- Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure
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The first-in-class soluble guanylate cyclase (sGC) stimulator riociguat was recently introduced as a novel treatment option for pulmonary hypertension. Despite its outstanding pharmacological profile, application of riociguat in other cardiovascular indications is limited by its short half-life, necessitating a three times daily dosing regimen. In our efforts to further optimize the compound class, we have uncovered interesting structure-Activity relationships and were able to decrease oxidative metabolism significantly. These studies resulting in the discovery of once daily sGC stimulator vericiguat (compound 24, BAY 1021189), currently in phase 3 trials for chronic heart failure, are now reported.
- Follmann, Markus,Ackerstaff, Jens,Redlich, Gorden,Wunder, Frank,Lang, Dieter,Kern, Armin,Fey, Peter,Griebenow, Nils,Kroh, Walter,Becker-Pelster, Eva-Maria,Kretschmer, Axel,Geiss, Volker,Li, Volkhart,Straub, Alexander,Mittendorf, Joachim,Jautelat, Rolf,Schirok, Hartmut,Schlemmer, Karl-Heinz,Lustig, Klemens,Gerisch, Michael,Knorr, Andreas,Tinel, Hanna,Mondritzki, Thomas,Trübel, Hubert,Sandner, Peter,Stasch, Johannes-Peter
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p. 5146 - 5161
(2017/06/28)
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