公开(公告)号：US07655468B2

公开(公告)日：2010-02-02

申请号：US11943434

申请日：2007-11-20

申请人： Leaf Huang ,  Xiang Gao ,  Frank L. Sorgi

发明人： Leaf Huang ,  Xiang Gao ,  Frank L. Sorgi

IPC分类号： C12N15/88 ,  A61K31/70 ,  A61K9/127

CPC分类号： A61K47/48315 ,  A61K9/1272 ,  A61K47/543 ,  A61K47/645 ,  C12N15/88

摘要： Novel stable, concentrated, biologically active and ready-to-use lipid-comprising drug delivery complexes and methods for their production are described. The biological activity of the complexes produced are comparable to the formulations prepared according to the prior art admixture method and upon purification, the complexes produced by the method of this invention are 50 to 500 fold more concentrated than the complexes formed by admixture. The method described herein provides for the large scale production of lipid-comprising drug delivery systems useful for gene therapy and other applications.

摘要翻译： 描述了新的稳定的，浓缩的，生物活性的和即用型含脂质的药物递送复合物及其生产方法。 所生成的络合物的生物活性与根据现有技术的混合方法制备的制剂相当，并且在纯化后，通过本发明的方法制备的络合物比通过混合物形成的络合物浓度多50至500倍。 本文所述的方法提供大规模生产用于基因治疗和其它应用的含脂质药物递送系统。

公开(公告)号：US20090017057A1

公开(公告)日：2009-01-15

申请号：US12049957

申请日：2008-03-17

申请人： Weihsu Chen ,  Weili Yan ,  Kenya Toney ,  Gregory Conn ,  Frank Bedu-Addo ,  Leaf Huang

发明人： Weihsu Chen ,  Weili Yan ,  Kenya Toney ,  Gregory Conn ,  Frank Bedu-Addo ,  Leaf Huang

IPC分类号： A61K39/00 ,  C07C69/602 ,  A61K39/12 ,  A61P37/02 ,  A61K39/02 ,  C07C217/46

CPC分类号： A61K31/231 ,  A61K31/14 ,  A61K31/20 ,  A61K39/00 ,  A61K39/0011 ,  A61K39/12 ,  A61K39/39 ,  A61K45/06 ,  A61K47/646 ,  A61K2039/55555 ,  C07C219/06

摘要： The present invention provides compositions and methods for stimulating an immune response using cationic lipids alone or in combination with antigens.

摘要翻译： 本发明提供了使用单独或与抗原组合的阳离子脂质来刺激免疫应答的组合物和方法。

公开(公告)号：US07361640B2

公开(公告)日：2008-04-22

申请号：US10426220

申请日：2003-04-29

申请人： Leaf Huang ,  Xiang Gao ,  Frank L. Sorgi

发明人： Leaf Huang ,  Xiang Gao ,  Frank L. Sorgi

IPC分类号： A61K31/715 ,  A61K9/127 ,  C12N15/88 ,  C07H21/02 ,  C07K17/00

CPC分类号： C12N15/88 ,  A61K9/1272

摘要： Novel stable, concentrated, biologically active and ready-to-use lipid-comprising drug delivery complexes and methods for their production are described. The biological activity of the complexes produced are comparable to the formulations prepared according to the prior art admixture method and upon purification, the complexes produced by the method of this invention are 50 to 500 fold more concentrated than the complexes formed by admixture. The method described herein provides for the large scale production of lipid-comprising drug delivery systems useful for gene therapy and other applications.

公开(公告)号：US06610321B2

公开(公告)日：2003-08-26

申请号：US09214546

申请日：1999-02-17

申请人： Leaf Huang ,  Toshifumi Hara

发明人： Leaf Huang ,  Toshifumi Hara

IPC分类号： A61K9127

CPC分类号： A61K9/1275 ,  A61K48/00 ,  Y02A50/409 ,  Y10S514/938

摘要： This invention includes emulsion formulations comprising an aqueous carrier and the following components: triglyceride, cholesterol, phospholipid, at least one charged lipid, at least one hydrophilic biologically active molecule and, optionally, cholesteryl ester, and/or apoprotein; methods of preparing these emulsions; and the use of these emulsions for the delivery of hydrophilic biologically active molecules to cells.

摘要翻译： 本发明包括包含水性载体和以下组分的乳液制剂：甘油三酸酯，胆固醇，磷脂，至少一种带电脂质，至少一种亲水生物活性分子和任选的胆固醇酯和/或脱蛋白; 制备这些乳液的方法; 以及使用这些乳液将亲水生物活性分子递送至细胞。

公开(公告)号：US06319516B1

公开(公告)日：2001-11-20

申请号：US09334313

申请日：1999-06-16

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。

公开(公告)号：US06258792B1

公开(公告)日：2001-07-10

申请号：US09669031

申请日：2000-09-25

申请人： Hermant M. Deshmukh ,  Leaf Huang

发明人： Hermant M. Deshmukh ,  Leaf Huang

IPC分类号： A01N4304

CPC分类号： C07J43/00 ,  C07J53/00

摘要： The present invention discloses compounds which are cationic cholesteryl derivatives having a nitrogen-containing ring structure as their polar head group. These compounds are useful for delivering biologically active substances to cells and for transfecting nucleic acids into cells.

摘要翻译： 本发明公开了具有含氮环结构作为其极性头基的阳离子胆固醇衍生物的化合物。 这些化合物可用于将生物活性物质递送至细胞并将核酸转染入细胞。

公开(公告)号：US6120794A

公开(公告)日：2000-09-19

申请号：US534180

申请日：1995-09-26

申请人： Dexi Liu ,  Feng Liu ,  Jing-Ping Yang ,  Leaf Huang

发明人： Dexi Liu ,  Feng Liu ,  Jing-Ping Yang ,  Leaf Huang

IPC分类号： A61K9/107 ,  A61K31/70 ,  A61K31/7088 ,  A61K38/00 ,  A61K39/00 ,  A61K47/18 ,  A61K47/24 ,  A61K48/00 ,  A61K9/127

CPC分类号： A61K9/1075 ,  Y10S514/938

摘要： New emulsion and micelle formulations are described as are complexes of these formulations with biologically active substances. The novel formulations are different from cationic lipid vectors such as cationic liposomes in that the complexes formed between biologically active substances and the emulsion and micellar formulations of this invention are physically stable and their transfection activity is resistant to the presence of serum. These novel formulations are disclosed to be useful in areas such as gene therapy or vaccine delivery.

公开(公告)号：US5908777A

公开(公告)日：1999-06-01

申请号：US494296

申请日：1995-06-23

申请人： Robert J. Lee ,  Leaf Huang

发明人： Robert J. Lee ,  Leaf Huang

IPC分类号： C07K14/285 ,  C12N15/88 ,  C12N15/63

CPC分类号： C12N15/88 ,  C07K14/285

摘要： A simple, rapid method for creating a lipidic vector for delivery of a therapeutic molecule entails bringing the molecule into contact with a polycation, thereby forming a complex, and then mixing the complex with an anionic lipidic preparation. Tissue-specific targeting peptides, fusogenic peptides and nucleus-targeting peptides also can be added to the lipid preparation. The result is a stable lipidic vector of reduced immunogenicity and cytotoxicity. The vector also displays enhanced transfection activity.

摘要翻译： 用于产生用于递送治疗性分子的脂质载体的简单且快速的方法需要使分子与聚阳离子接触，从而形成复合物，然后将该配合物与阴离子脂质制剂混合。 组织特异性靶向肽，融合肽和核 - 靶向肽也可加入到脂质制剂中。 结果是具有降低的免疫原性和细胞毒性的稳定的脂质载体。 载体还显示增强的转染活性。

公开(公告)号：US5795587A

公开(公告)日：1998-08-18

申请号：US376701

申请日：1995-01-23

申请人： Xiang Gao ,  Leaf Huang

发明人： Xiang Gao ,  Leaf Huang

IPC分类号： A61K9/127 ,  A61K48/00 ,  C12N15/88

CPC分类号： A61K47/48315 ,  A61K47/48046 ,  A61K9/1272 ,  C12N15/88

摘要： Novel stable, concentrated, biologically active and ready-to-use lipid-comprising drug delivery complexes and methods for their production are described. The biological activity of the complexes produced are comparable to the formulations prepared according to the prior art admixture method and upon purification, the complexes produced by the method of this invention are 50 to 500 fold more concentrated than the components of the complexes formed by admixture. The method described herein provides for the large scale production of lipid-comprising drug delivery systems useful for gene therapy and other applications.

摘要翻译： 描述了新的稳定的，浓缩的，生物活性的和即用型含脂质的药物递送复合物及其生产方法。 生产的络合物的生物活性与根据现有技术的混合方法制备的制剂相当，并且在纯化后，通过本发明的方法制备的络合物比通过混合物形成的络合物的组分浓度多50至500倍。 本文所述的方法提供大规模生产用于基因治疗和其它应用的含脂质药物递送系统。

公开(公告)号：US5637315A

公开(公告)日：1997-06-10

申请号：US349129

申请日：1994-12-02

申请人： Mark Zern ,  Leaf Huang ,  Tony Yoa

发明人： Mark Zern ,  Leaf Huang ,  Tony Yoa

IPC分类号： A61K9/127 ,  A61K9/133 ,  A61K31/05 ,  A61K31/19 ,  A61K31/355 ,  A61K31/375

CPC分类号： A61K31/19 ,  A61K31/05 ,  A61K31/355 ,  A61K31/375 ,  A61K9/127 ,  Y10S436/829

摘要： Liposome carrier systems, methods and pharmaceutical compositions that target an organ preferentially with high concentrations of at least one therapeutic agent utilize a liposome carrier having a lipid membrane and an aqueous space to deliver pharmacologically active agents, such as free radical scavengers and antioxidants, to a target organ such as the liver. At least one free radical scavenger and/or antioxidant and a liposome carrier may be provided to a liver donor prior to harvesting to preserve the liver for transplantation.

摘要翻译： 优选以高浓度的至少一种治疗剂靶向器官的脂质体载体系统，方法和药物组合物利用具有脂质膜和水性空间的脂质体载体将药理活性剂（例如自由基清除剂和抗氧化剂）递送至 目标器官如肝脏。 可以在收获之前将至少一种自由基清除剂和/或抗氧化剂和脂质体载体提供给肝供体以保留用于移植的肝脏。