公开(公告)号：US5824812A

公开(公告)日：1998-10-20

申请号：US710350

申请日：1996-09-17

申请人： Michael H. Nantz ,  Michael J. Bennett ,  Rajiv P. Balasubramaniam ,  Alfred M. Aberle ,  Robert W. Malone

发明人： Michael H. Nantz ,  Michael J. Bennett ,  Rajiv P. Balasubramaniam ,  Alfred M. Aberle ,  Robert W. Malone

IPC分类号： A61K9/127 ,  A61K47/48 ,  C07C217/28 ,  C07C217/42 ,  C07C219/06 ,  C07C219/08 ,  C07H21/00 ,  C07C101/00

CPC分类号： C07H21/00 ,  A61K47/48023 ,  A61K47/48046 ,  A61K9/1272 ,  C07C217/28 ,  C07C217/42 ,  C07C219/06 ,  C07C219/08

摘要： Amine containing compounds and their use in the generation of cytofectin:polynucleotide complexes for transfection of cells, formulations, counterions, and reaction conditions for maximizing the transfection include using cationic amine compounds that have the general structure: ##STR1## wherein R.sub.4 and R.sub.5 are a pair of same or different lipoyl moieties selected from a group consisting of an alkyl, alkenyl, alkynyl, alkanoyl, alkenoyl, or alkynoyl groups and for R.sub.1, R.sub.2, and R.sub.3 at least two are hydroxylated, ether containing, or acyloxy containing alkyl, alkenyl, or alkynyl groups or at least one amine bonded halogen containing moiety selected from a group consisting of a halogenated alkyl, alkenyl, or alkynyl group or a mixture of at least one halogen containing moiety selected from a group consisting of a halogenated alkyl, alkenyl, or alkynyl group and at least one hydroxylated, ether containing, or acyloxy containing alkyl, alkenyl, or alkynyl group, and X.sup.- is an oxyanion or halide counterion or ##STR2## wherein a, b, or d are the same or different and are from 0-10, usually between 0 and 3, preferably 0 or 1; R.sub.4 and R.sub.5 are the same or different with each an alkyl group, an alkenyl group, an alkynyl group, or an alkyl, alkenyl, or alkynyl containing acyl group; R.sub.8, R.sub.9, or R.sub.10 are the same or different with each an alkyl, alkenyl, or alkynyl group or halogenated alkyl, alkenyl, or alkynyl group as long as one is halogen containing; and X.sup.- is an anion, usually an oxyanion or halide counterion.

摘要翻译： 含胺化合物及其在产生细胞分裂素中的用途：用于转染细胞的多核苷酸复合物，制剂，抗衡离子和用于使转染最大化的反应条件包括使用具有以下通用结构的阳离子胺化合物：其中R 4和R 5为 一对相同或不同的选自烷基，烯基，炔基，烷酰基，烯酰基或炔酰基的脂酰基部分，对于R1，R2和R3至少两个是羟基化的，含醚的或含酰氧基的烷基，烯基 ，或炔基或至少一个与胺键合的含卤素的部分，其选自卤代烷基，烯基或炔基，或至少一种含卤素部分的混合物，所述部分选自卤代烷基，烯基， 或炔基和至少一个羟基化的含醚或含酰氧基的烷基，烯基或炔基，X是氧阴离子或卤化物 其中a，b或d相同或不同，为0-10，通常为0至3，优选为0或1; R4和R5与烷基，烯基，炔基或含酰基的烷基，链烯基或炔基相同或不同; R8，R9或R10与烷基，烯基或炔基或卤代烷基，烯基或炔基相同或不同，只要一个为含卤素; X-是阴离子，通常是氧阴离子或卤离子抗衡离子。

公开(公告)号：US6043390A

公开(公告)日：2000-03-28

申请号：US55021

申请日：1998-04-03

申请人： Michael H. Nantz ,  Alfred M. Aberle

发明人： Michael H. Nantz ,  Alfred M. Aberle

IPC分类号： C12N15/09 ,  A61K9/127 ,  A61K47/18 ,  A61K47/22 ,  A61K48/00 ,  C07C229/06 ,  C07C229/08 ,  C07C229/12 ,  C07D209/20 ,  C12N15/88 ,  C07C229/04 ,  C07C229/24 ,  C07C229/26

CPC分类号： A61K9/1272 ,  A61K48/00 ,  C07C229/08 ,  C07C229/12 ,  C07D209/20 ,  C12N15/88

摘要： This invention relates to pentaerythritol lipid derivatives which are useful for the intracellular delivery of polynucleotides. These cationic lipids are useful in the preparation of liposomes and other lipid vesicles for the delivery of nucleic acids into mammalian cells.

摘要翻译： 本发明涉及可用于细胞内递送多核苷酸的季戊四醇脂质衍生物。 这些阳离子脂质可用于制备用于将核酸递送到哺乳动物细胞中的脂质体和其它脂质囊泡。

公开(公告)号：US06316421B1

公开(公告)日：2001-11-13

申请号：US09536286

申请日：2000-03-27

申请人： Michael H. Nantz ,  Alfred M. Aberle

发明人： Michael H. Nantz ,  Alfred M. Aberle

IPC分类号： A61K3170

CPC分类号： A61K9/1272 ,  A61K48/00 ,  C07C229/08 ,  C07C229/12 ,  C07D209/20 ,  C12N15/88

摘要： This invention relates to pentaerythritol lipid derivatives which are useful for the intracellular delivery of polynucleotides. These cationic lipids are useful in the preparation of liposomes and other lipid vesicles for the delivery of nucleic acids into mammalian cells.

摘要翻译： 本发明涉及可用于细胞内递送多核苷酸的季戊四醇脂质衍生物。 这些阳离子脂质可用于制备用于将核酸递送到哺乳动物细胞中的脂质体和其它脂质囊泡。

公开(公告)号：US5925623A

公开(公告)日：1999-07-20

申请号：US679971

申请日：1996-07-15

申请人： Michael H. Nantz ,  Michael J. Bennett ,  Rajiv P. Balasubramaniam ,  Alfred M. Aberle ,  Robert W. Malone

发明人： Michael H. Nantz ,  Michael J. Bennett ,  Rajiv P. Balasubramaniam ,  Alfred M. Aberle ,  Robert W. Malone

IPC分类号： A61K9/127 ,  A61K47/48 ,  C07C217/28 ,  C07C217/42 ,  C07C219/06 ,  C07C219/08 ,  C07H21/00 ,  A01N43/04

CPC分类号： C07H21/00 ,  A61K47/48023 ,  A61K47/48046 ,  A61K9/1272 ,  C07C217/28 ,  C07C217/42 ,  C07C219/06 ,  C07C219/08

摘要： In the generation of cytofectin:polynucleotide complexes for transfection of cells, formulations, counterions, and reaction conditions for maximizing the transfection include using a cationic amine compound that has the general structure: ##STR1## wherein R.sub.4 and R.sub.5 are a pair of same or different lipoyl moieties selected from a group consisting of an alkyl, alkenyl, alkynyl, alkanoyl, alkenoyl, or alkynoyl groups and for R.sub.1, R.sub.2, and R.sub.3 at least two are hydroxylated, ether containing, or acyloxy containing alkyl, alkenyl, or alkynyl groups or at least one amine bonded halogen containing moiety selected from a group consisting of a halogenated alkyl, alkenyl, or alkynyl group or a mixture of at least one halogen containing moiety selected from a group consisting of a halogenated alkyl, alkenyl, or alkynyl group and at least one hydroxylated, ether containing, or acyloxy containing alkyl, alkenyl, or alkynyl group, and X.sup.- is an oxyanion or halide counterion.

摘要翻译： 细胞增生素的产生：用于转染细胞的多核苷酸复合物，用于使转染最大化的制剂，抗衡离子和反应条件包括使用具有以下通式结构的阳离子胺化合物：其中R 4和R 5是选中的一对相同或不同的脂酰基部分 由烷基，烯基，炔基，烷酰基，烯酰基或炔酰基组成的组，并且对于R 1，R 2和R 3，至少两个羟基化，含醚或含酰氧基的烷基，烯基或炔基或至少一个 胺键合的含卤素部分，其选自卤代烷基，烯基或炔基，或至少一种含卤素部分的选自卤代烷基，烯基或炔基的部分和至少一个羟基化的 醚，或含酰氧基的烷基，链烯基或炔基，X-是氧阴离子或卤化物的抗衡离子。