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1. 发明申请

WO0190136A2 TRITERPENOID DERIVATIVES 审中-公开
标题翻译： TRITERPENOID衍生物
公开(公告)号：WO0190136A2
公开(公告)日：2001-11-29
申请号：PCT/GB0102313
申请日：2001-05-23
申请人： UNIVERZITA PALACKEHO V OLOMOUC , UNIV KARLOVA , CYCLACEL LTD , HAJDUCH MARIAN , SAREK JAN
发明人： HAJDUCH MARIAN , SAREK JAN
IPC分类号： A61K31/19 , A61K31/215 , A61K31/365 , A61P35/00 , C07J63/00 , C07J
CPC分类号： C07J63/008 , A61K31/19 , A61K31/215 , A61K31/365
摘要： The present invention relates to the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in therapy. Preferably, the compound may be used for treating a patient suffering from leukaemia, cancer or other proliferative disorder. A further embodiment relates to the use of a compound of formula (I) in an assay for detecting the phosphorylation and acetylation state of cellular substrates. The present invention also relates to novel compounds of formula (Ia).
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐在治疗中的用途。优选地，该化合物可用于治疗患有白血病，癌症或其它增殖性病症的患者。另一个实施方案涉及式（I）化合物在用于检测细胞底物的磷酸化和乙酰化状态的测定中的用途。本发明还涉及新的式（Ia）化合物。

2. 发明申请

WO0190096A3 TRITERPENOID DERIVATIVES AND THEIR USE AS ANTIPROLIFERATIVE AGENTS 审中-公开
标题翻译：三磷酸酯衍生物及其用作抗增生剂
公开(公告)号：WO0190096A3
公开(公告)日：2002-03-07
申请号：PCT/GB0102341
申请日：2001-05-23
申请人： UNIVERZITA PALACKEHO V OLOMOUC , UNIV KARLOVA , CYCLACEL LTD , HAJDUCH MARIAN , SAREK JAN
发明人： HAJDUCH MARIAN , SAREK JAN
IPC分类号： A61K31/343 , A61P35/00 , C07D307/00
CPC分类号： C07D307/00 , A61K31/343
摘要： The present invention relates to the use of a compound of formula (I), or a pharmaceutically acceptable salt, crystal form, complex, hydrate, or hydrolysable ester thereof, in the preparation of a medicament for treating a patient suffering from leukaemia, cancer or other proliferative disorder. A further embodiment relates to the use of a compound of formula (I) in an assay for detecting the phosphorylation state of cellular substrates. The present invention also relates to novel compounds of formula (Ia), and the chemical synthesis thereof.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，晶体形式，复合物，水合物或可水解的酯在制备用于治疗患有白血病，癌症或其他增殖性疾病。另一实施方案涉及式（I）化合物在用于检测细胞底物的磷酸化状态的测定中的用途。本发明还涉及新的式（Ia）化合物及其化学合成。

3. 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。

4. 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。

5. 发明申请

WO03045971A3 SOLVATES OF 3.BETA., 28-DIACETOXY-18-OXO-19, 20, 21, 29, 30-PENTANORLUPAN-22-OIC ACID, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS THEREOF 审中-公开
标题翻译： 3.BETA。，28-二羧酸-18-OXO-19,20,21,29,30-泛醇 - 22-酸的溶液，其制备方法及其药物组合物
公开(公告)号：WO03045971A3
公开(公告)日：2003-07-31
申请号：PCT/GB0205231
申请日：2002-11-21
申请人： CYCLACEL LTD , UNIV KARLOVA , UNIV PALACKEHO , FISCHER PETER M , SAREK JAN , BLANEY PAUL M , COLLIER PIERS , FERGUSON JOHN R , HULL JONATHAN D
发明人： FISCHER PETER M , SAREK JAN , BLANEY PAUL M , COLLIER PIERS , FERGUSON JOHN R , HULL JONATHAN D , HAJDUCH MARIAN
IPC分类号： A61P35/00 , C07J63/00 , C07J71/00 , A61K31/565
CPC分类号： C07J63/008 , C07J71/0005
摘要： The present invention relates to 3beta,28-diacetoxy-18-oxo-19,20,21,29,30-pentanorlupan-22-oic acid methanol solvate, its use in medicine and processes for its preparation.
摘要翻译：本发明涉及3β，28-二乙酰氧基-18-氧代-19,20,21,29,30-戊酰氧基-22-酸甲醇溶剂化物，其用于医药及其制备方法。

6. 发明申请

WO2010054606A3 TRIPERPENOID 2 - DEOXY GLYCOSIDES AND USE THEREOF AS MEDICAMENTS 审中-公开
标题翻译：三倍体2 - 去氧果糖苷及其作为药物的用途
公开(公告)号：WO2010054606A3
公开(公告)日：2012-02-16
申请号：PCT/CZ2009000132
申请日：2009-11-06
申请人： UNIVERZITA PALACKEHO V OLOMOUCI , SAREK JAN , SPACILOVA PAVLA , HAJDUCH MARIAN
发明人： SAREK JAN , SPACILOVA PAVLA , HAJDUCH MARIAN
IPC分类号： A61K31/704 , A61K31/7004 , A61P35/00 , C07J63/00
CPC分类号： A61K31/704 , A61K31/7004 , C07J63/008
摘要： The invention describes novel triterpenoid 2-deoxy glycosides of general formula I, wherein at least one of the substituents X1 and R2 contains a 2-deoxy glycosidic group, method of preparation thereof, their cytotoxic activity and a pharmaceutical formulation containing these compounds.
摘要翻译：本发明描述了通式I的新型三萜化合物2-脱氧糖苷，其中至少一个取代基X1和R2含有2-脱氧糖苷基，其制备方法，它们的细胞毒性活性和含有这些化合物的药物制剂。

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