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发明授权
CN1935131B 1β-羟基冬青酸用于制备抑制乙肝病毒的药物用途 失效 - 权利终止

1β-羟基冬青酸用于制备抑制乙肝病毒的药物用途
摘要：
本发明涉及一种具有式(1)所示结构之桉烷型倍半萜衍生物1β-羟基冬青酸(1β-Hydroxyilicic acid)，即1β-羟基-5αH-桉烷-11(13)-烯12-酸及其可药用盐或溶剂化物及其药物组合物在制备治疗乙肝病毒感染疾病和抗乙肝病毒药物中的医药用途。式(1)化合物对HepG2.2.15细胞分泌的乙型肝炎表面抗原(HBsAg)和乙肝病毒脱氧核糖核酸(HBV-DNA)的复制具有较强的抑制作用，其抑制HBsAg能力在同一剂量超过阳性对照拉米呋啶；其在100μg/mL、20μg/mL和4μg/mL浓度时对乙肝病毒HBV-DNA的复制都有抑制活性，属于非核苷类抗乙肝病毒天然产物，可以预期应用于制备治疗乙肝病毒感染疾病的药物。
摘要（英）：

The present invention relates to an eudesmane type sesquiterpene derivative 1 beta-hydroxyilicic acid having a structure of formula (1), namely 1 beta-hydroxy-5 alpha H-eudesmane-11 (13)-ene-12-acid, a medicinal salt or solvent compound thereof and medicinal application of the medicine composition for preparing medicines capable of curing hepatitis B virus infective disease and resisting hepatitis B virus. Said invention also provides its chemical structure formula. The compound of formula (1) has stronger inhibition to the replication of the HBV-DNA and the HBsAg secreted by HepG2.2.15 cells, and the inhibition ability to the HBsAg exceeds positive control Lamivudine at the same dosage. The compound has inhibition activity to the HBV-DNA at concentration of 100mu g/mL, 20mu g/mL and 4mu g/mL, and belongs to non-nucleoside anti-HBV natural product, which is expected to apply to prepare the medicine for curing the hepatitis B virus infective disease.

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