83647-40-9Relevant articles and documents
Heterocyclic substituted biphenyl compound as well as preparation method and application thereof
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Paragraph 0296; 0298-0300, (2021/08/28)
The invention discloses a heterocyclic substituted biphenyl compound as well as a preparation method and application thereof. According to the present invention, the compound can block the PD-1/PD-L1 signal pathway, and can be used as the immune checkpoint PD-1/PD-L1 small molecule inhibitor; and according to the compound disclosed by the invention, the metabolic stability is improved while the high binding rate with PD-L1 protein is maintained. A hydrophilic group is introduced to a heterocyclic ring, and the PD-1/PD-L1 inhibitory activity is improved.
Addition of Fluorine and a Late-Stage Functionalization (LSF) of the Oral SERD AZD9833
Scott, James S.,Moss, Thomas A.,Barlaam, Bernard,Davey, Paul R. J.,Fairley, Gary,Gangl, Eric T.,Greenwood, Ryan D. R.,Hatoum-Mokdad, Holia,Lister, Andrew S.,Longmire, David,Polanski, Radoslaw,Stokes, Stephen,Tucker, Michael J.,Varnes, Jeffrey G.,Yang, Bin
supporting information, p. 2519 - 2525 (2020/11/16)
Herein we describe our efforts using a late stage functionalization together with more traditional synthetic approaches to generate fluorinated analogues of the clinical candidate AZD9833. The effects of the addition of fluorine on the lipophilicity, permeability, and metabolism are discussed. Many of these changes were tolerated in terms of pharmacology and resulted in high quality molecules which reached advanced stages of profiling in the testing cascade.
METHODS OF PROMOTING BETA CELL PROLIFERATION
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Paragraph 00158, (2018/06/30)
The present disclosure provides methods of promoting proliferation of a pancreatic cell. The methods are useful for the treatment of diabetes and other diseases characterized by impaired glucose tolerance.