2105905-46-0Relevant academic research and scientific papers
Development of a Scalable Method for Manufacturing the Central Core of CD73 Inhibitor AB680
Fournier, Jeremy,Yan, Xuelei,Tran, Anh T.,Grange, Rebecca L.,Jacob, Steven D.,Kalisiak, Jaroslaw,Lawson, Kenneth V.,Connor, Eric F.,Leleti, Manmohan R.,Powers, Jay P.
, p. 157 - 162 (2021)
AB680 is a highly potent CD73 small molecule inhibitor discovered and developed by Arcus Biosciences, currently in clinical trials for the treatment of pancreatic cancer. Here, we report the development of a scalable and practical method for the manufacturing of the azaindazole central core. This synthesis features an N-oxide formation followed by an α-chlorination with POCl3 leading to the formation of 4,6-dichloro-1H-pyrazolo[3,4-b]pyridine 1 in high yield and 99.5% UV purity. This method was successfully performed on multikilogram scale to support the synthesis of AB680.
CD73 INHIBITOR, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
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, (2022/03/22)
A CD73 inhibitor having the structure represented by formula (I), a preparation method therefor and an application thereof. The series of compounds can be widely applied in the preparation of drugs for treating cancers or tumors that are at least partially mediated by CD73, autoimmune diseases and disorders and metabolic diseases, in particular drugs for treating melanoma, colon cancer, pancreatic cancer, breast cancer, prostate cancer, lung cancer, leukemia, brain tumor, lymphoma, ovarian cancer and Kaposi's sarcoma. A new generation of CD73 inhibitor drugs is expected to be developed.
PARENTERALLY ADMINISTERED IMMUNE ENHANCING DRUGS
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, (2019/10/01)
Methods of identifying compounds that modulate the conversion of AMP to adenosine by 5'-nucleotidase, ecto, and that possess particular pharmacokinetic characteristics are described herein. Methods of such compounds, and compositions comprising same, for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, are also provided.
MODULATORS OF 5'-NUCLEOTIDASE, ECTO AND THE USE THEREOF
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, (2017/08/01)
Compounds that modulate the conversion of AMP to adenosine by 5'- nucleotidase, ecto, and compositions containing the compounds and methods for synthesizing the compounds, are described herein. The use of such compounds and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer- and immune-related disorders, that are mediated by 5'-nucleotidase, ecto is also provided.
