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1. 发明申请

US20170239182A1 PHARMACEUTICAL FORMULATIONS OF AND METHODS TO PREPARE CHELATING AGENTS FOR EFFICIENT METAL REMOVAL TREATMENT SYSTEMS 审中-公开
公开(公告)号：US20170239182A1
公开(公告)日：2017-08-24
申请号：US15503004
申请日：2015-08-12
申请人： Mark E. HAYES , Charles O. NOBLE , Francis C. SZOKA, JR. , ZONEONE PHARMA, INC.
发明人： Mark E. HAYES , Charles O. NOBLE , Francis C. SZOKA, JR.
IPC分类号： A61K9/127 , A61K31/4196 , A61K31/16
CPC分类号： A61K9/127 , A61K9/1272 , A61K9/1278 , A61K31/16 , A61K31/4196
摘要： The present invention provides liposomes loaded with chelating agents, pharmaceutical formulations including these liposomes and methods of making chelating agent liposomes. Because the chelating agents are loaded in the liposome with high efficiencies, the liposomes are of use in treatment of metal ion overload in subjects. The liposomes can also contain essential trace metals to compensate for the off target effect of removal of endogenous non-target trace metals by administration of the chelator. The liposomes can include two or more different chelating agents of different structures and affinities for metal ions.

2. 发明授权

US08956646B2 Zwitterionic lipids 有权
标题翻译：两性离子脂质
公开(公告)号：US08956646B2
公开(公告)日：2015-02-17
申请号：US13816882
申请日：2011-08-15
申请人： Francis C. Szoka, Jr. , Colin Walsh , Vincent Venditto , Juliane Nguyen , Emily Perttu
发明人： Francis C. Szoka, Jr. , Colin Walsh , Vincent Venditto , Juliane Nguyen , Emily Perttu
IPC分类号： C07C229/00 , C07C229/12 , A61K9/127 , C07C279/14 , C07C309/14 , C07F9/09 , C07F9/54 , C07F9/6509 , C07J9/00 , C40B40/04 , A61K47/18 , A61K47/28 , C07J41/00
CPC分类号： C07C229/12 , A61K9/1272 , A61K47/186 , A61K47/28 , C07C279/14 , C07C309/14 , C07F9/091 , C07F9/54 , C07F9/650952 , C07J9/00 , C07J41/0055 , C40B40/04
摘要： In various embodiments, the present invention provides zwitterionic lipids, encapsulants incorporating these zwitterionic lipids and such encapsulants encapsulating one or more bioactive agent. An exemplary bioactive agent is a nucleic acid. Also provided are pharmaceutical formulations of the encapsulants and methods of using such formulations to deliver a bioactive agent to a subject in treating or diagnosing disease in that subject.
摘要翻译：在各种实施方案中，本发明提供两性离子脂质，包含这些两性离子性脂质的密封剂和封装一种或多种生物活性剂的这种密封剂。示例性的生物活性剂是核酸。还提供了密封剂的药物制剂和使用这些制剂将生物活性剂递送到受试者以治疗或诊断该受试者的疾病的方法。

3. 发明授权

US06897196B1 pH sensitive lipids based on ortho ester linkers, composition and method 失效
标题翻译：基于原酸酯接头的pH敏感性脂质，组成和方法
公开(公告)号：US06897196B1
公开(公告)日：2005-05-24
申请号：US09778388
申请日：2001-02-07
申请人： Francis C. Szoka, Jr. , Xin Guo
发明人： Francis C. Szoka, Jr. , Xin Guo
IPC分类号： A61K9/127 , A61K31/00 , A01N43/04
CPC分类号： A61K9/1272 , A61K31/00
摘要： The invention comprises lipid derivatives that rapidly degrade in the pH range from 4.0 to 7.0 and lipidic delivery systems that contain them. These lipid derivatives can be used to modify the delivery properties of the lipidic delivery systems to enable prolonged circulation times or more rapid drug unloading in the target tissue. The lipid derivatives are amphipathic compounds comprising a hydrophilic head group joined to a hydrophobic group by an acid-labile ortho ester linkage. The delivery systems of the invention exhibit degradation of less than 10% within 3 hours at a pH of 7.4 and degradation greater than 50% within 60 min at a pH of 5.0.
摘要翻译：本发明包括在4.0至7.0的pH范围内迅速降解的脂质衍生物和含有它们的脂质递送系统。这些脂质衍生物可用于改变脂质递送系统的递送性质，以使靶组织中的延长循环时间或更快速的药物卸载。脂质衍生物是包含通过酸不稳定原酸酯键连接到疏水基团的亲水性头基的两亲性化合物。本发明的递送系统在pH为7.4时在3小时内显示小于10％的降解，并且在pH5.0的60分钟内降解大于50％。

4. 发明申请

US20110177156A1 Sterol-Modified Amphiphilic Lipids 审中-公开
标题翻译：甾醇修饰的两亲脂质
公开(公告)号：US20110177156A1
公开(公告)日：2011-07-21
申请号：US12742594
申请日：2008-11-10
申请人： Francis C. Szoka, JR. , Zhaohua Huang
发明人： Francis C. Szoka, JR. , Zhaohua Huang
IPC分类号： A61K9/127 , C07J51/00 , A61K31/203 , A61K33/24 , A61K31/7115 , G01N33/92 , A61P9/10
CPC分类号： A61K8/63 , A61Q19/00 , C07J41/0055 , C07J51/00
摘要： Disclosed are sterol-modified amphiphilic lipid compounds having two or more hydrophobic tails of which at least one is a sterol. Also disclosed are the processes for the synthesis of these compounds, compositions comprising such compounds, and the use of such compounds in delivery of an agent of interest, e.g., therapeutics, imaging agents, contrast materials for ultrasound applications, vaccines, biosensors, nutritional supplements and skin care products.
摘要翻译：公开了具有两个或更多个疏水尾部的固醇修饰的两亲脂质化合物，其至少一个是固醇。还公开了合成这些化合物的方法，包含这些化合物的组合物，以及这些化合物在感兴趣的药物递送中的用途，例如治疗剂，显像剂，用于超声应用的造影剂，疫苗，生物传感器，营养补品和护肤品。

5. 发明授权

US06593308B2 Targeted drug delivery with a hyaluronan ligand 有权
标题翻译：用透明质酸配体靶向药物递送
公开(公告)号：US06593308B2
公开(公告)日：2003-07-15
申请号：US09454811
申请日：1999-12-03
申请人： Francis C. Szoka, Jr.
发明人： Francis C. Szoka, Jr.
IPC分类号： A01N4304
CPC分类号： A61K9/1271 , A61K47/6911
摘要： The invention is a drug delivery system of a delivery vehicle having a low molecular weight hyaluronan ligand with an affinity for CD44 receptors. Preferably, the delivery vehicle is a liposome but other suitable delivery vehicles include microspheres, micelles, emulsions, lipid discs, polymers, viral particles and viruses. The systems of the invention may further comprise a drug, which can be any anticancer agent or other therapeutic or diagnostic agent. The invention also comprises methods of delivering a drug to a cell that expresses CD44 by contacting the cell with the drug delivery system. Further methods include treating a patient with cancer and targeting drug delivery to cells that express CD44 by attaching a glycosaminoglycan ligand.
摘要翻译：本发明是具有对CD44受体具有亲和力的低分子量透明质酸配体的递送载体的药物递送系统。优选地，递送载体是脂质体，但是其它合适的递送载体包括微球，胶束，乳剂，脂质盘，聚合物，病毒颗粒和病毒。本发明的系统还可以包含药物，其可以是任何抗癌剂或其它治疗或诊断剂。本发明还包括通过使细胞与药物递送系统接触来将药物递送至表达CD44的细胞的方法。其他方法包括治疗患有癌症的患者，并通过连接糖胺聚糖配体将药物递送靶向表达CD44的细胞。

6. 发明授权

US5567434A Preparation of liposome and lipid complex compositions 失效
标题翻译：脂质体和脂质复合物组合物的制备
公开(公告)号：US5567434A
公开(公告)日：1996-10-22
申请号：US480227
申请日：1995-06-07
申请人： Francis C. Szoka, Jr.
发明人： Francis C. Szoka, Jr.
IPC分类号： A61K9/127 , A61K9/16 , A61K47/48 , A61K51/12 , B01J13/02
CPC分类号： A61K47/48053 , A61K9/1277 , A61K9/1617 , Y10S436/829
摘要： Liposome and lipidic particle formulations of compounds are prepared by dissolving in a solution of liposome-forming lipids in an aprotic solvent such as DMSO, optionally containing a lipid-solubilizing amount of a lower alkanol, and either injecting the resulting solution into an aqueous solution, or the aqueous solution into the resulting solution. The resulting liposome or lipidic particle suspension may then be dialyzed or otherwise concentrated. This method is particularly useful for compounds which are poorly-soluble in aqueous solution, but is generally useful for any compound or combination of compounds which can be dissolved in the aprotic solvent or aprotic solvent/lower alkanol mixture.
摘要翻译：通过将脂质体形成脂质溶解在非质子溶剂如DMSO中，任选地含有脂溶性量的低级链烷醇，并将所得溶液注入水溶液中制备化合物的脂质体和脂质颗粒制剂，或将水溶液加入到所得溶液中。然后可以将所得的脂质体或脂质颗粒悬浮液透析或以其它方式浓缩。该方法对于难溶于水溶液的化合物特别有用，但通常可用于可溶于非质子溶剂或非质子溶剂/低级链烷醇混合物中的任何化合物或化合物的组合。

7. 发明授权

US4394448A Method of inserting DNA into living cells 失效
标题翻译：将DNA插入活细胞的方法
公开(公告)号：US4394448A
公开(公告)日：1983-07-19
申请号：US143455
申请日：1980-04-24
申请人： Francis C. Szoka, Jr. , Demetrios P. Papahadjopoulos
发明人： Francis C. Szoka, Jr. , Demetrios P. Papahadjopoulos
IPC分类号： A61K9/127 , C12N15/88 , C12N15/00
CPC分类号： C12N15/88 , A61K9/127 , Y10S435/82
摘要： A method of inserting deoxyribonucleic acid or fragments thereof into a living cell, which comprises; encapsulating the DNA or fragment in a lipid vesicle and bringing the vesicle in contact with said cell, whereby insertion occurs.
摘要翻译：将脱氧核糖核酸或其片段插入活细胞的方法，其包括：将DNA或片段包封在脂质囊泡中并使囊泡与所述细胞接触，从而进行插入。

8. 发明授权

US4394149A Plant nutriment compositions and method of their application 失效
标题翻译：植物营养成分及其应用方法
公开(公告)号：US4394149A
公开(公告)日：1983-07-19
申请号：US149516
申请日：1980-05-13
申请人： Francis C. Szoka, Jr. , Demetrios P. Papahadjopoulos
发明人： Francis C. Szoka, Jr. , Demetrios P. Papahadjopoulos
IPC分类号： A61K9/127 , C05C9/00 , C05G3/00
CPC分类号： C05C9/005 , A61K9/127 , C05G3/007 , Y10S71/02
摘要： The disclosure is of the use of plant nutriments encapsulated in synthetic lipid vesicles to nourish plants. SPCROSS-REFERENCE TO RELATED APPLICATIONThis application is a Continuation-in-Part of our copending application Ser. No. 881,116 filed Feb. 24, 1978 and now U.S. Pat. No. 4,235,871.
摘要翻译：本公开是使用包封在合成脂质囊泡中的植物营养物来滋养植物。

9. 发明授权

US08765171B2 Methods and compositions for liposomal formulation of antigens and uses thereof 有权
标题翻译：抗体脂质体制剂的方法和组合物及其用途
公开(公告)号：US08765171B2
公开(公告)日：2014-07-01
申请号：US12720592
申请日：2010-03-09
申请人： Gary Fujii , Francis C. Szoka, Jr. , Douglas S. Watson
发明人： Gary Fujii , Francis C. Szoka, Jr. , Douglas S. Watson
IPC分类号： A61K9/127 , A61K39/00 , A61K39/385 , C07J9/00 , A61P37/04
CPC分类号： A61K47/6913 , A61K9/1272 , A61K39/07 , A61K39/12 , A61K39/145 , A61K39/385 , A61K47/543 , A61K47/554 , A61K47/6911 , A61K2039/55555 , A61K2039/55572 , A61K2039/60 , A61K2039/6018 , A61K2039/627 , C07J9/00 , C07J41/0055 , C07J43/003 , C12N7/00 , C12N2740/16134 , C12N2760/16134 , C12N2770/00011 , C12N2770/00034
摘要： The present invention relates to liposomal vaccine compositions, methods for the manufacture thereof, and methods for the use thereof to stimulate an immune response in an animal. These compositions comprise dimyristoylphosphatidylcholine (“DMPC”); either dimyristoylphosphatidylglycerol (“DMPG”) or dimyristoyltrimethylammonium propane (“DMTAP”) or both DMPC and DMTAP; and at least one sterol derivative providing a covalent anchor for one or more immunogenic polypeptide(s) or carbohydrate(s).
摘要翻译：本发明涉及脂质体疫苗组合物，其制备方法及其用于刺激动物免疫应答的方法。这些组合物包含二肉豆蔻酰磷脂酰胆碱（“DMPC”）; 二肉豆蔻酰磷脂酰甘油（“DMPG”）或二肉豆蔻酰基三甲基铵丙烷（“DMTAP”）或DMPC和DMTAP两者; 和为一种或多种免疫原性多肽或碳水化合物提供共价锚的至少一种固醇衍生物。

10. 发明授权

US06300317B1 Self-assembling polynucleotide delivery system 失效
标题翻译：自组装多核苷酸递送系统
公开(公告)号：US06300317B1
公开(公告)日：2001-10-09
申请号：US08469899
申请日：1995-06-06
申请人： Francis C. Szoka, Jr. , Jean Haensler
发明人： Francis C. Szoka, Jr. , Jean Haensler
IPC分类号： A61K4800
CPC分类号： C07D401/14 , A61K9/1271 , A61K9/1272 , A61K47/54 , A61K47/543 , A61K47/55 , A61K47/645 , A61K47/6949 , A61K48/00 , B82Y5/00 , C07F9/10 , C08G83/003 , C08G2261/312 , C12N15/87
摘要： This invention provides a self-assembling polynucleotide delivery system comprising components aiding in the delivery of the polynucleotide to the desired address which are associated via noncovalent interactions with the polynucleotide. The components of this system include DNA-masking components, cell recognition components, charge-neutralization and membrane-permeabilization components, and subcellular localization components. Specific compounds useful in this system are also provided.
摘要翻译：本发明提供了一种自组装多核苷酸递送系统，其包含有助于将多核苷酸递送至通过与该多核苷酸的非共价相互作用相关的所需地址。该系统的组分包括DNA掩蔽组分，细胞识别组分，电荷中和和膜透化组分以及亚细胞定位组分。还提供了在该体系中有用的具体化合物。

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