| 摘要 |
Diazepane derivatives (I) are new. Diazepane derivatives of formula (I) and their salts are new. [Image] A : aryl or heteroaryl (both optionally substituted by 1-3 substituents); B : arylene or heteroarylene (both optionally substituted by 1-3 substituents); X 1CONR 4, NR 4CO, NR 4CH 2, OCH 2, CH 2O or CH=CH; X 3CONR 5or NR 5CO; R 1H, Alk (optionally substituted by aryl or heteroaryl), AlkOAlk, Cyc, aryl, heteroaryl, CycAlk or C=NR 6; Alk : lower alkyl; Cyc : 3-8C cycloalkyl; R 2OH, OAlk, OAlkOH, OSO 2OH, OSO 2AlkCOOH, OAlkCOOAlk, COOH, COOAlk or halo; R 3H, halo or Alk, and R 4-R 6H or Alk. ACTIVITY : Thrombolytic; anticoagulant; cerebroprotective; hemostatic; cardiant; antianginal; respiratory. MECHANISM OF ACTION : Factor-X inhibitor. In an assay using human factor Xa, 3-hydroxy-4'-methoxy-2-{[4-(4-methyl-1,4-diazepan-1-yl)benzoyl]amino}benzanilide (Ia) hydrochloric acid salt exhibited a CT 2of 1.71 mu M. |
