847801-39-2Relevant academic research and scientific papers
Structure-based design and optimization of potent renin inhibitors on 5- or 7-azaindole-scaffolds
Matter, Hans,Scheiper, Bodo,Steinhagen, Henning,B?cskei, Zsolt,Fleury, Valérie,McCort, Gary
, p. 5487 - 5492 (2011/10/12)
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
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Page/Page column 94, (2009/09/05)
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
Substituted indoles as inhibitors of poly (ADP-ribose) polymerase (PARP)
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Page/Page column 24, (2010/02/11)
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.
