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1. 发明申请

US20080112917A1 Sphingolipids' Polyalkylamines Conjugates 失效
标题翻译：鞘脂多烷基胺缀合物
公开(公告)号：US20080112917A1
公开(公告)日：2008-05-15
申请号：US10561394
申请日：2004-06-17
申请人： Yechezkel Barenholz , Dmitri Simberg , Elimelech Rochlin
发明人： Yechezkel Barenholz , Dmitri Simberg , Elimelech Rochlin
IPC分类号： A61K31/787 , C07F9/02 , A61K31/685
CPC分类号： A61K31/132 , A61K9/1272 , A61K38/47 , A61K39/39 , A61K48/0041 , A61K2039/543 , A61K2039/55555 , A61K2039/55561 , C07C271/20 , C12N15/88 , A61K2300/00
摘要： The present invention concerns novel sphingolipid-polyalkylamines conjugates, a process for their preparation and pharmaceutical compositions comprising the same.In particular, the present invention concerns ceramide based polyalkylamine conjugates and its use as a capturing agent. A preferred ceramide polyalkylamine conjugate is a ceramide-spermine conjugate, more preferably, N-palmitoyl D-erythro sphingosyl-1-carbamoyl spermine.
摘要翻译：本发明涉及新型鞘脂 - 多烷基胺缀合物，其制备方法和包含其的药物组合物。特别地，本发明涉及神经酰胺基聚烷基胺共轭物及其作为捕获剂的用途。优选的神经酰胺多烷基胺缀合物是神经酰胺精胺缀合物，更优选N-棕榈酰基D-赤藓糖鞘糖醇-1-氨基甲酰基精胺。

2. 发明授权

US07771711B2 Sphingolipids' polyalkylamines conjugates 失效
标题翻译：鞘脂的聚烷基胺共轭物
公开(公告)号：US07771711B2
公开(公告)日：2010-08-10
申请号：US10561394
申请日：2004-06-17
申请人： Yechezkel Barenholz , Dmitri Simberg , Elimelech Rochlin
发明人： Yechezkel Barenholz , Dmitri Simberg , Elimelech Rochlin
IPC分类号： A61K31/74
CPC分类号： A61K31/132 , A61K9/1272 , A61K38/47 , A61K39/39 , A61K48/0041 , A61K2039/543 , A61K2039/55555 , A61K2039/55561 , C07C271/20 , C12N15/88 , A61K2300/00
摘要： The present invention concerns novel sphingolipid-polyalkylamines conjugates, a process for their preparation and pharmaceutical compositions comprising the same. In particular, the present invention concerns ceramide based polyalkylamine conjugates and its use as a capturing agent. A preferred ceramide polyalkylamine conjugate is a ceramide-spermine conjugate, more preferably, N-palmitoyl D-erythro sphingosyl-1-carbamoyl spermine.
摘要翻译：本发明涉及新型鞘脂 - 多烷基胺缀合物，其制备方法和包含其的药物组合物。特别地，本发明涉及神经酰胺基聚烷基胺共轭物及其作为捕获剂的用途。优选的神经酰胺多烷基胺缀合物是神经酰胺精胺缀合物，更优选N-棕榈酰基D-赤藓糖鞘糖醇-1-氨基甲酰基精胺。

3. 发明授权

US08242089B2 Sphingolipids polyalkylamine conjugates for use in transfection 失效
标题翻译：用于转染的鞘脂聚烷基胺共轭物
公开(公告)号：US08242089B2
公开(公告)日：2012-08-14
申请号：US10560932
申请日：2004-06-17
申请人： Yechezkel Barenholz , Dmitri Simberg
发明人： Yechezkel Barenholz , Dmitri Simberg
IPC分类号： A61K48/00 , A61K9/127 , C12N15/00 , C12N15/88
CPC分类号： A61K31/132 , A61K9/1272 , A61K38/47 , A61K39/39 , A61K48/0041 , A61K2039/543 , A61K2039/55555 , A61K2039/55561 , C07C271/20 , C12N15/88 , A61K2300/00
摘要： The present invention concerns the use of a sphingoid-polyalkylamine conjugate comprising a sphingoid backbone carrying, via a carbamoyl bond, at least one polyalkylamine chains as a capturing agent of nucleic acid molecules. The present invention also provides the use of the sphingoid polyalkylamine conjugate for the preparation of a pharmaceutical composition for the delivery of a nucleic acid molecule into a target cell. In a further aspect the invention provides a method for transfecting a nucleic acid into a target cell, the method comprises contacting said target cell with the sphingoid-polyalkylamine conjugate associated with a nucleic acid molecule, thereby transfecting said target cell with said nucleic acid molecule. Other aspects of the invention concern pharmaceutical compositions comprising said conjugate, therapeutic methods as well as kits, making use of the said conjugate. A preferred conjugate according to the invention is N-palmitoyl D-erythrosphingosyl-1-carbamoyl spermine.
摘要翻译：本发明涉及包含通过氨基甲酰键携带至少一个聚烷基胺链作为核酸分子的捕获剂的鞘氨醇主链的鞘氨醇 - 多烷基胺缀合物的用途。本发明还提供了鞘氨醇多烷基胺缀合物用于制备用于将核酸分子递送至靶细胞的药物组合物的用途。在另一方面，本发明提供了将核酸转染到靶细胞中的方法，所述方法包括使所述靶细胞与与核酸分子相关联的类鞘氨醇 - 多烷基胺缀合物接触，由此用所述核酸分子转染所述靶细胞。本发明的其它方面涉及包含所述缀合物的药物组合物，治疗方法以及使用所述缀合物的试剂盒。根据本发明的优选的缀合物是N-棕榈酰基D-赤藻酰基-1-氨基甲酰基精胺。

4. 发明申请

US20060252718A1 Sphingolipids polyalkylamine conjugates for use in transfection 失效
标题翻译：用于转染的鞘脂聚烷基胺共轭物
公开(公告)号：US20060252718A1
公开(公告)日：2006-11-09
申请号：US10560932
申请日：2004-06-17
申请人： Yechezkel Barenholz , Dmitri Simberg
发明人： Yechezkel Barenholz , Dmitri Simberg
IPC分类号： A61K48/00 , A61K9/127 , C12N15/88
CPC分类号： A61K31/132 , A61K9/1272 , A61K38/47 , A61K39/39 , A61K48/0041 , A61K2039/543 , A61K2039/55555 , A61K2039/55561 , C07C271/20 , C12N15/88 , A61K2300/00
摘要： The present invention concerns the use of a sphingoid-polyalkylamine conjugate comprising a sphingoid backbone carrying, via a carbamoyl bond, at least one polyalkylamine chains as a capturing agent of nucleic acid molecules. The present invention also provides the use of the sphingoid polyalkylamine conjugate for the preparation of a pharmaceutical composition for the delivery of a nucleic acid molecule into a target cell. In a further aspect the invention provides a method for transfecting a nucleic acid into a target cell, the method comprises contacting said target cell with the sphingoid-polyalkylamine conjugate associated with a nucleic acid molecule, thereby transfecting said target cell with said nucleic acid molecule. Other aspects of the invention concern pharmaceutical compositions comprising said conjugate, therapeutic methods as well as kits, making use of the said conjugate. A preferred conjugate according to the invention is N-palmitoyl D-erythrosphingosyl-1-carbamoyl spermine.
摘要翻译：本发明涉及包含通过氨基甲酰键携带至少一个聚烷基胺链作为核酸分子的捕获剂的鞘氨醇主链的鞘氨醇 - 多烷基胺缀合物的用途。本发明还提供了鞘氨醇多烷基胺缀合物用于制备用于将核酸分子递送至靶细胞的药物组合物的用途。在另一方面，本发明提供了将核酸转染到靶细胞中的方法，所述方法包括使所述靶细胞与与核酸分子相关联的类鞘氨醇 - 多烷基胺缀合物接触，由此用所述核酸分子转染所述靶细胞。本发明的其它方面涉及包含所述缀合物的药物组合物，治疗方法以及使用所述缀合物的试剂盒。根据本发明的优选的缀合物是N-棕榈酰基D-赤藻酰基-1-氨基甲酰基精胺。

5. 发明申请

US20080305101A1 Methods and Compositions Related to Clot Binding Compounds 有权
标题翻译：与凝胶结合化合物相关的方法和组合物
公开(公告)号：US20080305101A1
公开(公告)日：2008-12-11
申请号：US11967509
申请日：2007-12-31
申请人： Erkki Ruoslahti , Dmitri Simberg
发明人： Erkki Ruoslahti , Dmitri Simberg
IPC分类号： A61K39/395 , C07K5/09 , C07K17/00 , C07K16/46 , C07K19/00 , C07K14/76 , A61K38/02 , C01G49/02 , B32B9/00 , C07D305/08 , C07F13/00 , C07H21/00 , A61K38/06
CPC分类号： A61K47/48861 , A61K47/48238 , A61K47/48815 , A61K47/48884 , A61K47/62 , A61K47/6911 , A61K47/6923 , A61K47/6929 , A61K49/1863 , A61K49/1866 , B82Y5/00 , Y10T428/2984
摘要： Disclosed are compositions and methods related to clot binding compounds. The disclosed targeting is useful for treatment of cancer and other diseases and disorders.
摘要翻译：公开了与凝块结合化合物相关的组合物和方法。所公开的靶向对于治疗癌症和其它疾病和病症是有用的。

6. 发明申请

US20140046181A1 ACOUSTICALLY RESPONSIVE PARTICLES WITH DECREASED CAVITATION THRESHOLD 审中-公开
标题翻译：具有降低裂隙阈值的有声响应的颗粒
公开(公告)号：US20140046181A1
公开(公告)日：2014-02-13
申请号：US13978140
申请日：2012-01-05
申请人： Michael Benchimol , Sadik C. Esener , Dmitri Simberg , Stuart Ibsen
发明人： Michael Benchimol , Sadik C. Esener , Dmitri Simberg , Stuart Ibsen
IPC分类号： A61K41/00 , A61M5/00 , A61M37/00
CPC分类号： A61K41/0047 , A61K9/0009 , A61K9/1273 , A61K41/0028 , A61M5/007 , A61M37/0092
摘要： Techniques, systems, devices and materials are disclosed for implementing and fabricating drug delivery and imaging vehicles, which are activated in the body at a tissue of interest by focused ultrasound. In one aspect, a drug delivery vehicle can include a carrier having an outer membrane that envelopes an acoustic sensitizer particle and a payload substance to be delivered to the target tissue. The outer membrane can protect the acoustic sensitizer particle and the payload substance from degradation and opsonization. The outer membrane can be functionalized with a tumor targeting ligand to cause the drug delivery vehicle to selectively accumulate in a tumor region over other tissues, as well as with an agent to increase circulation time by reducing uptake from undesired body tissues, organs, and systems.
摘要翻译：公开了用于实施和制造药物递送和成像载体的技术，系统，装置和材料，其通过聚焦超声在感兴趣的组织在体内被激活。在一个方面，药物递送载体可以包括具有外膜的载体，其包围声敏剂颗粒和有效载体物质被输送到目标组织。外膜可以保护声学敏化剂颗粒和有效载荷物质免于降解和调理。外膜可以用肿瘤靶向配体进行功能化，以使药物递送媒介物在其他组织上选择性地积聚在肿瘤区域中，以及通过减少来自不期望的身体组织，器官和系统的摄取而增加循环时间的试剂。

7. 发明授权

US09101671B2 Methods and compositions related to clot binding compounds 有权
标题翻译：与凝块结合化合物相关的方法和组合物
公开(公告)号：US09101671B2
公开(公告)日：2015-08-11
申请号：US11967509
申请日：2007-12-31
申请人： Erkki Ruoslahti , Dmitri Simberg
发明人： Erkki Ruoslahti , Dmitri Simberg
IPC分类号： A61K39/00 , A61K47/48 , A61K49/18 , B82Y5/00
CPC分类号： A61K47/48861 , A61K47/48238 , A61K47/48815 , A61K47/48884 , A61K47/62 , A61K47/6911 , A61K47/6923 , A61K47/6929 , A61K49/1863 , A61K49/1866 , B82Y5/00 , Y10T428/2984
摘要： Disclosed are compositions and methods related to clot binding compounds. For example, disclosed are conjugates comprising a surface molecule and a plurality of clot binding compounds. The clot binding compounds can selectively bind to clotted plasma protein. The conjugate can, for example, cause clotting and amplify the accumulation of the conjugate in tumors. In one example, the conjugate can comprise a sufficient number and composition of clot binding compounds such that the conjugate causes clotting and amplifies the accumulation of the conjugate in tumors. The disclosed targeting is useful for treatment of cancer and other diseases and disorders.
摘要翻译：公开了与凝块结合化合物相关的组合物和方法。例如，公开了包含表面分子和多个凝块结合化合物的缀合物。凝块结合化合物可以选择性地结合凝血的血浆蛋白。结合物可以例如引起凝血并且扩增缀合物在肿瘤中的积累。在一个实例中，缀合物可以包含足够数量和组合物的凝块结合化合物，使得缀合物引起凝血并扩增缀合物在肿瘤中的积累。所公开的靶向对于治疗癌症和其它疾病和病症是有用的。

8. 发明申请

US20130202625A1 USE OF HUMAN ERYTHROCYTES FOR PREVENTION AND TREATMENT OF CANCER DISSEMINATION AND GROWTH 审中-公开
标题翻译：用于预防和治疗癌症发病和生长的人类红细胞生成
公开(公告)号：US20130202625A1
公开(公告)日：2013-08-08
申请号：US13522909
申请日：2011-01-20
申请人： Dmitri Simberg , Guixin Shi
发明人： Dmitri Simberg , Guixin Shi
IPC分类号： A61K35/18
CPC分类号： A61K35/18 , A61K39/44 , C07K16/30
摘要： The technology relates in part to methods of preventing and treating diseases and conditions associated with cancer, including methods, compositions, and kits used for preventing and treating cancer dissemination and growth.
摘要翻译：该技术部分涉及预防和治疗与癌症相关的疾病和病症的方法，包括用于预防和治疗癌症传播和生长的方法，组合物和试剂盒。

9. 发明授权

US09730637B2 Layered particles for retrieving DNA released from cells from a gastrointestinal tract sample and methods for making and using them 有权
公开(公告)号：US09730637B2
公开(公告)日：2017-08-15
申请号：US14238189
申请日：2012-08-17
申请人： Dmitri Simberg , Yu-Tsueng Liu
发明人： Dmitri Simberg , Yu-Tsueng Liu
IPC分类号： G01N21/75 , B01D35/00 , C12M1/00 , A61B5/00 , C12Q1/68 , A61B5/145 , A61B5/1473 , A61B10/00
CPC分类号： A61B5/6861 , A61B5/14546 , A61B5/1473 , A61B5/4848 , A61B10/0045 , A61B2010/0061 , C12Q1/6806 , C12Q2563/143 , C12Q2563/155
摘要： In alternative embodiments, the invention provides compositions such as devices, pills, beads, capsules, products of manufacture, particles, microparticles, nanoparticles, gels, liquid gels, liquid gel capsules, capsules, tablets, geltabs, liquids, sprays, emulsions, suspensions, pastes or yogurts, for the detection and isolation of biomarkers, nucleic acids, proteins or peptides, proteoglycans, lipids, fats, sugars or polysaccharides in the gastrointestinal tract for e.g., detecting the presence of particular exogenous or endogenous nucleic acids, e.g., DNA or RNA, or proteins, in the gastrointestinal tract, for example, to diagnose the presence of an infectious or exogenous agent such as a virus, a fungus, a parasite, a bacteria, intestinal helminths and protozoan parasites, and the like, or a biomarker such as a cancer-causing or cancer-predisposing allele, e.g., mutations of the KRAS2 oncogene in pancreatic cancer. In alternative embodiments, compositions of the invention comprise magnetic particles such as a magnetically-responsive microparticle or nanoparticle; a superparamagnetic bead or polystyrene bead; a superparamagnetic fine particle; a ferrimagnetic particle; or, a magnetic microsphere, nanosphere, microbead or nanobeads. In alternative embodiments, the invention provides methods for detecting, retrieving, capturing or isolating a sample of a nucleic acid, or an anionic, cationic or hydrophobic protein or peptide, a mucin, a phosphoprotein, a proteoglycan or a polysaccharide, in vivo.

10. 发明申请

US20140288398A1 COMPOSITIONS AND DEVICES FOR THE DETECTION OF BIOMARKERS IN THE GASTROINTESTINAL TRACT AND METHODS FOR MAKING AND USING THEM 有权
标题翻译：用于检测气体诱导物中生物标志物的组合物和装置及其制备和使用它们的方法
公开(公告)号：US20140288398A1
公开(公告)日：2014-09-25
申请号：US14238189
申请日：2012-08-17
申请人： Dmitri Simberg , Yu-Tsueng Liu
发明人： Dmitri Simberg , Yu-Tsueng Liu
IPC分类号： A61B5/00 , A61B5/1473 , A61B5/145 , A61B10/00
CPC分类号： A61B5/6861 , A61B5/14546 , A61B5/1473 , A61B5/4848 , A61B10/0045 , A61B2010/0061 , C12Q1/6806 , C12Q2563/143 , C12Q2563/155
摘要： In alternative embodiments, the invention provides compositions such as devices, pills, beads, capsules, products of manufacture, particles, microparticles, nanoparticles, gels, liquid gels, liquid gel capsules, capsules, tablets, geltabs, liquids, sprays, emulsions, suspensions, pastes or yogurts, for the detection and isolation of biomarkers, nucleic acids, proteins or peptides, proteoglycans, lipids, fats, sugars or polysaccharides in the gastrointestinal tract for e.g., detecting the presence of particular exogenous or endogenous nucleic acids, e.g., DNA or RNA, or proteins, in the gastrointestinal tract, for example, to diagnose the presence of an infectious or exogenous agent such as a virus, a fungus, a parasite, a bacteria, intestinal helminths and protozoan parasites, and the like, or a biomarker such as a cancer-causing or cancer-predisposing allele, e.g., mutations of the KRAS2 oncogene in pancreatic cancer. In alternative embodiments, compositions of the invention comprise magnetic particles such as a magnetically-responsive microparticle or nanoparticle; a superparamagnetic bead or polystyrene bead; a superparamagnetic fine particle; a ferrimagnetic particle; or, a magnetic microsphere, nanosphere, microbead or nanobeads. In alternative embodiments, the invention provides methods for detecting, retrieving, capturing or isolating a sample of a nucleic acid, or an anionic, cationic or hydrophobic protein or peptide, a mucin, a phosphoprotein, a proteoglycan or a polysaccharide, in vivo.
摘要翻译：在替代实施方案中，本发明提供组合物，例如装置，丸剂，珠粒，胶囊，制造产品，颗粒，微粒，纳米颗粒，凝胶，液体凝胶，液体凝胶胶囊，胶囊，片剂，凝胶胶囊，液体，喷雾剂，乳液，悬浮液用于检测和分离胃肠道中的生物标志物，核酸，蛋白质或肽，蛋白聚糖，脂质，脂肪，糖或多糖的例如检测特定的外源或内源核酸的存在，例如DNA 或RNA或蛋白质，例如诊断感染性或外源性药物如病毒，真菌，寄生虫，细菌，肠蠕虫和原生动物寄生虫等的存在，或生物标志物如癌症或癌症易感性等位基因，例如胰腺癌中KRAS2致癌基因的突变。在替代实施方案中，本发明的组合物包含磁性颗粒，例如磁响应微粒或纳米颗粒; 超顺磁珠或聚苯乙烯珠; 超顺磁细粒; 亚铁磁颗粒; 或磁性微球，纳米球，微珠或纳米棒。在替代实施方案中，本发明提供了用于在体内检测，检索，捕获或分离核酸或阴离子，阳离子或疏水蛋白或肽，粘蛋白，磷蛋白，蛋白多糖或多糖的样品的方法。

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