944140-65-2

Upstream product

• 170564-98-4 (R)-3-amino-3-phenyl-1-propanol 
• 191544-71-5 1-(tert-butoxycarbonyl)-3-(methoxycarbonyl)piperidine-5-carboxylic acid 
• 534572-17-3 (3R,5S)-1-(tert-butoxycarbonyl)piperidine-3,5-dicarboxylic acid 
• 499-81-0 3,5-Pyridinedicarboxylic acid 
• 944140-66-3 C₂₂H₃₂N₂O₆ 
• 157226-76-1 1-tert-butyl 3,5-dimethyl piperidine-1,3,5-tricarboxylate 

Downstream Products

• 944140-64-1 C₃₇H₅₀N₄O₆ 

Relevant academic research and scientific papers

Structure-based design of substituted piperidines as a new class of highly efficacious oral direct renin inhibitors

A cis-configured 3,5-disubstituted piperidine direct renin inhibitor, (syn,rac)-1, was discovered as a high-throughput screening hit from a target-family tailored library. Optimization of both the prime and the nonprime site residues flanking the central piperidine transition-state surrogate resulted in analogues with improved potency and pharmacokinetic (PK) properties, culminating in the identification of the 4-hydroxy-3,5-substituted piperidine 31. This compound showed high in vitro potency toward human renin with excellent off-target selectivity, 60% oral bioavailability in rat, and dose-dependent blood pressure lowering effects in the double-transgenic rat model.

3 , 5-SUBSTITΓUED PIPERIDINE COMPOUNDS AS RENIN INHIBITORS

The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (= disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3, 5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. The preferred compounds (which can also be present as salts) have the formula (I'), wherein R1 , R2, T, R3 and R4 are as defined in the specification.