公开(公告)号：WO2010144740A1

公开(公告)日：2010-12-16

申请号：PCT/US2010/038224

申请日：2010-06-10

Applicant: ALNYLAM PHARMACEUTICALS, INC. ,  CHEN, Jianxin ,  ANSELL, Steven ,  AKINC, Akin ,  DORKIN, Joseph, R. ,  QIN, Xiaojun ,  CANTLEY, William ,  MANOHARAN, Muthiah ,  RAJEEV, Kallanthottathil, G. ,  NARAYANANNAIR, Jayaprakash, K. ,  JAYARAMAN, Muthusamy

Inventor： CHEN, Jianxin ,  ANSELL, Steven ,  AKINC, Akin ,  DORKIN, Joseph, R. ,  QIN, Xiaojun ,  CANTLEY, William ,  MANOHARAN, Muthiah ,  RAJEEV, Kallanthottathil, G. ,  NARAYANANNAIR, Jayaprakash, K. ,  JAYARAMAN, Muthusamy

IPC: A61K9/127 ,  C07C211/00 ,  A61K31/20

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2005120461A3

公开(公告)日：2006-03-16

申请号：PCT/US2005017054

申请日：2005-05-16

Applicant: INEX PHARMACEUTICALS CORP ,  HERMANNS KARL R ,  CULLIS PIETER R ,  MADDEN THOMAS D ,  HOPE MICHAEL J ,  ANSELL STEVEN M ,  MUI BARBARA L S ,  SEMPLE SEAN C ,  MAURER NORBERT

Inventor： CULLIS PIETER R ,  MADDEN THOMAS D ,  HOPE MICHAEL J ,  ANSELL STEVEN M ,  MUI BARBARA L S ,  SEMPLE SEAN C ,  MAURER NORBERT

IPC: A61K9/127

CPC classification number: A61K31/4745 ,  A61K9/1272 ,  A61K9/1278 ,  A61K33/32 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2010054401A1

公开(公告)日：2010-05-14

申请号：PCT/US2009/063927

申请日：2009-11-10

Applicant: ALNYLAM PHARMACEUTICALS, INC. ,  MANOHARAN, Muthiah ,  JAYARAMAN, Muthusamy ,  RAJEEV, Kallanthottathil, G, ,  ELTEPU, Laxman ,  ANSELL, Steven ,  CHEN, Jianxin

Inventor： MANOHARAN, Muthiah ,  JAYARAMAN, Muthusamy ,  RAJEEV, Kallanthottathil, G, ,  ELTEPU, Laxman ,  ANSELL, Steven ,  CHEN, Jianxin

IPC: A61K47/00 ,  A61K31/01

CPC classification number: 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

Abstract: 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: R 1 and R 2 are each independently for each occurrence optionally substituted C 10 -C 30 alkyl, optionally substituted C 10 -C 30 alkenyl, optionally substituted C 10 -C 30 alkynyl, optionally substituted C 10 -C 30 acyl, or -linker-ligand; R 3 is H, optionally substituted C 1 - C 10 alkyl, optionally substituted C 2 -C 10 alkenyl, optionally substituted C 2 -C 10 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).

Abstract translation: 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为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，烷基二硫代磷酸酯，烷基膦酸酯，烷基胺，羟基烷基， - （取代的）氨基烷基， - 磷酸烷基 - 硫代磷酸烷基，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）。

公开(公告)号：WO2009070761A1

公开(公告)日：2009-06-04

申请号：PCT/US2008/085030

申请日：2008-11-26

Applicant: CELATOR PHARMACEUTICALS, INC ,  ANSELL, Steven, M. ,  JOHNSTONE, Sharon ,  TARDI, Paul ,  MAYER, Lawrence

Inventor： ANSELL, Steven, M. ,  JOHNSTONE, Sharon ,  TARDI, Paul ,  MAYER, Lawrence

IPC: A61K9/127

CPC classification number: A61K9/1075 ,  A61K9/5123 ,  A61K9/5146 ,  A61K31/337 ,  A61K47/543 ,  C07D305/14

Abstract: Nanoparticulate formulations for delivery of taxane conjugate prodrug formed from a taxane coupled to a hydrophobic moiety through a glycolate linker are described.

Abstract translation: 描述了通过乙醇酸酯连接体与通过疏水部分偶联的紫杉烷形成的用于递送紫杉烷结合物前药的纳米颗粒制剂。

公开(公告)号：WO2005120461A2

公开(公告)日：2005-12-22

申请号：PCT/US2005/017054

申请日：2005-05-16

Applicant: INEX PHARMACEUTICALS CORPORATION ,  HERMANNS, Karl, R. ,  CULLIS, Pieter, R. ,  MADDEN, Thomas, D. ,  HOPE, Michael, J. ,  ANSELL, Steven, M. ,  MUI, Barbara, L.S. ,  SEMPLE, Sean, C. ,  MAURER, Norbert

Inventor： CULLIS, Pieter, R. ,  MADDEN, Thomas, D. ,  HOPE, Michael, J. ,  ANSELL, Steven, M. ,  MUI, Barbara, L.S. ,  SEMPLE, Sean, C. ,  MAURER, Norbert

IPC: A61K9/127

CPC classification number: A61K31/4745 ,  A61K9/1272 ,  A61K9/1278 ,  A61K33/32 ,  A61K2300/00

Abstract: 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.

Abstract translation: 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。