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1. 发明授权

US06239139B1 13,13A-Didehydroberbine derivatives 失效
标题翻译： 13,13A-脱氢ber嗪衍生物
公开(公告)号：US06239139B1
公开(公告)日：2001-05-29
申请号：US09233323
申请日：1999-01-20
申请人： Jung Ho Kim , Tae Neung Jhong , Young Ki Paik , Joon Seo Park , Eui Deok Kim , You Suk Lee , Seung Un Kim
发明人： Jung Ho Kim , Tae Neung Jhong , Young Ki Paik , Joon Seo Park , Eui Deok Kim , You Suk Lee , Seung Un Kim
IPC分类号： C07D491056
CPC分类号： C07D471/04 , C07D491/04
摘要： The present invention provides a cholesterol biosynthesis inhibitor which specifically inhibits the sterol 14-reductase which is involved in the distal pathway of cholesterol biosynthesis, a compound of formula (1) below and the use of an extract or the compound of formula (1) for treating hypercholesterolaemia or hyperlipidaemia. The inhibitor comprises an extract obtained by extracting Corydalis Turtschaninowii Besser with a solvent, or an organic layers obtained by partitioning an extract from Corydalis Turtschaninowii Besser with an organic solvent. The extract contains 7,8,13,13&agr;-tetrahydrocoridaline or its derivative, as the active ingredients, which specifically inhibits the enzyme which is involved in the distal pathway of the cholesterol biosynthesis. R1 and R2 which may be the same or different from each other, represent a hydroxy group or an alkoxy group having 1 to 4 carbon atoms or both of R1 and R2 represent a methylenedioxy group; R3 represents a hydrogen atom; R4 and R5 which may be the same or different from each other, represent a hydroxy group, a hydroxyethylamino group or an alkoxy group having 1 to 4 carbon atoms; R6 represents a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkenyl group having 3 to 8 carbon atoms, a cycloalkylalkyl group having 1 to 7 carbon atoms, a holoalkyl group having 1 to 4 carbon atoms, an ethoxycarbonyl group, an ethoxycarbonylmethyl group, a hydroxycarbonylmethyl group, 1-ethoxycarbonylethyl group, or 2-valerolactonyl group.
摘要翻译：本发明提供了一种胆固醇生物合成抑制剂，其特异性抑制参与胆固醇生物合成的远端途径的甾醇14-还原酶，以下式（1）的化合物以及提取物或式（1）化合物用于治疗高胆固醇血症或高脂血症。抑制剂包括通过用溶剂提取紫茎泽兰植物提取物获得的提取物或通过用有机溶剂分离来自紫堇（Corydalis Turtschaninowii Besser）的提取物获得的有机层。提取物含有7,8,13,13α-四氢花青苷或其衍生物作为活性成分，其特异性抑制参与胆固醇生物合成的远端途径的酶.R1和R2可以相同或不同另一个表示羟基或具有1至4个碳原子的烷氧基，或者R 1和R 2都表示亚甲二氧基; R 3表示氢原子; R 4和R 5可以相同或不同，表示羟基基团，羟乙基氨基或具有1〜4个碳原子的烷氧基; R6表示氢原子，碳原子数1〜8的烷基，碳原子数3〜8的烯基，碳原子数为1〜7的环烷基烷基原子，具有1至4个碳原子的全烷基，乙氧基羰基，乙氧基羰基甲基，羟基羰基甲基，1-乙氧基羰基乙基或2-戊内酰基。

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