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. 2020 Aug 15;30(16):127298.
doi: 10.1016/j.bmcl.2020.127298. Epub 2020 Jun 1.

Discovery of the potent non-steroidal glucocorticoid receptor modulator BAY 1003803 as clinical candidate

Markus Berger  1 , Ekkehard May  2 , Hartmut Rehwinkel  3 , Heike Schäcke  4 , Roland Neuhaus  5 , Antje Rottmann  5 , Thomas M Zollner  4 , Stefan Jaroch  6
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Free article

Discovery of the potent non-steroidal glucocorticoid receptor modulator BAY 1003803 as clinical candidate

Markus Berger et al. Bioorg Med Chem Lett. .
Free article

Abstract

We report on the discovery of the new clinical candidate BAY 1003803 as glucocorticoid receptor agonist for the topical treatment of psoriasis or severe atopic dermatitis. In the course of optimizing the amino alcohol series as a highly potent new non-steroidal lead structure, considerations were made as to how physicochemical properties and safety concerns relate to structural motifs. BAY 1003803 demonstrates strong anti-inflammatory activity in vitro paired with a pharmacokinetic profile suitable for topical application.

Keywords: Amino alcohol; Glucocorticoid; SEGRA; Transactivation; Transrepression.

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Conflict of interest statement

Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

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