| 摘要 |
<p>bis(oxy) benzamides of formula (I), their quat. ammonium salts, oxides, and their dextrorotatory and laevorotatory isomers, are new. In (I) A=1-3C alkylene, opt. substd. by 1-4C alkyl, 2-4C alkenyl or hydroxyalkyl, R=H, 1-4C alkyl or a group-B-N-R1 R2 B=a single bond, 1-3C alkylene opt. substd. by 1-4C alkyl or 2-4C alkenyl, R1=H, 1-4C alkyl, 2-4C alkenyl or alkynyl, alkyl substd. by OH, SH, acyl, thioacyl alkoxy, alkylthio, amino or may be attached to B to form a satd or unsatd. N-heterocycle, R2=H, 1-4C alkyl, 2-4C alkenyl or alkynyl, alkyl substd by OH, SH, acyl, thioacyl, alkoxy, alkyl thio, amino, or a satd. or unsatd. opt. substd. heterocycle phenyl, adamantyl, cycloalkyl, bicyclolakyl, cycloalkenyl, attached directly or through an alkylene chain, or R1 & R2 together form a heterocycle which contain further heteroatoms, and may be substd by 1-4C alkyl, 2-4C alkenyl or alkynyl, phenyl, benzyl, cycloalkyl, cycloalkenyl, cycloalkanealkyl, adamantyl, bicycloalkyl or alkyl substd by OH, SH acyl, thioacyl, alkoxy or alklthio. R'=H, 1-4C alkyl, 2-4C alkenyl or alkynyl, adamantyl, pyrimidinyl, pyrazinyl, diazepinyl, quinuclidinyl, azabicycloalkyl, diazabicyloalkyl, bicycloalkyl, phenyl opt. substd. or R' & B may together form a N heterocycle, which may be substd, or R' & R1 a di-N heterocycle which may be substd. X=H, halogen, OH, 1-4C alkoxy or alkyl, amino, mono or di-alkyl substd, amino, acyl, aralkyl, furanyl, pyranyl, or alkoxycarbonyl. Y=H, halogen, OH, 1-4C alkoxy, NO2, amino, alkyl substd. amono, acyl, aralkyl, furanyl, pyranyl, alkoxy-carbonyl, 1-4C alkylsulphonyl, adamantyl sulphoncycloalkyl sulphonyl or sulphonyl substd by a mono - or di-substd amino gp. Z=H, halogen, OH, 1-4C alkoxy, NO2 amino opt. mono-or di- substd. by 1-4C alkyl, acyl, aralkyl, furanyl, pyranyl, or alkoxycarbonyl, or X & Y or Y & Z may be bonded together by one or ore heteroatoms, which may be substd. to form a ring. Daily dose is 50-900 (50-300)mg.</p> |
