872059-27-3Relevant academic research and scientific papers
Structure-based drug design of novel, potent, and selective azabenzimidazoles (ABI) as ATR inhibitors
Barsanti, Paul A.,Pan, Yue,Lu, Yipin,Jain, Rama,Cox, Matthew,Aversa, Robert J.,Dillon, Michael P.,Elling, Robert,Hu, Cheng,Jin, Xianming,Knapp, Mark,Lan, Jiong,Ramurthy, Savithri,Rudewicz, Patrick,Setti, Lina,Subramanian, Sharadha,Mathur, Michelle,Taricani, Lorena,Thomas, George,Xiao, Linda,Yue, Qin
, p. 42 - 46 (2015/01/30)
Compound 13 was discovered through morphing of the ATR biochemical HTS hit 1. The ABI series was potent and selective for ATR. Incorporation of a 6-azaindole afforded a marked increase in cellular potency but was associated with poor PK and hERG ion channel inhibition. DMPK experiments established that CYP P450 and AO metabolism in conjunction with Pgp and BCRP efflux were major causative mechanisms for the observed PK. The series also harbored the CYP3A4 TDI liability driven by the presence of both a morpholine and an indole moiety. Incorporation of an adjacent fluorine or nitrogen into the 6-azaindole addressed many of the various medicinal chemistry issues encountered. (Chemical Presented).
SUBSTITUTED IMIDAZOPYRIMIDINES AND TRIAZOLOPYRIMIDINES
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Page/Page column 27, (2010/05/13)
The invention relates to substituted imidazopyrimidines and triazolopyrimidines, to methods for the production thereof, and to the use of same for producing medicaments for the treatment and/or prophylaxis of diseases, especially haematological diseases, preferably leucopenia and neutropenia.
Substituted heterocyclic compounds and methods of use
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Page/Page column 20, (2008/06/13)
The present invention relates to triazolopyrimidines, imidazolopyrimidines and derivatives thereof, and pharmaceutically acceptable salts thereof. Also included is a method of treatment of inflammation, rheumatoid arthritis, Pagets disease, osteoporosis,
