482374-63-0Relevant articles and documents
Design, synthesis, and SAR of cis-1,2-diaminocyclohexane derivatives as potent factor Xa inhibitors. Part II: Exploration of 6-6 fused rings as alternative S1 moieties
Yoshikawa, Kenji,Kobayashi, Shozo,Nakamoto, Yumi,Haginoya, Noriyasu,Komoriya, Satoshi,Yoshino, Toshiharu,Nagata, Tsutomu,Mochizuki, Akiyoshi,Watanabe, Kengo,Suzuki, Makoto,Kanno, Hideyuki,Ohta, Toshiharu
experimental part, p. 8221 - 8233 (2010/03/25)
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.