Details

Autor(en) / Beteiligte

• 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

Titel

Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure

Ist Teil von

• Journal of medicinal chemistry, 2017-06, Vol.60 (12), p.5146-5161

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2017

Quelle

MEDLINE

Beschreibungen/Notizen

• 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.