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Discovery of the potent non-steroidal glucocorticoid receptor modulator BAY 1003803 as clinical candidate.
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2020-06-01 , DOI: 10.1016/j.bmcl.2020.127298
Markus Berger 1 , Ekkehard May 2 , Hartmut Rehwinkel 1 , Heike Schäcke 3 , Roland Neuhaus 4 , Antje Rottmann 4 , Thomas M Zollner 3 , Stefan Jaroch 5
Affiliation  

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.



中文翻译:

发现有效的非甾体糖皮质激素受体调节剂BAY 1003803作为临床候选药物。

我们报告了新的临床候选药物BAY 1003803作为糖皮质激素受体激动剂用于牛皮癣或严重异位性皮炎局部治疗的发现。在优化氨基醇系列作为一种高效的新型非甾体铅结构的过程中,考虑了理化性质和安全性与结构基序之间的关系。BAY 1003803在体外具有很强的抗炎活性并具有适合局部应用的药代动力学特征。

更新日期:2020-06-01
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