公开(公告)号：EP2771319A1

公开(公告)日：2014-09-03

申请号：EP12783791.2

申请日：2012-10-26

申请人： Massachusetts Institute Of Technology

发明人： DONG, Yizhou ,  LOVE, Kevin, Thomas ,  LANGER, Robert, S. ,  ANDERSON, Daniel, Griffith ,  CHEN, Delai ,  CHEN, Yi ,  VEGAS, Arturo, Jose ,  ALABI, Akinleye ,  ZHANG, Yunlong

IPC分类号： C07D207/16 ,  C07D209/20 ,  C07D233/64 ,  C07D241/08 ,  C07D403/06 ,  C07D487/06 ,  C07C227/18 ,  C07C229/12 ,  C07C229/16 ,  C07C229/22 ,  C07C229/26 ,  C07C229/28 ,  A61K48/00 ,  C12N15/87

CPC分类号： A61K31/7105 ,  A61K31/711 ,  A61K47/22 ,  A61K2121/00 ,  C07C229/12 ,  C07C229/22 ,  C07C229/24 ,  C07C229/26 ,  C07C229/36 ,  C07C237/08 ,  C07C237/12 ,  C07C271/22 ,  C07C279/14 ,  C07C323/58 ,  C07D207/16 ,  C07D209/20 ,  C07D209/24 ,  C07D233/64 ,  C07D241/08 ,  C07D265/32 ,  C07D403/06 ,  C07D413/06 ,  C07D487/04 ,  C07D487/06 ,  C12N15/87 ,  C12N15/88 ,  C12Q1/025 ,  G01N33/15

摘要： Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as "APPLs". Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R', R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.

摘要翻译： worin M，N，P，R”，R1，R2，R3，R4，R5，R8，Z，W，Y，和Z如在定义。

公开(公告)号：EP2365962B1

公开(公告)日：2017-07-05

申请号：EP09825132.5

申请日：2009-11-06

申请人： Massachusetts Institute of Technology

发明人： MAHON, Kerry, Peter ,  LOVE, Kevin, Thomas ,  LEVINS, Christopher, G. ,  WHITEHEAD, Kathryn, Ann ,  LANGER, Robert, S. ,  ANDERSON, Daniel, Griffith

IPC分类号： A61K48/00 ,  C12N15/11 ,  C07D295/13

CPC分类号： C07D295/13 ,  A61K9/107 ,  A61K9/1271 ,  A61K9/5123 ,  A61K31/7088 ,  A61K38/02 ,  A61K47/16 ,  A61K47/54 ,  A61K47/545 ,  A61K48/0025 ,  B01J2531/0252 ,  B01J2531/845 ,  C07C215/14 ,  C07C217/08 ,  C12N15/111 ,  C12N15/1137 ,  C12N15/88 ,  C12N2310/14 ,  C12N2310/3515 ,  C12N2320/32

摘要： Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.

公开(公告)号：EP3269395A1

公开(公告)日：2018-01-17

申请号：EP17179391.2

申请日：2009-11-06

申请人： Massachusetts Institute Of Technology

发明人： MAHON, Kerry, Peter ,  LOVE, Kevin, Thomas ,  WHITEHEAD, Kathryn, Ann ,  LANGER, Robert S. ,  ANDERSON, Daniel, Griffith ,  LEVINS, Christopher, G.

IPC分类号： A61K48/00 ,  C12N15/11 ,  C07D295/13

CPC分类号： C07D295/13 ,  A61K9/107 ,  A61K9/1271 ,  A61K9/5123 ,  A61K31/7088 ,  A61K38/02 ,  A61K47/16 ,  A61K47/54 ,  A61K47/545 ,  A61K48/0025 ,  B01J2531/0252 ,  B01J2531/845 ,  C07C215/14 ,  C07C217/08 ,  C12N15/111 ,  C12N15/1137 ,  C12N15/88 ,  C12N2310/14 ,  C12N2310/3515 ,  C12N2320/32

摘要： Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.

摘要翻译： 描述了通过使胺与环氧化物封端的化合物反应制备氨基醇类脂质。 还提供了由市售原料制备氨基醇类脂质的方法。 氨基醇类脂质可由外消旋或立体化学纯的环氧化物制备。 氨基醇类脂质或其盐形式优选是可生物降解的和生物相容的，并且可以用于各种药物递送系统。 鉴于这些氨基醇类脂质化合物的氨基部分，它们特别适合于递送多核苷酸。 已经制备了含有本发明的类脂质和多核苷酸的复合物，胶束，脂质体或颗粒。 本发明的类脂质也可以用于制备用于药物递送的微粒。 考虑到它们缓冲周围环境pH的能力，它们在提供不稳定剂方面特别有用。

公开(公告)号：EP2365962A2

公开(公告)日：2011-09-21

申请号：EP09825132.5

申请日：2009-11-06

申请人： Massachusetts Institute of Technology

发明人： MAHON, Kerry, Peter ,  LOVE, Kevin, Thomas ,  LEVINS, Christopher, G. ,  WHITEHEAD, Kathryn, Ann ,  LANGER, Robert, S. ,  ANDERSON, Daniel, Griffith

IPC分类号： C07C217/42 ,  A61K47/18 ,  C07D241/04 ,  B01J31/12

CPC分类号： C07D295/13 ,  A61K9/107 ,  A61K9/1271 ,  A61K9/5123 ,  A61K31/7088 ,  A61K38/02 ,  A61K47/16 ,  A61K47/54 ,  A61K47/545 ,  A61K48/0025 ,  B01J2531/0252 ,  B01J2531/845 ,  C07C215/14 ,  C07C217/08 ,  C12N15/111 ,  C12N15/1137 ,  C12N15/88 ,  C12N2310/14 ,  C12N2310/3515 ,  C12N2320/32

摘要： Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.

摘要翻译： 氨基醇类固醇通过使胺与环氧化物封端的化合物反应来制备。 还提供了从市售的起始原料制备氨基醇类固醇的方法。 氨基醇类固醇可以由外消旋或立体化学纯环氧化物制备。 氨基醇类固醇或其盐形式优选是可生物降解的和生物相容的并且可以用于各种药物递送系统中。 鉴于这些氨基醇类脂质化合物的氨基部分，它们特别适用于递送多核苷酸。 已经制备了包含本发明的类脂和多核苷酸的复合物，胶束，脂质体或颗粒。 本发明的类脂质也可用于制备用于药物递送的微粒。 考虑到缓冲其周围环境的pH值，它们特别适用于提供不稳定剂。