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1. 发明申请

WO2004013154A1 METHOD FOR PREPARING OLIGONUCLEOTIDES 审中-公开
标题翻译：制备寡核苷酸的方法
公开(公告)号：WO2004013154A1
公开(公告)日：2004-02-12
申请号：PCT/EP2003/008447
申请日：2003-07-30
申请人： GIRINDUS AG , CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE , UNIVERSITY OF MONTPELLIER II , ADAMO, Ilaria , DUEYMES, Cécile , SCHÖNBERGER, Andreas , IMBACH, Jean-Louis , MEYER, Albert , MORVAN, Francois , DEBART, Francoise , VASSEUR, Jean-Jacques , LANGE, Meinolf , LINK, Fritz
发明人： ADAMO, Ilaria , DUEYMES, Cécile , SCHÖNBERGER, Andreas , IMBACH, Jean-Louis , MEYER, Albert , MORVAN, Francois , DEBART, Francoise , VASSEUR, Jean-Jacques , LANGE, Meinolf , LINK, Fritz
IPC分类号： C07H21/00
CPC分类号： C07H21/00 , C07H21/02 , C07H21/04 , Y02P20/55 , Y02P20/582
摘要： A method for preparing an oligonucleotide comprising the steps ofa) providing a 3 -protected compound having the formula: whereinB is a heterocyclic baseR2 is H, a protected 2 -hydroxyl group, F, a protected amino group, an O-alkyl group, an O-substituted alkyl, a substituted alkylamino or a C4′- O2′methylen linkage R3 is OR′3, NHR′′3, NR′′3R′′′3, a 3′-protected nucleotide or a 3′-protected oligonucleotide,R′3 is a hydroxyl protecting group,R′′3, R′′′3 are independently an amine protecting group, b) reacting said compound with a nucleotide derivative having a 5 -proctection group in the presence of a solid supported activator to give an elongated oligonucleotide with a P(III)-internucleotide bondc) optionally processing the elongated oligonucleotide with a P(III)-internucleotide bond by either or both of steps c1) and c2) in any sequencec1) capping preferably by reacting with a solid supported capping agentc2) oxidizing preferably by reacting the oligonucleotide with a solid supported oxidizing reagent d) removing the 5′ -protection group.
摘要翻译：一种制备寡核苷酸的方法，包括以下步骤：a）提供具有下式的3-保护的化合物：其中B是杂环碱基R2是H，受保护的2-羟基，F，被保护的氨基，O-烷基， O-取代的烷基，取代的烷基氨基或C 4'- O 2'亚甲基键R3是OR'3，NHR'3，NR''3R“'，3'-保护的核苷酸或3'-保护的寡核苷酸 R'3为羟基保护基，R“3”，“3”独立地为胺保护基团，b）在固体支持的活化剂存在下使所述化合物与具有5-保护基团的核苷酸衍生物反应给出具有P（III） - 核苷酸键的细长寡核苷酸c）任选地通过任何序列c1）和c2）中的任一个或两个步骤c1）和c2）用P（III） - 核苷酸键处理细长寡核苷酸，优选通过与固体负载的封端剂c2）优选通过使寡核苷酸与支持的固体反应而氧化氧化剂d）除去5'保护基。

2. 发明申请

WO2006079660A1 PURIFICATION OF OLIGONUCLEOTIDES 审中-公开
标题翻译：纯化寡核苷酸
公开(公告)号：WO2006079660A1
公开(公告)日：2006-08-03
申请号：PCT/EP2006/050503
申请日：2006-01-30
申请人： GIRINDUS AG , LANGE, Meinolf , GRÖSSEL, Olaf , LINK, Fritz , SCHÖNBERGER, Andreas , HOHLFELD, Andreas
发明人： LANGE, Meinolf , GRÖSSEL, Olaf , LINK, Fritz , SCHÖNBERGER, Andreas , HOHLFELD, Andreas
IPC分类号： C07H21/00
CPC分类号： C07H21/00
摘要： A method for purifying a protected oligonucleotide comprising the steps of: a) - providing a solution of the protected oligonucleotide in at least one solvent A having a boiling point below the boiling point of a solvent B, - heating the solution at a temperature of at least 30°C and below the boiling point of the at least solvent A, - adding solvent B until precipitation of a material is visible in the solution, said solvent B being an alcohol having 1 to 6 C-atoms or a diol having 2 to 6 C-atoms, - allowing the solution to cool down under stirring until formation of a supernatant and a residue, - removing the supernatant or b) - providing solvent B, said solvent B being an alcohol having 1 to 6 C- atoms or a diol having 2 to 6 C-atoms, - heating solvent B at a temperature above 30°C and below the boiling point of solvent B, - adding a solution of a protected oligonucleotide in at least one solvent A until precipitation of a material is visible in the solution, - allowing the solution to cool down under stirring until formation of a supernatant and a residue, - removing the supernatant.
摘要翻译：一种用于纯化受保护的寡核苷酸的方法，包括以下步骤：a） - 将受保护的寡核苷酸的溶液提供在沸点低于溶剂B的沸点的至少一种溶剂A中， - 在至少30℃且低于至少溶剂A的沸点， - 加入溶剂B，直到在溶液中可见材料沉淀，所述溶剂B是具有1至6个C原子的醇或具有2至 6个C原子， - 允许溶液在搅拌下冷却直到形成上清液和残余物， - 去除上清液或b）提供溶剂B，所述溶剂B是具有1-6个C原子的醇或具有2至6个C原子的二醇， - 在高于30℃且低于溶剂B的沸点的温度下加热溶剂B， - 在至少一种溶剂A中加入受保护的寡核苷酸的溶液，直到材料沉淀可见在解决方案中， - 允许soluti 在搅拌下冷却直到形成上清液和残余物， - 除去上清液。

3. 发明申请

WO2006094963A1 SYNTHESIS OF OLIGONUCLEOTIDES 审中-公开
标题翻译：合成寡核苷酸
公开(公告)号：WO2006094963A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/060489
申请日：2006-03-06
申请人： GIRINDUS AG , LANGE, Meinolf , SCHÖNBERGER, Andreas , HOHLFELD, Andreas , GRÖSSEL, Olaf , KIRCHHOFF, Christine , LINK, Fritz
发明人： LANGE, Meinolf , SCHÖNBERGER, Andreas , HOHLFELD, Andreas , GRÖSSEL, Olaf , KIRCHHOFF, Christine , LINK, Fritz
IPC分类号： C07H21/00
CPC分类号： C07H21/00 , Y02P20/55
摘要： A method for preparing an oligonucleotide comprising the steps of a) providing a hydroxyl containing compound having the formula (A), wherein B is a heterocyclic base and i) R 2 is H, a protected 2'-hydroxyl group, F, a protected amino group, an O-alkyl group, an O-substituted alkyl, a substituted alkylamino or a C4 '-O2 ' methylen linkage; R 3 is OR' 3 , NHR" 3 , NR" 3 R' 3 , wherein R 3 is a hydroxyl protecting group, a protected nucleotide or a protected oligonucleotide, R" 3 , R" 3 are independently amine protecting groups, and R 5 is OH or ii) R 2 is H, a protected 2'-hydroxyl group, F, a protected amino group, an O-alkyl group, an O-substituted alkyl, a substituted alkylamino or a C4'-O2 'methylen linkage; R 3 is OH and R 5 is OR' 5 and R' 5 is a hydroxyl protecting group, a protected nucleotide or a protected oligonucleotide or iii) R 2 is OH, R 3 is OR' 3 , NHR" 3 , NR" 3 R'" 3 , wherein R 3 is a hydroxyl protecting group, a protected nucleotide or a protected oligonucleotide, R" 3 , R" 3 are independently amine protecting groups, and R 5 is OR' 5 and R' 5 is a hydroxyl protecting group, a protected nucleotide or a protected oligonucleotide b) reacting said compound with a phosphitylating agent in the presence of an activator having the formula (I) (activator I) wherein R = alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl; R 1 , R 2 = either H or form a 5 to 6-membered ring together; X 1 , X 2 = independently either N or CH; Y = H or Si(R 4 ) 3 , with R 4 = alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl; B = deprotonated acid to prepare a phosphitylated compound; c) reacting said phosphitylated compound without isolation with a second compound having the formula (A) wherein R 5 , R 3 , R 2 , B are independently selected, but have the same definition as above in the presence of an activator II different from activator I.
摘要翻译：一种制备寡核苷酸的方法，包括以下步骤：a）提供具有式（A）的含羟基化合物，其中B是杂环碱基，i）R 2是H，被保护的2'- 羟基，F，被保护的氨基，O-烷基，O-取代的烷基，取代的烷基氨基或C 4'-O 2'亚甲基键; R 3是OR 3，NHR“3”，“NR”3 R“3” 其中R 3是羟基保护基，被保护的核苷酸或被保护的寡核苷酸，R“3，R”3个独立地是胺保护基，R 5是OH或ii）R 2是H，被保护的2'-羟基，F，被保护的氨基，O-烷基基团，O-取代的烷基，取代的烷基氨基或C4'-O2'亚甲基键; R 3是OH，R 5是OR 5，并且R 5是羟基保护基，受保护的核苷酸或受保护的寡核苷酸或iii）R 2是OH，R 3是OR 3，NHR“3，其中R 3是羟基保护基，受保护的核苷酸或受保护的寡核苷酸，R 3，R 3，R 3，R 3， “3”，R“3”3“独立地为胺保护基，R 5为OR'5和R' b）羟基保护基，受保护的核苷酸或受保护的寡核苷酸b）使所述化合物与磷酸化剂在存在下具有式（I）的活化剂（活化剂I）（其中R =烷基，环烷基，芳基，芳烷基，杂烷基，杂芳基; R 1，R 2 = H或一起形成5至6元环; X 1， X 2独立地是N或CH; Y = H或Si（R 4）3，其中R 1， 4 = alk 芳基，芳烷基，杂烷基，杂芳基; B =脱质子酸以制备磷酸化化合物; c）使所述磷化物化合物与不与其分离的具有式（A）的第二化合物反应，其中R 5，R 3，R 2，B，在不同于活化剂I的活化剂II的存在下，它们具有与上述相同的定义。

4. 发明申请

WO2006064039A1 SYNTHESIS OF PHOSPHITYLATED COMPOUNDS USING A QUATERNARY HETEROCYCLIC ACTIVATOR 审中-公开
标题翻译：使用四元杂环激活剂合成磷酸化合物
公开(公告)号：WO2006064039A1
公开(公告)日：2006-06-22
申请号：PCT/EP2005/056815
申请日：2005-12-15
申请人： GIRINDUS AG , LANGE, Meinolf , SCHÖNBERGER, Andreas , KIRCHHOFF, Christina , GRÖSSEL, Olaf , OMELCENKO, Nadja , HOHLFELD, Andreas , LINK, Fritz
发明人： LANGE, Meinolf , SCHÖNBERGER, Andreas , KIRCHHOFF, Christina , GRÖSSEL, Olaf , OMELCENKO, Nadja , HOHLFELD, Andreas , LINK, Fritz
IPC分类号： C07H21/00 , C07D233/54
CPC分类号： C07H21/04 , B01J31/0271 , C07H19/10 , C07H19/20 , C07H21/00 , C07H21/02
摘要： A method for preparing a phosphitylated compound comprising the step of: - reacting a hydroxy! containing compound with a phosphitylating agent in the presence of an activator having the formula (I) wherein R = alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl R 1 , R 2 = either H or form a 5 to 6-membered ring together. X 1, X 2 = independently either N or CH Y = H or Si(R 4 ) 3 , with R 4 = alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl B = deprotonated acid. The hydroxyl containing compound is preferably a sugar moiety or a nucleoside or an oligomer derived therefrom.
摘要翻译：一种制备磷酸化化合物的方法，包括以下步骤： - 使羟基在具有式（I）的活化剂存在下，将含磷酸化合物与磷酸化剂反应，其中R =烷基，环烷基，芳基，芳烷基，杂烷基，杂芳基R 1，R 2 > = H或形成5至6元环。 X 1，X 2独立地是N或CHY = H或Si（R 4）3， R 4 =烷基，环烷基，芳基，芳烷基，杂烷基，杂芳基B =去质子化的酸。含羟基化合物优选为糖部分或核苷或由其衍生的低聚物。

5. 发明申请

WO2005123712A1 VERFAHREN ZUR HERSTELLUNG VON 4-(ALPHA-HYDROXYALKYL)-1,3-DIOXAN-5-ONEN 审中-公开
标题翻译：为4-（ALPHA-羟烷基）]制造方法-1,3-二恶烷-5-酮
公开(公告)号：WO2005123712A1
公开(公告)日：2005-12-29
申请号：PCT/EP2005/052757
申请日：2005-06-15
申请人： GIRINDUS AG , WESTERMANN, Bernhard , LANGE, Meinolf , HAYAT, Nasir , NEUHAUS, Christiane , LINK, Fritz
发明人： WESTERMANN, Bernhard , LANGE, Meinolf , HAYAT, Nasir , NEUHAUS, Christiane , LINK, Fritz
IPC分类号： C07D319/06
CPC分类号： C07D319/06
摘要： Verfahren zur Synthese von Verbindungen der allgemeinen Formel (1), (2), (3), (4) umfassend den Schritt der Umsetzung von Formeln (5) und (6) in Gegenwart von Formel (7) wobei R = substituierte oder unsubstituierte Alkyl, Aryl, Heterozyklen enthaltend ein oder mehr O, N, S, P oder B; R 1 und R 2 unabhängig voneinander H, substituierte oder unsubstituierte Alkyl, Aryl, Heterozyklen enthaltend ein oder mehr O, N, S, P oder B, R' = H, OH, OR oder OSiX 3 wobei X unabhängig voneinander Alkyl oder Aryl sind.
摘要翻译：一种通式的化合物的合成方法（1），（2），（3），（4），包括使化学式的步骤（5）和（6）在式（7），其中R =取代或未取代的存在烷基，芳基，含有一个或多个O，N，S，P或B的杂环; R1和R2独立地是H，取代或未取代的烷基，芳基，杂环，OH，OR或OSiX3其中X独立地表示烷基或含有一个或多个O，N，S，P或B，R“= H的芳基

6. 发明申请

WO2008141682A1 SYNTHESIS OF OLIGONUCLEOTIDES 审中-公开
标题翻译：合成寡核苷酸
公开(公告)号：WO2008141682A1
公开(公告)日：2008-11-27
申请号：PCT/EP2007/062660
申请日：2007-11-21
申请人： GIRINDUS AG , LANGE, Meinolf , HOHLFELD, Andreas , SCHÖNBERGER, Andreas , KIRCHHOFF, Christina , GRÖSSEL, Olaf
发明人： LANGE, Meinolf , HOHLFELD, Andreas , SCHÖNBERGER, Andreas , KIRCHHOFF, Christina , GRÖSSEL, Olaf
IPC分类号： C07H21/00
CPC分类号： C07H21/00
摘要： A method for preparing an oligonucleotide comprising the steps of a) providing a hydroxyl containing compound having the formula (1), wherein B is a heterocyclic base and the radicals R 2 , R 3 and R 5 are as defined in the description; b) reacting said compound with a phosphitylating agent in the presence of an activator having the formula (I) (activator I)), wherein R = alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl; R 1 , R 2 = either H or form a 5 to 6-membered ring together; X 1 , X 2 = independently either N or CH; Y = H or Si(R 4 ) 3 , with R 4 = alkyl, cycloalkyl, aryl, aralkyl, heteroalkyl, heteroaryl; B = deprotonated acid; to prepare a phosphitylated compound; c) reacting said phosphitylated compound without isolation with a second compound having the formula (1), wherein R 5 , R 3 , R 2 , B are independently selected, but have the same definition as above in the presence of an activator II selected from the group of imidazole imidazolium salts and mixtures thereof.
摘要翻译：一种制备寡核苷酸的方法，包括以下步骤：a）提供具有式（1）的含羟基化合物，其中B是杂环碱基，R 2，R 3， SUB＆gt;和R 5 5如说明书中所定义; b）在具有式（I）的活化剂（活化剂I））的存在下使所述化合物与磷酸酯化剂反应，其中R =烷基，环烷基，芳基，芳烷基，杂烷基，杂芳基; R 1，R 2，H或H或一起形成5至6元环; X 1，X 2独立地是N或CH; Y = H或Si（R 4）3，其中R 4 =烷基，环烷基，芳基，芳烷基，杂烷基，杂芳基; B =去质子酸制备磷酸化化合物; c）使所述磷化物化合物与所述式（1）的第二化合物分离而不分离，其中R 5，R 3，R 2， B独立选择，但在选自咪唑咪唑盐及其混合物的活化剂II的存在下具有与上述相同的定义。

7. 发明授权

EP1525212B1 METHOD FOR PREPARING OLIGONUCLEOTIDES 有权
标题翻译：制备寡核苷酸的方法
公开(公告)号：EP1525212B1
公开(公告)日：2012-09-12
申请号：EP03766373.9
申请日：2003-07-30
申请人： Girindus AG , Centre National de la Recherche Scientifique - CNRS , L'Université Montpellier II
发明人： ADAMO, Ilaria , DUEYMES, Cécile , SCHÖNBERGER, Andreas , IMBACH, Jean-Louis , MEYER, Albert , MORVAN, Francois , DEBART, Francoise , VASSEUR, Jean-Jacques , LANGE, Meinolf , LINK, Fritz
IPC分类号： C07H21/00
CPC分类号： C07H21/00 , C07H21/02 , C07H21/04 , Y02P20/55 , Y02P20/582

8. 发明公开

EP1846431A1 PURIFICATION OF OLIGONUCLEOTIDES 审中-公开
标题翻译：清洁的寡核苷酸
公开(公告)号：EP1846431A1
公开(公告)日：2007-10-24
申请号：EP06707883.2
申请日：2006-01-30
申请人： Girindus AG
发明人： LANGE, Meinolf , GRÖSSEL, Olaf , LINK, Fritz , SCHÖNBERGER, Andreas , HOHLFELD, Andreas
IPC分类号： C07H21/00
CPC分类号： C07H21/00
摘要： A method for purifying a protected oligonucleotide comprising the steps of: a) - providing a solution of the protected oligonucleotide in at least one solvent A having a boiling point below the boiling point of a solvent B, - heating the solution at a temperature of at least 30°C and below the boiling point of the at least solvent A, - adding solvent B until precipitation of a material is visible in the solution, said solvent B being an alcohol having 1 to 6 C-atoms or a diol having 2 to 6 C-atoms, - allowing the solution to cool down under stirring until formation of a supernatant and a residue, - removing the supernatant or b) - providing solvent B, said solvent B being an alcohol having 1 to 6 C- atoms or a diol having 2 to 6 C-atoms, - heating solvent B at a temperature above 30°C and below the boiling point of solvent B, - adding a solution of a protected oligonucleotide in at least one solvent A until precipitation of a material is visible in the solution, - allowing the solution to cool down under stirring until formation of a supernatant and a residue, - removing the supernatant.

9. 发明授权

EP1828218B1 SYNTHESIS OF PHOSPHITYLATED COMPOUNDS USING A QUATERNARY HETEROCYCLIC ACTIVATOR 有权
标题翻译：连接操作PHOSPHITYLIERTER使用四进制HETEROZYKLISHEN激活
公开(公告)号：EP1828218B1
公开(公告)日：2014-04-30
申请号：EP05850457.2
申请日：2005-12-15
申请人： Girindus AG
发明人： LANGE, Meinolf , SCHÖNBERGER, Andreas , KIRCHHOFF, Christina , GRÖSSEL, Olaf , OMELCENKO, Nadja , HOHLFELD, Andreas , LINK, Fritz
IPC分类号： C07H21/00 , C07D233/54
CPC分类号： C07H21/04 , B01J31/0271 , C07H19/10 , C07H19/20 , C07H21/00 , C07H21/02

10. 发明授权

EP1858909B1 SYNTHESIS OF OLIGONUCLEOTIDES 有权
标题翻译：寡核苷酸合成
公开(公告)号：EP1858909B1
公开(公告)日：2014-09-10
申请号：EP06708653.8
申请日：2006-03-06
申请人： Girindus AG
发明人： LANGE, Meinolf , SCHÖNBERGER, Andreas , HOHLFELD, Andreas , GRÖSSEL, Olaf , KIRCHHOFF, Christina , LINK, Fritz
IPC分类号： C07H21/00
CPC分类号： C07H21/00 , Y02P20/55

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