92534-73-1Relevant articles and documents
DNA POLYMERASE IIIC INHIBITORS AND USE THEREOF
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, (2020/07/14)
The present invention relates to compounds and methods useful for inhibiting the DNA polymerase IIIC enzyme. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of Gram-positive bacterial infections.
A hit to lead discovery of novel N-methylated imidazolo-, pyrrolo-, and pyrazolo-pyrimidines as potent and selective mTOR inhibitors
Lee, Wendy,Ortwine, Daniel F.,Bergeron, Philippe,Lau, Kevin,Lin, Lichuan,Malek, Shiva,Nonomiya, Jim,Pei, Zhonghua,Robarge, Kirk D.,Schmidt, Stephen,Sideris, Steve,Lyssikatos, Joseph P.
, p. 5097 - 5104 (2013/09/12)
A series of N-7-methyl-imidazolopyrimidine inhibitors of the mTOR kinase have been designed and prepared, based on the hypothesis that the N-7-methyl substituent on imidazolopyrimidine would impart selectivity for mTOR over the related PI3Kα and δ kinases. The corresponding N-Me substituted pyrrolo[3,2-d]pyrimidines and pyrazolo[4,3-d]pyrimidines also show potent mTOR inhibition with selectivity toward both PI3α and δ kinases. The most potent compound synthesized is pyrazolo[4,3-d]pyrimidine 21c. Compound 21c shows a Ki of 2 nM against mTOR inhibition, remarkable selectivity (>2900×) over PI3 kinases, and excellent potency in cell-based assays.
PYRAZOLEPYRIMIDINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE and INFLAMMATORY DISEASES
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Page/Page column 39-40, (2009/07/17)
The present invention relates to compounds that are inhibitors of PDElA, a phosphodiesterase that is involved in the modulation of the degradation of cartilage, joint degeneration and diseases involving such degradation and/or inflammation, and particular