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1. 发明授权

EP0923600B1 NEUARTIGE KATIONISCHE AMPHIPHILE FÜR DEN LIPOSOMALEN GENTRANSFER 失效
标题翻译：新的阳离子双亲基因转移的脂质体
公开(公告)号：EP0923600B1
公开(公告)日：2006-06-21
申请号：EP97936602.8
申请日：1997-08-01
申请人： MAX-DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN , SCHNEIDER, Manfred P.
发明人： SCHNEIDER, Manfred , KEIL, Oliver , RESZKA, Regina , GROTH, Detlef
IPC分类号： C07J41/00 , A61K31/575 , A61K9/127 , C12N15/63 , C07C271/20 , C07C279/14 , C07C237/08 , A61K31/325 , A61K31/16 , A61K31/155
CPC分类号： A61K48/00 , A61K9/1272 , C07C237/12 , C07C271/20 , C07C279/14 , C07J41/0055 , C07J41/0072 , C12N15/88
摘要： The synthesis of novel cationic, amphiphilic lipids is disclosed, as well as their use as gene transfer vesicles in vitro and in vivo. A series of different lipids (diglycerides, steroids) was synthesised by modification with variable cationic molecules (amino acids, biogenic amines). Because of their ability to form complexes with polynucleotides (DNA, RNA, antisense oligonucleotides, ribozymes, etc.), compounds of this type are useful as vectors for gene transfer (transfection).

2. 发明公开

EP0923600A2 NEUARTIGE KATIONISCHE AMPHIPHILE FÜR DEN LIPOSOMALEN GENTRANSFER 失效
标题翻译：新的阳离子双亲基因转移的脂质体
公开(公告)号：EP0923600A2
公开(公告)日：1999-06-23
申请号：EP97936602.0
申请日：1997-08-01
申请人： MAX-DELBRÜCK-CENTRUM FÜR MOLEKULARE MEDIZIN , SCHNEIDER, Manfred P.
发明人： SCHNEIDER, Manfred , KEIL, Oliver , RESZKA, Regina , GROTH, Detlef
IPC分类号： C12N15 , A61K9 , A61K31 , A61K48 , C07C237 , C07C271 , C07C279 , C07J41
CPC分类号： A61K48/00 , A61K9/1272 , C07C237/12 , C07C271/20 , C07C279/14 , C07J41/0055 , C07J41/0072 , C12N15/88
摘要： The synthesis of novel cationic, amphiphilic lipids is disclosed, as well as their use as gene transfer vesicles in vitro and in vivo. A series of different lipids (diglycerides, steroids) was synthesised by modification with variable cationic molecules (amino acids, biogenic amines). Because of their ability to form complexes with polynucleotides (DNA, RNA, antisense oligonucleotides, ribozymes, etc.), compounds of this type are useful as vectors for gene transfer (transfection).

3. 发明授权

EP0571421B1 ENZYMATIC REVERSE HYDROLYSIS OF HYDROPHILIC SUBSTRATES - PREPARATION OF AMPHIPHILIC COMPOUNDS 失效
标题翻译： REVERSE亲水性基板酶解; 连接操作双亲。
公开(公告)号：EP0571421B1
公开(公告)日：1995-07-26
申请号：EP92903973.3
申请日：1992-02-12
申请人： SCHNEIDER, Manfred P. , LAUMEN, Kurt, E. , BERGER, Matthias
发明人： SCHNEIDER, Manfred P. , LAUMEN, Kurt, E. , BERGER, Matthias
IPC分类号： C12P1/00 , C12P7/64 , C12P7/62 , C12P19/00
CPC分类号： C12P13/001 , C12P1/00 , C12P7/62 , C12P7/6436 , C12P7/6454 , C12P7/6481 , C12P9/00 , C12P13/00 , C12P13/02 , C12P13/04 , C12P19/00 , C12P19/02 , C12P19/44 , C12P21/02
摘要： The invention relates to methods for the production of amphiphilic products such as esters, sugar-esters, peptide-esters, glycolipids, glycoproteins, lipoproteins, peptides, and phosphates of alcohols, sugars, and nucleosides. The methods promote enzymatically catalyzed reactions between hydrophilic substrates such as glucerol, glucose, amino acids, and nucleosides, and second substrates such as free fatty acids, triglycerides, vinylesters, amino acids, and phosphates. The method is also applied to enzymatic reactions with saccharides and polyalcohols. The hydrophilic substrates are adsorbed to finely divided solid supports such as silica gel, diatomaceous earths, or activated chracoals in order to promote the dispersion of the hydrophilic substrates within hydrophobic substrates and solvents. Hydrophobic solvents such as n-hexane and t-butylmethylether may be included in the reaction mixtures. Reactions are conducted under non-aqueous conditions in order to promote reverse hydrolysis. Methods are provided for the production of isomerically pure 1,3-diglycerides. Further methods are disclosed for the production and specific precipitation of pure 1-monogycerides through the use of a reactor/separator system. Enzymes used in the methods include lipases from M. mihei and P. fluorescens, glycosidases such as β - galactosidase, proteases such as chymotrypsin, and acid or alkaline phosphatases. Compositions are provided comprising alcohols, carbohydrates, amino acids, or peptides adsorbed onto solid supports such as silica gel.

4. 发明公开

EP0571421A1 ENZYMATIC REVERSE HYDROLYSIS OF HYDROPHILIC SUBSTRATES - PREPARATION OF AMPHIPHILIC COMPOUNDS 失效
标题翻译： REVERSE亲水性基板酶解; 连接操作双亲。
公开(公告)号：EP0571421A1
公开(公告)日：1993-12-01
申请号：EP92903973.0
申请日：1992-02-12
申请人： SCHNEIDER, Manfred P. , LAUMEN, Kurt, E. , BERGER, Matthias
发明人： SCHNEIDER, Manfred P. , LAUMEN, Kurt, E. , BERGER, Matthias
IPC分类号： C12P1 , C12P7 , C12P9 , C12P13 , C12P19 , C12P21
CPC分类号： C12P13/001 , C12P1/00 , C12P7/62 , C12P7/6436 , C12P7/6454 , C12P7/6481 , C12P9/00 , C12P13/00 , C12P13/02 , C12P13/04 , C12P19/00 , C12P19/02 , C12P19/44 , C12P21/02
摘要： Procédés de production des produits amphiphiles tels que des esters, des esters de sucre, des esters de peptides, des glycolipides, des glycoprotéines, des lipoprotéines, des peptides, ainsi que des phosphates d'alcools, de sucres et des nucléosides. Les procédés favorisent les réactions catalysées par voie enzymatique entre des substrats hydrophiles tels que le glycérol, le glucose, des acides aminés et des nucléosides, ainsi que des seconds substrats tels que des acides gras libres, des triglycérides, des esters vinyliques, des acides aminés et des phosphates. On peut également appliquer le procédé à des réactions enzymtiques avec des saccharides et des polyalcools. Les substrats hydrophiles sont adsorbés sur des supports solides finement divisés tels que du gel de silice, des diatomites ou des charbons activés afin de stimuler la dispersion des substrats hydrophiles dans des substrats et des solvants hydrophobes. On peut ajouter aux mélanges des réaction des solvants hydrophobes tels que n-hexane et t-butylméthyléther. On fait intervenir les réactions dans des conditions non aqueuses afin de stimuler l'hydrolyse inverse. Des procédés permettent la production de 1,3-diglycérides isomériquement purs. D'autres procédés permettent la production et la précipitation spécifique de 1-monoglycérides purs par l'utilisation d'un système de réacteurs/séparateurs. On compte parmi les enzymes utilisés dans les procédésdes lipases de M. mihei et P. fluorescens, des glycosidases telles que la beta-galactosidase, des protéases telles que la chymotrypsine, ainsi que des phosphatases d'acide ou alcalines. L'invention concerne également des compositions comprenant des alcools, des glucides, des acides aminés ou des peptides adsorbés sur des supports solides tel que du gel de silice.

5. 发明申请

WO1992014830A1 ENZYMATIC REVERSE HYDROLYSIS OF HYDROPHILIC SUBSTRATES - PREPARATION OF AMPHIPHILIC COMPOUNDS 审中-公开
标题翻译：水解底物的酶反向水解 - 大分子化合物的制备
公开(公告)号：WO1992014830A1
公开(公告)日：1992-09-03
申请号：PCT/EP1992000307
申请日：1992-02-12
申请人： SCHNEIDER, Manfred, P. , LAUMEN, Kurt, E. , BERGER, Matthias
IPC分类号： C12P01/00
CPC分类号： C12P13/001 , C12P1/00 , C12P7/62 , C12P7/6436 , C12P7/6454 , C12P7/6481 , C12P9/00 , C12P13/00 , C12P13/02 , C12P13/04 , C12P19/00 , C12P19/02 , C12P19/44 , C12P21/02
摘要： The invention relates to methods for the production of amphiphilic products such as esters, sugar-esters, peptide-esters, glycolipids, glycoproteins, lipoproteins, peptides, and phosphates of alcohols, sugars, and nucleosides. The methods promote enzymatically catalyzed reactions between hydrophilic substrates such as glucerol, glucose, amino acids, and nucleosides, and second substrates such as free fatty acids, triglycerides, vinylesters, amino acids, and phosphates. The method is also applied to enzymatic reactions with saccharides and polyalcohols. The hydrophilic substrates are adsorbed to finely divided solid supports such as silica gel, diatomaceous earths, or activated chracoals in order to promote the dispersion of the hydrophilic substrates within hydrophobic substrates and solvents. Hydrophobic solvents such as n-hexane and t-butylmethylether may be included in the reaction mixtures. Reactions are conducted under non-aqueous conditions in order to promote reverse hydrolysis. Methods are provided for the production of isomerically pure 1,3-diglycerides. Further methods are disclosed for the production and specific precipitation of pure 1-monogycerides through the use of a reactor/separator system. Enzymes used in the methods include lipases from M. mihei and P. fluorescens, glycosidases such as beta - galactosidase, proteases such as chymotrypsin, and acid or alkaline phosphatases. Compositions are provided comprising alcohols, carbohydrates, amino acids, or peptides adsorbed onto solid supports such as silica gel.
摘要翻译：本发明涉及制备醇，糖和核苷类的两亲产物如酯，糖酯，肽 - 酯，糖脂，糖蛋白，脂蛋白，肽和磷酸酯的方法。这些方法促进亲水底物如葡萄糖，葡萄糖，氨基酸和核苷之间的酶催化反应，以及第二底物如游离脂肪酸，甘油三酸酯，乙烯基酯，氨基酸和磷酸酯。该方法也适用于与糖和多元醇的酶反应。为了促进亲水性底物在疏水性底物和溶剂中的分散，亲水性底物被吸附到细分散的固体载体如硅胶，硅藻土或活化的色母体上。疏水性溶剂如正己烷和叔丁基甲基醚可以包括在反应混合物中。反应在非水性条件下进行，以促进反向水解。提供了用于生产异构纯的1,3-甘油二酯的方法。公开了通过使用反应器/分离器系统来生产和特异性沉淀纯的1-单加氧化物的其它方法。用于该方法的酶包括来自M.mehei和荧光假单胞菌的脂肪酶，糖苷酶如β-半乳糖苷酶，蛋白酶如胰凝乳蛋白酶和酸或碱性磷酸酶。提供了包含醇，碳水化合物，氨基酸或吸附在固体支持物例如硅胶上的肽的组合物。

6. 发明专利

CA2101733C ENZYMATIC REVERSE HYDROLYSIS OF HYDROPHILIC SUBSTRATES-PREPARATION OF AMPHIPHILIC COMPOUNDS 未知
公开(公告)号：CA2101733C
公开(公告)日：2003-02-11
申请号：CA2101733
申请日：1992-02-12
申请人： SCHNEIDER MANFRED P , LAUMEN KURT E , BERGER MATTHIAS
发明人： SCHNEIDER MANFRED P , LAUMEN KURT E , BERGER MATTHIAS
IPC分类号： C07K17/02 , C12P1/00 , C12P7/62 , C12P7/64 , C12P9/00 , C12P13/00 , C12P19/00 , C12P21/00
摘要： The invention relates to methods for he production of amphiphilic pro- ducts such as esters, sugar-esters, pep- tide-esters, glycolipids, glycoproteins, lipoproteins, peptides, and phosphates of alcohols, sugars, and nucleosides. The methods promote enzymatically catalyzed reactions between hydrophil- ic substrates such as glucerol, glucose, amino acids, and nucleosides, and sec- ond substrates such as free fatty acids, triglycerides, vinylesters, amino acids, and phosphates. The method is also applied to enzymatic reactions with saccharides and polyalcohols. The hy- drophilic substrates are adsorbed to finely divided solid supports such as si- lica gel, diatomaceous earths, or acti- vated chracoals in order to promote the dispersion of the hydrophilic substrates within hydrophobic substrates and solvents. Hydrophobic solvents such as n-hexane and t-butylmethylether may be included in the reaction mixtures. Reactions are conducted under non-aqueous conditions in order to promote reverse hydrolysis. Methods are provided for the production of isomerically pure 1,3-diglycerides. Further methods are disclosed for the production and specific precipitation of pure 1- monogycerides through the use of a reactor/separator system. Enzymes used in the methods include lipases from M. mihei and P. fluorescens , glycosidases such as .beta. - galactosidase, proteases such as chymotrypsin, and acid or alkaline phosphatases. Compositions are provided comprising alcohols, carbohydrates, amino acids, or peptides adsorbed onto solid supports such as silica gel.

7. 发明专利

AT330964T 未知
公开(公告)号：AT330964T
公开(公告)日：2006-07-15
申请号：AT97936602
申请日：1997-08-01
申请人： MAX DELBRUECK CENTRUM , SCHNEIDER MANFRED P
发明人： SCHNEIDER MANFRED , KEIL OLIVER , RESZKA REGINA , GROTH DETLEF
IPC分类号： C12N15/09 , A61K9/127 , A61K31/575 , A61K48/00 , C07C237/08 , C07C237/12 , C07C271/20 , C07C279/14 , C07J41/00 , C12N15/88 , C12N15/63 , A61K31/325
摘要： This invention relates to the synthesis of novel cationic, amphiphilic lipids and their application as gene transfer vehicles in vitro and in vivo. For this a series of different lipids (diglycerides, steroids) were synthesized by modification with variable cationic molecules (amino acids, biogenic amines). Compounds of this kind are, due to their capability of producing complexes with polynucleotides (DNA, RNA, Antisense oligonucleotides, ribozymes etc) suitable as vectors for gene transfer (transfection).

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