申请人:Senju Pharmaceutical Co., Ltd.
公开号:EP0433679A2
公开(公告)日:1991-06-26
Presented are pharmaceutical compositions comprising in admixture with a carrier a compound of;
(a) the formula (I) or a pharmaceutically acceptable salt thereof:
wherein R₁ and R₂ are each hydrogen, methyl, trifluoromethyl, carboxy, methoxycarbonyl or ethoxycarbonyl, and R₃ is hydrogen or hydroxy;
(b) the formula (I) or a pharmaceutically acceptable salt thereof:
wherein R, R₂ and R₃ are as defined;
(c) the formula (III) or a pharmaceutically acceptable salt thereof:
wherein R₄ and R₅ are each hydrogen or form, by incorporation of C₁ and C₂ carbon atoms, a condensed [2.1-b] pyridine ring optionally substituted with a hydroxyl group or a carboxyl group, and R₆ is hydrogen or hydroxy; or
(d) the formula (IV) or a pharmaceutically acceptable salt thereof:
wherein R₄, R₅ and R₆ are as defined.
The compositions are used to inhibit Maillard's reaction in human body, the reaction which may be responsible for the development of diabetic complications and age-associated disorders. Methods of treatment and prophylaxis of such complications and disorders are also presented.
所提出的药物组合物包括与载体混合的下列化合物
(a) 式(I)或其药学上可接受的盐:
其中R₁和R₂各自为氢、甲基、三氟甲基、羧基、甲氧羰基或乙氧羰基,R₃为氢或羟基;
(b) 式 (I) 或其药学上可接受的盐:
其中 R、R₂ 和 R₃ 如所定义;
(c) 式 (III) 或其药学上可接受的盐:
其中 R₄ 和 R₅ 各为氢或通过加入 C₁ 和 C₂ 碳原子形成任选被羟基或羧基取代的缩合[2.1-b]吡啶环,且 R₆ 为氢或羟基;或
(d) 式 (IV) 或其药学上可接受的盐:
其中 R₄、R₅ 和 R₆ 如所定义。
这些组合物用于抑制人体内的 Maillard 反应,该反应可能是导致糖尿病并发症和老年性疾病发生的原因。此外,还介绍了治疗和预防此类并发症和疾病的方法。