571189-23-6Relevant articles and documents
PYRIDINYL HETEROCYCLYL COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE
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Page/Page column 39-40, (2020/01/08)
The present invention relates to compounds of formula (I), a b (I), wherein R1 to R4 and L are as described herein, and their pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.
Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active Factor Xa inhibitors
Imaeda, Yasuhiro,Kawamoto, Tetsuji,Tobisu, Mamoru,Konishi, Noriko,Hiroe, Katsuhiko,Kawamura, Masaki,Tanaka, Toshimasa,Kubo, Keiji
, p. 3125 - 3140 (2008/09/19)
We have recently reported the discovery of orally active sulfonylalkylamide Factor Xa (FXa) inhibitors, as typified by compound 1 (FXa IC50 = 0.061 μM). Since the pyridylpiperidine moiety was not investigated in our previous study, we conducted detailed structure-activity relationship studies on this S4 binding element. This investigation led to the discovery of piperazinylimidazo[1,2-a]pyridine 2b as a novel and potent FXa inhibitor (FXa IC50 = 0.021 μM). Further modification resulted in the discovery of 2-hydroxymethylimidazo[1,2-a]pyridine 2e (FXa IC50 = 0.0090 μM), which was found to be a selective and orally bioavailable FXa inhibitor with reduced CYP3A4 inhibition.