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1. 发明申请

WO2012159704A1 STABLE CRYSTAL MODIFICATIONS OF DOTAP CHLORIDE 审中-公开
标题翻译：氯化钠稳定的水晶修饰
公开(公告)号：WO2012159704A1
公开(公告)日：2012-11-29
申请号：PCT/EP2012/001882
申请日：2012-05-02
申请人： MERCK PATENT GMBH , PLATSCHER, Michael Wilhelm , HEIDINGER, Alfred
发明人： PLATSCHER, Michael Wilhelm , HEIDINGER, Alfred
IPC分类号： C07C219/08
CPC分类号： C07C219/08 , A61K31/231 , A61K45/06 , C07B2200/07 , C07B2200/13
摘要： The present invention relates to crystal modifications of racemic (2R,S)- and enantiomerically pure (2R)- resp. (2S)-DOTAP chloride, to processes for the preparation thereof, and to the use thereof for the preparation of pharmaceutical compositions.
摘要翻译：本发明涉及外消旋（2R，S） - 和对映体纯（2R） - （2S）-DOTAP氯化物，其制备方法及其用于制备药物组合物的用途。

2. 发明申请

WO2013135360A1 AMINOACID LIPIDS 审中-公开
标题翻译：氨基酸脂肪酸
公开(公告)号：WO2013135360A1
公开(公告)日：2013-09-19
申请号：PCT/EP2013/000699
申请日：2013-03-11
申请人： MERCK PATENT GMBH
发明人： PLATSCHER, Michael Wilhelm , BEHRENDT, Raymond , GROEHN, Viola , HOERTNER, Simone Rachel , PASSAFARO, Marco Silvio , BAUER, Finn
IPC分类号： A61K9/127 , C07C271/22 , C07C237/08
CPC分类号： C07C237/30 , A61K9/1272 , C07C59/185 , C07C237/06 , C07C237/08 , C07C237/10 , C07C237/22 , C07C271/22 , C07C2603/18 , Y02P20/55
摘要： The present invention is directed to a new class of lipids, more specifically ether-lipids having a polar headgroup, as well as vesicles comprising these lipids, methods of their preparation as well as their uses in medical applications, wherein the ether-lipids are represented by general formula (I) wherein Y represents O, N, S or a covalent bond; P 1 represents H, an Y- protecting group or an Y-activating group or a spacer group; P 2 , P 3 represent independently of each other H, an amino-protecting group or a spacer group, or P 2 and P 3 form together with the N to which they are bound a ring structure; L is a group of formula (a) wherein the dashed line represents the linkage to N; R 1 represents H or a group of formula -(CH 2 ) 2 -OR b1 ; R 1 represents H or a group of formula - (CH 2 ) 2 -OR b2 , R 2 represents H or a group of formula -CH 2 -OR c ; R 2 Represents H or a group of formula -OR d or -CH 2 -OR c ,' R 2 represents H or a group of formula -(CH 2 ) 2 -OR e or -(CH 2 ) 3 -OR e ; R a , R b1 , R b2 , R c , R d ,R e represent independently of each other a saturated or unsaturated, straight or branched hydrocarbon chain, and m is 1, 2 or 3; with the proviso that at least one of R 1 , R 1' , R 2 , R 2' , R 3 is not H.
摘要翻译：本发明涉及一类新的脂质，更具体地是具有极性头团的醚 - 脂质，以及包含这些脂质的囊泡，其制备方法及其在医学应用中的用途，其中所述醚 - 脂质被代表通式（I）其中Y表示O，N，S或共价键; P1表示H，Y-保护基或Y-活化基或间隔基; P2，P3彼此独立地表示H，氨基保护基或间隔基，或者P2和P3与它们所结合的N一起形成环结构; L是式（a）的基团，其中虚线表示与N的连接; R1表示H或式 - （CH2）2-ORb1的基团; R1表示H或式 - （CH2）2-ORb2的基团，R2表示H或式-CH2-ORc的基团; R 2表示H或式-OR 1或-CH 2 OR c的基团，R 2表示H或式 - （CH 2）2 ORe或 - （CH 2）3 -O-的基团; Ra，Rb1，Rb2，Rc，Rd，Re彼此独立地表示饱和或不饱和的直链或支链烃链，m为1,2或3; 条件是R1，R1'，R2，R2'，R3中的至少一个不是H.

3. 发明申请

WO2013135359A1 TARGETING AMINOACID LIPIDS 审中-公开
标题翻译：靶向氨基酸脂
公开(公告)号：WO2013135359A1
公开(公告)日：2013-09-19
申请号：PCT/EP2013/000698
申请日：2013-03-08
申请人： MERCK PATENT GMBH
发明人： PLATSCHER, Michael Wilhelm , BEHRENDT, Raymond , GROEHN, Viola , HOERTNER, Simone Rachel , PASSAFARO, Marco Silvio , BAUER, Finn
IPC分类号： A61K9/127 , C07D475/04 , A61K47/24 , A61K47/28 , C07K7/08 , C07K7/64
CPC分类号： A61K47/60 , A61K47/543 , A61K47/6911 , C07C237/06 , C07C237/30 , C07D475/04 , C07K5/02 , C07K7/08 , C07K7/64
摘要： The present invention is directed to carrier systems comprising ether-lipids conjugated to one or more bioactive ligands and exposed on the surface of the carrier system for use in targeted delivery and/or antigen display systems. Optionally one or more further bioactive agents may be encapsulated or embedded within or attached to or adsorbed onto the carrier system. The present invention is further directed to methods of their preparation and their uses in medical applications, such as targeted delivery of bioactive agents to specific tissues or cells and antigen display systems for the study, diagnosis, and treatment of traits, diseases and conditions that respond to said bioactive agents.
摘要翻译：本发明涉及载体系统，其包含与一种或多种生物活性配体结合的醚 - 脂质，并暴露于载体系统的表面上用于靶向递送和/或抗原显示系统。任选地，一种或多种另外的生物活性剂可以被包封或嵌入或附着于载体系统或吸附到载体系统上。本发明进一步涉及其制备方法及其在医疗应用中的用途，例如将生物活性剂靶向递送至特定组织或细胞，以及用于研究，诊断和治疗响应的性状，疾病和状况的抗原显示系统至所述生物活性剂。

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