title: 2-aminomethylphenylamine as a novel scaffold for factor Xa inhibitor.
abstract: We have been researching orally active factor Xa inhibitor for a long time. We explored the new diamine linker using effective ligands to obtain a new attractive original scaffold 2-aminomethylphenylamine derivative. Compound 1D showed very strong in vitro and in vivo factor Xa inhibitory activity, as well as favorable PK profiles in po administration to monkeys.
authors.affiliation: Research and Development Division, Daiichi Sankyo Co., Ltd, Edogawa-ku, Tokyo, Japan. mochizuki.akiyoshi.yk@daiichisankyo.co.jp
authors.forename: Akiyoshi
authors.initials: A
authors.lastname: Mochizuki
authors.forename: Tsutomu
authors.initials: T
authors.lastname: Nagata
authors.forename: Hideyuki
authors.initials: H
authors.lastname: Kanno
authors.forename: Makoto
authors.initials: M
authors.lastname: Suzuki
authors.forename: Toshiharu
authors.initials: T
authors.lastname: Ohta
mesh_terms: D000814:Aniline Compounds / Q000138:chemical synthesis* / Q000737:chemistry*; D000818:Animals; D019774:Blood Coagulation Factor Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry; D018360:Crystallography, X-Ray; D065427:Factor Xa Inhibitors; D000882:Haplorhini; D006801:Humans; D020128:Inhibitory Concentration 50; D008024:Ligands; D015394:Molecular Structure; D051381:Rats
chemical_list: C558704:2-aminomethylphenylamine; D000814:Aniline Compounds; D019774:Blood Coagulation Factor Inhibitors; D065427:Factor Xa Inhibitors; D008024:Ligands