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CN101513401B 一种β-间二羟基苯甲酸大环内酯衍生物在制备防治疟疾的药物中的应用 失效 - 权利终止

一种β-间二羟基苯甲酸大环内酯衍生物在制备防治疟疾的药物中的应用
摘要：
本发明涉及通式(1)表示的β-间二羟基苯甲酸大环内酯衍生物在预防和治疗疟疾中的应用，其中化合物1：R1＝OH，R2＝H，R3＝CH3，为单键，R4和R5合并为一个氧原子，为双键，R6＝OH；或化合物2：R1＝H，R2＝OH，R3＝CH3，为单键，R4和R5合并为一个氧原子，为双键，R6＝OH；或化合物3：R1＝OH，R2＝H，R3＝CH3，为单键，R4和R6合并为一个氧原子，为双键，R5＝OH；或化合物4：R1＝OH，R2＝H，R3＝CH3，为双键，R4和R5不存在，为单键，R6＝OH；或化合物5：R1＝H，R2＝OH，R3＝CH3，为双键，R4和R5不存在，为单键，R6＝OH。实验证明该系列化合物具有很强的抗疟原虫药物敏感株活性和抗疟原虫药物抗性株活性。
摘要（英）：

The invention relates to the application of beta-m-dihydroxy-benzoic acid macrocyclic lactone derivative shown in general formula (1) in the prevention of malaria, wherein, compound 1: R1=OH, R2=H, R3=CH3, * is single bond, R4 and R5 are merged into one oxygen atom, * is double bond and R6=OH; or compound 2: R1=H, R2=OH, R3=CH3, * is single bond, R4 and R5 are merged into one oxygen atom, * is double bond and R6=OH; or compound 3: R1=OH, R2=H, R3=CH3, * is single bond, R4 and R6 are merged into one oxygen atom, * is double bond and R5=OH; or compound 4: R1=OH, R2=H, R3=CH3, * is double bond, R4 and R5 are not available, * is single bond and R6=OH; or compound 5: R1=H, R2=OH, R3=CH3, * is double bond, R4 and R5 are not available, * is single bond and R6=OH. The experiments prove that series compound has stronger plasmodium resisting drug sensitive strain activity and plasmodium resisting drug resistant strain activity.

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