||Haginoya, N., Kanno, H., Kobayashi, S., Komoriya, S., Mochizuki, A., Nagata, T., Nakamoto, Y., Ohta, T., Suzuki, M., Watanabe, K., Yoshikawa, K., Yoshino, T.
A series of cis-1,2-diaminocyclohexane derivatives possessing a 6-6 fused ring for the S1 moiety were synthesized as novel factor Xa (fXa) inhibitors. The synthesis, structure-activity relationship (SAR), and physicochemical properties are reported herein, together with the discovery of compound 45c, which has potent anti-fXa activity, good physicochemical properties and pharmacokinetic (PK) profiles, including a reduced negative food effect.
Bioorg.Med.Chem. 2009 Dec; 17(24):8221-8233 doi:10.1016/j.bmc.2009.10.024