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1. 发明申请

WO2012167869A1 AMINO LIPIDS, THEIR SYNTHESIS AND USES THEREOF 审中-公开
标题翻译： AMINO脂肪，它们的合成及其用途
公开(公告)号：WO2012167869A1
公开(公告)日：2012-12-13
申请号：PCT/EP2012/002101
申请日：2012-05-15
申请人： KARLSRUHER INSTITUT FÜR TECHNOLOGIE , DAVIDSON, Gary , LEVKIN, Pavel , LI, Linxian , SU, Yi , ZAHNER, David
发明人： DAVIDSON, Gary , LEVKIN, Pavel , LI, Linxian , SU, Yi , ZAHNER, David
IPC分类号： C07C317/44 , C07C323/60 , C07D295/00 , A61K31/16 , A61P35/00
CPC分类号： A61K9/1272 , C07C317/44 , C07C323/60 , C07D295/125 , C07D295/185 , Y10T428/2982
摘要： The present invention provides new amino lipids and a convenient method for synthesising these compounds. These (cationic) amino lipids have good properties as transfection agents. The method is an economic versatile two step synthesis allowing the preparation of various amino lipids thus leading to the assembly of a combinatorial library of transfection agents. Moreover, the present invention provides lipid particles (liposomes) containing said amino lipids and their use for delivering bioactive agents into cells. The invention encompasses also the use of lipid particles containing the cationic amino lipids as medicament.
摘要翻译：本发明提供新的氨基脂质和合成这些化合物的方便方法。这些（阳离子）氨基脂质作为转染剂具有良好的性质。该方法是经济通用的两步合成，允许制备各种氨基脂质，从而导致转染试剂组合文库的组装。此外，本发明提供含有所述氨基脂质的脂质颗粒（脂质体）及其将生物活性剂递送到细胞中的用途。本发明还包括使用含有阳离子氨基脂质的脂质颗粒作为药物。

2. 发明申请

WO2016005318A1 SYNTHESIS AND USE OF AMINO LIPIDS 审中-公开
标题翻译：氨基酸的合成与利用
公开(公告)号：WO2016005318A1
公开(公告)日：2016-01-14
申请号：PCT/EP2015/065334
申请日：2015-07-06
申请人： INCELLA GMBH , KARLSRUHER INSTITUT FÜR TECHNOLOGIE
发明人： LI, Linxian , SHANKARA, Girish Karadka , DU, Xing , WU, Yihang , DAVIDSON, Gary , LEVKIN, Pavel
IPC分类号： C07D295/04 , C07C317/04 , C07C321/14 , C07D295/215 , A61K9/127
CPC分类号： C07D295/215 , A61K9/1272 , A61K31/7088 , C07C315/04 , C07C317/18 , C07C317/28 , C07C319/12 , C07C323/12 , C07C323/25 , C07C323/44 , C07C323/65 , C07D295/04 , C07D295/13 , C12N15/113 , C12N2310/14 , C12N2320/32
摘要： The present invention provides novel amino lipids and a method for synthesizing these compounds. According to the invention, the amino lipids have a structure of the following formula (I) wherein Z is either hydrogen or -X 1 R 1 , R 1 and R 2 are the same or different and independently C 6 -C 24 alkyl, C 6 -C 24 alkenyl, C 6 -C 24 alkynyl, or C 6 -C 24 acyl, which can be optionally substituted with a C 1 -C 6 hydrocarbyl group, X 1 and X 2 are the same or different, either S or S=O or S(=O) 2 , Y is either (II) or heterocycles of the formula (III) or (IV) wherein k and I are integers from 0 to 2, R 3 and R 4 are either the same or different and independently C 1 -C 12 alkyl, C 1 -C 12 alkenyl, or C 1 -C 12 alkynyl, wherein alkyl, alkenyl or alkynyl may be optionally substituted with a C 1 -C 6 hydrocarbyl group, or R 3 and R 4 optionally join to form, together with the nitrogen atom to which they are bound, an optionally substituted N-heterocyclic ring of 3 to 10 atoms comprising 1 to 7 nitrogen atoms, or R 3 and R 4 are the same or different alkyl amines; R 5 and R 6 are either absent or is hydrogen or C 1 -C 12 alkyl to provide a quaternary amine, R 7 is either hydrogen or C 1 -C 12 alkyl, m is an integer from 1 to 12, n is an integer from 1 to 12, and p is an integer from 1 to 3, wherein preferably Y = N for p = 2 or 3.
摘要翻译：本发明提供新的氨基脂质和这些化合物的合成方法。根据本发明，氨基脂质具有下式（I）的结构，其中Z为氢或-X1R1，R1和R2相同或不同，并且独立地为C6-C24烷基，C6-C24烯基，C6- C24炔基或可以任选被C 1 -C 6烃基取代的C 6 -C 24酰基，X 1和X 2相同或不同，S或S = O或S（= O）2，Y是（II ）或式（III）或（IV）的杂环，其中k和I是0-2的整数，R 3和R 4可以相同或不同，并且独立地是C 1 -C 12烷基，C 1 -C 12链烯基或C 1 -C 12炔基其中烷基，烯基或炔基可以任选地被C 1 -C 6烃基取代，或者R 3和R 4任选地连接以与它们所连接的氮原子一起形成3至10个任选取代的N-杂环包含1至7个氮原子的原子，或者R 3和R 4是相同或不同的烷基胺; R 5和R 6不存在或为氢或C 1 -C 12烷基以提供季胺，R 7为氢或C 1 -C 12烷基，m为1至12的整数，n为1至12的整数，p为是1至3的整数，其中对于p = 2或3，优选Y = N。

3. 发明申请

WO2014079914A1 CD44V6-DERIVED PEGYLATED PEPTIDES 审中-公开
标题翻译： CD44V6衍生的聚乙烯肽
公开(公告)号：WO2014079914A1
公开(公告)日：2014-05-30
申请号：PCT/EP2013/074353
申请日：2013-11-21
申请人： KARLSRUHER INSTITUT FÜR TECHNOLOGIE
发明人： ORIAN-ROUSSEAU, Véronique , MATZKE, Alexandra , LEVKIN, Pavel , SCHMITT, Mark , LI, Linxian , PARVESH, Wadhwani
IPC分类号： A61K38/17 , A61P35/00 , A61K47/48
CPC分类号： A61K38/177 , A61K47/60
摘要： The present invention relates to pegylated compounds and pharmaceutical compositions thereof, which are suitable for treatments for cancers.
摘要翻译：本发明涉及适用于癌症治疗的聚乙二醇化合物及其药物组合物。

4. 发明公开

EP4186981A1 PARALLEL DIRECT ISOLATION AND MANIPULATION OF NUCLEIC ACID FROM CULTURED CELLS IN NANOLITER DROPLETS 审中-公开
公开(公告)号：EP4186981A1
公开(公告)日：2023-05-31
申请号：EP21210945.8
申请日：2021-11-29
申请人： Karlsruher Institut für Technologie
发明人： LEVKIN, Pavel , CHAKRABORTY, Shraddha , POPOVA, Anna
IPC分类号： C12Q1/6806
摘要： The present invention relates to methods for the direct and parallel isolation of nucleic acid from cells in a multitude of nano- or microdroplets, comprising steps of providing a patterned substrate comprising a solid support coated with or carrying a layer or film, said layer or film comprising a multitude of hydrophilic areas having a desired shape and size, surrounded by hydrophobic areas separating the hydrophilic areas into a desired spatial pattern; applying an aqueous fluid comprising cells to the multitude of hydrophilic areas, thereby forming an array of a multitude of separated aqueous fluid nano- or microdroplets, wherein the separated aqueous fluid nano- or microdroplets comprise cells; and isolating nucleic acid from the cells in the multitude of separated aqueous fluid nano- or microdroplets on the patterned substrate in parallel.

5. 发明授权

EP3141582B1 SYNTHESIS AND USE OF POLYALKYLAMINES 有权
公开(公告)号：EP3141582B1
公开(公告)日：2018-06-13
申请号：EP15184762.1
申请日：2015-09-10
申请人： Karlsruher Institut für Technologie
发明人： LEVKIN, Pavel , DAVIDSON, Gary , WU, Yihang , LI, Linxian
IPC分类号： C08L79/02 , A61K31/13
CPC分类号： C08L79/02 , A61K9/1273 , A61K31/713
摘要： The present invention provides polyalkylamines and a method for synthesising these compounds. These polyalkylamines have good properties as transfection agents. The method is an economic versatile two-step synthesis allowing the combination of various polyalkylamines, thus leading to the assembly of a combinatorial library of transfection agents. Moreover, the present invention provides polyalkylamine particles (polymersomes) containing said polyalkylamines and their use for delivering bioactive agents into cells. The invention also encompasses the use of lipid particles containing the cationic polyalkylamines as a medicament.

6. 发明公开

EP3733277A1 PATTERNED SUBSTRATE HAVING HYDROPHILIC AND HYDROPHOBIC AREAS 审中-公开
公开(公告)号：EP3733277A1
公开(公告)日：2020-11-04
申请号：EP19172282.6
申请日：2019-05-02
申请人： Karlsruher Institut für Technologie (KIT)
发明人： LEVKIN, Pavel , GRUNZE, Michael , DONG Zheqin , DEMIR, Konstantin , WIDMAIER, Simon , BREHM, Marius , POPOVA, Anna
IPC分类号： B01J19/00 , B05D1/00 , B82Y30/00
摘要： The present invention relates to a patterned substrate including a surface having a patterned coating comprising hydrophilic areas including nanoparticles carrying hydrophilic thioether groups that are surrounded by hydrophobic areas including nanoparticles carrying hydrophobic thioether groups. The present invention moreover relates to methods for producing said patterned substrate.

7. 发明公开

EP3141582A1 SYNTHESIS AND USE OF POLYALKYLAMINES 有权
标题翻译：合成VERWENDUNG VON POLYALKYLAMINEN
公开(公告)号：EP3141582A1
公开(公告)日：2017-03-15
申请号：EP15184762.1
申请日：2015-09-10
申请人： Incella GmbH , Karlsruher Institut für Technologie
发明人： LEVKIN, Pavel , DAVIDSON, Gary , WU, Yihang , LI, Linxian
IPC分类号： C08L79/02 , A61K31/13
CPC分类号： C08L79/02 , A61K9/1273 , A61K31/713
摘要： The present invention provides polyalkylamines and a method for synthesising these compounds. These polyalkylamines have good properties as transfection agents. The method is an economic versatile two-step synthesis allowing the combination of various polyalkylamines, thus leading to the assembly of a combinatorial library of transfection agents.
Moreover, the present invention provides polyalkylamine particles (polymersomes) containing said polyalkylamines and their use for delivering bioactive agents into cells. The invention also encompasses the use of lipid particles containing the cationic polyalkylamines as a medicament.
摘要翻译：本发明提供聚烷基胺和合成这些化合物的方法。这些多烷基胺作为转染剂具有良好的性质。该方法是经济通用的两步合成，允许各种多烷基胺的组合，从而导致转染试剂组合文库的组装。此外，本发明提供了含有所述多烷基胺的聚烷基胺颗粒（聚合物囊泡）及其将生物活性剂递送到细胞中的用途。本发明还包括使用含有阳离子聚烷基胺作为药物的脂质颗粒。

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