1357947-08-0Relevant articles and documents
CD73 INHIBITORS
-
Paragraph 0207, (2020/03/23)
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.
Discovery of 3,5-substituted 6-azaindazoles as potent pan-Pim inhibitors
Hu, Huiyong,Wang, Xiaojing,Chan, Grace Ka Yan,Chang, Jae H.,Do, Steven,Drummond, Jake,Ebens, Allen,Lee, Wendy,Ly, Justin,Lyssikatos, Joseph P.,Murray, Jeremy,Moffat, John G.,Chao, Qi,Tsui, Vickie,Wallweber, Heidi,Kolesnikov, Aleksandr
, p. 5258 - 5264 (2015/11/09)
Pim kinase inhibitors are promising cancer therapeutics. Pim-2, among the three Pim isoforms, plays a critical role in multiple myeloma yet inhibition of Pim-2 is challenging due to its high affinity for ATP. A co-crystal structure of a screening hit 1 bound to Pim-1 kinase revealed the key binding interactions of its indazole core within the ATP binding site. Screening of analogous core fragments afforded 1H-pyrazolo[3,4-c]pyridine (6-azaindazole) as a core for the development of pan-Pim inhibitors. Fragment and structure based drug design led to identification of the series with picomolar biochemical potency against all three Pim isoforms. Desirable cellular potency was also achieved.
PYRAZOLO[3,4-c]PYRIDINE COMPOUNDS AND METHODS OF USE
-
Page/Page column 128, (2013/03/26)
Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.