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    Targeted delivery system
    2.
    发明授权
    Targeted delivery system 有权
    目标传送系统

    公开(公告)号：US07803398B2

    公开(公告)日：2010-09-28

    申请号：US11020773

    申请日：2004-12-23

    申请人： Shyh-Dar Li ,  Ae-June Wang ,  Leaf Huang

    发明人： Shyh-Dar Li ,  Ae-June Wang ,  Leaf Huang

    IPC分类号： A61K9/127

    CPC分类号： A61K31/685 ,  A61K9/1272 ,  A61K47/60

    摘要： A targeting delivery system. The targeted delivery system includes a carrier for a drug and a targeted ligand modifying the carrier to target the encapsulated drug to a sigma receptor over-expressed cell.

    摘要翻译： 定位投放系统 靶向递送系统包括用于药物的载体和修饰载体以将包封的药物靶向西格玛受体过表达细胞的靶向配体。

    METHODS AND COMPOSITIONS FOR THE DELIVERY OF BIOACTIVE COMPOUNDS
    3.
    发明申请
    METHODS AND COMPOSITIONS FOR THE DELIVERY OF BIOACTIVE COMPOUNDS 审中-公开
    用于提供生物化合物的方法和组合物

    公开(公告)号：US20110117026A1

    公开(公告)日：2011-05-19

    申请号：US12993424

    申请日：2009-05-01

    申请人： Yu-Chen Tseng ,  Sang Kyoon Kim ,  Michael Hackett ,  Sumio Chono ,  Leaf Huang ,  Shyh-dar Li

    发明人： Yu-Chen Tseng ,  Sang Kyoon Kim ,  Michael Hackett ,  Sumio Chono ,  Leaf Huang ,  Shyh-dar Li

    IPC分类号： A61K9/127 ,  C12Q1/02 ,  C12N5/071 ,  A61K31/713 ,  A61K49/00 ,  A61P35/00

    CPC分类号： C07C279/10 ,  A61K9/1271 ,  A61K9/1272 ,  A61K47/6911 ,  C07C279/20 ,  C12N15/88

    摘要： The present invention provides compositions comprising delivery systems comprising a lipid vehicle, a bioactive compound, and a polyanionic carrier macromolecule that is not a carrier polynucleotide, wherein the lipid vehicle encapsulates the polynucleotide of interest and the polyanionic carrier macromolecule, and wherein the delivery system is essentially free of carrier polynucleotides. Compositions also include delivery systems comprising a lipid vehicle and a bioactive agent, wherein the lipid vehicle encapsulates the bioactive agent, and wherein the lipid vehicle comprises a covalent bilayer or a core supported bilayer comprising polycationic lipids. Other compositions provided herein comprise a delivery system comprising a polypeptide of interest and a means for delivering the polypeptide into a cell. Also provided herein are methods for making the delivery systems, methods for delivering bioactive compounds, methods for treating a disease or unwanted condition in a subject with the delivery systems, and methods for detecting apoptosis in a cell.

    摘要翻译： 本发明提供包含递送系统的组合物，其包含脂质载体，生物活性化合物和不是载体多核苷酸的聚阴离子载体大分子，其中所述脂质载体包封感兴趣的多核苷酸和聚阴离子载体大分子，并且其中递送系统是 基本上不含载体多核苷酸。 组合物还包括包含脂质载体和生物活性剂的递送系统，其中所述脂质载体包封所述生物活性剂，并且其中所述脂质载体包含共价双层或包含聚阳离子脂质的核心负载双层。 本文提供的其它组合物包含包含感兴趣多肽的递送系统和用于将多肽递送至细胞的手段。 本文还提供了制备递送系统的方法，用于递送生物活性化合物的方法，用于用递送系统治疗受试者的疾病或不需要的病症的方法，以及用于检测细胞凋亡的方法。

    Methods and compositions comprising novel cationic lipids
    4.
    发明授权
    Methods and compositions comprising novel cationic lipids 有权
    包含新型阳离子脂质的方法和组合物

    公开(公告)号：US08389768B2

    公开(公告)日：2013-03-05

    申请号：US12993421

    申请日：2009-05-01

    申请人： Leaf Huang ,  Yunching Chen ,  Joyeeta Sen ,  Surendar Reddy Bathula ,  Sumio Chono ,  Shyh-Dar Li ,  Michael Hackett

    发明人： Leaf Huang ,  Yunching Chen ,  Joyeeta Sen ,  Surendar Reddy Bathula ,  Sumio Chono ,  Shyh-Dar Li ,  Michael Hackett

    IPC分类号： C07C237/00 ,  C07C279/00 ,  A61K31/16 ,  A61K31/155

    CPC分类号： C07C279/10 ,  A61K9/1271 ,  A61K9/1272 ,  A61K47/6911 ,  C07C279/20 ,  C12N15/88

    摘要： Provided herein are novel cationic lipids, compositions comprising the cationic lipids, and methods of using the cationic lipids. In some claims, the cationic lipids have cytotoxic activity and can be used alone or in combination with a cytotoxic bioactive compound to kill a cell. In some of these claims, the cationic lipid enhances the cytotoxic activity of the cytotoxic bioactive compound. Methods for treating a subject afflicted with a disease or unwanted condition are provided, wherein the method comprises administering a delivery system comprising a novel cationic lipid to the subject. The invention further provides methods for making delivery systems comprising the novel cationic lipids of the invention.

    摘要翻译： 本文提供了新型阳离子脂质，包含阳离子脂质的组合物和使用阳离子脂质的方法。 在一些权利要求中，阳离子脂质具有细胞毒性活性，并且可以单独使用或与细胞毒性生物活性化合物组合用于杀死细胞。 在这些权利要求中的一些中，阳离子脂质增强细胞毒性生物活性化合物的细胞毒性活性。 提供了治疗患有疾病或不需要的病症的受试者的方法，其中所述方法包括向所述受试者施用包含新型阳离子脂质的递送系统。 本发明还提供了制备包含本发明的新型阳离子脂质的递送系统的方法。

    METHODS AND COMPOSITIONS COMPRISING NOVEL CATIONIC LIPIDS
    5.
    发明申请
    METHODS AND COMPOSITIONS COMPRISING NOVEL CATIONIC LIPIDS 有权
    包含新型阳离子脂肪的方法和组合物

    公开(公告)号：US20110117141A1

    公开(公告)日：2011-05-19

    申请号：US12993421

    申请日：2009-05-01

    申请人： Leaf Huang ,  Yunching Chen ,  Joyeeta Sen ,  Surendar Reddy Bathula ,  Sumio Chono ,  Shyh-Dar Li ,  Michael Hackett

    发明人： Leaf Huang ,  Yunching Chen ,  Joyeeta Sen ,  Surendar Reddy Bathula ,  Sumio Chono ,  Shyh-Dar Li ,  Michael Hackett

    IPC分类号： A61K31/164 ,  C07C279/14 ,  A61K31/713 ,  A61K9/00 ,  A61K33/24 ,  A61P35/00 ,  C12N5/071

    CPC分类号： C07C279/10 ,  A61K9/1271 ,  A61K9/1272 ,  A61K47/6911 ,  C07C279/20 ,  C12N15/88

    摘要： Provided herein are novel cationic lipids, compositions comprising the cationic lipids, and methods of using the cationic lipids. In some claims, the cationic lipids have cytotoxic activity and can be used alone or in combination with a cytotoxic bioactive compound to kill a cell. In some of these claims, the cationic lipid enhances the cytotoxic activity of the cytotoxic bioactive compound. Methods for treating a subject afflicted with a disease or unwanted condition are provided, wherein the method comprises administering a delivery system comprising a novel cationic lipid to the subject. The invention further provides methods for making delivery systems comprising the novel cationic lipids of the invention.

    摘要翻译： 本文提供了新型阳离子脂质，包含阳离子脂质的组合物和使用阳离子脂质的方法。 在一些权利要求中，阳离子脂质具有细胞毒性活性，并且可以单独使用或与细胞毒性生物活性化合物组合用于杀死细胞。 在这些权利要求中的一些中，阳离子脂质增强细胞毒性生物活性化合物的细胞毒性活性。 提供了治疗患有疾病或不需要的病症的受试者的方法，其中所述方法包括向所述受试者施用包含新型阳离子脂质的递送系统。 本发明还提供了制备包含本发明的新型阳离子脂质的递送系统的方法。

    Sphingomyelin liposomes for the treatment of hyperactive bladder disorders
    6.
    发明授权
    Sphingomyelin liposomes for the treatment of hyperactive bladder disorders 有权
    鞘磷脂脂质体用于治疗膀胱过动症

    公开(公告)号：US08110217B2

    公开(公告)日：2012-02-07

    申请号：US11546025

    申请日：2006-10-11

    申请人： Michael B. Chancellor ,  Pradeep Tyagi ,  Matthew O. Fraser ,  Yao-Chi Chuang ,  William C de Groat ,  Leaf Huang ,  Naoki Yoshimura

    发明人： Michael B. Chancellor ,  Pradeep Tyagi ,  Matthew O. Fraser ,  Yao-Chi Chuang ,  William C de Groat ,  Leaf Huang ,  Naoki Yoshimura

    IPC分类号： A61K9/127

    CPC分类号： A61K9/127 ,  A61K9/0034 ,  A61K9/1272 ,  Y02A50/469

    摘要： The present invention provides pharmaceutical compositions and methods for the instillation of lipid vehicles comprised of liposomes containing sphingomyelin or sphingomyelin metabolites to prevent, manage, ameliorate and/or treat disorders involving neuropathic pain and aberrant muscle contractions, such as what occurs in bladder hyperactivity disorders such as interstitial cystitis (IC) in animals or humans in need thereof. Also provided is a liposome-based delivery of drugs, e.g., antibiotics, pain treatments and anticancer agents, to the bladder, genitourinary tract, gastrointestinal system, pulmonary system and other organs or body systems. In particular, liposome-based delivery of vanilloid compounds, such as resiniferatoxin, capsaicin, or tinyatoxin and toxins, such as botulinum toxin is provided for the treatment of bladder conditions, including pain, inflammation, incontinence and voiding dysfunction.

    摘要翻译： 本发明提供用于滴注含有鞘磷脂或鞘磷脂代谢物的脂质体的脂质载体的药物组合物和方法，以预防，治疗，改善和/或治疗涉及神经性疼痛和异常肌肉收缩的疾病，例如膀胱多动障碍 作为有需要的动物或人类的间质性膀胱炎（IC）。 还提供了对膀胱，泌尿生殖道，胃肠系统，肺系统和其他器官或身体系统的基于脂质体的药物递送，例如抗生素，疼痛治疗和抗癌剂。 特别地，提供了基于脂质体的递送香草素化合物，例如树脂毒素，辣椒素或微量毒素和毒素，例如肉毒杆菌毒素，用于治疗膀胱状况，包括疼痛，炎症，失禁和排尿功能障碍。

    Stable aqueous dispersions including cationic lipids
    8.
    发明授权
    Stable aqueous dispersions including cationic lipids 失效
    稳定的水分散体包括阳离子脂质

    公开(公告)号：US06361791B1

    公开(公告)日：2002-03-26

    申请号：US08580779

    申请日：1995-12-28

    申请人： Leaf Huang ,  Richard M. Epand ,  Remo Bottega

    发明人： Leaf Huang ,  Richard M. Epand ,  Remo Bottega

    IPC分类号： A61K9127

    CPC分类号： C07J41/0055 ,  A61K9/1272 ,  A61K47/54 ,  A61K47/554 ,  C07J9/00 ,  C12N15/64 ,  C12N15/88 ,  Y10T428/2984

    摘要： A stable aqueous dispersion which comprises a cationic lipid which is a molecule which comprises a cholesterol-derived lipophilic group, a linker bond which is hydrolyzable by cellular enzymes and relatively resistant to base-catalyzed hydrolysis, a spacer arm and a cationic amino group, and an appropriate co-lipid. The invention also includes the cationic lipids and mammalian plasmid DNA or other cells in admixture with the aqueous dispersion.

    摘要翻译： 一种稳定的水分散体，其包含阳离子脂质，其是包含胆固醇衍生的亲脂基团的分子，可被细胞酶水解并且相对抗碱基催化水解的连接体键，间隔臂和阳离子氨基，以及 合适的辅助脂质。 本发明还包括与水分散体混合的阳离子脂质和哺乳动物质粒DNA或其它细胞。

    Fused liposome and acid induced method for liposome fusion
    9.
    发明授权
    Fused liposome and acid induced method for liposome fusion 失效
    融合脂质体和酸诱导的脂质体融合方法

    公开(公告)号：US5283122A

    公开(公告)日：1994-02-01

    申请号：US836125

    申请日：1992-02-14

    申请人： Leaf Huang ,  Jerome Connor

    发明人： Leaf Huang ,  Jerome Connor

    IPC分类号： A61K9/127 ,  C12N15/88

    CPC分类号： A61K9/1272 ,  C12N15/88 ,  Y10S436/829 ,  Y10T428/2984

    摘要： Liposomes containing phosphatidylethanolamine, palmitoyl homocysteine or oleic acid or palmitic acid, fuse rapidly when the pH of the medium is reduced below 7. Liposome fusion was measured by (a) mixing of the liposomal lipids as shown by resonance energy transfer, (b) gel filtration and (c) electron microscopy. The presence of phosphatidylethanolamine or acid addition esters thereof in the liposomes greatly enhances fusion; whereas the presence of phosphatidylcholine inhibits fusion. During fusion of liposomes containing phosphatidylethanolamine:palmitoyl homocysteine (8:2), almost all of the encapsulated calcein is released. Inclusion of cholesterol (40%) in the liposomes substantially decreases leakage without impairing fusion. Those pH sensitive liposomes are fused to deliver biologically active molecules such as DNA, into living cells.

    摘要翻译： 含有磷脂酰乙醇胺，棕榈酰高半胱氨酸或油酸或棕榈酸的脂质体当培养基的pH值降至7以下时迅速融合。脂质体融合通过（a）如共振能量转移所示脂质体脂质的混合，（b）凝胶 过滤和（c）电子显微镜。 磷脂酰乙醇胺或其酸加成酯在脂质体中的存在大大增强了融合; 而磷脂酰胆碱的存在抑制融合。 在含有磷脂酰乙醇胺的脂质体融合过程中，棕榈酰同型半胱氨酸（8：2）几乎全部被包裹的钙黄绿素释放出来。 在脂质体中包含胆固醇（40％）可显着减少渗漏而不损害融合。 将这些pH敏感的脂质体融合以将生物活性分子例如DNA递送到活细胞中。

    Fused liposome and acid induced method for liposome fusion
    10.
    发明授权
    Fused liposome and acid induced method for liposome fusion 失效
    融合脂质体和酸诱导的脂质体融合方法

    公开(公告)号：US4789633A

    公开(公告)日：1988-12-06

    申请号：US602177

    申请日：1984-04-19

    申请人： Leaf Huang ,  Jerome Connor

    发明人： Leaf Huang ,  Jerome Connor

    IPC分类号： A01H1/00 ,  A01H5/00 ,  A61K9/00 ,  A61K9/127 ,  B01J13/02 ,  C12N5/00 ,  C12N5/02 ,  C12N5/10 ,  C12N15/00 ,  C12N15/88 ,  A61J5/00 ,  B32B5/16

    CPC分类号： A61K9/127 ,  A61K9/1272 ,  C12N15/88 ,  Y10T428/2984

    摘要： Liposomes containing phosphatidylethanolamine, palmitoyl homocysteine or oleic acid or palmitic acid, fuse rapidly when the pH of the medium is reduced below 7. Liposome fusion was measured by (a) mixing of the liposomal lipids as shown by resonance energy transfer, (b) gel filtration and (c) electron microscopy. The presence of phosphatidylethanolamine or acid addition esters thereof in the liposomes greatly enhances fusion; whereas the presence of phosphatidylcholine inhibits fusion. During fusion of liposomes containing phosphatidylethanolamine:palmitoyl homocysteine (8:2), almost all of the encapsulate calcein is released. Inclusion of cholesterol (40%) in the liposomes substantially decreases leakage without impairing fusion. Those pH sensitive liposomes are fused to deliver biologically active molecules such as DNA, into living cells.

    摘要翻译： 含有磷脂酰乙醇胺，棕榈酰高半胱氨酸或油酸或棕榈酸的脂质体当培养基的pH值降至7以下时迅速融合。脂质体融合通过（a）如共振能量转移所示脂质体脂质的混合，（b）凝胶 过滤和（c）电子显微镜。 磷脂酰乙醇胺或其酸加成酯在脂质体中的存在大大增强了融合; 而磷脂酰胆碱的存在抑制融合。 在含有磷脂酰乙醇胺的脂质体融合过程中，棕榈酰同型半胱氨酸（8：2）几乎全部释放出钙黄绿素。 在脂质体中包含胆固醇（40％）可显着减少渗漏而不损害融合。 将这些pH敏感的脂质体融合以将生物活性分子例如DNA递送到活细胞中。