| 摘要 |
N-((Benzo-heterocyclic amino)-alkyl)-2-(hydroxy-benzazolonyl or -benzazolonyl)-2-hydroxyethylamine derivatives (I) are new. Benzo-heterocyclic substituted ethanolamine derivatives of formula (I) (including individual optical isomers, enantiomer mixtures and racemates) and their acid addition salts are new. X : O, NH, CH 2O, CHMeO, CMe 2O, CH 2NH, CHMeNH, CMe 2NH, CH=CH or CH 2CH 2; V' : CH 2, NH or O; R a>, R b> : H, alkyl or haloalkyl; or R a> + R b> : 2-5C alkylene (optionally substituted by one or more halo); R 1>, R 1>' : H, alkyl, cycloalkyl, haloalkyl, halocycloalkyl or cycloalkylalkyl; or R 1> + R 1>' : 2-5C alkylene (optionally substituted by one or more halo); R 2>, R 2>', R 2'''>, R 2>''' : H, alkyl, haloalkyl, OH, hydroxyalkyl, alkoxy, aryl, aryl-(1-4C) alkyl, arylalkyoxy, COOH, alkoxycarbonyl, carboxyalkoxy, alkoxycarbonyl-alkoxy, alkylsulfonylamino, CN, NH 2, mono- or dialkylamino, NO 2, alkylthio, alkylsulfonyl, alkylsulfinyl, alkylcarbonyloxy, alkylcarbonyl, alkylcarbonylamino or halo; and n : 0-2. unless specified otherwise alkyl groups have 1-6C, cycloalkyl groups 3-6C and aryl groups 6-10C. [Image] ACTIVITY : Antiinflammatory; Antiasthmatic; Tocolytic; Antiarrhythmic; Vasotropic; Antipruritic; Dermatological. MECHANISM OF ACTION : beta -Mimetic; beta -2 Agonist. |
