申请人:Ciba-Geigy Corporation
公开号:US05190933A1
公开(公告)日:1993-03-02
Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.2 denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R.sup.6, or Z represents a protected or latent amino group Z.sup.o and R.sup.4 denotes hydrogen or a hydroxy-protective group R.sup.5, any group R.sup.5 or R.sup.6 is replaced by hydrogen, and/or any group Z.sup.o is converted into --NH.sub.2.
公式I的化合物如下:##STR1## 其中R表示具有2个或更多碳原子的脂肪族,环脂族,环脂族-脂肪族或芳基脂肪族基团,其中R.sup.1,R.sup.2和R.sup.3中的一个表示氢或脂肪族,环脂族,芳基脂肪族或芳香族基团,另一个R.sup.1,R.sup.2和R.sup.3中的一个是氢或,在R.sup.1和R.sup.2的情况下,是羟基,而R.sup.1,R.sup.2和R.sup.3中的剩余一个是氢,或其中R表示甲基,R.sub.1表示氢或羟基,R.sub.2表示芳基基团,而R.sub.3表示氢,它们的盐具有GABA.sub.B-拮抗性质,并且可以用作GABA.sub.B-拮抗剂。当在化合物II的情况下获得它们时,化合物II的公式如下:##STR2## 其中R,R.sup.1,R.sup.2和R.sup.3具有其先前的意义,Z表示--NH.sub.2,而R.sup.4表示羟基保护基团R.sup.5或,当R.sup.1和R.sup.3表示氢,而R.sup.2表示氢或烷基时,表示碱金属或铵离子R.sup.6,或Z表示受保护或潜在的氨基团Z.sup.o,而R.sup.4表示氢或羟基保护基团R.sup.5,任何R.sup.5或R.sup.6基团被氢替换,和/或任何Z.sup.o基团被转化为--NH.sub.2。