申请人:CIBA-GEIGY AG
公开号:EP0319482A2
公开(公告)日:1989-06-07
Compounds of the formula I
wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R¹, R² and R³ represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R¹, R² and R³ is hydrogen or, in the case of R¹ and R², is hydroxy, and the remaining one of R¹, R² and R³ is hydrogen, and their salts have GABAB-antagonistic properties and can be used as GABAB-antagonists. They are obtained when in a compound of formula II
in which R, R¹, R² and R³ have their previous significances, Z represents -NH₂ and R⁴ denotes a hydroxy-protective group R⁵ or, when R¹ and R³ denote hydrogen and R² denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R⁶, or Z represents a protected or latent amino group Zo and R⁴ denotes hydrogen or a hydroxy-protective group R⁵, any group R⁵ or R⁶ is replaced by hydrogen, and/or any group Zo is converted into -NH₂.
式 I 的化合物
其中 R 表示具有 2 个或 2 个以上碳原子的脂肪族、环脂族、环脂族-脂肪族或芳香族基团,其中基团 R¹、R² 和 R³ 中的一个代表氢或脂肪族、环脂族、芳香族或芳香族基团、R¹、R² 和 R³ 中的另一个为氢,或在 R¹ 和 R² 的情况下为羟基,R¹、R² 和 R³ 中的其余一个为氢,它们的盐具有 GABAB 拮抗特性,可用作 GABAB 拮抗剂。当式 II 的化合物中
其中 R、R¹、R² 和 R³ 具有其先前的意义,Z 表示-NH₂,R⁴ 表示羟基保护基团 R⁵,或当 R¹ 和 R³ 表示氢,R² 表示氢或烷基时,表示碱金属或铵离子 R⁶、或 Z 代表受保护或潜在的氨基 Zo,R⁴ 表示氢或羟基保护基团 R⁵,任何基团 R⁵ 或 R⁶ 被氢取代,和/或任何基团 Zo 转化为-NH₂。