公开(公告)号：US20160206740A1

公开(公告)日：2016-07-21

申请号：US14995842

申请日：2016-01-14

Applicant: Massachusetts Institute of Technology

Inventor： James E. Dahlman ,  Avraham D. Schroeder ,  Daniel Griffith Anderson ,  Robert S. Langer ,  Christopher G. Levins

IPC: A61K47/22 ,  C07D273/00 ,  C07D295/084 ,  C12N15/113 ,  A61K9/127

CPC classification number: A61K47/22 ,  A61K9/0019 ,  A61K9/1272 ,  A61K47/34 ,  A61K47/543 ,  A61K47/59 ,  A61K47/6907 ,  A61K47/6911 ,  A61K47/6921 ,  C07D257/02 ,  C07D273/00 ,  C07D273/08 ,  C07D295/084 ,  C08G73/10 ,  C12N15/1137 ,  C12N15/1138 ,  C12N2310/14 ,  C12N2320/32

Abstract: The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as “conjugated lipomers” or “lipomers”) containing one or more groups of the formula (iii): wherein R3 and R4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.

Abstract translation: 本发明提供含有一个或多个式（ⅲ）基团的本发明共轭聚乙烯亚胺（PEI）聚合物和共轭氮杂 - 大环化合物（统称为“共轭脂族”或“脂聚合物”）：其中R3和R4定义如上 这里。 还提供了包含本发明的共轭脂族物的组合物，以及制备和使用方法。

公开(公告)号：US20150203439A1

公开(公告)日：2015-07-23

申请号：US14599004

申请日：2015-01-16

Applicant: Massachusetts Institute of Technology

Inventor： Kerry Peter Mahon ,  Kevin Thomas Love ,  Christopher G. Levins ,  Kathryn Ann Whitehead ,  Robert S. Langer ,  Daniel Griffith Anderson

IPC: C07C217/08 ,  A61K38/02 ,  A61K31/7088 ,  A61K47/16 ,  C07C215/14

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。 已经制备了含有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。

公开(公告)号：US20210101875A1

公开(公告)日：2021-04-08

申请号：US17070486

申请日：2020-10-14

Applicant: Massachusetts Institute of Technology

Inventor： Kerry Peter Mahon ,  Kevin Thomas Love ,  Christopher G. Levins ,  Kathryn Ann Whitehead ,  Robert S. Langer ,  Daniel Griffith Anderson

IPC: C07D295/13 ,  A61K9/127 ,  A61K9/51 ,  A61K47/16 ,  A61K48/00 ,  C07C215/14 ,  C12N15/11 ,  C12N15/88 ,  A61K47/54 ,  C07C217/08 ,  A61K31/7088 ,  A61K38/02 ,  A61K9/107 ,  C12N15/113

Abstract: 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：US20190167795A1

公开(公告)日：2019-06-06

申请号：US16181109

申请日：2018-11-05

Applicant: Massachusetts Institute of Technology

Inventor： James E. Dahlman ,  Avraham D. Schroeder ,  Daniel Griffith Anderson ,  Robert S. Langer ,  Christopher G. Levins

IPC: A61K47/22 ,  C12N15/113 ,  A61K47/69 ,  C07D273/08 ,  A61K47/59 ,  A61K47/54 ,  A61K47/34 ,  C07D295/084 ,  A61K9/127 ,  C07D273/00 ,  C07D257/02 ,  C08G73/10 ,  A61K9/00

Abstract: The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as “conjugated lipomers” or “lipomers”) containing one or more groups of the formula (iii): wherein R3 and R4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.

公开(公告)号：US10933139B2

公开(公告)日：2021-03-02

申请号：US16181109

申请日：2018-11-05

Applicant: Massachusetts Institute of Technology

Inventor： James E. Dahlman ,  Avraham D. Schroeder ,  Daniel Griffith Anderson ,  Robert S. Langer ,  Christopher G. Levins

IPC: A61K47/22 ,  A61K47/54 ,  A61K47/59 ,  A61K47/69 ,  C07D257/02 ,  C07D273/08 ,  A61K9/00 ,  A61K47/34 ,  C08G73/10 ,  A61K9/127 ,  C07D273/00 ,  C07D295/084 ,  C12N15/113

Abstract: The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as “conjugated lipomers” or “lipomers”) containing one or more groups of the formula (iii): wherein R3 and R4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.

公开(公告)号：US11414393B2

公开(公告)日：2022-08-16

申请号：US17070486

申请日：2020-10-14

Applicant: Massachusetts Institute of Technology

Inventor： Kerry Peter Mahon ,  Kevin Thomas Love ,  Christopher G. Levins ,  Kathryn Ann Whitehead ,  Robert S. Langer ,  Daniel Griffith Anderson

IPC: C07D295/13 ,  A61K9/127 ,  A61K9/51 ,  A61K47/16 ,  A61K48/00 ,  C07C215/14 ,  C12N15/11 ,  C12N15/88 ,  A61K47/54 ,  C07C217/08 ,  A61K31/7088 ,  A61K38/02 ,  A61K9/107 ,  C12N15/113

Abstract: 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：US20210260195A1

公开(公告)日：2021-08-26

申请号：US17122068

申请日：2020-12-15

Applicant: Massachusetts Institute of Technology

Inventor： James E. Dahlman ,  Avraham D. Schroeder ,  Daniel Griffith Anderson ,  Robert S. Langer ,  Christopher G. Levins

IPC: A61K47/22 ,  A61K47/54 ,  A61K47/59 ,  A61K47/69 ,  C07D257/02 ,  C07D273/08 ,  A61K9/00 ,  A61K47/34 ,  C08G73/10 ,  A61K9/127 ,  C07D273/00 ,  C07D295/084 ,  C12N15/113

Abstract: The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as “conjugated lipomers” or “lipomers”) containing one or more groups of the formula (iii): wherein R3 and R4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.

公开(公告)号：US20190177289A1

公开(公告)日：2019-06-13

申请号：US16208295

申请日：2018-12-03

Applicant: Massachusetts Institute of Technology

Inventor： Kerry Peter Mahon ,  Kevin Thomas Love ,  Christopher G. Levins ,  Kathryn Ann Whitehead ,  Robert S. Langer ,  Daniel Griffith Anderson

IPC: C07D295/13 ,  A61K31/7088 ,  A61K9/127 ,  A61K47/54 ,  C12N15/113 ,  A61K38/02 ,  A61K9/107 ,  A61K9/51 ,  A61K47/16 ,  A61K48/00 ,  C07C215/14 ,  C12N15/88 ,  C12N15/11 ,  C07C217/08

Abstract: 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：US10189802B2

公开(公告)日：2019-01-29

申请号：US15417530

申请日：2017-01-27

Applicant: Massachusetts Institute of Technology

Inventor： Kerry Peter Mahon ,  Kevin Thomas Love ,  Christopher G. Levins ,  Kathryn Ann Whitehead ,  Robert S. Langer ,  Daniel Griffith Anderson

IPC: C07D295/13 ,  A61K9/107 ,  A61K9/127 ,  A61K9/51 ,  A61K47/16 ,  A61K48/00 ,  C07C215/14 ,  C07C217/08 ,  C12N15/11 ,  C12N15/88 ,  A61K31/7088 ,  A61K38/02 ,  C12N15/113 ,  A61K47/54

Abstract: 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：US10117934B2

公开(公告)日：2018-11-06

申请号：US14995842

申请日：2016-01-14

Applicant: Massachusetts Institute of Technology

Inventor： James E. Dahlman ,  Avraham D. Schroeder ,  Daniel Griffith Anderson ,  Robert S. Langer ,  Christopher G. Levins

IPC: C07D257/02 ,  A61K47/22 ,  C07D273/08 ,  C08G73/10 ,  A61K9/00 ,  A61K47/34 ,  A61K9/127 ,  C07D273/00 ,  C07D295/084 ,  C12N15/113 ,  A61K47/54 ,  A61K47/59 ,  A61K47/69

Abstract: The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as “conjugated lipomers” or “lipomers”) containing one or more groups of the formula (iii): wherein R3 and R4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.