromophenol 
• 1026787-16-5 tert-butyl (3R,4S)-3-{[[3-hydroxy-5-(3-methoxypropyl)benzyl](cyclopropyl)amino]carbonyl}-4-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}piperidine-1-carboxylate 
• 1303607-08-0 C₄₇H₆₀Cl₂N₂O₉ 
• 1026787-15-4 tert-butyl (3R,4S)-3-({[3-{[(tert-butyl)(dimethyl)silyl]oxy}-5-(3-methoxypropyl)benzyl](cyclopropyl)amino}carbonyl)-4-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}piperidine-1-carboxylate 
• 921630-48-0 [(3-{[(tert-butyl)(dimethyl)silyl]oxy}-5-{3-methoxypropyl}benzyl)amino]cyclopropane 
• 1026786-89-9 [(3-{[(tert-butyl)(dimethyl)silyl]oxy}-5-{(1E)-3-methoxyprop-1-en-1-yl}benzyl)amino]cyclopropane 
• 1026786-87-7 3-((tert-butyl(dimethyl)silyl)oxy)-5-[(1E)-3-methoxy-prop-1-en-1-yl]-benzaldehyde 
• 1026786-84-4 3-hydroxy-5-[(1E)-3-(methyloxy)-1-propen-1-yl]benzaldehyde 
• 109716-55-4 ethyl (1S,2S)-2-(hydroxymethyl)cyclopropane-1-carboxylate 

Downstream Products

• 1087347-12-3 (1S,2S)-2-{[3-({cyclopropyl[((3R,4S)-4-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}piperidin-3-yl)carbonyl]amino}methyl)-5-(3-methoxypropyl)phenoxy]methyl}cyclopropane-1-carboxylic acid 
• 1303607-17-1 C₄₆H₅₂Cl₂N₂O₁₂ 

Relevant academic research and scientific papers

The discovery and synthesis of potent zwitterionic inhibitors of renin

The incorporation of a carboxylic acid within in a series of 3-amido-4-aryl substituted piperidines (represented by general structure 32) led to the discovery of potent, zwitterionic, renin inhibitors with improved off-target profiles (CYP3A4 time-dependent inhibition and hERG affinity) relative to analogous non-zwitterionic inhibitors of the past (i.e., 3). Strategies to address the oral absorption of these zwitterions are also discussed within.

NOVEL CASE OF RENIN INHIBITORS

The present invention relates to piperidine-based renin inhibitor compounds having carboxylate or carboxylic acid terminal groups. The disclosed low molecular weight, orally active renin inhibitors are of non-peptide nature and have long duration of action. The compounds can be used in the treatment of cardiovascular events and renal insufficiency.