RHEIN CONJUGATES, PREPARATION METHOD THEREOF AND THEIR USES IN PRODUCING MEDICINES FOR TREATING DIABETIC NEPHROSIS, INTESTINAL ADHESION AND OSTEOARTHRITIS
申请人:Jiangsu Lianchuang Pharmaceutical Technology Co.
公开号:EP1913940A1
公开(公告)日:2008-04-23
The conjugates of present invention are formed by the combination of rhein or their analogues with the organic bases or amino acids in molecular force between them. The methods for preparing the conjugates and their uses for manufacturing medicines in the treatment of diabetic nephrosis, recovery of gastrointestinal function and prevention of intestinal adhesion, as well as treatment of osteoarthritis, rheumatic arthritis and rheumatoid arthritis are also described. Rhein or their analogues as the left part of general formula (I) is selected from (1) the compounds of rhein or their analogues, in which one or two substituents of R2~R3 and R6~R7 are COOH at least two substituents of R1~8 are -H; or (2) the rhein-containing extract derived from plants. In general formula (I), M represents nitrogen-containing organic bases or basic amino acids.
本发明的共轭物是由风湿素或其类似物与有机碱或氨基酸以分子间的作用力结合而成。本发明还描述了制备这些共轭物的方法及其在治疗糖尿病肾病、恢复胃肠功能和预防肠粘连以及治疗骨关节炎、风湿性关节炎和类风湿性关节炎方面的药物制造用途。作为通式(I)左侧部分的流苏素或其类似物选自(1)流苏素化合物或其类似物,其中 R2~R3 和 R6~R7 的一个或两个取代基为 COOH,R1~8 的至少两个取代基为 -H;或(2)从植物中提取的含流苏素的提取物。在通式(I)中,M 代表含氮有机碱或碱性氨基酸。