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1. 发明申请

US20110311582A1 NOVEL LIPIDS AND COMPOSITIONS FOR THE DELIVERY OF THERAPEUTICS 有权
标题翻译：用于输送治疗药物的新型脂肪和组合物
公开(公告)号：US20110311582A1
公开(公告)日：2011-12-22
申请号：US13128283
申请日：2009-11-10
申请人： Muthiah Manoharan , Muthusamy Jayaraman , Kallanthottathil G. Rajeev , laxman Eltepu , Steven Ansell , Jianxin Chen
发明人： Muthiah Manoharan , Muthusamy Jayaraman , Kallanthottathil G. Rajeev , laxman Eltepu , Steven Ansell , Jianxin Chen
IPC分类号： A61K39/12 , C07D203/08 , A61K47/44 , A61K31/7088 , A61K31/7105 , A61K31/713 , C12N5/071 , C12N15/85 , A61K39/00 , A61K39/02 , A61P37/04 , A61P31/12 , A61P31/04 , A61P33/00 , A61P35/00 , C07C229/30
CPC分类号： A61K47/44 , A61K9/1272 , A61K31/7088 , A61K31/713 , A61K39/00 , A61K39/39 , A61K47/10 , A61K47/18 , A61K47/20 , A61K47/28 , A61K2039/55555 , A61K2039/55561 , C07C229/08 , C07C229/30 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25 , C07D203/10 , C07D317/28 , C07D317/44 , C07D317/46 , C07D317/72 , C07D319/06 , C07D405/12 , C07D491/056 , C07D491/113 , C12N15/111 , C12N15/113 , C12N2310/14 , C12N2310/3515 , C12N2320/32 , Y02A50/464
摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention formula (I) provides lipids having the following structure XXXIII wherein: R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alky lhetro cycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O).
摘要翻译：本发明提供有利地用于脂质颗粒以用于体内递送治疗剂至细胞的脂质。具体地，本发明式（I）提供具有以下结构XXXIII的脂质，其中：R1和R2各自独立地为任何取代的C 10 -C 30烷基，任选取代的C 10 -C 30烯基，任选取代的C 10 -C 30炔基，任选取代的 C10-C30酰基或 - 连接子 - 配体; R 3是H，任选取代的C 1 -C 10烷基，任选取代的C 2 -C 10烯基，任选取代的C 2 -C 10炔基，烷基杂芳基，烷基磷酸酯，烷基硫代磷酸酯，烷基磷酸二烷基酯，烷基膦酸酯，烷基胺，羟基烷基，ω-氨基烷基，ω-（取代的）氨基烷基，ω-磷酸烷基酯，ω-硫代磷酰基烷基，任选取代的聚乙二醇（PEG，mw 100-40K），任选取代的mPEG（mw 120-40K），杂芳基，杂环或连接体 - 配体; 并且E是C（O）O或OC（O）。

2. 发明授权

US09186325B2 Lipids and compositions for the delivery of therapeutics 有权
标题翻译：用于递送治疗剂的脂质和组合物
公开(公告)号：US09186325B2
公开(公告)日：2015-11-17
申请号：US13128283
申请日：2009-11-10
申请人： Muthiah Manoharan , Muthusamy Jayaraman , Kallanthottathil G. Rajeev , Laxman Eltepu , Steven Ansell , Jianxin Chen
发明人： Muthiah Manoharan , Muthusamy Jayaraman , Kallanthottathil G. Rajeev , Laxman Eltepu , Steven Ansell , Jianxin Chen
IPC分类号： A61K39/12 , A61K9/127 , A61K39/00 , C12N15/11
CPC分类号： A61K47/44 , A61K9/1272 , A61K31/7088 , A61K31/713 , A61K39/00 , A61K39/39 , A61K47/10 , A61K47/18 , A61K47/20 , A61K47/28 , A61K2039/55555 , A61K2039/55561 , C07C229/08 , C07C229/30 , C07C237/16 , C07C251/38 , C07C251/78 , C07C271/12 , C07C271/20 , C07C323/25 , C07D203/10 , C07D317/28 , C07D317/44 , C07D317/46 , C07D317/72 , C07D319/06 , C07D405/12 , C07D491/056 , C07D491/113 , C12N15/111 , C12N15/113 , C12N2310/14 , C12N2310/3515 , C12N2320/32 , Y02A50/464
摘要： The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention formula (I) provides lipids having the following structure XXXIII wherein: R1 and R2 are each independently for each occurrence optionally substituted C10-C30 alkyl, optionally substituted C10-C30 alkenyl, optionally substituted C10-C30 alkynyl, optionally substituted C10-C30 acyl, or -linker-ligand; R3 is H, optionally substituted C1-C10 alkyl, optionally substituted C2-C10 alkenyl, optionally substituted C2-C10 alkynyl, alky lhetro cycle, alkylphosphate, alkylphosphorothioate, alkylphosphorodithioate, alkylphosphonates, alkylamines, hydroxyalkyls, ω-aminoalkyls, ω-(substituted)aminoalkyls, ω-phosphoalkyls, ω-thiophosphoalkyls, optionally substituted polyethylene glycol (PEG, mw 100-40K), optionally substituted mPEG (mw 120-40K), heteroaryl, heterocycle, or linker-ligand; and E is C(O)O or OC(O).
摘要翻译：本发明提供有利地用于脂质颗粒以用于体内递送治疗剂至细胞的脂质。具体地，本发明式（I）提供具有以下结构XXXIII的脂质，其中：R1和R2各自独立地为任何取代的C 10 -C 30烷基，任选取代的C 10 -C 30烯基，任选取代的C 10 -C 30炔基，任选取代的 C10-C30酰基或 - 连接子 - 配体; R 3是H，任选取代的C 1 -C 10烷基，任选取代的C 2 -C 10烯基，任选取代的C 2 -C 10炔基，烷基杂芳基，烷基磷酸酯，烷基硫代磷酸酯，烷基磷酸二烷基酯，烷基膦酸酯，烷基胺，羟基烷基，ω-氨基烷基，ω-（取代的）氨基烷基，ω-磷酸烷基酯，ω-硫代磷酰基烷基，任选取代的聚乙二醇（PEG，mw 100-40K），任选取代的mPEG（mw 120-40K），杂芳基，杂环或连接体 - 配体; 并且E是C（O）O或OC（O）。

3. 发明授权

US08158601B2 Lipid formulation 有权
标题翻译：脂质配方
公开(公告)号：US08158601B2
公开(公告)日：2012-04-17
申请号：US12813448
申请日：2010-06-10
申请人： Jianxin Chen , Steven Ansell , Akin Akinc , Joseph Robert Dorkin , Xiaojun Qin , William Cantley , Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Muthusamy Jayaraman
发明人： Jianxin Chen , Steven Ansell , Akin Akinc , Joseph Robert Dorkin , Xiaojun Qin , William Cantley , Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Muthusamy Jayaraman
IPC分类号： A61K31/70 , A61K47/00 , C07C229/00
CPC分类号： A61K9/1272 , A61K9/1278 , A61K31/22 , A61K31/7088 , A61K31/712 , A61K31/713 , A61K38/1709 , A61K38/4846 , A61K47/14 , A61K47/549 , A61K47/551 , A61K47/6911 , A61K48/0033 , C07C29/58 , C07C227/18 , C07C227/40 , C07C229/12 , C07D475/04 , C12N15/113 , C12N15/1137 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/341 , C12N2310/346 , C12N2310/351 , C12N2310/3515 , C12N2320/32 , Y02A50/463 , A61K2300/00 , C12N2310/3521 , C12N2310/3533
摘要： The invention features a cationic lipid of formula I, an improved lipid formulation comprising a cationic lipid of formula I and corresponding methods of use. Also disclosed are targeting lipids, and specific lipid formulations comprising such targeting lipids.
摘要翻译：本发明的特征在于式I的阳离子脂质，包含式I的阳离子脂质和相应的使用方法的改进的脂质制剂。还公开了靶向脂质和包含这种靶向脂质的特定脂质制剂。

4. 发明申请

US20100324120A1 LIPID FORMULATION 有权
标题翻译：脂质配方
公开(公告)号：US20100324120A1
公开(公告)日：2010-12-23
申请号：US12813448
申请日：2010-06-10
申请人： Jianxin Chen , Steven Ansell , Akin Akinc , Joseph Robert Dorkin , Xiaojun Qin , William Cantley , Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Muthusamy Jayaraman
发明人： Jianxin Chen , Steven Ansell , Akin Akinc , Joseph Robert Dorkin , Xiaojun Qin , William Cantley , Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Muthusamy Jayaraman
IPC分类号： A61K31/711 , C07C229/30 , A61K47/16 , A61K31/713 , A61K47/26 , C12N5/00 , A61P43/00
CPC分类号： A61K9/1272 , A61K9/1278 , A61K31/22 , A61K31/7088 , A61K31/712 , A61K31/713 , A61K38/1709 , A61K38/4846 , A61K47/14 , A61K47/549 , A61K47/551 , A61K47/6911 , A61K48/0033 , C07C29/58 , C07C227/18 , C07C227/40 , C07C229/12 , C07D475/04 , C12N15/113 , C12N15/1137 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/341 , C12N2310/346 , C12N2310/351 , C12N2310/3515 , C12N2320/32 , Y02A50/463 , A61K2300/00 , C12N2310/3521 , C12N2310/3533
摘要： The invention features a cationic lipid of formula I, an improved lipid formulation comprising a cationic lipid of formula I and corresponding methods of use. Also disclosed are targeting lipids, and specific lipid formulations comprising such targeting lipids.
摘要翻译：本发明的特征在于式I的阳离子脂质，包含式I的阳离子脂质和相应的使用方法的改进的脂质制剂。还公开了靶向脂质和包含这种靶向脂质的特定脂质制剂。

5. 发明授权

US08802644B2 Lipid formulation 有权
标题翻译：脂质配方
公开(公告)号：US08802644B2
公开(公告)日：2014-08-12
申请号：US13357856
申请日：2012-01-25
申请人： Jianxin Chen , Steven Ansell , Akin Akinc , Joseph Robert Dorkin , Xiaojun Qin , William Cantley , Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Muthusamy Jayaraman
发明人： Jianxin Chen , Steven Ansell , Akin Akinc , Joseph Robert Dorkin , Xiaojun Qin , William Cantley , Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Muthusamy Jayaraman
IPC分类号： C12N15/113 , C07C229/06 , A61K47/12 , A61K47/14
CPC分类号： A61K9/1272 , A61K9/1278 , A61K31/22 , A61K31/7088 , A61K31/712 , A61K31/713 , A61K38/1709 , A61K38/4846 , A61K47/14 , A61K47/549 , A61K47/551 , A61K47/6911 , A61K48/0033 , C07C29/58 , C07C227/18 , C07C227/40 , C07C229/12 , C07D475/04 , C12N15/113 , C12N15/1137 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/341 , C12N2310/346 , C12N2310/351 , C12N2310/3515 , C12N2320/32 , Y02A50/463 , A61K2300/00 , C12N2310/3521 , C12N2310/3533
摘要： The invention features a cationic lipid of formula I, an improved lipid formulation comprising a cationic lipid of formula I and corresponding methods of use. Also disclosed are targeting lipids, and specific lipid formulations comprising such targeting lipids.
摘要翻译：本发明的特征在于式I的阳离子脂质，包含式I的阳离子脂质和相应的使用方法的改进的脂质制剂。还公开了靶向脂质和包含这种靶向脂质的特定脂质制剂。

6. 发明申请

US20120183602A1 LIPID FORMULATION 有权
标题翻译：脂质配方
公开(公告)号：US20120183602A1
公开(公告)日：2012-07-19
申请号：US13357856
申请日：2012-01-25
申请人： Jianxin CHEN , Steven Ansell , Akin Akinc , Joseph Robert Dorkin , Xiaojun Qin , William Cantley , Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Muthusamy Jayaraman
发明人： Jianxin CHEN , Steven Ansell , Akin Akinc , Joseph Robert Dorkin , Xiaojun Qin , William Cantley , Muthiah Manoharan , Kallanthottathil G. Rajeev , Jayaprakash K. Narayanannair , Muthusamy Jayaraman
IPC分类号： A61K9/127 , A61K31/7088 , C12N5/02 , A61K47/44
CPC分类号： A61K9/1272 , A61K9/1278 , A61K31/22 , A61K31/7088 , A61K31/712 , A61K31/713 , A61K38/1709 , A61K38/4846 , A61K47/14 , A61K47/549 , A61K47/551 , A61K47/6911 , A61K48/0033 , C07C29/58 , C07C227/18 , C07C227/40 , C07C229/12 , C07D475/04 , C12N15/113 , C12N15/1137 , C12N2310/14 , C12N2310/315 , C12N2310/321 , C12N2310/322 , C12N2310/341 , C12N2310/346 , C12N2310/351 , C12N2310/3515 , C12N2320/32 , Y02A50/463 , A61K2300/00 , C12N2310/3521 , C12N2310/3533
摘要： The invention features a cationic lipid of formula I, an improved lipid formulation comprising a cationic lipid of formula I and corresponding methods of use. Also disclosed are targeting lipids, and specific lipid formulations comprising such targeting lipids.
摘要翻译：本发明的特征在于式I的阳离子脂质，包含式I的阳离子脂质和相应的使用方法的改进的脂质制剂。还公开了靶向脂质和包含这种靶向脂质的特定脂质制剂。

7. 发明申请

US20050255153A1 High efficiency encapsulation of charged therapeutic agents in lipid vesicles 有权
标题翻译：电荷治疗剂在脂质囊泡中的高效包封
公开(公告)号：US20050255153A1
公开(公告)日：2005-11-17
申请号：US10658947
申请日：2003-09-09
申请人： Sean Semple , Sandra Klimuk , Troy Harasym , Michael Hope , Steven Ansell , Pieter Cullis , Peter Scherrer , Dan Debeyer
发明人： Sean Semple , Sandra Klimuk , Troy Harasym , Michael Hope , Steven Ansell , Pieter Cullis , Peter Scherrer , Dan Debeyer
IPC分类号： A61K9/127 , A61K9/50 , A61K31/7105 , A61K31/711 , A61K47/28 , A61K47/44 , A61K48/00
CPC分类号： A61K9/1277 , A61K9/1272 , Y10T428/2984
摘要： Methods for the preparation of a lipid-nucleic acid composition are provided. According to the methods, a mixture of lipids containing a protonatable or deprotonatable lipid, for example an amino lipid and a lipid such as a PEG- or Polyamide oligomer-modified lipid is combined with a buffered aqueous solution of a charged therapeutic agent, for example polyanionic nucleic acids, to produce particles in which the therapeutic agent is encapsulated in a lipid vesicle. Surface charges on the lipid particles are at least partially neutralized to provide surface-neutralized lipid-encapsulated compositions of the therapeutic agents. The method permits the preparation of compositions with high ratios of therapeutic agent to lipid and with encapsulation efficiencies in excess of 50%.
摘要翻译：提供了制备脂质 - 核酸组合物的方法。根据该方法，将包含可质子化或不可质令排泄的脂质，例如氨基脂质和脂质如PEG-或聚酰胺低聚物修饰的脂质的脂质混合物与带电疗法的缓冲水溶液组合，例如聚阴离子核酸，以产生其中治疗剂包封在脂质囊泡中的颗粒。脂质颗粒上的表面电荷至少部分被中和，以提供治疗剂的表面中和的脂质包封的组合物。该方法允许制备具有高比例的治疗剂与脂质并且包封效率超过50％的组合物。

8. 发明申请

US20060008909A1 Liposomal formulations comprising dihydrosphingomyelin and methods of use thereof 有权
标题翻译：包含二氢鞘磷脂的脂质体制剂及其使用方法
公开(公告)号：US20060008909A1
公开(公告)日：2006-01-12
申请号：US11131436
申请日：2005-05-16
申请人： Pieter Cullis , Thomas Madden , Michael Hope , Steven Ansell , Barbara Mui , Sean Semple , Norbert Maurer
发明人： Pieter Cullis , Thomas Madden , Michael Hope , Steven Ansell , Barbara Mui , Sean Semple , Norbert Maurer
IPC分类号： C12N15/88
CPC分类号： A61K31/4745 , A61K9/1272 , A61K9/1278 , A61K33/32 , A61K2300/00
摘要： The present invention includes novel liposomes comprising dihydrosphingomyelin. The invention also includes compositions comprising these liposomes and a therapeutic agent, in addition to methods and kits for delivering a therapeutic agent or treating a disease, e.g., a cancer, using these compositions.
摘要翻译：本发明包括含有二氢鞘磷脂的新型脂质体。除了使用这些组合物递送治疗剂或治疗疾病例如癌症的方法和试剂盒外，本发明还包括包含这些脂质体和治疗剂的组合物。

9. 发明申请

US20050086299A1 Territorial determination of remote computer location in a wide area network for conditional delivery of digitized products 有权
标题翻译：广域网远程计算机位置的领土确定，用于数字化产品的有条件传送
公开(公告)号：US20050086299A1
公开(公告)日：2005-04-21
申请号：US10985130
申请日：2004-11-10
申请人： Steven Ansell , Andrew Cherenson
发明人： Steven Ansell , Andrew Cherenson
IPC分类号： G06F12/14 , G06F20060101 , G06F12/00 , G06F13/00 , G06F15/00 , G06F15/16 , G06F17/30 , G06F21/00 , G06F21/24 , G06Q10/08 , G06Q30/06 , H04L29/08 , H04L29/12
CPC分类号： G06F17/30876 , G06Q10/087 , G06Q30/0639 , H04L29/12216 , H04L29/12594 , H04L61/2007 , H04L61/30 , H04L67/18
摘要： Digital products are delivered to a client computer through a wide area network such as the Internet only upon determination that the client computer is located in a geopolitical territory, such as a country or state, for which delivery of the digital product is authorized. A server computer estimates the geopolitical location of the client computer from the client computer's network address through contact information in a network address allocation database. Alternatively, the server computer estimates the geopolitical location of the client computer from the client computer's custom name, e.g., domain name. The domain name itself can specify a country within which the client computer is located. Such can be conventional or can be parse according to ad hoc patterns developed by large, international organizations identified by a root domain name. In addition, contact information for the domain name can be retrieved and geopolitical territory information parsed from the contact information. A super-classification of the domain name can indicate a geopolitical territory. Records associating geopolitical territories with network address ranges are stored in such a manner that maximizes resolution within a cache of such records, perhaps at the expense of reduce efficiency but so as to maximum currency and accuracy.
摘要翻译：数字产品只有在确定客户端计算机位于地理政治领域（如国家或国家）中才能通过广域网（例如互联网）传送到客户端计算机，从而为数字产品的交付授权。服务器计算机通过网络地址分配数据库中的联系人信息，从客户端计算机的网络地址估计客户端计算机的地理政治位置。或者，服务器计算机根据客户端计算机的自定义名称（例如域名）来估计客户端计算机的地缘政治位置。域名本身可以指定客户端计算机所在的国家/地区。这可以是常规的，或者可以根据由根域名识别的大型国际组织开发的特定模式来解析。此外，可以检索域名的联系信息，并从联系人信息中解析地缘政治领域信息。域名的超级分类可以表示地缘政治领域。将地缘政治地区与网络地址范围相关联的记录以最大限度地提高此类记录的缓存中的分辨率的方式进行存储，这可能以降低效率为代价，但是最大限度地提高了货币和准确性。

10. 发明申请

US20050033974A1 Adaptable security mechanism for preventing unauthorized access of digital data 有权
标题翻译：适应性安全机制，防止数字数据的未经授权的访问
公开(公告)号：US20050033974A1
公开(公告)日：2005-02-10
申请号：US10941509
申请日：2004-09-14
申请人： Steven Ansell , Andrew Cherenson , Leon Rishniw , Susan Cannon , Edward Allard , Jason Brownell , Micah Stroud
发明人： Steven Ansell , Andrew Cherenson , Leon Rishniw , Susan Cannon , Edward Allard , Jason Brownell , Micah Stroud
IPC分类号： H04L9/08 , G06F21/00 , H04L9/10 , H04L9/32 , H04L9/00
CPC分类号： G06F21/10 , G06F2221/0704 , G06F2221/072
摘要： Content such as computer software, data representing audiovisual works, and electronic documents can converted from a machine-bound state to user-bound state without modification to the content data itself. Instead, keys used to access the content are converted from the machine-bound state to the user-bound state. In particular, the keys are kept in a passport data structure which can represent either a machine-binding or a user-binding. A machine-bound passport can be upgraded to a user-bound passport without modifying the bound content. The private key of the machine-bound passport, in cleartext form, is included in the user-bound passport and encrypted using a user-supplied password to bind the private key to the user. In addition, private user information is collected and verified and included in the user-bound passport. Upgrading a machine-bound passport can be initiated automatically upon detection that an attempt is made to play back machine-bound content on a machine other than the one to which the content is bound.
摘要翻译：诸如计算机软件，表示视听作品的数据和电子文档的内容可以从机器绑定状态转换为用户绑定状态，而不修改内容数据本身。相反，用于访问内容的密钥从机器绑定状态转换为用户绑定状态。特别地，密钥保存在可以表示机器绑定或用户绑定的护照数据结构中。机器护照可以升级为用户的护照，而不修改绑定的内容。机密护照的私钥以明文形式包含在用户绑定护照中，并使用用户提供的密码加密，以将私钥绑定到用户。此外，收集和验证私人用户信息并将其包含在用户绑定的护照中。检测到机器绑定护照的升级可以在检测到尝试在除内容绑定的机器之外的机器上重放机器绑定的内容时自动启动。

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