847801-94-9

Upstream product

• 847801-92-7 2-chloro-1H-pyrrolo[2,3-c]pyridine-3-carboxaldehyde 
• 98-80-6 phenylboronic acid 
• 271-29-4 6-azaindole 
• 1175014-98-8 1-phenyl-1H-pyrrolo[2,3-c]pyridine 
• 1175014-99-9 1-phenyl-1,3-dihydro-pyrrolo[2,3-c]pyridin-2-one 
• 591-50-4 iodobenzene 

Downstream Products

• 1175015-04-9 4-[2-(3-fluoro-2-methyl-benzyl)-1-phenyl-1H-pyrrolo[2,3-c]pyridine-3-carbonyl]-piperazine-1-carboxylic acid tert-butyl ester 
• 1175015-03-8 4-(2-benzyl-1-phenyl-1H-pyrrolo[2,3-c]pyridine-3-carbonyl)-piperazine-1-carboxylic acid tert-butyl ester 
• 1175015-01-6 4-(2-chloro-1-phenyl-1H-pyrrolo[2,3-c]pyridine-3-carbonyl)-piperazine-1-carboxylic acid tert-butyl ester 
• 1175015-00-5 2-chloro-1-phenyl-1H-pyrrolo[2,3-c]pyridine-3-carboxylic acid 

Relevant academic research and scientific papers

Structure-based optimization of potent 4- and 6-azaindole-3-carboxamides as renin inhibitors

The control of hypertension and associated cardiovascular risk factors is possible by selective inhibition of the aspartyl protease renin due to its unique position in the renin-angiotensin system. Starting from a previously disclosed series of potent and nonchiral indole-3-carboxamides, we further explored this motif by structure-based drug design guided by X-ray crystallography in combination with efficient parallel synthesis. This resulted in the discovery of 4- or 6-azaindole derivatives with remarkable potency for renin inhibition. The best compound from these series showed an IC50 value of 1.3 nM.

Substituted indoles as inhibitors of poly (ADP-ribose) polymerase (PARP)

The present invention relates to a series of substituted indole derivatives of the formula I: wherein R, R1, R2, R3, R4, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are inhibitors of poly(adenosine 5′-diphosphate ribose) polymerase (PARP) and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases, including diseases associated with the central nervous system and cardiovascular disorders.