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：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：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：US20170204075A1

公开(公告)日：2017-07-20

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 ,  C07C215/14 ,  C12N15/113 ,  A61K9/107 ,  A61K31/7088

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.

公开(公告)号：US09556110B2

公开(公告)日：2017-01-31

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 ,  A61K9/127 ,  A61K9/51 ,  A61K47/16 ,  A61K48/00 ,  C07C215/14 ,  C07D295/13 ,  C12N15/11 ,  C12N15/88 ,  A61K31/7088 ,  A61K38/02

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。