申请人:Otsuka Pharmaceutical Company Limited
公开号:US04022784A1
公开(公告)日:1977-05-10
5-[1-Hydroxy-2-(substituted-amino)]alkyl-8-substituted-carbostyril derivatives and 5-[1-hydroxy-2-(substituted-amino)]-alkyl-8-substituted-3,4-dihydrocarbost yril derivatives represented by the formulas (Ia) and (Ib) ##STR1## WHEREIN R.sup.1, R.sup.4 and R.sup.5 each represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, with at least one of R.sup.4 and R.sup.5 being an alkyl group, and R.sup.2 and R.sup.3, which may be the same or different, each represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an aralkyl group containing a straight or branched chain alkyl moiety having 1 to 4 carbon atoms or a cycloalkyl group having 4 to 6 carbon atoms, or R.sup.2 and R.sup.3 may, when taken together with the nitrogen atom to which they are attached, form a 5- or 6-membered substituted or unsubstituted heterocyclic ring containing 1 or 2 nitrogen, oxygen or sulfur atoms as hetero atoms, the pharmaceutically acceptable acid addition salts thereof, and a process for preparing the same.
5-[1-羟基-2-(取代氨基)]烷基-8-取代-碳基喹啉衍生物和5-[1-羟基-2-(取代氨基)]-烷基-8-取代-3,4-二氢碳基喹啉衍生物由以下式(Ia)和(Ib)所表示:其中R.sup.1、R.sup.4和R.sup.5分别代表氢原子或具有1至4个碳原子的烷基基团,其中至少一个为烷基基团,而R.sup.2和R.sup.3,可以相同也可以不同,分别代表氢原子、具有1至4个碳原子的烷基基团、包含具有1至4个碳原子的直链或支链烷基基团的芳基烷基基团或具有4至6个碳原子的环烷基基团,或者R.sup.2和R.sup.3可以与它们连接的氮原子一起形成一个含有1或2个氮、氧或硫原子作为杂原子的5-或6-成员取代或未取代杂环的环,以及其药学上可接受的酸盐和制备方法。