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1. 发明授权

US4213911A Process for preparing high-melting chenodeoxycholic acid 失效
标题翻译：制备高熔点鹅脱氧胆酸的方法
公开(公告)号：US4213911A
公开(公告)日：1980-07-22
申请号：US958508
申请日：1978-11-07
申请人： Michael C. Attwell , Thomas F. Massiah , Roberto A. Vergottini , Peter Ziegler
发明人： Michael C. Attwell , Thomas F. Massiah , Roberto A. Vergottini , Peter Ziegler
IPC分类号： C07J9/00
CPC分类号： C07J9/005
摘要： A process for preparing a high-melting form of CDCA having a melting point of at least about 160.degree. C. is disclosed which comprises the steps of:(a) suspending at least one form of CDCA having a melting point of below 160.degree. C. in a non-aromatic liquid hydrocarbon, preferably cyclohexane, to form a suspension having a boiling point of at least 65.degree. C.;(b) heating the suspension to a sufficiently high temperature of between about 65.degree. and about 140.degree. C., preferably between about 75.degree. and about 100.degree. C., during a sufficiently long period of time for converting substantially all of the CDCA into the high-melting form;(c) recovering the high-melting form of CDCA from the suspension.Low-melting amorphous and/or crystalline forms of CDCA, as well as CDCA-solvent inclusion complexes can be treated in the above-described process. The high-melting CDCA is obtained in form of a substantially granular powder, which is suitable to be formulated into therapeutical compositions.
摘要翻译：公开了一种制备熔点至少为约160℃的高熔点形式的CDCA的方法，其包括以下步骤：（a）将至少一种形式的熔点低于160℃的CDCA悬浮在非芳族液体烃，优选环己烷中，形成沸点至少为65℃的悬浮液。（b）在足够长的时间内将悬浮液加热至约65℃至约140℃，优选约75℃至约100℃的足够高的温度，以将基本上所有的CDCA转化为高熔点形式; （c）从悬浮液中回收高熔点形式的CDCA。可以在上述方法中处理低熔点无定形和/或结晶形式的CDCA，以及CDCA-溶剂包合物。获得高熔点CDCA，其形式为基本上粒状粉末，其适于配制成治疗组合物。

2. 发明授权

US4186143A Chenodeoxycholic acid recovery process 失效
标题翻译：去氧胆酸恢复过程
公开(公告)号：US4186143A
公开(公告)日：1980-01-29
申请号：US932176
申请日：1978-08-09
申请人： Peter Ziegler , Michael C. Attwell , Thomas F. Massiah , Roberto A. Vergottini
发明人： Peter Ziegler , Michael C. Attwell , Thomas F. Massiah , Roberto A. Vergottini
IPC分类号： C07J9/00
CPC分类号： C07J9/005
摘要： A method of isolating chenodeoxycholic acid from hog bile is provided, which comprises the steps of treating the hog bile under saponifying conditions separating the bile acids from the water-soluble constituents of the saponified bile; esterifying the bile acids to obtain a mixture of bile acid esters; isolating from the mixture of bile acid esters the hyodeoxycholic acid ester as its adduct with a compound selected from the group consisting of benzene and toluene; treating the remaining bile acid esters under acetylating conditions; isolating the hyocholic acid ester triacetate; isolating the chenodeoxycholic acid ester diacetate; treating the chenodeoxycholic acid ester diacetate under saponifying conditions; isolating the chenodeoxycholic acid thus obtained; and, optionally purifying the chenodeoxycholic acid.The method described yields chenodeoxycholic acid of exceedingly high purity, which may be used in the treatment of gallstones by their dissolution in vivo.
摘要翻译：提供了从猪胆中分离鹅脱氧胆酸的方法，其包括在皂化条件下将胆汁酸与皂化胆汁的水溶性成分分离的步骤：酯化胆汁酸以获得胆汁酸酯的混合物; 从胆汁酸酯的混合物中分离猪脱氧胆酸酯作为其加合物与选自苯和甲苯的化合物; 在乙酰化条件下处理剩余的胆汁酸酯; 隔离天holic酸酯三醋酸酯; 分离鹅脱氧胆酸酯二乙酸酯; 在皂化条件下处理鹅脱氧胆酸酯二乙酸酯; 分离由此获得的鹅脱氧胆酸; 和任选地纯化鹅脱氧胆酸。所述方法得到具有非常高纯度的鹅脱氧胆酸，其可用于通过其在体内溶解来治疗胆结石。

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