公开(公告)号：US5869715A

公开(公告)日：1999-02-09

申请号：US534471

申请日：1995-09-27

申请人： Michael H. Nantz ,  Michael J. Bennett ,  Rajiv P. Balasubramaniam

发明人： Michael H. Nantz ,  Michael J. Bennett ,  Rajiv P. Balasubramaniam

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： For use in transporting biologically active species into and through membrane barriers, a cationic amine compound is utilized 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 anion.

摘要翻译： 为了用于将生物活性物质输送到膜屏障中并通过膜屏障，使用具有以下一般结构的阳离子胺化合物：其中R 4和R 5是一对相同或不同的脂酰基部分，其选自烷基， 烯基，炔基，烷酰基，烯酰基或炔炔基，对于R 1 R 2，并且R 3至少两个被羟基化，含醚或含酰氧基的烷基，烯基或炔基或至少一个与胺键合的含卤素的部分， 由卤代烷基，烯基或炔基组成，或至少一种选自卤代烷基，烯基或炔基的含卤素部分和至少一个羟基化的，含醚的或含酰氧基的烷基的混合物， 烯基或炔基，X-是阴离子。

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。

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。