Rhein Conjugates, Preparation Method Thereof and Their Uses in Producing Medicines for Treating Diabetic Nephrosis, Intestinal Adhesion and Osteoarthritis
申请人:Cong Xiaodong
公开号:US20080207758A1
公开(公告)日:2008-08-28
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.
本发明的共轭物由大黄素或其类似物与有机碱或氨基酸在它们之间的分子力相互作用而形成。描述了制备这些共轭物的方法以及它们在制造治疗糖尿病性肾病、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的药物中的用途。大黄素或其类似物作为通式(I)的左部分,从(1)大黄素或其类似物的化合物中选择,其中R2˜R3和R6˜R7的一个或两个取代基至少有两个R1˜8的取代基为—H;或(2)来自植物的含有大黄素的提取物。在通式(I)中,M代表含氮有机碱或碱性氨基酸。