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1. 发明申请

WO2008037226A3 METHOD OF PREPARATION OF A SOLUBLE FORMULATION OF WATER-INSOLUBLE PENTACYCLIC AND TETRACYCLIC TERPENOIDS, A SOLUBLE FORMULATION OF A PENTACYCLIC OR TETRACYCLIC TERPENOID AND A PHARMACEUTICAL COMPOSITION CONTAINING THIS SOLUBLE FORMULATION 审中-公开
标题翻译：制备水不溶性的五邻和四环萜烯的可溶配方，戊二酸或四环萜烯的可溶配方和含该可溶配方的药物组合物的制备方法
公开(公告)号：WO2008037226A3
公开(公告)日：2008-07-31
申请号：PCT/CZ2007000088
申请日：2007-09-25
申请人： UNIVERZITA KARLOVA V PRAZE PRI , UNIVERZITA PALACKEHO V OLOMOUC , I Q A A S , SAREK JAN , HAJDUCH MARIAN , SVOBODA MICHAL , NOVAKOVA KATERINA , SPACILOVA PAVLA , KUBELKA TOMAS , BIEDERMANN DAVID
发明人： SAREK JAN , HAJDUCH MARIAN , SVOBODA MICHAL , NOVAKOVA KATERINA , SPACILOVA PAVLA , KUBELKA TOMAS , BIEDERMANN DAVID
IPC分类号： A61K31/56 , C07J63/00 , C07J71/00
CPC分类号： C07J71/0047 , A61K31/56 , A61K47/6951 , B82Y5/00 , C07J63/008
摘要： The invention relates to a method of preparation of a soluble formulation of water-insoluble pentacyclic and tetracyclic terpenoids, wherein the water-insoluble terpenoid having a free carboxylic, hydroxy or amino functional group is derivatized on this functional group with a substituent selected from the group comprising substituents of general formula Xa bound to the hydroxy group of the terpenoid, wherein Xa is -OC-R-COOH, substituents of general formula Xa bound to the amino group of the terpenoid, wherein Xa is -OC-R-COOH, quarternary ammonium substituents of general formula Xb bound to the carboxy group of the terpenoid, wherein Xb is -(CH2)nN+R3Y-, quarternary ammonium substituents of general formula Xc bound to the carboxy group of the terpenoid, wherein Xc je -(CH2)nR+Y-, substituents of general formula Xd bound to the carboxy group of the terpenoid, wherein Xd represents -R-COOH, glycosylic substituents Xe bound by alpha or beta glycosidic bond to the hydroxy group or to the carboxy group of the terpenoid, wherein Xe is selected from the group comprising glucosyl, galactosyl, arabinosyl, rhamnosyl, lactosyl, cellobiosyl, maltosyl and the 2-deoxyanalogues thereof, and subsequently, the prepared derivative is dissolved in the solution containing water, a cyclodextrin and optionally pharmaceutically acceptable auxiliary substances, forming an inclusion derivative with the cyclodextrin. Object of the invention is further a soluble formulation of a pentacyclic or tetracyclic triterpenoid, containing an inclusion complex of the derivatized pentacyclic or tetracyclic terpenoid with a cyclodextrin, and optionally water and pharmaceutically acceptable auxiliary substances and further a pharmaceutical composition containing the soluble formulation.
摘要翻译：本发明涉及制备水不溶性五环和四环萜类的可溶性制剂的方法，其中具有游离羧酸，羟基或氨基官能团的水不溶性萜类在该官能团上被选自以下的取代基衍生化包含与萜类化合物的羟基结合的通式Xa的取代基，其中Xa是-OC-R-COOH，通式Xa的取代基与萜类化合物的氨基结合，其中Xa是-OC-R-COOH，四元其中Xb是 - （CH2）nN + R3Y-的通式Xb的铵取代基与通式Xc的季铵取代基结合到萜类化合物的羧基上，其中Xc - （CH2） nR + Y-，通式Xd的取代基与萜类化合物的羧基结合，其中Xd表示-R-COOH，糖基取代基Xe通过α或β糖苷键与羟基或β 其中Xe选自葡糖基，半乳糖基，阿拉伯糖基，鼠李糖基，乳糖基，纤维二糖基，麦芽糖基及其2-脱氧类似物，然后将制备的衍生物溶于含有水，环糊精和任选的药学上可接受的辅助物质，与环糊精形成包合物衍生物。本发明的目的还在于含有衍生的五环或四环萜类化合物与环糊精的包合配合物，以及任选的水和药学上可接受的辅助物质的五环或四环三萜类化合物的可溶性制剂以及含有该可溶性制剂的药物组合物。

2. 发明申请

WO2008086759A3 METHOD OF PREPARATION AND ISOLATION OF BETULIN DIACETATE FROM BIRCH BARK FROM PAPER MILLS AND ITS OPTIONAL PROCESSING TO BETULIN 审中-公开
标题翻译：制备和分离来自纸浆的BIRCH BARK的白芥子酸酯的方法及其对BETULIN的可选处理
公开(公告)号：WO2008086759A3
公开(公告)日：2009-02-26
申请号：PCT/CZ2008000004
申请日：2008-01-09
申请人： UNIVERZITA KARLOVA V PRAZE PRI , I Q A A S , UNIVERZITA PALACKEHO V OLOMOUC , SAREK JAN , SVOBODA MICHAL , HAJDUCH MARIAN
发明人： SAREK JAN , SVOBODA MICHAL , HAJDUCH MARIAN
IPC分类号： C07J63/00
CPC分类号： C07J63/008 , Y02P20/544
摘要： The invention relates to a method of preparation and isolation of betulin diacetate from birch bark from paper mills and its optional processing to betulin, wherein the birch bark is ground, mixed with two- to twenty-fold excess volume of water and is stirred so that all birch bark is dipped, then the fraction of the birch bark which floats on the surface is collected, said collected fraction is dried at the temperature in the range of from 50 to 85 °C and the betulin contained in the dried birch bark is then subjected to an acetylation reaction, after the acetylation the birch bark is dried at the temperature of from 50 to 100 °C and the formed betulin diacetate is then isolated from the birch bark by supercritical extraction of the birch bark with carbon dioxide at the pressure of 28-35 MPa and the temperature of from 50 to 100 °C and subsequently, the supercritical extract is recrystallized for direct use or for further processing. The further processing can be basic hydrolysis of the re-crystallized betulin diacetate to betulin.
摘要翻译：本发明涉及从造纸厂的桦树皮制备和分离桦木二乙酸酯的方法及其对桦木醇的任选加工，其中将桦树皮研磨，与二至二十倍体积的水混合并搅拌，使得将所有桦树皮浸渍，然后收集漂浮在表面上的桦树皮部分，收集的部分在50至85℃的温度范围内干燥，然后将干燥的桦树皮中含有的桦木醇进行乙酰化反应，乙酰化后，桦木树皮在50〜100℃的温度下干燥，然后通过超临界萃取桦树皮与二氧化碳在压力下从桦木树皮中分离形成的桦木醇二乙酸酯 28-35MPa，温度为50〜100℃，然后将超临界萃取物重结晶直接使用或进一步处理。进一步的处理可以是重结晶的桦木醇二乙酸酯至桦木醇的碱性水解。

3. 发明专利

CA2666437A1 METHOD OF PREPARATION OF A SOLUBLE FORMULATION OF WATER-INSOLUBLE PENTACYCLIC AND TETRACYCLIC TERPENOIDS, A SOLUBLE FORMULATION OF A PENTACYCLIC OR TETRACYCLIC TERPENOID AND A PHARMACEUTICAL COMPOSITION CONTAINING THIS SOLUBLE FORMULATION 未知
公开(公告)号：CA2666437A1
公开(公告)日：2008-04-03
申请号：CA2666437
申请日：2007-09-25
申请人： UNIVERZITA KARLOVA V PRAZE PRI , UNIVERZITA PALACKEHO V OLUMOUC , I Q A A S
发明人： BIEDERMANN DAVID , KUBELKA TOMAS , SPACILOVA PAVLA , NOVAKOVA KATERINA , SAREK JAN , SVOBODA MICHAL , HAJDUCH MARIAN
IPC分类号： A61K31/56 , C07J63/00 , C07J71/00
摘要： The invention relates to a method of preparation of a soluble formulation of water-insoluble pentacyclic and tetracyclic terpenoids, wherein the wate r-insoluble terpenoid having a free carboxylic, hydroxy or amino functional group is derivatized on this functional group with a substituent selected fr om the group comprising substituents of general formula Xa bound to the hydr oxy group of the terpenoid, wherein Xa is -OC-R-COOH, substituents of genera l formula Xa bound to the amino group of the terpenoid, wherein Xa is -OC-R- COOH, quarternary ammonium substituents of general formula Xb bound to the c arboxy group of the terpenoid, wherein Xb is -(CH2)nN+R3Y-, quarternary ammo nium substituents of general formula Xc bound to the carboxy group of the te rpenoid, wherein Xc je -(CH2)nR+Y-, substituents of general formula Xd bound to the carboxy group of the terpenoid, wherein Xd represents -R-COOH, glyco sylic substituents Xe bound by alpha or beta glycosidic bond to the hydroxy group or to the carboxy group of the terpenoid, wherein Xe is selected from the group comprising glucosyl, galactosyl, arabinosyl, rhamnosyl, lactosyl, cellobiosyl, maltosyl and the 2-deoxyanalogues thereof, and subsequently, th e prepared derivative is dissolved in the solution containing water, a cyclo dextrin and optionally pharmaceutically acceptable auxiliary substances, for ming an inclusion derivative with the cyclodextrin. Object of the invention is further a soluble formulation of a pentacyclic or tetracyclic triterpenoi d, containing an inclusion complex of the derivatized pentacyclic or tetracy clic terpenoid with a cyclodextrin, and optionally water and pharmaceuticall y acceptable auxiliary substances and further a pharmaceutical composition c ontaining the soluble formulation.

4. 发明专利

CA2673226A1 METHOD OF PREPARATION AND ISOLATION OF BETULIN DIACETATE FROM BIRCH BARK FROM PAPER MILLS AND ITS OPTIONAL PROCESSING TO BETULIN 未知
公开(公告)号：CA2673226A1
公开(公告)日：2008-07-24
申请号：CA2673226
申请日：2008-01-09
申请人： I Q A A S , UNIVERZITA KARLOVA V PRAZE PRI , UNIVERZITA PALACKEHO V OLOMOUC
发明人： HAJDUCH MARIAN , SVOBODA MICHAL , SAREK JAN
IPC分类号： C07J63/00
摘要： The invention relates to a method of preparation and isolation of betulin diacetate from birch bark from paper mills and its optional processing to b etulin, wherein the birch bark is ground, mixed with two- to twenty-fold exc ess volume of water and is stirred so that all birch bark is dipped, then th e fraction of the birch bark which floats on the surface is collected, said collected fraction is dried at the temperature in the range of from 50 to 85 °C and the betulin contained in the dried birch bark is then subjected to a n acetylation reaction, after the acetylation the birch bark is dried at the temperature of from 50 to 100 °C and the formed betulin diacetate is then i solated from the birch bark by supercritical extraction of the birch bark wi th carbon dioxide at the pressure of 28-35 MPa and the temperature of from 5 0 to 100 °C and subsequently, the supercritical extract is recrystallized fo r direct use or for further processing. The further processing can be basic hydrolysis of the re-crystallized betulin diacetate to betulin.

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