申请人:Asahi Kasei Kogyo Kabushiki Kaisha
公开号:US05340811A1
公开(公告)日:1994-08-23
Disclosed is a sulfonamide derivative represented by following formula (I) and a medicine for the treatment of asthma comprising the sulfonamide derivative as an active ingredient which exhibits bronchodilation effect. ##STR1## wherein X represents a quinoline residue represented by formula (II) or an isoquinoline residue represented by formula (III) ##STR2## where R.sup.1 is a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group, or ##STR3## where R.sup.2 is a hydrogen atom or a hydroxyl group, and wherein: when X is quinoline residue (II), n is zero or 1, in which, when n is zero, R.sup.4 is an unsubstituted or substituted diazacycloalkyl group, and when n is 1, R.sup.3 is a hydrogen atom or a lower alkyl group and R.sup.4 is an unsubstituted or substituted aralkylamino group or an unsubstituted or substituted diazacycloalkyl group; and when X is isoquinoline residue (III), n is 1, in which, R.sup.3 is a hydrogen atom or a lower alkyl group and R.sup.4 is a 3,4-methylenedioxyphenethylamino group, a 3,4-methylenedioxybenzylamino group or an unsubstituted or substituted diazacycloalkyl group, with the proviso that when R.sup.4 is an unsubstituted or substituted diazacycloalkyl group, the diazacycloalkyl group is bonded at a nitrogen atom thereof.
本发明公开了一种
磺胺衍
生物,其表示为以下式(I),以及包含所述
磺胺衍
生物作为活性成分的治疗哮喘的药物,该药物具有支气管扩张作用。其中,X代表由式(II)表示的
喹啉残基或由式(III)表示的
异喹啉残基。其中,R.sup.1是
氢原子、卤素原子、低
碳基团或低烷
氧基团,或者R.sup.2是
氢原子或羟基,且当X为
喹啉残基(II)时,n为零或1,其中当n为零时,R.sup.4是未取代或取代的二
氮杂环烷基团,当n为1时,R.sup.3是
氢原子或低
碳基团,R.sup.4是未取代或取代的芳基
氨基团或未取代或取代的二
氮杂环烷基团;当X为
异喹啉残基(III)时,n为1,其中,R.sup.3是
氢原子或低
碳基团,R.sup.4是
3,4-亚甲二氧基苯乙胺基团、
3,4-亚甲二氧基苄胺基团或未取代或取代的二
氮杂环烷基团,但当R.sup.4是未取代或取代的二
氮杂环烷基团时,该二
氮杂环烷基团与其
氮原子结合。