365996-31-2Relevant articles and documents
Cycloalkanediamine derivatives as novel blood coagulation factor Xa inhibitors
Nagata, Tsutomu,Yoshino, Toshiharu,Haginoya, Noriyasu,Yoshikawa, Kenji,Isobe, Yumiko,Furugohri, Taketoshi,Kanno, Hideyuki
, p. 4683 - 4688 (2008/02/12)
This paper describes the synthesis of orally available potent fXa inhibitors 2 and 3 by modification of the piperazine part of lead compound 1. Carbonyl derivative 3 showed potent fXa activity but not sulfonyl derivative 2. Among the compounds synthesized, cyclohexane derivatives 3g and 3h and cycloheptane derivative 3j had potent anticoagulant activity as well as anti-fXa activity. Synthetic study of the optical isomers of 3g demonstrated that (-)-3g had more potent activity.