701300-00-7Relevant articles and documents
Synthesis and biological evaluation of the metabolites of 2-(1-{3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl}piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one
Fujimoto, Takuya,Tobisu, Mamoru,Konishi, Noriko,Kawamura, Masaki,Tada, Norio,Takagi, Terufumi,Kubo, Keiji
experimental part, p. 7993 - 8002 (2010/03/30)
We have recently discovered imidazo[1,5-c]imidazol-3-one derivative 1 as a potent, selective, and orally bioavailable factor Xa (FXa) inhibitor. In this study, we have synthesized metabolites of 1 and evaluated their biological activities. As a result, we identified the active metabolites S-5 and 6 with a potent FXa inhibitory activity comparable to 1 and a favorable pharmacokinetic profile in monkeys.