97455-61-3Relevant academic research and scientific papers
Novel indirect AMP-activated protein kinase activators: Identification of a second-generation clinical candidate with improved physicochemical properties and reduced hERG inhibitory activity
Kuramoto, Kazuyuki,Sawada, Yuki,Yamada, Tomohiro,Nagashima, Takeyuki,Ohnuki, Kei,Shin, Takashi
, p. 452 - 465 (2020/09/09)
This study reports the synthesis and evaluation of novel indirect AMP-activated protein kinase (AMPK) activators. The series of compounds selectively inhibited cell growth in several human breast cancer cell lines by activating AMPK. We performed back-up medicinal chemistry synthetic research on ASP4132, a previously reported as a compound for clinical development that acts as an indirect AMPK activator. This led to the successful identification of 4-({4-[5-({1-[(5-ethoxypyrazin-2-yl)methyl]-4-fluoropiperidin-4-yl}methoxy)-3-methylpyridine-2-carbonyl]piperazin-1-yl}methyl)benzonitrile succinate (27b), a potent, highly aqueous soluble and metabolically stable compound in human hepatocytes. Compound 27b also showed weaker human Ether-a-go-go Related Gene (hERG) inhibitory activity than that of compound 13 and ASP4132. Therefore, 27b was a promising AMPK activator and a second-generation clinical candidate for treatment for human cancer.
TRICYCLIC PIPERIDINE COMPOUNDS
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Page/Page column 75; 77, (2016/11/21)
The present invention relates to compounds of the formula (I) wherein R1a, R1b, R2, R3, (R4)n and ring (A) are as described in the description, to their preparation, to pharmaceutically acc
6-n-Alkoxy-3-Pyridinecarboxaldehydes: New Intermediates to Liquid Crystals. Properties of Some Derivatives.
Barbera, J.,Melendez, E.,Romero, P.,Serrano, J. L.
, p. 259 - 268 (2007/10/02)
The synthesis of new intermediates to liquid crystals, a series of 6-n-alkoxy-3-pyridinecarboxaldehydes is described.The mesomorphic properties of their precursors, the 6-n-alkoxy-3-pyridinecarboxylic acids are reported.Some derivatives of the carboxaldeh
