1093955-41-9

Upstream product

• 1093955-43-1 C₈H₇Cl₂NO₂ 
• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 1830-54-2 3-oxopentanedioic acid dimethyl ester 
• 887572-34-1 2-chloro-4-ethoxypyridine-5-carboxylic acid 
• 73027-79-9 4,6-dichloro-nicotinic acid 
• 65973-52-6 methyl 4,6-dichloropyridine-3-carboxylate 
• 79398-27-9 methyl 4,6-dihydroxypyridine-3-carboxylate 

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.

ORGANIC COMPOUNDS

The present invention relates to a compound of the formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, 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 a compound of that class; a method of treatment comprising administering a compound of that class and a method for its manufacture.