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1. 发明申请

WO0045878A3 COMPRESSED AIR INHALER FOR PULMONARY APPLICATION OF LIPOSOMAL POWDER AEROSOLS AND POWDER AEROSOLS SUITABLE THEREFOR 审中-公开
标题翻译： DRUCKLUFTINHALATOR肺应用脂质体粉末涂料，适合的粉末气溶胶
公开(公告)号：WO0045878A3
公开(公告)日：2000-09-28
申请号：PCT/DE0000337
申请日：2000-02-03
申请人： MAX DELBRUECK CENTRUM , FRAUNHOFER GES FORSCHUNG , DIEDERICHS JULIA EVA , KOCH WOLFGANG , LOEDDING HUBERT , RESZKA REGINA , WINDT HORST
发明人： DIEDERICHS JULIA EVA , KOCH WOLFGANG , LOEDDING HUBERT , RESZKA REGINA , WINDT HORST
IPC分类号： A61K9/12 , A61K9/00 , A61K9/127 , A61K9/16 , A61K9/51 , A61K9/72 , A61K47/24 , A61K47/28 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/42 , A61L9/12 , A61M11/02 , A61M11/06 , A61M15/00 , A61P11/00 , B05B7/00 , B05B7/06
CPC分类号： A61K9/0075 , A61K9/0078 , A61K9/127 , A61K9/1272 , A61K9/1277 , A61M11/001 , A61M11/06 , A61M15/0086 , B05B7/0012 , B05B7/066
摘要： The invention relates to a compressed air inhaler for the pulmonary application of a liposomal powder aerosol that carries active agents or is uncharged. The aim of the invention is to provide an inhaler by means of which the pulmonary application of especially liposomes that carry active agents is possible without forced breathing manoeuvres and by means of which the active agent can be transferred to the desired place of action in a sufficient amount without the active agent escaping. To this end, said compressed air inhaler comprises a receptacle (20) for the aqueous dispersion of liposomes. The liposomes carrying the active agents are dispersed in water in said receptacle. The receptacle is connected to an anatomising nozzle (1) and to a drying unit (17) via a device that doses liquids (19), whereby the drying unit can be an atomising chamber for spray drying the liposomes. An outlet (18) and a mouth piece are joined to said drying unit. The anatomising nozzle (1) is provided with separate supply channels (14, 16) for the compressed air and the dispersion of the liposomes (fig.1). The invention also relates to a novel powder aerosol consisting of liposomes or nanoparticles.
摘要翻译：本发明涉及一种用于承载无负载或脂质体粉末气雾剂的活性剂的肺部给药的Druckluftinhalator。本发明的目的是提供一种吸入器，用于处理与特定药物携带脂质体的肺部给药而无需用力呼吸动作成为可能与活性剂可以以期望的作用位点足够量带来不活性剂逸出，在该Druckluftinhalator为脂质体粉末气雾剂，对于其中药物携带脂质体分散在水中含有液体充电（19）用雾化器喷嘴的水性脂质体分散液的容器（20）的肺应用（1实现）和（与干燥单元17）是连接到所述脂质体的喷雾干燥雾化室，其输出端（18）作为吹口相邻接，其中，所述喷嘴（1）分开的进料（14，包括16个）用于将压缩空气和该脂质体分散体，包括（图1）。本发明还涉及一种新的粉末气雾剂，其中包括脂质体或纳米颗粒。

2. 发明申请

WO9840049A3 SPECIFIC MAGNETOSOME, METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
标题翻译：特定磁体，其生产和使用方法
公开(公告)号：WO9840049A3
公开(公告)日：1999-01-07
申请号：PCT/DE9800668
申请日：1998-03-06
申请人： MAX DELBRUECK CENTRUM , MAX PLANCK GESELLSCHAFT , BAEUERLEIN EDMUND , SCHUELER DIRK , RESZKA REGINA , PAEUSER SABINE
发明人： BAEUERLEIN EDMUND , SCHUELER DIRK , RESZKA REGINA , PAEUSER SABINE
IPC分类号： C12P3/00 , A61K9/127 , A61K33/26 , A61K39/395 , A61K41/00 , A61K47/48 , A61K48/00 , A61K49/00 , A61K49/18 , A61N2/06 , A61P3/00 , A61P29/00 , A61P35/00 , C01G49/08 , C12N1/20 , C12N15/88 , A61K9/00
CPC分类号： A61K49/1812 , A61K33/26 , A61K41/0004 , A61K41/0052 , A61K48/00 , A61N2/06 , C12N15/88
摘要： The invention relates to specific magnetosomes consisting of a magnetic iron oxide magnetite Fe3O4 monocrystal with a diameter ≤45 nm and a phospholipid membrane surrounding said crystal, in addition to magnetoliposomes which can be obtained from said magnetosomes by liposomal encapsulation. The invention further relates to a method for the production and use thereof as NMR contrast agents, in purging (removal of pathogenic cells), as diagnostic agents for tumoral diseases or in lymphography, for inflammatory processes, for multiple sclerosis, Alzheimer disease, Parkinson's disease and as therapeutic agents.
摘要翻译：本发明涉及由直径<= 45nm的磁性氧化铁磁铁矿Fe3O4单晶和围绕所述晶体的磷脂膜组成的特定磁小体，以及通过脂质体封装可从所述磁小体获得的磁性脂质体。本发明还涉及一种用于生产和使用其作为NMR造影剂的方法，用于清除（除去致病细胞），作为肿瘤疾病或淋巴造影的诊断剂，用于炎症过程，多发性硬化，阿尔茨海默病，帕金森病并作为治疗剂。

3. 发明申请

WO9924602A3 PROCESS FOR DETERMINING CELL VITALITY AND EFFICIENCY IN PARALLEL 审中-公开
标题翻译：方法细胞活力和转基因效率的平行测定
公开(公告)号：WO9924602A3
公开(公告)日：1999-07-15
申请号：PCT/DE9803245
申请日：1998-11-06
申请人： MAX DELBRUECK CENTRUM , GROTH DETLEF , RESZKA REGINA
发明人： GROTH DETLEF , RESZKA REGINA
IPC分类号： C12Q1/02 , C12Q1/42 , G01N33/50 , C12Q1/54
CPC分类号： C12Q1/02 , G01N33/5005
摘要： A process and dual test system are disclosed for determining cell vitality and efficiency in parallel by using a reporter gene after a gene transfer into eukaryotic cells in the same culture vessel. A modified acid phosphatase assay is combined with a report gene assay (beta-galactosidase assay) for simultaneously determining cell vitality and reporter gene expression.
摘要翻译：本发明涉及一种用于平行测定细胞活力，并使用基因转移到真核细胞在相同的培养容器后的报道基因的效率，以及一个双分析系统的方法。对于报告基因的细胞活力和表达同时测定，经修饰的酸性磷酸酶测定法与报告基因测定（β-半乳糖苷酶测定法）相结合。

4. 发明申请

WO9855103A9 ANTI-TUMORAL THERAPY AGENT 审中-公开
标题翻译：手段抗肿瘤治疗
公开(公告)号：WO9855103A9
公开(公告)日：1999-04-08
申请号：PCT/DE9801514
申请日：1998-06-04
申请人： MAX DELBRUECK CENTRUM , RESZKA REGINA , BERGER GERD , POHLEN UWE , JUNG MARION
发明人： RESZKA REGINA , BERGER GERD , POHLEN UWE , JUNG MARION
IPC分类号： A61K9/10 , A61K9/127 , A61K31/28 , A61K31/505 , A61K45/00 , A61K47/34 , A61K47/42 , A61K47/46 , A61K47/48 , A61K49/04 , A61P35/00 , A61K49/00
CPC分类号： A61K9/1271 , A61K9/10 , A61K47/6913 , A61K47/6927 , Y10S977/808 , Y10S977/907 , Y10S977/911 , Y10S977/912 , Y10S977/927
摘要： The invention relates to a new anti-tumoral therapy agent based on liposome-encapsulated cytostatic agents and/or the metabolites thereof. The invention can be used in the pharmaceutical industry and in medicine. The aim of the invention is to build up drug targeting to combat cancer through suitable carrier systems. The invention is characterized by the fact that it clearly increases the concentration of cytostatic agents and residence time in tumors. At the same time, toxic side-effects on the remaining organs are reduced. The inventive agent contains PEG, immuno or immuno/PEG liposome-encapsulated cytostatic agents and/or the metabolites thereof, degradable starch particles and/or gelatin and/or nanoparticles, contrast agents containing iodine, gadolinium or magnetite. A preferred agent is characterized by the cytostatic agent Carboplatinum, encapsulated in SUV-PEG, starch particle Spherex or Gelfoam and the contrast agent Gadolinium-DTPA.
摘要翻译：本发明涉及一种用于脂质体包囊的细胞生长抑制剂和/或它们的代谢物的基础上，抗肿瘤治疗的新的试剂。本发明的应用领域是医药工业和医药。本发明具有构建药物靶向通过合适的载体系统，以打击癌症的目的。本发明具有的目的是增加显著细胞抑制剂在肿瘤的富集并且停留时间在肿瘤。在对其他器官一样毒副作用降低。本发明的组合物包括PEG，免疫或免疫脂质体的PEG包封细胞抑制剂和/或它们的代谢物，可降解的淀粉颗粒和/或明胶和/或纳米颗粒，碘，钆或磁铁矿造影剂。一种优选的方法是通过抑制细胞生长卡铂，封装在SUV-PEG SPHEREX或明胶海绵淀粉颗粒和造影剂钆DTPA标记。

5. 发明申请

WO0200991A9 METHOD FOR IMPROVING TRANSFECTION EFFICIENCY 审中-公开
标题翻译：提高转染效率的方法
公开(公告)号：WO0200991A9
公开(公告)日：2002-05-23
申请号：PCT/DE0102336
申请日：2001-06-28
申请人： MAX DELBRUECK CENTRUM , CARTIER REGIS , BOETTGER MICHAEL , HABERLAND ANNEKATHRIN , RESZKA REGINA
发明人： CARTIER REGIS , BOETTGER MICHAEL , HABERLAND ANNEKATHRIN , RESZKA REGINA
IPC分类号： C12N15/09 , C07K14/00 , C07K19/00 , C12N15/88 , C12N15/67
CPC分类号： C12N15/88 , C07K14/001 , C07K19/00 , C07K2319/00
摘要： The invention relates to a method for improving transfection efficiency by using K16 peptides. The invention further relates to novel K16 peptides, especially to the K16-CYC having the peptide sequence: K16-CYC (1), and to K16mVprN having the peptide sequence KKKKKKKKKKKKKKKGGGCNEWTLELLEELKNEAVRHF.
摘要翻译：本发明涉及使用K16肽改善转染效率的方法。此外，本发明涉及新的K16肽。特别地，具有该肽序列的K16-CYC：K16-CYC（1）和与K16mVprN肽序列KKKKKKKKKKKKKKKGGGCNEWTLELLEELKNEAVRHF。

6. 发明申请

WO0110411A3 IMPLANTABLE ACTIVE INGREDIENT DEPOT 审中-公开
标题翻译：可植入活性物质
公开(公告)号：WO0110411A3
公开(公告)日：2001-06-21
申请号：PCT/DE0002615
申请日：2000-08-04
申请人： MAX DELBRUECK CENTRUM , RESZKA REGINA , SCHLUETER ROLAND
发明人： RESZKA REGINA , SCHLUETER ROLAND
IPC分类号： A61K9/00 , A61K9/127 , A61K9/22 , A61K31/132 , A61K31/337 , A61K31/437 , A61K31/485 , A61K31/704 , A61K31/7072 , A61K31/7105 , A61K31/711 , A61K33/24 , A61K38/00 , A61K45/00 , A61K47/24 , A61K47/34 , A61K48/00 , A61P9/10 , A61P25/04 , A61P25/16 , A61P25/28 , A61P29/00 , A61P35/00
CPC分类号： A61K9/1274 , A61K9/0024 , A61K9/0085
摘要： This invention relates to an implantable active ingredient depot for therapeutically active substances. The fields of application are in medicine and the pharmaceutical industry. The aim of the invention is the application of gel-like cubic mesophases of the monooleine-water system as an implantable active ingredient depot for the treatment of tumors during oncological therapy and in gene therapy. A rational membrane design has been developed to control the release of the active ingredient over time and to control the amount released. The implantable active ingredient according to the invention consists of a lipid matrix which is capable of forming cubic phases in which modifier-molecules have been integrated and contains pharmaceutically active substances. Monooleine is the preferred lipid matrix.
摘要翻译：本发明涉及用于治疗活性物质的可植入药物贮存库。应用领域是医药和制药工业。本发明的目的是使用单油酸甘油酯水系统的凝胶状立方中间相作为用于治疗癌症治疗和基因治疗中的肿瘤的可植入药物贮存库。开发合理的膜设计以控制活性成分在时间和数量方面的释放。根据本发明的可植入药物贮存库由脂质基质组成，所述脂质基质能够形成其中掺入了改性剂分子并且含有药物活性物质的立方相。优选的脂质基质是单油酸甘油酯。

7. 发明申请

WO9930741A3 AGENT FOR GENE THERAPY OF TUMOR, NEURODEGENERATIVE, CARDIOVASCULAR AND AUTOIMMUNE DISEASES 审中-公开
标题翻译：手段肿瘤疾病基因疗法，神经变性，心血管疾病和自身免疫性
公开(公告)号：WO9930741A3
公开(公告)日：1999-08-19
申请号：PCT/DE9803763
申请日：1998-12-14
申请人： MAX DELBRUECK CENTRUM , RESZKA REGINA , BERNDT ANTJE
发明人： RESZKA REGINA , BERNDT ANTJE
IPC分类号： A61K47/48 , A61K48/00 , A61P9/00 , A61P25/00 , A61P35/00 , A61P37/02
CPC分类号： A61K48/00
摘要： Disclosed is an agent for gene therapy of tumor, neurodegenerative, cardiovascular and autoimmune diseases, which can be used both in the medical field and in the pharmaceutical industry. The aim of the invention is to provide a totally new starting point for loco-regional therapy of tumors, more particularly liver metastasis, by combined application of liposomes/plasmid DNA complexes having different composition, quantities and concentrations. The essential point of the invention is a pharmaceutical agent comprising the following: one or more genetic materials which are nonencapsulated or encapsulated in PEG, immuno, immuno/PEG, cationic, optionally polymer-modified liposomes; lyophilized or degradable starch particles and/or gelatin and/or polymer particles, i.e. nanoparticles, and a contrast agent containing iodine, gadolinium, magnetite or fluorine.
摘要翻译：本发明涉及用于肿瘤疾病，神经变性疾病，心血管疾病和自身免疫疾病的基因治疗剂。本发明的医药和医药行业的应用领域。本发明的目的是基于对肿瘤的局部区域治疗完全新的方法，特别是肝脏转移，通过组合使用不同的组成，大小和装载的脂质体/质粒DNA复合物被递送。本发明的核心是一种药物组合物：一种或多种非包封或PEG，免疫，免疫/ PEG，阳离子型，如果需要的话，聚合物改性，脂质体包封的遗传物质; 冻干或可分解淀粉颗粒和/或明胶和/或聚合物颗粒，如例如纳米颗粒和碘，钆，磁铁矿的或含氟的造影剂。

8. 发明申请

WO9805678A3 NOVEL CATIONIC AMPHIPHILIC LIPIDS FOR LIPOSOMAL GENE TRANSFER 审中-公开
标题翻译：用于脂质体基因转移的新型阳离子脂质体
公开(公告)号：WO9805678A3
公开(公告)日：1999-02-25
申请号：PCT/DE9701669
申请日：1997-08-01
申请人： MAX DELBRUECK CENTRUM , SCHNEIDER MANFRED , KEIL OLIVER , RESZKA REGINA , GROTH DETLEF
发明人： SCHNEIDER MANFRED , KEIL OLIVER , RESZKA REGINA , GROTH DETLEF
IPC分类号： C12N15/09 , A61K9/127 , A61K31/575 , A61K48/00 , C07C237/08 , C07C237/12 , C07C271/20 , C07C279/14 , C07J41/00 , C12N15/88 , A61K31/155 , A61K31/16 , A61K31/325 , C12N15/63
CPC分类号： A61K48/00 , A61K9/1272 , C07C237/12 , C07C271/20 , C07C279/14 , C07J41/0055 , C07J41/0072 , C12N15/88
摘要： The synthesis of novel cationic, amphiphilic lipids is disclosed, as well as their use as gene transfer vesicles in vitro and in vivo. A series of different lipids (diglycerides, steroids) was synthesised by modification with variable cationic molecules (amino acids, biogenic amines). Because of their ability to form complexes with polynucleotides (DNA, RNA, antisense oligonucleotides, ribozymes, etc.), compounds of this type are useful as vectors for gene transfer (transfection).

9. 发明申请

WO9620208A3 NEW CHOLESTEROL DERIVATIVE FOR LIPOSOMAL GENE TRANSFER 审中-公开
标题翻译：新型胆固醇衍生物用于脂质体基因转移
公开(公告)号：WO9620208A3
公开(公告)日：1996-09-06
申请号：PCT/DE9501879
申请日：1995-12-28
申请人： MAX DELBRUECK CENTRUM , RESZKA REGINA
发明人： RESZKA REGINA
IPC分类号： A61K9/127 , A61K47/48 , C07J41/00 , A61K48/00
CPC分类号： C07J41/0055 , A61K9/1272
摘要： The invention pertains to a new cholesterol derivative for liposomal gene transfer, applicable in the fields of medicine and genetic engineering. The new cholesterol derivative 3β N-(N,N'-dimethylaminoethane)-carbamoyl cholesterol (DAC-chol) is produced by reacting N,N'-dimethylethylenediamine and chloroformyl cholesterol in equimolar amounts and is purified by chromatography. DAC-chol is nontoxic and can be used advantageously for direct liposomal gene transfer. The invention also pertains to new methods of direct liposomal gene transfer in vivo, characterized in that liposome-DNA complexes can be applied repeatedly using automatic or reprimable pump systems either continuously or with purposeful time intervals.

10. 发明专利

DE10004860A1 Pressurized air inhaler for administering drug-containing liposomal powder aerosol for treatment of respiratory disease, has nebulization chamber for drying aqueous liposome suspension 未知
公开(公告)号：DE10004860A1
公开(公告)日：2000-10-05
申请号：DE10004860
申请日：2000-02-03
申请人： MAX DELBRUECK CENTRUM , FRAUNHOFER GES FORSCHUNG
发明人： DIEDERICHS JULIA EVA , KOCH WOLFGANG , LOEDDING HUBERT , RESZKA REGINA , WINDT HORST
IPC分类号： A61K9/12 , A61K9/00 , A61K9/127 , A61K9/16 , A61K9/51 , A61K9/72 , A61K47/24 , A61K47/28 , A61K47/32 , A61K47/34 , A61K47/36 , A61K47/42 , A61L9/12 , A61M11/02 , A61M11/06 , A61M15/00 , A61P11/00 , B05B7/00 , B05B7/06
摘要： A pressurized air inhaler for pulmonary administration of a liposomal powder aerosol comprises: (i) a container for aqueous liposome suspension, linked via a liquid dosing device with an atomizing nozzle and with a drying unit (e.g. nebulization chamber) for spray drying the liposomes; (ii) a mouthpiece outlet; and (iii) separate lines for supplying pressurized air and liposome dispersion to the atomizing nozzle. Independent claims are included for the following: (a) a powder aerosol consisting of liposomes and/or nanoparticles, which is free of moisture and cryoprotective agents and comprises spherical, amorphous or crystalline particles of size 0.5-10 mu m or is prepared by pressurized air nebulization of liposomes and/or a nanoparticle dispersion via a 2-component nozzle at a nebulization pressure of 1-5 bars and a dispersion concentration of 0.2-1%; (b) liposomal powder aerosols comprising: (1) phospholipids, cholesterol, natural or artificial pulmonary surfactant or cationic amphiphiles and active agent; (2) large multilamellar vesicles (MLV) or small unilamellar vesicles (SUV) as liposomes; (3) hydrogenated soya phosphatidyl choline and cholesterol in molar ratio 1 : 0.25, plus SUV's prepared by ultrasonication or MLV's prepared by homogenization; (4) hydrogenated soya phosphatidyl choline, cholesterol and polyethylene glycol in molar ratio 1 : 1 : 0.1, plus SUV's prepared by ultrasonication or MLV's prepared by shaking a lipid film; (5) phosphatidyl choline and cholesterol in molar ratio 1 : 0.5 charged with 5,6-carboxyfluorescein, plus SUV's prepared by ultrasonication; or (6) DAC-Chol and DOPE in weight ratio 2 : 3 (optionally complexed with protamine sulfate or poly-L-lysine); and (c) nanoparticulate powder aerosols, consisting exclusively of active agent crystals of polymer particles charged with active agent.

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