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1. 发明申请

WO2006052767A2 COMPOSITIONS AND METHODS FOR STABILIZING LIPOSOMAL DRUG FORMULATIONS 审中-公开
标题翻译：用于稳定药物制剂的组合物和方法
公开(公告)号：WO2006052767A2
公开(公告)日：2006-05-18
申请号：PCT/US2005040061
申请日：2005-11-04
申请人： INEX PHARMACEUTICALS CORP , HERMANNS KARL R , HOPE MICHAEL J , MUI BARBARA , MADDEN THOMAS D
发明人： HOPE MICHAEL J , MUI BARBARA , MADDEN THOMAS D
IPC分类号： A61K9/127 , A61K31/47
CPC分类号： A61K31/4745 , A61K9/127 , A61K31/47
摘要： The present invention is directed to liposomal compositions comprising a camptothecin, which are optimized to reduce camptothecin degradation and/or precipitation of camptothecin degradation products in the external medium. The invention further provides improved methods of formulating liposomal camptothecins, kits comprising liposome-encapsulated camptothecins, and methods of using the same to treat a variety of diseases and disorders, including cancer.
摘要翻译：本发明涉及包含喜树碱的脂质体组合物，其被优化以降低喜树碱降解和/或在外部培养基中的喜树碱降解产物的沉淀。本发明进一步提供了制备脂质体喜树碱的改进方法，包含脂质体包封的喜树碱的试剂盒及其使用方法来治疗各种疾病和病症，包括癌症。

2. 发明申请

WO2005120461A3 LIPOSOMAL FORMULATIONS COMPRISING DIHYDROSPHINGOMYELIN AND METHODS OF USE THEREOF 审中-公开
标题翻译：包含二氢吡啶并咪唑的药物制剂及其使用方法
公开(公告)号：WO2005120461A3
公开(公告)日：2006-03-16
申请号：PCT/US2005017054
申请日：2005-05-16
申请人： INEX PHARMACEUTICALS CORP , HERMANNS KARL R , CULLIS PIETER R , MADDEN THOMAS D , HOPE MICHAEL J , ANSELL STEVEN M , MUI BARBARA L S , SEMPLE SEAN C , MAURER NORBERT
发明人： CULLIS PIETER R , MADDEN THOMAS D , HOPE MICHAEL J , ANSELL STEVEN M , MUI BARBARA L S , SEMPLE SEAN C , MAURER NORBERT
IPC分类号： A61K9/127
CPC分类号： A61K31/4745 , A61K9/1272 , A61K9/1278 , A61K33/32 , A61K2300/00
摘要： The present invention includes novel liposomes comprising dihydrosphingomyelin. The invention also includes compositions comprising these liposomes and a therapeutic agent, in addition to methods and kits for delivering a therapeutic agent or treating a disease, e.g., a cancer, using these compositions.
摘要翻译：本发明包括含有二氢鞘磷脂的新型脂质体。除了使用这些组合物递送治疗剂或治疗疾病例如癌症的方法和试剂盒外，本发明还包括包含这些脂质体和治疗剂的组合物。

3. 发明申请

WO2009088891A8 SCREENING METHOD FOR SELECTED AMINO LIPID-CONTAINING COMPOSITIONS 审中-公开
公开(公告)号：WO2009088891A8
公开(公告)日：2009-07-16
申请号：PCT/US2008/088587
申请日：2008-12-31
申请人： ALNYLAM PHARMACEUTICALS, INC. , CIUFOLINI, Marco , MADDEN, Thomas, D. , HOME, Michael, J. , MUI, Barbara , DE FOUGEROLLES, Antonin , NOVOBRANTSEVA, Tatiana , BORODOVSKY, Anna , AKINC, Akin , TRACY, Mark , CULLIS, Pieter, Rutter
发明人： CIUFOLINI, Marco , MADDEN, Thomas, D. , HOME, Michael, J. , MUI, Barbara , DE FOUGEROLLES, Antonin , NOVOBRANTSEVA, Tatiana , BORODOVSKY, Anna , AKINC, Akin , TRACY, Mark , CULLIS, Pieter, Rutter
IPC分类号： A61K9/127 , G01N33/50
摘要： The invention features a method of identifying therapeutically relevant compositions which include a therapeutic agent and 2,2-Dilinoley 1-4- dimethylaminomethyl-[l,3]-dioxolane by screening for an effect of the agent on the liver of a model subject.

4. 发明申请

WO2006052767A3 COMPOSITIONS AND METHODS FOR STABILIZING LIPOSOMAL CAMPTOTHECIN FORMULATIONS 审中-公开
公开(公告)号：WO2006052767A3
公开(公告)日：2006-05-18
申请号：PCT/US2005/040061
申请日：2005-11-04
申请人： INEX PHARMACEUTICALS CORPORATION , HERMANNS, Karl, R. , HOPE, Michael, J. , MUI, Barbara , MADDEN, Thomas, D.
发明人： HOPE, Michael, J. , MUI, Barbara , MADDEN, Thomas, D.
IPC分类号： A61K9/127 , A61K31/47 , A61K31/4745 , A61P35/00
摘要： The present invention is directed to liposomal compositions comprising a camptothecin, which are optimized to reduce camptothecin degradation and/or precipitation of camptothecin degradation products in the external medium. The invention further provides improved methods of formulating liposomal camptothecins, kits comprising liposome-encapsulated camptothecins, and methods of using the same to treat a variety of diseases and disorders, including cancer.

5. 发明申请

WO2010042877A1 IMPROVED AMINO LIPIDS AND METHODS FOR THE DELIVERY OF NUCLEIC ACIDS 审中-公开
标题翻译：改进的氨基酸和提供核酸的方法
公开(公告)号：WO2010042877A1
公开(公告)日：2010-04-15
申请号：PCT/US2009/060251
申请日：2009-10-09
申请人： TEKMIRA PHARMACEUTICALS CORPORATION , THE UNIVERSITY OF BRITISH COLUMBIA , HOPE, Michael, J. , SEMPLE, Sean, C. , CHEN, Jianxin , MADDEN, Thomas, D. , CULLIS, Pieter, R. , CIUFOLINI, Marco, A. , LAHERTY, Carol, D. , MUI, Barbara
发明人： HOPE, Michael, J. , SEMPLE, Sean, C. , CHEN, Jianxin , MADDEN, Thomas, D. , CULLIS, Pieter, R. , CIUFOLINI, Marco, A. , MUI, Barbara
IPC分类号： C07D345/00 , C07D517/00 , A61K9/127
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。

6. 发明申请

WO2009086558A1 IMPROVED COMPOSITIONS AND METHODS FOR THE DELIVERY OF NUCLEIC ACIDS 审中-公开
标题翻译：改进的组合物和提供核酸的方法
公开(公告)号：WO2009086558A1
公开(公告)日：2009-07-09
申请号：PCT/US2008/088676
申请日：2008-12-31
申请人： TEKMIRA PHARMACEUTICALS CORPORATION , THE UNIVERSITY OF BRITISH COLUMBIA , ALNYLAM PHARMACEUTICALS , HOPE, Michael, J. , SEMPLE, Sean, C. , CHEN, Jianxin , MADDEN, Thomas, D. , MUI, Barbara , CULLIS, Pieter, R. , CIUFOLINI, Marco, A. , WONG, Kim, F. , MANOHARAN, Muthiah , KALLANTHOTTATHIL, Rajeev, G.
发明人： HOPE, Michael, J. , SEMPLE, Sean, C. , CHEN, Jianxin , MADDEN, Thomas, D. , MUI, Barbara , CULLIS, Pieter, R. , CIUFOLINI, Marco, A. , WONG, Kim, F. , MANOHARAN, Muthiah , KALLANTHOTTATHIL, Rajeev, G.
IPC分类号： A61K9/127 , A61K31/7088
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。

7. 发明申请

WO0115726A3 COMPOSITIONS FOR STIMULATING CYTOKINE SECRETION AND INDUCING AN IMMUNE RESPONSE 审中-公开
标题翻译：用于刺激细胞因子分泌和诱导免疫应答的组合物
公开(公告)号：WO0115726A3
公开(公告)日：2001-07-26
申请号：PCT/CA0001013
申请日：2000-08-28
申请人： INEX PHARMACEUTICALS CORP , SEMPLE SEAN C , HARASYM TROY O , KLIMUK SANDRA K , KOJIC LJILJIANA D , BRAMSON JONATHAN L , MUI BARBARA , HOPE MICHAEL J
发明人： SEMPLE SEAN C , HARASYM TROY O , KLIMUK SANDRA K , KOJIC LJILJIANA D , BRAMSON JONATHAN L , MUI BARBARA , HOPE MICHAEL J
IPC分类号： A61K9/00 , A61K9/127 , A61K31/711 , A61K38/00 , A61K39/39 , A61K47/48 , A61P37/02 , A61P37/04 , A61P43/00 , A61K31/7088 , A61P35/00
CPC分类号： A61K31/7088 , A61K9/1272 , A61K31/711 , A61K31/7125 , A61K39/39 , A61K2039/55555 , A61K2039/55561 , C12N2310/18
摘要： Lipid-nucleic acid particles can provide therapeutic benefits, even when the nucleic acid is not complementary to coding sequences in target cells. It has been found that lipid-nucleic acid particles, including those containing non-sequence specific oligodeoxynucleotides, can be used to stimulate cytokine secretion, thus enhancing the overall immune response of a treated mammal. Further, immune response to specific target antigens can be induced by administration of an antigenic molecule in association with lipid particles containing non-sequence specific oligodeoxynucleotides. The nucleic acid which is included in the lipid-nucleic acid particle can be a phosphodiester (i.e., an oligodeoxynucleotide consisting of nucleotide residues joined by phosphodiester linkages) or a modified nucleic acid which includes phosphorothioate or other modified linkages, and may suitably be one which is non-complementary to the human genome, such that it acts to provide immunostimulation in a manner which is independent of conventional base-pairing interactions between the nucleic acid and nucleic acids of the treated mammal. In particular, the nucleic acid may suitably contain an immune-stimulating motif such as a CpG motif, or an immune stimulating palindromic sequence. The cationic lipid included in the nucleic acid particles may be suitably selected from among DODAP, DODMA, DMDMA, DOTAP, DC-Chol, DDAB, DODAC, DMRIE, DOSPA and DOGS. In addition, the lipid particle may suitably contain a modified aggregation-limiting lipid such as a PEG-lipid, a PAO-lipid or a ganglioside.
摘要翻译：即使当核酸与靶细胞中的编码序列不互补时，脂质 - 核酸颗粒也可提供治疗益处。已经发现，包括含有非序列特异性寡脱氧核苷酸的脂质核酸颗粒可用于刺激细胞因子分泌，从而增强被治疗哺乳动物的总体免疫应答。此外，可以通过与含有非序列特异性寡脱氧核苷酸的脂质颗粒结合施用抗原分子来诱导对特异性靶抗原的免疫应答。包含在脂质 - 核酸颗粒中的核酸可以是磷酸二酯（即，由通过磷酸二酯键连接的核苷酸残基组成的寡脱氧核苷酸）或包括硫代磷酸酯或其它修饰的连接的修饰的核酸，并且可以适当地是与人类基因组不互补，使得其以不依赖于经处理的哺乳动物的核酸和核酸之间的常规碱基配对相互作用的方式提供免疫刺激。特别地，核酸可以适当地含有免疫刺激基序，例如CpG基序或免疫刺激回文序列。包含在核酸颗粒中的阳离子脂质可以适当地选自DODAP，DODMA，DMDMA，DOTAP，DC-Chol，DDAB，DODAC，DMRIE，DOSPA和DOGS。此外，脂质颗粒可以适当地含有修饰的聚集限制性脂质，例如PEG-脂质，PAO-脂质或神经节苷脂。

8. 发明申请

WO2009088891A1 SCREENING METHOD FOR SELECTED AMINO LIPID-CONTAINING COMPOSITIONS 审中-公开
标题翻译：选择的含氨基脂的组合物的筛选方法
公开(公告)号：WO2009088891A1
公开(公告)日：2009-07-16
申请号：PCT/US2008088587
申请日：2008-12-31
申请人： ALNYLAM PHARMACEUTICALS INC , MADDEN THOMAS D , CIUFOLINI MARCO , HOPE MICHAEL J , DE FOUGEROLLES ANTONIN , NOVOBRANTSEVA TATIANA , AKINC AKIN , BORODOVSKY ANNA , MUI BARBARA , CULLIS PIETER RUTTER , TRACY MARK
发明人： MADDEN THOMAS D , CIUFOLINI MARCO , HOPE MICHAEL J , DE FOUGEROLLES ANTONIN , NOVOBRANTSEVA TATIANA , AKINC AKIN , BORODOVSKY ANNA , MUI BARBARA , CULLIS PIETER RUTTER , TRACY MARK
IPC分类号： A61K9/127 , G01N33/50
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-[l,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作用来鉴定包含治疗剂和2,2-二烯-4-基二甲基氨基甲基 - [1,3] - 二氧戊环的治疗相关组合物的方法。

9. 发明申请

WO2005120461A2 LIPOSOMAL FORMULATIONS COMPRISING DIHYDROSPHINGOMYELIN AND METHODS OF USE THEREOF 审中-公开
标题翻译：包含二氢吡啶并咪唑的药物制剂及其使用方法
公开(公告)号：WO2005120461A2
公开(公告)日：2005-12-22
申请号：PCT/US2005/017054
申请日：2005-05-16
申请人： INEX PHARMACEUTICALS CORPORATION , HERMANNS, Karl, R. , CULLIS, Pieter, R. , MADDEN, Thomas, D. , HOPE, Michael, J. , ANSELL, Steven, M. , MUI, Barbara, L.S. , SEMPLE, Sean, C. , MAURER, Norbert
发明人： CULLIS, Pieter, R. , MADDEN, Thomas, D. , HOPE, Michael, J. , ANSELL, Steven, M. , MUI, Barbara, L.S. , SEMPLE, Sean, C. , MAURER, Norbert
IPC分类号： A61K9/127
CPC分类号： A61K31/4745 , A61K9/1272 , A61K9/1278 , A61K33/32 , A61K2300/00
摘要： The present invention includes novel liposomes comprising dihydrosphingomyelin. The invention also includes compositions comprising these liposomes and a therapeutic agent, in addition to methods and kits for delivering a therapeutic agent or treating a disease, e.g., a cancer, using these compositions.
摘要翻译：本发明包括含有二氢鞘磷脂的新型脂质体。除了使用这些组合物递送治疗剂或治疗疾病例如癌症的方法和试剂盒外，本发明还包括包含这些脂质体和治疗剂的组合物。

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