1026786-89-9

Upstream product

• 18162-48-6 tert-butyldimethylsilyl chloride 
• 1026786-87-7 3-((tert-butyl(dimethyl)silyl)oxy)-5-[(1E)-3-methoxy-prop-1-en-1-yl]-benzaldehyde 
• 765-30-0 Cyclopropylamine 
• 199177-26-9 3-bromo-5-hydroxybenzaldehyde 
• 626-41-5 3,5-dibromophenol 
• 1026786-84-4 3-hydroxy-5-[(1E)-3-(methyloxy)-1-propen-1-yl]benzaldehyde 

Downstream Products

• 1303607-06-8 C₄₃H₅₇Cl₂N₃O₇ 
• 1303607-34-2 C₃₉H₅₁Cl₂N₃O₇S 
• 1303607-36-4 C₄₁H₅₄Cl₂N₄O₆ 
• 1026787-25-6 (3R,4S)-N-cyclopropyl-4-(4-(2-(2,6-dichloro-4-methylphenoxy)ethoxy)-phenyl)-N-[3-(2-hydroxy-2-methyl-propoxy)-5-(3-methoxypropyl)benzyl]piperidine-3-carboxamide 
• 1087347-11-2 ethyl (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-carboxylate 
• 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 
• 1303607-09-1 C₄₅H₅₆Cl₂N₂O₉ 
• 1303607-11-5 C₄₄H₅₅Cl₂N₃O₈ 
• 1303607-13-7 C₄₅H₅₆Cl₂N₂O₁₀ 
• 1303607-15-9 C₄₆H₅₈Cl₂N₂O₉ 
• 1303607-17-1 C₄₆H₅₂Cl₂N₂O₁₂ 
• 1087347-18-9 (3R,4S)-4-{4-[2-(2,6-dichloro-4-methylphenoxy)ethoxy]phenyl}piperidine-3-carboxylic acid (cyclopropyl)(3-(3-methoxypropyl)-5-{[1-(2H-tetrazol-5-ylmethyl)cyclopropyl]methoxy}benzyl)amide 
• 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 
• 1026787-28-9 tert-butyl (3R,4S)-3-(((3-((1-(cyanomethyl)cyclopropyl)methoxy)-5-(3-methoxypropyl)-benzyl)(cyclopropyl)amino)carbonyl)-4-(4-(2-(2,6-dichloro-4-methylphenoxy)ethoxy)phenyl)-piperidine-1-carboxylate 

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.

RENIN INHIBITORS

The present invention relates to disubstituted piperidinyl renin inhibitor compounds having the structure (Formula I) and their use in treating cardiovascular events and renal insufficiency.

RENIN INHIBITORS

The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.