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1. 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。

2. 发明申请

WO1996040964A2 LIPID-NUCLEIC ACID PARTICLES PREPARED VIA A HYDROPHOBIC LIPID-NUCLEIC ACID COMPLEX INTERMEDIATE AND USE FOR GENE TRANSFER 审中-公开
标题翻译：通过疏水性脂质 - 核酸复合物中间体制备的脂质 - 核酸颗粒和用于基因转移的用途
公开(公告)号：WO1996040964A2
公开(公告)日：1996-12-19
申请号：PCT/US1996009949
申请日：1996-06-06
申请人： INEX PHARMACEUTICALS CORPORATION , WHEELER, Jeffery, J. , BALLY, Marcel, B. , ZHANG, Yuan-Peng , REIMER, Dorothy, L. , HOPE, Michael , CULLIS, Pieter, R. , SCHERRER, Peter
发明人： INEX PHARMACEUTICALS CORPORATION
IPC分类号： C12N15/88
CPC分类号： C12N15/88 , A61K9/1272 , A61K47/6911
摘要： Novel lipid-nucleic acid particulate complexes which are useful for in vitro or in vivo gene transfer are described. The particles can be formed using either detergent dialysis methods or methods which utilize organic solvents. Upon removal of a solubilizing component (i.e, detergent or an organic solvent) the lipid-nucleic acid complexes form particles wherein the nucleic acid is serum-stable and is protected from degradation. The particles thus formed have access to extravascular sites and target cell populations and are suitable for the therapeutic delivery of nucleic acids.
摘要翻译：描述了可用于体外或体内基因转移的新型脂质 - 核酸颗粒复合物。可以使用洗涤剂透析方法或利用有机溶剂的方法形成颗粒。在除去增溶组分（即洗涤剂或有机溶剂）后，脂质 - 核酸复合物形成其中核酸是血清稳定的并且被保护免于降解的颗粒。由此形成的颗粒可以进入血管外部位和靶细胞群，并且适合于治疗性递送核酸。

3. 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.

4. 发明申请

WO2003094963A2 METHYLATED IMMUNOSTIMULATORY OLIGONUCLEOTIDES AND METHODS OF USING THE SAME 审中-公开
标题翻译：甲基化免疫球蛋白寡核苷酸及其使用方法
公开(公告)号：WO2003094963A2
公开(公告)日：2003-11-20
申请号：PCT/CA2003/000678
申请日：2003-05-12
申请人： INEX PHARMACEUTICALS CORPORATION , TAM, Ying, K. , SEMPLE, Sean , KLIMUK, Sandra , CHIKH, Ghania
发明人： TAM, Ying, K. , SEMPLE, Sean , KLIMUK, Sandra , CHIKH, Ghania
IPC分类号： A61K39/39
CPC分类号： C12N15/117 , A61K39/0011 , A61K39/39 , A61K2039/541 , A61K2039/55555 , A61K2039/55561 , C12N2310/315 , C12N2310/3341
摘要： The invention discloses that methylated nucleic acids, particularly methylated oligonucleotides, and more particularly methylated oligonucleotides bearing a methylated cytosine of a CpG dinucleotide motif can be made immunostimulatory in vivo , by encapsulation of the nucleic acid in a lipid particle. It is further disclosed that encapsulated methylated nucleic acids that are ordinarily not immunostimulatory in vivo are as effective or even more effective than their encapsulated unmethylated counterparts. Also disclosed are methods for activating and/or expanding dendritic cell populations in response to antigenic stimulation using the compositions and methods disclosed herein.
摘要翻译：本发明公开了通过将核酸包封在脂质颗粒中，甲基化的核酸，特别是甲基化寡核苷酸，更特别是带有CpG二核苷酸基序的甲基化胞嘧啶的甲基化寡核苷酸可以在体内免疫刺激。进一步公开了通常在体内通常不是免疫刺激的包封的甲基化核酸与其包封的未甲基化的对应物一样有效或甚至更有效。还公开了使用本文公开的组合物和方法来响应于抗原刺激激活和/或扩增树突细胞群体的方法。

5. 发明申请

WO2003094829A2 PATHOGEN VACCINES AND METHODS FOR USING THE SAME 审中-公开
标题翻译：病毒疫苗及其使用方法
公开(公告)号：WO2003094829A2
公开(公告)日：2003-11-20
申请号：PCT/CA2003/000680
申请日：2003-05-12
申请人： INEX PHARMACEUTICALS CORPORATION , SEMPLE, Sean , CHIKH, Ghania , HOPE, Michael, J. , TAM, Ying, K.
发明人： SEMPLE, Sean , CHIKH, Ghania , HOPE, Michael, J. , TAM, Ying, K.
IPC分类号： A61K
CPC分类号： C12N15/117 , A61K39/0011 , A61K39/39 , A61K2039/55555 , A61K2039/55561 , C12N2310/315 , C12N2310/3341
摘要： The invention is based on the discovery that vaccines against pathogens, exemplified herein by hepatitis B, can be formulated to enhance stimulation of Th1 type humoral and cellular immune responses by combining a lipid particle with an encapsulated immunostimulatory oligonucleotide (LNA). The LNA is further associated with an antigen from the pathogen. The vaccines may also use two or more different epitopes from the same antigen, or different antigens from the pathogen. Such vaccines are particularly effective in enhancing a Th1 type humoral response when the antigen is coupled to the lipid nucleic acid particle and when the nucleic acid particle has phosphorothioate (PS) backbone. An enhanced humoral response is demonstrated, for example, by a strong early peak of IFN-gamma production observed within hours of vaccination followed by second stronger peak of IFN-gamma production observed several days later, correlated with antibody isotype switching.
摘要翻译：本发明基于以下发现：通过将脂质颗粒与包封的免疫刺激寡核苷酸（LNA）组合，可以配制抗乙型肝炎病原体疫苗以增强对Th1型体液和细胞免疫应答的刺激。 LNA还与来自病原体的抗原相关联。疫苗还可以使用来自相同抗原的两个或多个不同表位或来自病原体的不同抗原。当抗原与脂质核酸颗粒偶联并且当核酸颗粒具有硫代磷酸酯（PS）主链时，这种疫苗特别有效地增强Th1型体液应答。证明了增强的体液应答，例如，在接种后数小时内观察到IFN-γ产生强烈的早期峰值，随后几天观察到IFN-γ产生的第二个更强的峰值，与抗体同种型转换相关。

6. 发明申请

WO2005011698A1 COMBINATION COMPRISING A LIPOSOME-ENCAPSULATED VINCA ALKALOID AND A TOPOISOMERASE II INHIBITOR AND THE USE THEREOF FOR TREATING NEOPLASIA 审中-公开
标题翻译：包含脂质体包封的VINCA碱性物质和TOPOISOMERASE II抑制剂的组合及其用于治疗NEOPLASIA的用途
公开(公告)号：WO2005011698A1
公开(公告)日：2005-02-10
申请号：PCT/CA2004/001038
申请日：2004-07-23
申请人： INEX PHARMACEUTICALS CORPORATION , SALTMAN, David
发明人： SALTMAN, David
IPC分类号： A61K31/475
CPC分类号： A61K45/06 , A61K9/127 , A61K31/475 , A61K31/704 , A61K2300/00
摘要： This invention provides methods for treating neoplasias in a mammal. In particular, the invention provides methods for treating various types of lymphomas, including relapsed forms of non-Hodgkin’s Lymphoma. These methods involve the co-administration of liposome-encapsulated vinca alkaloids, e.g ., vincristine, with a topoisomerase II inhibitor, e.g ., etoposide or NK-611, to a mammal with a lymphoma or a sarcoma.
摘要翻译：本发明提供了治疗哺乳动物肿瘤的方法。特别地，本发明提供了治疗各种淋巴瘤的方法，包括非霍奇金淋巴瘤的复发形式。这些方法涉及将脂质体包封的长春花生物碱例如长春新碱与拓扑异构酶II抑制剂如依托泊苷或NK-611共同给予具有淋巴瘤或肉瘤的哺乳动物。

7. 发明申请

WO2002089772A1 ANTI-ANGIOGENIC THERAPY USING LIPOSOME-ENCAPSULATED CHEMOTHERAPEUTIC AGENTS 审中-公开
标题翻译：使用脂质体包封的化学治疗剂进行抗血栓治疗
公开(公告)号：WO2002089772A1
公开(公告)日：2002-11-14
申请号：PCT/US2002/014608
申请日：2002-05-09
申请人： INEX PHARMACEUTICALS CORPORATION , FLOWERS, Clay , SALTMAN, David , TAM, Patrick, M., S. , BURGE, Clive, T., R. , HARASYM, Troy, O.
发明人： FLOWERS, Clay , SALTMAN, David , TAM, Patrick, M., S. , BURGE, Clive, T., R. , HARASYM, Troy, O.
IPC分类号： A61K9/127
CPC分类号： A61K9/127 , A61K9/1271 , A61K9/1272
摘要： The present invention provides methods and compositions for the treatment and prevention of any of a large number of diseases and conditions with an angiogenic component, e.g., cancer. The present invention is based upon the discovery that liposome-encapsulated chemotherapeutic agents, such as alkaloids (e.g., vinca alkaloids such as vincristine), are surprisingly effective at treating such diseases or conditions when administered at a higher frequency than those used with conventional administration strategies. Such methods can be used to treat diseases such as cancer even when the cancer comprises cells that are resistant to the chemotherapeutic alkaloid. The liposome encapsulation of the chemotherapeutic agents , e.g., alkaloids, imparts dramatic improvements in the stability, biodistribution, and delivery of the agents, thereby allowing more efficacious and convenient administration to a patient with any of the herein-described diseases or conditions.
摘要翻译：本发明提供用于治疗和预防具有血管生成成分例如癌症的大量疾病和病症中的任何一种的方法和组合物。本发明基于以下发现：当以比常规施用策略使用的那些更高的频率施用时，脂质体包封的化学治疗剂，例如生物碱（例如长春花碱长春花生物碱）在治疗这些疾病或病症方面是惊人的有效的。即使当癌症包含对化学治疗性生物碱具有抗性的细胞时，也可以使用这样的方法来治疗诸如癌症的疾病。化学治疗剂（例如生物碱）的脂质体包封赋予了药剂的稳定性，生物分布和递送的显着改善，从而允许对具有任何本文描述的疾病或病症的患者更有效和方便的给药。

8. 发明申请

WO2002036767A3 THERAPEUTIC OLIGONUCLEOTIDES OF REDUCED TOXICITY 审中-公开
公开(公告)号：WO2002036767A3
公开(公告)日：2002-05-10
申请号：PCT/CA2001/001540
申请日：2001-10-31
申请人： INEX PHARMACEUTICALS CORPORATION , MADDEN, Thomas, D. , WEBB, Murray, S.
发明人： MADDEN, Thomas, D. , WEBB, Murray, S.
IPC分类号： A61K31/7125
摘要： It has now been discovered that oligonucleotides which tend to form multimeric aggregates have greater toxicity in the aggregate form than in monomeric form. Thus, the present invention provides therapeutic oligonucleotide compositions of reduced in vivo toxicity, and a method for making such compositions, as well as a method for administration of the therapeutic oligonucleotide, where the therapeutic oligonucleotide in one that tends to form multimeric aggregates. Compositions containing such aggregate-forming oligonucleotides are treated by heating, preferably no more than 24 hours prior to administration, or using chemical species such as mannitol which disrupt aggregates.

9. 发明申请

WO2006020618A1 COMPOSITIONS AND METHODS FOR TREATING LYMPHOMA 审中-公开
标题翻译：用于治疗淋巴瘤的组合物和方法
公开(公告)号：WO2006020618A1
公开(公告)日：2006-02-23
申请号：PCT/US2005/028233
申请日：2005-08-09
申请人： INEX PHARMACEUTICALS CORPORATION , THOMAS, Deborah, A.
发明人： THOMAS, Deborah, A.
IPC分类号： A61K9/127 , A61K31/475 , A61K31/573
CPC分类号： A61K9/1272 , A61K31/475 , A61K31/573 , A61K2300/00
摘要： The present invention provides methods for treating neoplasias in a mammal. In particular, the invention provides methods for treating various types of leukemias, including acute lymphoblastic leukemia (ALL). These methods involve the administration of liposome-encapsulated vinca alkaloids, e.g., vincristine, in combination with dexamethasone to a mammal with a leukemia.
摘要翻译：本发明提供了治疗哺乳动物肿瘤的方法。特别地，本发明提供了治疗各种类型的白血病（包括急性成淋巴细胞白血病（ALL））的方法。这些方法涉及将脂质体包封的长春花生物碱例如长春新碱与地塞米松组合给具有白血病的哺乳动物。

10. 发明申请

WO2005034979A2 METHODS AND COMPOSITIONS FOR ENHANCING INNATE IMMUNITY AND ANTIBODY DEPENDENT CELLULAR CYTOTOXICITY 审中-公开
标题翻译：用于增强早期免疫力和抗体依赖性细胞毒性的方法和组合物
公开(公告)号：WO2005034979A2
公开(公告)日：2005-04-21
申请号：PCT/IB2004/003317
申请日：2004-10-11
申请人： INEX PHARMACEUTICALS CORPORATION , TAM, Ying, K. , CHIKH, Ghania , SEKIROV, Laura , BRODSKY, Irina , RANEY, Sameersingh, G.
发明人： TAM, Ying, K. , CHIKH, Ghania , SEKIROV, Laura , BRODSKY, Irina , RANEY, Sameersingh, G.
IPC分类号： A61K38/00
CPC分类号： A61K31/7088 , A61K9/0019 , A61K9/127 , A61K31/7115 , A61K31/712 , A61K39/39541 , A61K39/39558 , A61K45/06 , A61K2039/505 , A61K2039/55555 , C07K16/2896 , C07K16/30 , C07K16/3084 , C07K16/32 , C07K2317/24 , C07K2317/73 , C07K2317/732 , A61K2300/00
摘要： Cationic liposomes with immunostimulatory nucleic acids are shown to stimulate the innate immune response, and synergistic combinations of such liposomal nucleic acids and therapeutic antibodies are provided to dramatically improve antibody dependent cellular cytotoxicity and target cell lysis.
摘要翻译：显示具有免疫刺激性核酸的阳离子脂质体刺激先天性免疫应答，并提供此类脂质体核酸与治疗性抗体的协同组合以显着改善抗体依赖性细胞毒性和靶细胞溶解。 p>

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