51135-56-9Relevant academic research and scientific papers
2-(PYRAZOLOPYRIDIN-3-YL)PYRIMIDINE DERIVATIVES AS JAK INHIBITORS
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Page/Page column 61-62, (2016/12/26)
New 2-(pyrazolopyridin-3-yl)pyrimidine derivatives are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
PYRAZOLOPYRIMIDIN-2-YL DERIVATIVES AS JAK INHIBITORS
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Page/Page column 51; 52, (2015/06/25)
New pyrazolopyridmiin-2-yl derivatives are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
Structure-kinetics relations holding in the amination of six-membered nitrogen-containing heterocyclic compounds
Borodkin,Vorob'ev,Shubin
experimental part, p. 897 - 903 (2011/10/04)
Relative rates of the amination of 3-X- and 4-X-substituted pyridines (X = H, 3-Me, 4-Me, 3-F3C, 3-CN, 4-CN, 3-Cl, 3-Br, 4-MeO, 4-Me 2N), pyrazine, quinoline, isoquinoline, 2,2′- and 4,4′-bipyridines, and 1,10-phenanthroline with O-
Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors
Qiao, Lixin,Choi, Sungwoon,Case, April,Gainer, Thomas G.,Seyb, Kathleen,Glicksman, Marcie A.,Lo, Donald C.,Stein, Ross L.,Cuny, Gregory D.
supporting information; experimental part, p. 6122 - 6126 (2010/06/16)
A structure-activity relationship study for a 2-chloroanilide derivative of pyrazolo[1,5-a]pyridine revealed that increased EphB3 kinase inhibitory activity could be accomplished by retaining the 2-chloroanilide and introducing a phenyl or small electron donating substituents to the 5-position of the pyrazolo[1,5-a]pyridine. In addition, replacement of the pyrazolo[1,5-a]pyridine with imidazo[1,2-a]pyridine was well tolerated and resulted in enhanced mouse liver microsome stability. The structure-activity relationship for EphB3 inhibition of both heterocyclic series was similar. Kinase inhibitory activity was also demonstrated for representative analogs in cell culture. An analog (32, LDN-211904) was also profiled for inhibitory activity against a panel of 288 kinases and found to be quite selective for tyrosine kinases. Overall, these studies provide useful molecular probes for examining the in vitro, cellular and potentially in vivo kinase-dependent function of EphB3 receptor.
Synthesis and antitumor activities of 2-(substituted)phenyl-1,2,4- triazolo[1,5-a]pyridines
Zhang, Guolin,Hu, Yongzhou
, p. 919 - 922 (2008/03/29)
(Chemical Equation Presented) Twenty-three 2-(substituted)phenyl-1,2,4- triazolo[1,5-a]pyridines have been synthesized by cyclo-additison reaction between N-amino methylpyridinium mesitylenesulfonates and substituted benzonitriles under the presence of po
Non-steroidal pregnancy-terminating agents: Design, synthesis and structure-activity relationships of 2-aryl-1,2,4-triazolo[1,5-a]pyridine
Liu, Tao,Hu, Yongzhou
, p. 2411 - 2413 (2007/10/03)
The syntheses and the pregnancy-terminating activity relationships of compounds 5a-n are reported. Compounds 5b and 5l are found to be more potent than DL-111 - a known drug having effective pregnancy-terminating activity in vitro. Further research shows compounds 5b and 5l have the same activity as DL-111 in vivo. We also found an exciting result that they have excellent anti-implantation activity after oral administration.
