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New and loss tang 17 carboxylic acid ester, the manufacturing method and includes that the medicine

机译:新型损耗糖17羧酸酯,药物的制造方法和包括

摘要

The invention relates to androstane-17-carboxylic acid esters, represented by general formula (I): IMAGE wherein R1 represents a lower alkyl group containing 1 to 4 carbon atoms, a lower alkyl group containing 2 to 4 carbon atoms substituted by an amino group, or an aralkyl group from 6 to 12 carbon atoms, R2 and R3, which may be the same or different, represent a hydrogen atom or a lower alkyl group containing 1 to 4 carbon atoms, R4 represents a hydrogen atom, a hydroxy group or an acetoxy group, R5 represents a hydroxy or acetoxy group, or R4 and R5 represent together a divalent alkylenedioxy group, R6 represents a hydroxy group, a methoxy group, or an acetoxy group, R7 represents a methyl group or a hydroxymethyl group, R8 represents an hydrogen atom or a hydroxy group and IMAGE represents either a IMAGE group or a IMAGE carbon atom having the double linkage in the 4- or 5-position of the steroid nucleus. Such esters are prepared by coupling reaction of the corresponding 14-azido-derivatives with a sugar, followed by a reduction. Application in therapy, especially in the treatment of heart failure.
机译:本发明涉及由通式(I)表示的雄甾烷17-羧酸酯:其中R1代表被1至4个碳原子取代的低级烷基,被2至4个碳原子取代的低级烷基。氨基或6至12个碳原子的芳烷基,R 2和R 3可以相同或不同,表示氢原子或含1-4个碳原子的低级烷基,R 4表示氢原子,羟基R 5表示羟基或乙酰氧基,或R 4和R 5一起表示二价亚烷基二氧基,R 6表示羟基,甲氧基或乙酰氧基,R 7表示甲基或羟甲基, R 8表示氢原子或羟基,并且表示在类固醇核的4-或5-位具有双键的基团或碳原子。通过使相应的14-叠氮基衍生物与糖偶联反应,然后还原,来制备这种酯。在治疗中的应用,尤其是在心力衰竭的治疗中。

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