165894-06-4Relevant academic research and scientific papers
INHIBITORS OF TYPED 1 METHIONYL-TRNA SYNTHETASE AND METHODS OF USING THEM
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, (2019/01/11)
The present disclosure is generally directed to compositions useful in the inhibition of MetRS and methods for treating diseases that are ameliorated by the inhibition of MetRS.
THERAPEUTIC COMPOUNDS
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, (2018/11/21)
The present embodiments relate to substituted heterocyclic derivative therapeutic compounds, compositions comprising said compounds, and the use of said compounds and compositions for epigenetic regulation by inhibition of bromodomain-mediated recognition
NOVEL PYRAZINE COMPOUNDS WITH OXYGEN, SULFUR AND NITROGEN LINKER FOR THE TREATMENT OF INFECTIOUS DISEASES
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, (2017/12/18)
The present invention relates to compounds of the formula (I), or pharmaceutically acceptable salts, enantiomer or diastereomer thereof, wherein R1 to R3 are as described above. The compounds may be useful for the treatment or prophylaxis of hepatitis B virus infection.
Structure-based drug design of novel potent and selective tetrahydropyrazolo[1,5-a]pyrazines as ATR inhibitors
Barsanti, Paul A.,Aversa, Robert J.,Jin, Xianming,Pan, Yue,Lu, Yipin,Elling, Robert,Jain, Rama,Knapp, Mark,Lan, Jiong,Lin, Xiaodong,Rudewicz, Patrick,Sim, Janet,Taricani, Lorena,Thomas, George,Xiao, Linda,Yue, Qin
, p. 37 - 41 (2015/01/30)
A saturation strategy focused on improving the selectivity and physicochemical properties of ATR inhibitor HTS hit 1 led to a novel series of highly potent and selective tetrahydropyrazolo[1,5-a]pyrazines. Use of PI3Kα mutants as ATR crystal structure surrogates was instrumental in providing cocrystal structures to guide the medicinal chemistry designs. Detailed DMPK studies involving cyanide and GSH as trapping agents during microsomal incubations, in addition to deuterium-labeled compounds as mechanistic probes uncovered the molecular basis for the observed CYP3A4 TDI in the series. (Chemical Equation Presented).
