On July 22, 2004, Takemura, Makoto; Ota, Toshiharu; Uoto, Koichi; Kawakami, Katsuhiro; Yoshino, Toshiharu; Yokomizo, Yoshihiro; Yoshikawa, Kenji published a patent.COA of Formula: C11H14N2O5 The title of the patent was Preparation of 1,2-phenylenediamine amides as activated blood coagulation factor X inhibitors. And the patent contained the following:
The title thiazolopyridinecarboxylic acid 1,2-phenylenediamine amides with general formula of Q1-Q2-A0-Q3-A00-Q4 [wherein Q1 = (un)substituted cyclohydrocarbyl, heterocyclyl, etc.; Q2 = a single bond, alkylene, alkenylene, etc.; Q3 = (un)substituted phenylene or any other (hetero)arylene; Q4 = (un)substituted aryl, arylalkenyl, etc.; A0 = (un)substituted CONH or CSNH; A00 = OCH2, (un)substituted CONH, SO2NH, etc.] or salts, solvates, or N-oxides thereof are prepared as activated blood coagulation factor X inhibitors. For example, the compound I was prepared in a multi-step synthesis. I inhibited human FXa with IC50 of 1.9 nM. The compounds are useful for the treatment of blood coagulation, thrombosis, embolism, etc. (no data). The experimental process involved the reaction of tert-Butyl (4-hydroxy-2-nitrophenyl)carbamate(cas: 201811-20-3).COA of Formula: C11H14N2O5
The Article related to phenylene amine amide preparation activated blood coagulation factor inhibitor, preparation thiazole carboxamide treatment blood coagulation thrombosis embolism human, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.COA of Formula: C11H14N2O5
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