molecules of the month


oral QD sGC stimulator

Ph. I in healthy volunteers completed

from HTS + optimization

J. Med. Chem., April 11, 2023

Bayer, Wuppertal, DE

BAY-747, sGC, oral QD sGC stimulator, Ph. I in healthy volunteers completed, from HTS + optimization, J. Med. Chem., April 11, 2023, BAYER, WUPPERTAL, DE
5 mins read

Potential for an improved sGC stimulator for resistant hypertension. BAY 1165747 (BAY-747) is a new, structurally distinct, soluble guanylate cyclase (sGC) stimulator with potential in the treatment of resistant hypertension. Identified through ultrahigh-throughput screening, it features an imidazo[1,2-a]pyridine core, distinct from the previously described 2-(1-benzyl-1H-pyrazol-3-yl) pyrimidine sGC stimulators. The property-based design led to an improved human PK profile compared to Bayer’s approved sGC stimulator, riociguat (2013). As Drug Hunter has highlighted previously, treatment-resistant hypertension remains an area with high unmet need, with up to 15M Americans not adequately treated after 3 or more medications. current oral sGC stimulators Current sGC stimulators for hypertension require frequent dosing. To date the only sGC stimulator approved for treatment of hypertension is riociguat, with…

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