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

Authors :: Berger M
May E
Rehwinkel H
Schäcke H
Neuhaus R
Rottmann A
Zollner TM
Jaroch S
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2020 Aug 15; Vol. 30 (16), pp. 127298. Date of Electronic Publication: 2020 Jun 01.
Publication Year :: 2020
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.<br />Competing Interests: 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.<br /> (Copyright © 2020 The Authors. Published by Elsevier Ltd.. All rights reserved.)

Subjects :: Animals
Anti-Inflammatory Agents, Non-Steroidal chemical synthesis
Anti-Inflammatory Agents, Non-Steroidal chemistry
Dogs
Dose-Response Relationship, Drug
Female
Hepatocytes drug effects
Hepatocytes metabolism
Male
Molecular Structure
Rats
Receptors, Glucocorticoid metabolism
Structure-Activity Relationship
Anti-Inflammatory Agents, Non-Steroidal pharmacology
Drug Discovery
Receptors, Glucocorticoid agonists

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