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2. 发明授权

EP2523658B1 A MATRIX COMPOSITION FOR DELIVERY OF HYDROPHOBIC ACTIVES 有权
公开(公告)号：EP2523658B1
公开(公告)日：2018-05-30
申请号：EP11732279.2
申请日：2011-01-10
申请人： ISP Investments LLC
发明人： NARAYANAN, Kolazi , JON, Domingo , PATEL, Jayanti, V.
IPC分类号： A61K9/66 , A01N25/02 , A01N53/00 , A01N65/00 , A61K8/42 , A61K8/86 , A61K47/10 , A61K8/55 , A61Q19/00 , A61K9/00 , A61K47/16 , A61K47/20 , A61K47/22 , A61K47/34 , A61K47/14 , A61K9/107 , A61K9/10 , A61K8/06 , C09K3/00
CPC分类号： A01N25/00 , A01N25/02 , A01N37/18 , A61K8/06 , A61K8/42 , A61K8/556 , A61K8/86 , A61K9/0014 , A61K9/10 , A61K9/107 , A61K9/1075 , A61K47/10 , A61K47/14 , A61K47/16 , A61K47/20 , A61K47/22 , A61K47/34 , A61K2800/30 , A61Q19/00 , C09K3/00 , A01N25/04 , A01N25/30 , A01N53/00 , A01N65/06
摘要： A matrix composition capable of forming an emulsion/micro-emulsion comprising an emulsifiable matrix, essentially free of alkyl pyrrolidone and alkoxylated alcohol, comprising: (i) a long chain substituted amide; (ii) a surface active agent; and (iii) optionally, an organic diluent.

3. 发明公开

EP3269391A1 FORMULATION COMPRISING A GEMCITABINE-PRODRUG 审中-公开
标题翻译：包含吉西他滨 - 前药的制剂
公开(公告)号：EP3269391A1
公开(公告)日：2018-01-17
申请号：EP17189351.4
申请日：2015-06-25
申请人： Nucana Biomed Limited
发明人： GRIFFITH, Hugh , KENNOVIN, Gordon
IPC分类号： A61K47/16 , A61K9/08 , A61K47/20 , A61K47/22 , A61K31/7068 , C07H19/10 , A61P35/00
CPC分类号： A61K31/7068 , A61K9/0019 , A61K9/08 , A61K47/16 , A61K47/18 , A61K47/20 , A61K47/22 , A61K47/26 , A61K47/44 , A61K47/548
摘要： This invention relates to pharmaceutical formulations of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate, a monophosphate derivative of the well-known oncology drug gemcitabine. In particular, the invention relates to formulations which comprise a polar aprotic solvent, preferably dimethyl acetamide (DMA). Formulations comprising these solvent provide therapeutically effective treatments of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate. The invention also relates to methods of using said formulations and kits comprising said formulations.
摘要翻译：本发明涉及吉西他滨 - [苯基 - 苯甲酰基-L-丙氨酰基]] - 磷酸酯的药物制剂，其为着名的肿瘤药物吉西他滨的单磷酸酯衍生物。特别地，本发明涉及包含极性非质子溶剂，优选二甲基乙酰胺（DMA）的制剂。包含这些溶剂的制剂提供吉西他滨 - [苯基 - 苯甲酰基-L-丙氨酰基]] - 磷酸酯的治疗有效治疗。本发明还涉及使用包含所述制剂的所述制剂和试剂盒的方法。

4. 发明授权

EP2231195B1 TARGETING LIPIDS 有权
标题翻译：靶向脂质体
公开(公告)号：EP2231195B1
公开(公告)日：2017-03-29
申请号：EP08865121.1
申请日：2008-12-04
申请人： Arbutus Biopharma Corporation
发明人： MANOHARAN, Muthiah , RAJEEV, Kallanthottathil, G. , NARAYANANNAIR, Jayaprakash, K. , JAYARAMAN, Muthusamy
IPC分类号： A61K47/56 , A61K31/70 , A61K31/713
CPC分类号： A61K47/28 , A61K31/70 , A61K31/7004 , A61K31/7052 , A61K31/7088 , A61K31/713 , A61K47/16 , A61K47/22 , A61K47/543 , A61K47/549 , A61K47/60 , A61K48/00 , C07H21/02 , Y02A50/385 , Y02A50/411 , Y02A50/467 , Y02P20/55
摘要： The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(R N ) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, - P(Z')(Z")0- nucleoside, -P(Z')(Z")O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, P(Z')(Z")O-Linker-OP(Z"')(Z"")O-oligonucleotide, a nucleotide, an oligonucleotide, - P(Z')(Z")-formula(I), -P(Z')(Z")- or -Linker-R; R is L G , -Linker-L G , or has the structure shown below: L G is independently for each occurence a carbohydrate, e.g., monosaccharide, disaccharide, trisaccharide, tetrasaccharide, oligosaccharide, polysaccharide; R N is independently for each occurrence H, methyl, ethyl, propyl, isopropyl, butyl, or benzyl; and Z', Z", Z'" and Z"" are each independently for each occurrence O or S.
摘要翻译：本发明提供了包含至少一个式（I）的亚基的iRNA试剂：其中：A和B各自独立为O，N（R N）或S; X和Y各自独立为H，OH，羟基保护基，磷酸酯基，磷酸二酯基，活化磷酸酯基，活化亚磷酸酯基，亚磷酰胺，固体载体，-P（Z'）（ Z“）O-核苷，-P（Z'）（Z”）O-寡核苷酸，脂质，PEG，类固醇，亲脂体，聚合物，P（Z'）（Z“）O-连接体-OP （Z“'）（Z”“）O-寡核苷酸，核苷酸，寡核苷酸，-P（Z'）（Z”） - 式（I）， - P（Z'）（Z“） - 或 - -R; R是L G， - 接头-L G，或具有如下所示的结构：L G独立地为碳水化合物，例如单糖，二糖，三糖，四糖，寡糖，多糖; R N每次出现时独立地为H，甲基，乙基，丙基，异丙基，丁基或苄基; 和Z'，Z“，Z”'和Z“”各自独立地为O或S.

5. 发明公开

EP3141265A1 CARBOHYDRATE CONJUGATES AS DELIVERY AGENTS FOR OLIGONUCLEOTIDES 审中-公开
标题翻译：碳水化合物共轭物作为寡核苷酸的递送剂
公开(公告)号：EP3141265A1
公开(公告)日：2017-03-15
申请号：EP16001273.8
申请日：2008-12-04
申请人： Alnylam Pharmaceuticals, Inc.
发明人： Manoharan, Muthiah , Rajeev, Kallanthottathil, G. , Narayanannair, Jayaprakash, K. , Maier, Martin
IPC分类号： A61K47/54
CPC分类号： A61K47/28 , A61K31/70 , A61K31/7004 , A61K31/7052 , A61K31/7088 , A61K31/713 , A61K47/16 , A61K47/22 , A61K47/543 , A61K47/549 , A61K47/60 , A61K48/00 , C07H21/02 , Y02A50/385 , Y02A50/411 , Y02A50/467 , Y02P20/55
摘要： The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(R N ) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, - P(Z')(Z")0- nucleoside, -P(Z')(Z")O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, P(Z')(Z")O-Linker-OP(Z"')(Z"")O-oligonucleotide, a nucleotide, an oligonucleotide, - P(Z')(Z")-formula(I), -P(Z')(Z")- or -Linker-R; R is L G , -Linker-L G , or has the structure shown below: L G is independently for each occurence a carbohydrate, e.g., monosaccharide, disaccharide, trisaccharide, tetrasaccharide, oligosaccharide, polysaccharide; R N is independently for each occurrence H, methyl, ethyl, propyl, isopropyl, butyl, or benzyl; and Z', Z", Z'" and Z"" are each independently for each occurrence O or S.
摘要翻译：本发明提供了包含至少一个式（I）的亚基的iRNA试剂：其中：A和B各自独立为O，N（RN）或S; X和Y各自独立为H，OH，羟基保护基，磷酸酯基，磷酸二酯基，活化磷酸酯基，活化亚磷酸酯基，亚磷酰胺，固体载体，-P（Z'）（ Z“）O-核苷，-P（Z'）（Z”）O-寡核苷酸，脂质，PEG，类固醇，亲脂体，聚合物，P（Z'）（Z“）O-连接体-OP （Z“'）（Z”“）O-寡核苷酸，核苷酸，寡核苷酸，-P（Z'）（Z”） - 式（I）， - P（Z'）（Z“） - 或 - -R; R是LG，-Linker-LG，或具有如下所示的结构：LG独立地为碳水化合物，例如单糖，二糖，三糖，四糖，寡糖，多糖; RN在每次出现时独立地为H，甲基，乙基，丙基，异丙基，丁基或苄基; 和Z'，Z“，Z”'和Z“”各自独立地为O或S.

6. 发明授权

EP2460515B1 Oral calcitonin compositions and applications thereof 有权
标题翻译： Orale Calcitonin-Zusammensetzungen und ihre Anwendungen
公开(公告)号：EP2460515B1
公开(公告)日：2017-03-08
申请号：EP12155823.3
申请日：2008-08-07
申请人： Novartis AG
发明人： Arnold, Michel , Azria, Moise
IPC分类号： A61K9/20 , A61K31/198 , A61K38/23 , A61K9/16
CPC分类号： A61K38/23 , A61K9/0053 , A61K9/1635 , A61K9/1652 , A61K9/2027 , A61K9/2054 , A61K9/4866 , A61K31/198 , A61K31/59 , A61K33/06 , A61K47/16

7. 发明授权

EP1656158B1 LIQUID, AQUEOUS PHARMACEUTICAL COMPOSITION OF FACTOR VII POLYPEPTIDES 有权
标题翻译：液体水性药物组合因子VII多肽的
公开(公告)号：EP1656158B1
公开(公告)日：2016-03-09
申请号：EP04739034.9
申请日：2004-08-12
申请人： Novo Nordisk Health Care AG
发明人： JENSEN, Michael, Bech , PETERSEN, Anders, Klarskov , BOWLER, Andrew, Neil
IPC分类号： A61K38/36 , A61K47/16 , A61K38/48 , A61K31/17 , A61K47/02 , A61K47/18 , A61K47/42
CPC分类号： A61K38/4846 , A61K9/0019 , A61K31/17 , A61K38/36 , A61K47/02 , A61K47/16 , A61K47/183 , A61K47/42

8. 发明公开

EP2393854A4 NANOSCALE PLATINUM COMPOUNDS AND METHODS OF USE THEREOF 审中-公开
标题翻译：纳米级铂化合物及其使用方法
公开(公告)号：EP2393854A4
公开(公告)日：2015-12-02
申请号：EP10739130
申请日：2010-02-04
申请人： BRIGHAM & WOMENS HOSPITAL
发明人： SENGUPTA SHILADITYA , PARASKAR ABHIMANYU , SONI SHIVANI , SENGUPTA POULOMI , BASU SUDIPTA
IPC分类号： C08F222/06 , A61K47/48 , A61P35/00 , C08F8/42 , C08F22/06
CPC分类号： A61K47/489 , A61K31/282 , A61K31/382 , A61K33/24 , A61K47/16 , A61K47/24 , A61K47/48046 , A61K47/48053 , A61K47/48176 , A61K47/48215 , A61K47/543 , A61K47/544 , A61K47/58 , A61K47/60 , A61K47/6933 , C07J41/0055 , C08F8/32 , C08F22/06 , C08F222/06

9. 发明公开

EP2464334A4 COMPOSITIONS AND METHODS FOR TREATING FUNGAL INFECTION OF THE NAIL 审中-公开
标题翻译：组合物和方法治疗真菌指甲
公开(公告)号：EP2464334A4
公开(公告)日：2014-03-26
申请号：EP10808425
申请日：2010-08-13
申请人： MOBERG DERMA AB
发明人： LINDAHL AAKE
IPC分类号： A61K9/10 , A61K9/00 , A61K31/137 , A61K45/06 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/18 , A61K47/32 , A61P31/10
CPC分类号： A61K45/06 , A61K9/0014 , A61K31/137 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/16 , A61K47/183 , A61K47/32 , A61K2300/00

10. 发明公开

EP2658577A2 CARRIER FOR NEGATIVELY CHARGED DRUGS COMPRISING A CATIONIC LIPID AND A PREPARATION METHOD THEREOF 审中-公开
标题翻译：支持负随着对阳离子脂质毒品和法充电用于生产
公开(公告)号：EP2658577A2
公开(公告)日：2013-11-06
申请号：EP11852588.0
申请日：2011-12-30
申请人： Samyang Biopharmaceuticals Corporation
发明人： CHOI, Sung-Won , LA, Muhn-Ho , SON, Ji-Yeon , SEO, Min-Hyo
IPC分类号： A61K47/18 , A61K47/08 , A61K31/175 , A61K9/127 , A61K47/48
CPC分类号： A61K47/16 , A61K9/107 , A61K9/1075 , A61K9/1272 , A61K31/713 , A61K47/18 , A61K47/34 , A61K47/59 , A61K47/595 , C12N15/88
摘要： Disclosed are a carrier for delivering a negatively charged drug, comprising a cationic lipid represented by formula 1, and a preparation method thereof. Also disclosed is a pharmaceutical composition comprising a negatively charged drug and a cationic lipid represented by formula 1, wherein the negatively charged drug forms a complex with the cationic lipid. The composition can increase the in vivo stability of the negatively charged drug after local or systemic administration and allows the intracellular delivery of the negatively charged drug. Thus, the composition will be useful for improving the therapeutic effect of the negatively charged drug.

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