827026-45-9Relevant articles and documents
Influence of Linker Attachment Points on the Stability and Neosubstrate Degradation of Cereblon Ligands
Bricelj, Ale?a,Dora Ng, Yuen Lam,Ferber, Dominic,Gütschow, Michael,Kr?nke, Jan,Kuchta, Robert,Müller, Sina,Monschke, Marius,Sosi?, Izidor,Steinebach, Christian,Wagner, Karl G.
, p. 1733 - 1738 (2021/11/16)
Proteolysis targeting chimeras (PROTACs) hijacking the cereblon (CRBN) E3 ubiquitin ligase have emerged as a novel paradigm in drug development. Herein we found that linker attachment points of CRBN ligands highly affect their aqueous stability and neosubstrate degradation features. This work provides a blueprint for the assembly of future heterodimeric CRBN-based degraders with tailored properties.
Compound for targeted degradation of BTK protein
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Paragraph 0458; 0465-0467, (2021/06/22)
The invention provides a compound with the capability of degrading Bruton's tyrosine protein kinase (Btk) protein in a targeted manner, and particularly provides a compound as shown in the following formula I0, wherein the definition of each group is described in the specification. The compound provided by the invention can well degrade Btk protein in a targeted manner, so that the compound can be used for treating diseases related to Btk activity or expression quantity, such as tumors.
Anhydrous preparation method of lenalidomide
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Paragraph 0035-0044, (2020/07/24)
The invention relates to an anhydrous preparation method of lenalidomide. The invention discloses a novel method for preparing a 3-(4-amino-1-oxo-1,3-dihydro-2H-isoindole-2-yl) piperidine-2,6-diketoneanhydrous compound, and belongs to the technical field of chemical synthesis. The process route is short in steps, simple and convenient to operate and mild in reaction conditions, and the finally obtained product is excellent in quality and easy for industrial production.