1174929-07-7Relevant academic research and scientific papers
Discovery and optimization of a new class of potent and non-chiral indole-3-carboxamide-based renin inhibitors
Scheiper, Bodo,Matter, Hans,Steinhagen, Henning,Stilz, Ulrich,B?cskei, Zsolt,Fleury, Valérie,McCort, Gary
scheme or table, p. 6268 - 6272 (2010/11/18)
Selective inhibition of the aspartyl protease renin has gained attraction as an interesting approach to control hypertension and associated cardiovascular risk factors given its unique position in the renin-angiotensin system. Using a combination of high-throughput screening, parallel synthesis, X-ray crystallography and structure-based design, we identified and optimized a novel series of potent and non-chiral indole-3-carboxamides with remarkable potency for renin. The most potent compound 5k displays an IC50 value of 2 nM.
CYCLIC INDOLE-3-CARBOXAMIDES, THEIR PREPARATION AND THEIR USE AS PHARMACEUTICALS
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Page/Page column 61-62, (2009/09/05)
The present invention relates to cyclic indole-3-carboxamides of the Formula (I), wherein A, R, R10, R20, R30, R40, n, p and q have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they inhibit the enzyme renin and modulate the activity of the renin-angiotensin system, and are useful for the treatment of diseases such as hypertension, for example. The invention furthermore relates to processes for the preparation of the compounds of the Formula (I), their use and pharmaceutical compositions comprising them.
