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1. 发明申请

US20110256175A1 AMINO LIPIDS AND METHODS FOR THE DELIVERY OF NUCLEIC ACIDS 有权
标题翻译：氨基酸和提供核酸的方法
公开(公告)号：US20110256175A1
公开(公告)日：2011-10-20
申请号：US13123307
申请日：2009-10-09
申请人： Michael J. Hope , Sean C. Semple , Jianxin Chen , Thomas D. Madden , Pieter R. Cullis , Marco A. Ciufolini , Barbara Low Shoud Mui
发明人： Michael J. Hope , Sean C. Semple , Jianxin Chen , Thomas D. Madden , Pieter R. Cullis , Marco A. Ciufolini , Barbara Low Shoud Mui
IPC分类号： A61K39/12 , C07D319/06 , C07D405/06 , C07D413/06 , A61K47/44 , A61K31/7088 , A61K48/00 , A61K31/713 , C12N5/071 , C12N15/63 , A61K39/02 , A61K39/00 , A61P37/04 , A61P35/00 , A61P31/12 , A61P31/04 , A61P33/00 , C07D317/28
CPC分类号： A61K47/22 , A61K9/1271 , A61K31/713 , A61K39/39 , A61K2039/55511 , C07D317/28 , C07D319/06
摘要： The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.
摘要翻译：本发明提供优异的用于将治疗剂递送至细胞的组合物和方法。特别地，这些包括提供核酸的有效包封的新型脂质和核酸 - 脂质颗粒，并将包封的核酸有效地递送到细胞体内。本发明的组合物是高度有效的，从而允许在相对低的剂量下有效击倒特异性靶蛋白。此外，与本领域已知的组合物和方法相比，本发明的组合物和方法毒性低，并提供更大的治疗指数。

2. 发明授权

US09139554B2 Amino lipids and methods for the delivery of nucleic acids 有权
标题翻译：氨基脂质和递送核酸的方法
公开(公告)号：US09139554B2
公开(公告)日：2015-09-22
申请号：US13123307
申请日：2009-10-09
申请人： Michael J. Hope , Sean C. Semple , Jianxin Chen , Thomas D. Madden , Pieter R. Cullis , Marco A. Ciufolini , Barbara Low Shoud Mui
发明人： Michael J. Hope , Sean C. Semple , Jianxin Chen , Thomas D. Madden , Pieter R. Cullis , Marco A. Ciufolini , Barbara Low Shoud Mui
IPC分类号： C07D317/28 , A61K9/127 , C07D319/06
CPC分类号： A61K47/22 , A61K9/1271 , A61K31/713 , A61K39/39 , A61K2039/55511 , C07D317/28 , C07D319/06
摘要： The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.
摘要翻译：本发明提供优异的用于将治疗剂递送至细胞的组合物和方法。特别地，这些包括提供核酸的有效包封的新型脂质和核酸 - 脂质颗粒，并将包封的核酸有效地递送到细胞体内。本发明的组合物是高度有效的，从而允许在相对低的剂量下有效击倒特异性靶蛋白。此外，与本领域已知的组合物和方法相比，本发明的组合物和方法毒性低，并提供更大的治疗指数。

3. 发明申请

US20110117125A1 COMPOSITIONS AND METHODS FOR THE DELIVERY OF NUCLEIC ACIDS 审中-公开
标题翻译：用于提供核酸的组合物和方法
公开(公告)号：US20110117125A1
公开(公告)日：2011-05-19
申请号：US12811195
申请日：2008-12-31
申请人： Michael J. Hope , Sean C. Semple , Jianxin Chen , Thomas D. Madden , Barbara Mui , Pieter R. Cullis , Marco A. Ciufolini , Kim F. Wong , Muthiah Manoharan , Rajeev G. Kallanthottathil
发明人： Michael J. Hope , Sean C. Semple , Jianxin Chen , Thomas D. Madden , Barbara Mui , Pieter R. Cullis , Marco A. Ciufolini , Kim F. Wong , Muthiah Manoharan , Rajeev G. Kallanthottathil
IPC分类号： A61K39/12 , A61K39/00 , A61K39/02 , C12N5/02 , A61K31/7088 , A61P37/00 , C07D295/12 , C07D241/04 , C07D317/00 , C11C3/00 , C07C229/00 , C07C229/30 , C07C321/00
CPC分类号： A61K31/7088 , A61K9/127 , A61K9/1275 , C07C215/10 , C07C217/08 , C07C217/28 , C07C219/08 , C07C229/12 , C07C271/12 , C07C323/25 , C07D317/28
摘要： The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.
摘要翻译：本发明提供了将治疗剂递送至细胞的组合物和方法。特别地，这些包括提供核酸的有效包封的新型脂质和核酸 - 脂质颗粒，并将包封的核酸有效地递送到细胞体内。本发明的组合物是高度有效的，从而允许以相对低的剂量有效击倒特异性靶蛋白。此外，与本领域已知的组合物和方法相比，本发明的组合物和方法毒性低，并提供更大的治疗指数。

4. 发明授权

US08021686B2 Lipid-encapsulated polyanionic nucleic acid 有权
标题翻译：脂质包封的聚阴离子核酸
公开(公告)号：US08021686B2
公开(公告)日：2011-09-20
申请号：US12028696
申请日：2008-02-08
申请人： Sean C. Semple , Sandra K. Klimuk , Troy Harasym , Michael J. Hope , Steven M. Ansell , Pieter R. Cullis , Peter Scherrer , Dan Debeyer
发明人： Sean C. Semple , Sandra K. Klimuk , Troy Harasym , Michael J. Hope , Steven M. Ansell , Pieter R. Cullis , Peter Scherrer , Dan Debeyer
IPC分类号： A61K9/127 , A61K31/70 , C12N11/02 , C12N15/88 , C07H21/00
CPC分类号： A61K9/1277 , A61K9/1272 , Y10T428/2984
摘要： Methods for the preparation of a lipid-nucleic acid composition are provided. According to the methods, a mixture of lipids containing a protonatable or deprotonatable lipid, for example an amino lipid and a lipid such as a PEG- or Polyamide oligomer-modified lipid is combined with a buffered aqueous solution of a charged therapeutic agent, for example polyanionic nucleic acids, to produce particles in which the therapeutic agent is encapsulated in a lipid vesicle. Surface charges on the lipid particles are at least partially neutralized to provide surface-neutralized lipid-encapsulated compositions of the therapeutic agents. The method permits the preparation of compositions with high ratios of therapeutic agent to lipid and with encapsulation efficiencies in excess of 50%.
摘要翻译：提供了制备脂质 - 核酸组合物的方法。根据该方法，将包含可质子化或不可质令排泄的脂质，例如氨基脂质和脂质如PEG-或聚酰胺低聚物修饰的脂质的脂质混合物与带电疗法的缓冲水溶液组合，例如聚阴离子核酸，以产生其中治疗剂包封在脂质囊泡中的颗粒。脂质颗粒上的表面电荷至少部分被中和，以提供治疗剂的表面中和的脂质包封的组合物。该方法允许制备具有高比例的治疗剂与脂质并且包封效率超过50％的组合物。

5. 发明授权

US06835395B1 Composition containing small multilamellar oligodeoxynucleotide-containing lipid vesicles 失效
标题翻译：含有小的多层寡脱氧核苷酸的脂质囊泡的组合物
公开(公告)号：US06835395B1
公开(公告)日：2004-12-28
申请号：US09654373
申请日：2000-09-01
申请人： Sean C. Semple , Sandra K. Klimuk , Troy O. Harasym , Nancy Dos Santos , Steven M. Ansell , Pieter R Cullis , Michael J. Hope , Peter Scherrer , Deirdre McIntosh , Kim F. Wong , Norbert Maurer
发明人： Sean C. Semple , Sandra K. Klimuk , Troy O. Harasym , Nancy Dos Santos , Steven M. Ansell , Pieter R Cullis , Michael J. Hope , Peter Scherrer , Deirdre McIntosh , Kim F. Wong , Norbert Maurer
IPC分类号： A61K9127
CPC分类号： A61K9/1272 , Y10T428/2984
摘要： Lipidic compositions with superior characteristics for in vivo delivery of oligodeoxynucleotides (ODN) can easily and efficiently be made in the form of small multilamellar vesicles. The compositions contain a population of nucleic acid-containing lipid vesicles in a liquid carrier, and at least a portion of the lipid vesicles are small multilamellar vesicles. The small multilamellar vesicles are made from a lipid component including 20-30 mol % of an ionizable amino lipid such as DODAP, and a steric barrier lipid such as PEG-CerC14; and an oligodeoxynucleotide contained in the lumen or interlamellar spaces of the small multilamellar vesicles. The ODN and lipid components are preferably present in the small multilamellar vesicles in a mole ratio of from 0.15 to 0.25. The compositions of the invention can be made by preparing two solutions: a lipid mixture with 20-30 mol % of the ionizable amino lipid, the steric barrier lipid and additional lipid components selected from among neutral lipids and sterols in an ethanolic solvent; and a solution of oligodeoxynucleotide in an aqueous solvent having a pH at which the ionizable amino lipid is positively charged. The lipid mixture is added to the solution of oligodeoxynucleotide to form a mixture containing lipid vesicles which is then massed through a filter to produce sized lipid vesicles in a solution containing ethanol. The ethanol is then removed, for example by dialysis. Then, the pH of the solution surrounding the sized lipid vesicles is increased to reduce the net positive charge on the exterior of the sized lipid vesicles.
摘要翻译：寡脱氧核苷酸（ODN）的体内递送具有优异特性的脂质体组合物可以容易且有效地以小的多层囊泡的形式进行。组合物在液体载体中含有含有核酸的脂质囊泡，并且至少一部分脂质囊泡是小的多层囊泡。小的多层泡囊由包含20-30mol％的可离子化氨基脂质如DODAP和空间屏障脂质如PEG-CerC14的脂质组分制成; 和包含在小多层囊泡的内腔或层间空间中的寡脱氧核苷酸。 ODN和脂质组分优选以0.15至0.25的摩尔比存在于小多层囊泡中。本发明的组合物可以通过制备两种溶液：在乙醇溶剂中具有20-30mol％的可电离氨基脂质的脂质混合物，空间屏障脂质和选自中性脂质和甾醇中的另外的脂质组分; 和寡脱氧核苷酸在具有可电离氨基脂质带正电荷的pH的水性溶剂中的溶液。将脂质混合物加入到寡脱氧核苷酸的溶液中以形成含有脂质囊泡的混合物，然后通过过滤器将其混合，以在含有乙醇的溶液中产生大小的脂质囊泡。然后例如通过透析除去乙醇。然后，增加围绕大小的脂质囊泡的溶液的pH以降低大小的脂质囊泡外部的净正电荷。

6. 发明申请

US20110097720A1 SCREENING METHOD FOR SELECTED AMINO LIPID-CONTAINING COMPOSITIONS 审中-公开
标题翻译：选择含氨基脂肪的组合物的筛选方法
公开(公告)号：US20110097720A1
公开(公告)日：2011-04-28
申请号：US12811503
申请日：2008-12-31
申请人： Marco A. Ciufolini , Thomas D. Madden , Michael J. Hope , Barbara Mui , De Fougerolles Antonin , Tatiana Novobrantseva , Anna Borodovsky , Akin Akinc , Mark Tracy , Pieter Rutter Cullis
发明人： Marco A. Ciufolini , Thomas D. Madden , Michael J. Hope , Barbara Mui , De Fougerolles Antonin , Tatiana Novobrantseva , Anna Borodovsky , Akin Akinc , Mark Tracy , Pieter Rutter Cullis
IPC分类号： C12Q1/68 , C12Q1/02
CPC分类号： G01N33/5088 , A01K2207/05 , A01K2227/105 , A01K2267/0381 , C12N15/111 , C12N15/1137 , C12N2310/14 , C12N2320/10 , C12Q1/6876 , C12Q2600/136 , C12Q2600/158 , C12Q2600/178 , C12Y304/21021 , G01N33/5023 , G01N33/5067 , G01N33/86 , G01N2333/745 , G01N2333/96447
摘要： The invention features a method of identifying therapeutically relevant compositions which include a therapeutic agent and 2,2-Dilinoley 1-4-dimethylaminomethyl-[1,3]-dioxolane by screening for an effect of the agent on the liver of a model subject.
摘要翻译：本发明的特征在于通过筛选试剂对模型受试者的肝脏的影响来鉴定治疗相关组合物的方法，所述组合物包括治疗剂和2,2-二苯胺基-4-二甲基氨基甲基 - [1,3] - 二氧杂环戊烷。

7. 发明授权

US5837279A Encapsulation of ionizable agents in liposomes 失效
标题翻译：电离剂在脂质体中的封装
公开(公告)号：US5837279A
公开(公告)日：1998-11-17
申请号：US450831
申请日：1995-05-25
申请人： Andrew S. Janoff , Pieter R. Cullis , Marcel B. Bally , Michael W. Fountain , Richard S. Ginsberg , Michael J. Hope , Thomas D. Madden , Hugh P. Schieren , Regina L. Jablonski
发明人： Andrew S. Janoff , Pieter R. Cullis , Marcel B. Bally , Michael W. Fountain , Richard S. Ginsberg , Michael J. Hope , Thomas D. Madden , Hugh P. Schieren , Regina L. Jablonski
IPC分类号： C07D475/08 , A61K9/00 , A61K9/10 , A61K9/127 , A61K31/435 , A61K31/505 , A61K31/519 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/715 , A61K45/00 , A61K45/08 , A61K47/26 , A61K47/36 , A61K47/48 , A61P35/00 , B01J13/02 , B01J13/04 , C07D519/00 , C07H15/252 , C07H19/09
CPC分类号： A61K9/1277 , A61K9/1271 , A61K9/1278
摘要： Dehydrated liposomes are prepared by drying liposome preparations under reduced pressure in the presence of one or more protective sugars, e.g., the disaccharides trehalose and sucrose. Preferably, the protective sugars are present at both the inside and outside surfaces of the liposome membranes. Freezing of the liposome preparation prior to dehydration is optional. Alternatively, the protective sugar can be omitted if: (1) the liposomes are of the type which have multiple lipid layers; (2) the dehydration is done without prior freezing; and (3) the dehydration is performed to an end point which results in sufficient water being left in the preparation (e.g., at least 12 moles water/mole lipid) so that the integrity of a substantial portion of the multiple lipid layers is retained upon rehydration. Concentration gradients capable of generating transmembrane potentials can be created across the liposome membranes either before or after dehydration, and the transmembrane potentials resulting from these gradients can be used to load charged materials, e.g., drugs, into the liposomes.
摘要翻译：通过在一种或多种保护性糖例如二糖类海藻糖和蔗糖的存在下，减压干燥脂质体制剂来制备脱水脂质体。优选地，保护性糖存在于脂质体膜的内表面和外表面。在脱水之前冻干脂质体制剂是任选的。或者，如果：（1）脂质体是具有多个脂质层的类型，则可以省略保护性糖; （2）脱水是在没有预先冻结的情况下进行的; 和（3）脱水进行到终点，导致制剂中留有足够的水（例如，至少12摩尔水/摩尔脂质），使得大部分多脂质层的完整性保持在补液。可以在脱水之前或之后在脂质体膜上产生能够产生跨膜电位的浓度梯度，并且由这些梯度产生的跨膜电位可用于将带电材料（例如药物）加载到脂质体中。

8. 发明授权

US5736155A Encapsulation of antineoplastic agents in liposomes 失效
标题翻译：抗肿瘤剂在脂质体中的封装
公开(公告)号：US5736155A
公开(公告)日：1998-04-07
申请号：US461212
申请日：1995-06-05
申请人： Marcel B. Bally , Pieter R. Cullis , Michael J. Hope , Thomas D. Madden , Lawrence D. Mayer
发明人： Marcel B. Bally , Pieter R. Cullis , Michael J. Hope , Thomas D. Madden , Lawrence D. Mayer
IPC分类号： A61K9/127 , A61K47/48
CPC分类号： A61K9/1278 , A61K9/1271 , A61K9/1277
摘要： Methods for encapsulating ionizable antineoplastic agents in liposomes using transmembrane potentials are provided. Trapping efficiencies approaching 100% and rapid loading are readily achieved. Dehydration protocols which allow liposomes to be conveniently used in the administration of antineoplastic agents in a clinical setting are also provided. In accordance with other aspects of the invention, transmembrane potentials are used to reduce the rate of release of ionizable drugs from liposomes.
摘要翻译：提供了使用跨膜电位将可电离抗肿瘤剂包封在脂质体中的方法。捕获效率接近100％，快速加载容易实现。还提供允许脂质体在临床环境中方便地用于施用抗肿瘤剂的脱水方案。根据本发明的其他方面，使用跨膜电位来降低可离子化药物从脂质体释放的速率。

9. 发明授权

US5922350A Methods of dehydrating, storing and rehydrating liposomes 失效
标题翻译：脱脂，储存和再水化脂质体的方法
公开(公告)号：US5922350A
公开(公告)日：1999-07-13
申请号：US876938
申请日：1997-06-16
申请人： Andrew S. Janoff , Pieter R. Cullis , Marcel B. Bally , Michael W. Fountain , Richard S. Ginsberg , Michael J. Hope , Thomas D. Madden , Hugh P. Schieren , Regina L. Jablonski
发明人： Andrew S. Janoff , Pieter R. Cullis , Marcel B. Bally , Michael W. Fountain , Richard S. Ginsberg , Michael J. Hope , Thomas D. Madden , Hugh P. Schieren , Regina L. Jablonski
IPC分类号： C07D475/08 , A61K9/00 , A61K9/10 , A61K9/127 , A61K31/435 , A61K31/505 , A61K31/519 , A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/715 , A61K45/00 , A61K45/08 , A61K47/26 , A61K47/36 , A61K47/48 , A61P35/00 , B01J13/02 , B01J13/04 , C07D519/00 , C07H15/252 , C07H19/09
CPC分类号： A61K9/1277 , A61K9/1271 , A61K9/1278
摘要： Dehydrated liposomes are prepared by drying liposome preparations under reduced pressure in the presence of one or more protective sugars, e.g., the disaccharides trehalose and sucrose. Preferably, the protective sugars are present at both the inside and outside surfaces of the liposome membranes. Freezing of the liposome preparation prior to dehydration is optional. Alternatively, the protective sugar can be omitted if: (1) the liposomes are of the type which have multiple lipid layers; (2) the dehydration is done without prior freezing; and (3) the dehydration is performed to an end point which results in sufficient water being left in the preparation (e.g., at least 12 moles water/mole lipid) so that the integrity of a substantial portion of the multiple lipid layers is retained upon rehydration. Concentration gradients capable of generating transmembrane potentials can be created across the liposome membranes either before or after dehydration, and the transmembrane potentials resulting from these gradients can be used to load charged materials, e.g., drugs, into the liposomes.
摘要翻译：通过在一种或多种保护性糖例如二糖类海藻糖和蔗糖的存在下，减压干燥脂质体制剂来制备脱水脂质体。优选地，保护性糖存在于脂质体膜的内表面和外表面。在脱水之前冻干脂质体制剂是任选的。或者，如果：（1）脂质体是具有多个脂质层的类型，则可以省略保护性糖; （2）脱水是在没有预先冻结的情况下进行的; 和（3）脱水进行到终点，导致制剂中留有足够的水（例如，至少12摩尔水/摩尔脂质），使得大部分多脂质层的完整性保持在补液。可以在脱水之前或之后在脂质体膜上产生能够产生跨膜电位的浓度梯度，并且由这些梯度产生的跨膜电位可用于将带电材料（例如药物）加载到脂质体中。

10. 发明申请

US20120225434A1 SCREENING METHOD FOR SELECTED AMINO LIPID-CONTAINING COMPOSITIONS 审中-公开
标题翻译：选择含氨基脂肪的组合物的筛选方法
公开(公告)号：US20120225434A1
公开(公告)日：2012-09-06
申请号：US13460963
申请日：2012-05-01
申请人： Marco A. CIUFOLINI , Thomas D. Madden , Michael J. Hope , Barbara Mui , Antonin de Fougerolles , Tatiana Novobrantseva , Anna Borodovsky , Akin Akinc , Mark Tracy , Pieter Rutter Cullis
发明人： Marco A. CIUFOLINI , Thomas D. Madden , Michael J. Hope , Barbara Mui , Antonin de Fougerolles , Tatiana Novobrantseva , Anna Borodovsky , Akin Akinc , Mark Tracy , Pieter Rutter Cullis
IPC分类号： C12Q1/68 , G01N21/76
CPC分类号： G01N33/5088 , A01K2207/05 , A01K2227/105 , A01K2267/0381 , C12N15/111 , C12N15/1137 , C12N2310/14 , C12N2320/10 , C12Q1/6876 , C12Q2600/136 , C12Q2600/158 , C12Q2600/178 , C12Y304/21021 , G01N33/5023 , G01N33/5067 , G01N33/86 , G01N2333/745 , G01N2333/96447
摘要： The invention features a method of identifying therapeutically relevant compositions which include a therapeutic agent and 2,2-Dilinoley 1-4-dimethylaminomethyl-[1,3]-dioxolane by screening for an effect of the agent on the liver of a model subject.
摘要翻译：本发明的特征在于通过筛选试剂对模型受试者的肝脏的影响来鉴定治疗相关组合物的方法，所述组合物包括治疗剂和2,2-二苯胺基-4-二甲基氨基甲基 - [1,3] - 二氧杂环戊烷。

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