Pharmaceutical composition for the treatment of underlying nonpharmacologically induced nervous system cholinergic deficit state comprising monoamine acridine derivatives
申请人:Summers, William Koopmans
公开号:EP0595365A1
公开(公告)日:1994-05-04
A pharmaceutical composition for treatment of underlying nonpharmacologically induced central or peripheral nervous system cholinergic deficit state in humans comprising a monoamine acridine derivative of the formula:
wherein R₁ represents hydrogen, hydroxy, methyl, methoxy, ethyl or ethoxy; R₁ and R₂ together may form a double bond, R₃ and R₄ together may form a double bond, or R₁, R₂, R₃ and R₄ are all hydrogen; R₅ represents hydrogen, hydroxy, methoxy or ethoxy; R₆ represents hydrogen, hydroxy, methoxy or ethoxy; and R₇ is without a substituent or R₇ represents an oxygen atom, a C₁-C₂₀ alkyl radical or a radical selected from the group consisting of
-R-N(R)₂,
wherein each R is independently selected from C₁-C₂₀ alkyl; or a pharmaceutically acceptable salts thereof, and a pharmaceutically acceptable inert carrier therefor; with the provisos that the monoamine acridine derivative is a compound in which (i) if R₁, R₂, R₃, R₄, R₅ and R₆ are each hydrogen, then R₇ cannot be without a substituent, (ii) if R₁ and R₂ together form a double bond, R₃ and R₄ together form a double bond and R₅ and R₆ are each hydrogen, then R₇ cannot be without a substituent, and (iii) if R₃ and R₄ together form a double bond and R₇ is without a substituent, then R₁ cannot be a hydrogen atom is provided.
一种用于治疗非药物诱导的人体中枢或外周神经系统胆碱能缺失状态的药物组合物,包含一种式的单胺吖啶衍生物:
其中 R₁ 代表氢、羟基、甲基、甲氧基、乙基或乙氧基;R₁ 和 R₂ 一起可形成双键,R₃ 和 R₄ 一起可形成双键,或 R₁、R₂、R₃ 和 R₄ 均为氢;R₅ 代表氢、羟基、甲氧基或乙氧基; R₆ 代表氢、羟基、甲氧基或乙氧基;且 R₇ 不含取代基,或 R₇ 代表氧原子、C₁-C₂₀ 烷基或选自以下组别的基团
-R-N(R)₂、
其中每个 R 独立地选自 C₁-C₂₀ 烷基;或其药学上可接受的盐,以及药学上可接受的惰性载体;但条件是,单胺吖啶衍生物是一种化合物,其中 (i) 如果 R₁、R₂、R₃、R₄、R₅ 和 R₆ 各为氢,则 R₇ 不能没有取代基,(ii) 如果 R₁ 和 R₂ 一起形成双键、R₃ 和 R₄ 共同形成双键,且 R₅ 和 R₆ 各为氢原子,则 R₇ 不能不含取代基,以及 (iii) 如果 R₃ 和 R₄ 共同形成双键,且 R₇ 不含取代基,则 R₁ 不能为氢原子。