| Literature DB >> 28557445 |
Markus Follmann1, Jens Ackerstaff1, Gorden Redlich1, Frank Wunder1, Dieter Lang1, Armin Kern1, Peter Fey1, Nils Griebenow1, Walter Kroh1, Eva-Maria Becker-Pelster1, Axel Kretschmer1, Volker Geiss1, Volkhart Li1, Alexander Straub1, Joachim Mittendorf1, Rolf Jautelat1, Hartmut Schirok1, Karl-Heinz Schlemmer1, Klemens Lustig1, Michael Gerisch1, Andreas Knorr1, Hanna Tinel1, Thomas Mondritzki1, Hubert Trübel1, Peter Sandner1, Johannes-Peter Stasch1.
Abstract
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.Entities:
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Year: 2017 PMID： 28557445 DOI： 10.1021/acs.jmedchem.7b00449
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446