23596-33-0

Upstream product

• 271-34-1 5-azaindole 
• 591-50-4 iodobenzene 

Downstream Products

• 1175014-84-2 2-chloro-1-phenyl-1H-pyrrolo[3,2-c]pyridine-3-carbaldehyde 
• 1175014-87-5 4-[2-(5-fluoro-2-methyl-phenoxy)-1-phenyl-1H-pyrrolo[3,2-c]pyridine-3-carbonyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 1175014-88-6 4-(2-benzyl-1-phenyl-1H-pyrrolo[3,2-c]pyridine-3-carbonyl)-piperazine-1-carboxylic acid tert-butyl ester 
• 1175014-89-7 4-[2-(2-methyl-benzyl)-1-phenyl-1H-pyrrolo[3,2-c]pyridine-3-carbonyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 1175014-91-1 4-[2-(3-fluoro-2-methyl-benzyl)-1-phenyl-1H-pyrrolo[3,2-c]pyridine-3-carbonyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 1175014-90-0 4-[2-(2-chloro-6-fluoro-benzyl)-1-phenyl-1H-pyrrolo[3,2-c]pyridine-3-carbonyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 1175014-19-3 C₂₅H₂₄N₄O₂ 
• 1175142-59-2 C₂₅H₂₃FN₄O₂ 
• 1175014-21-7 C₂₅H₂₃FN₄O₂ 
• 1175014-23-9 C₂₅H₂₂F₂N₄O₂ 
• 1175013-01-0 C₂₅H₂₄N₄O 
• 1175013-03-2 C₂₆H₂₆N₄O 
• 1175142-60-5 C₂₆H₂₅FN₄O 
• 1175013-05-4 C₂₅H₂₂ClFN₄O 

Relevant academic research and scientific papers

Structure-based design and optimization of potent renin inhibitors on 5- or 7-azaindole-scaffolds

The selective inhibition of the aspartyl protease renin is of high interest to control hypertension and associated cardiovascular risk factors. Following on preceding contributions, we report herein on the optimization of two series of azaindoles to arrive at potent and non-chiral renin inhibitors. The previously discovered azaindole scaffold was further explored by structure-based drug design in combination with parallel synthesis. This results in the identification of novel 5- or 7-azaindole derivatives with remarkable potency for renin inhibition. The best compounds on both series show IC50 values between 3 and 8 nM.

CYCLIC AZAINDOLE-3-CARBOXAMIDES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS

The present invention relates to cyclic azaindole-3-carboxamides of the formula (I) wherein A, R, R10, R20, R30, R40, Y1, Y2, Y3, Y4, n, p and q have the meanings indi