934481-43-3Relevant articles and documents
Discovery of novel indazole derivatives as dual angiotensin II antagonists and partial PPARγ agonists
Lamotte, Yann,Faucher, Nicolas,Sancon, Julien,Pineau, Olivier,Sautet, Stephane,Fouchet, Marie-Helene,Beneton, Veronique,Tousaint, Jean-Jacques,Saintillan, Yannick,Ancellin, Nicolas,Nicodeme, Edwige,Grillot, Didier,Martres, Paul
, p. 1098 - 1103 (2014/03/21)
Identification of indazole derivatives acting as dual angiotensin II type 1 (AT1) receptor antagonists and partial peroxisome proliferator-activated receptor-γ (PPARγ) agonists is described. Starting from Telmisartan, we previously described that indole derivatives were very potent partial PPARγ agonists with loss of AT1 receptor antagonist activity. Design, synthesis and evaluation of new central scaffolds led us to the discovery of pyrrazolopyridine then indazole derivatives provided novel series possessing the desired dual activity. Among the new compounds, 38 was identified as a potent AT1 receptor antagonist (IC50 = 0.006 μM) and partial PPARγ agonist (EC50 = 0.25 μM, 40% max) with good oral bioavailability in rat. The dual pharmacology of compound 38 was demonstrated in two preclinical models of hypertension (SHR) and insulin resistance (Zucker fa/fa rat).
Non-nucleoside reverse transcriptase inhibitors
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Page/Page column 20, (2008/06/13)
The present invention provides for compounds useful for treating an HIV-1 infection, or preventing an HIV-1 infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5 and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds. [image]