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  • Title: 1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as potent GR antagonists with reduced hERG inhibition and an improved pharmacokinetic profile.
    Author: Hunt HJ, Belanoff JK, Golding E, Gourdet B, Phillips T, Swift D, Thomas J, Unitt JF, Walters I.
    Journal: Bioorg Med Chem Lett; 2015 Dec 15; 25(24):5720-5. PubMed ID: 26546213.
    Abstract:
    We report the further optimization of our series 1H-pyrazolo[3,4-g]hexahydro-isoquinoline sulfonamides as GR antagonists. By incorporating a heteroaryl ketone group at the ring junction, we have obtained compounds with excellent functional GR antagonism. Optimization of the sulfonamide substituent has provided compounds with a very desirable overall profile, including minimal hERG activity, good bioavailability and in vivo efficacy.
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