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公开(公告)号：US10086013B2
公开(公告)日：2018-10-02
申请号：US15340082
申请日：2016-11-01
Applicant: Massachusetts Institute of Technology
Inventor： Yizhou Dong , Kevin Thomas Love , Robert S. Langer , Daniel Griffith Anderson , Delai Chen , Yi Chen , Arturo Jose Vegas , Akinleye C. Alabi , Yunlong Zhang
IPC: A61K31/535 , A61K31/7105 , A61K31/711 , C07D241/08 , A61K47/22
Abstract: 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.
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12.发明申请公开(公告)号：US20180036333A9
公开(公告)日：2018-02-08
申请号：US15340082
申请日：2016-11-01
Applicant: Massachusetts Institute of Technology
Inventor： Yizhou Dong , Kevin Thomas Love , Robert S. Langer , Daniel Griffith Anderson , Delai Chen , Yi Chen , Arturo Jose Vegas , Akinleye C. Alabi , Yunlong Zhang
IPC: A61K31/7105 , A61K47/22 , C07D241/08 , A61K31/711
CPC classification number: 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
Abstract: 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.
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公开(公告)号：US09840479B2
公开(公告)日：2017-12-12
申请号：US14789227
申请日：2015-07-01
Applicant: Massachusetts Institute of Technology
IPC: A61K31/495 , C07D241/08 , C07C219/06 , C07C219/08 , C07D295/088
CPC classification number: C07D241/08 , C07C219/06 , C07C219/08 , C07D295/088
Abstract: The present disclosure provides polyamine-fatty acid derived lipidoids (e.g., compounds of Formula (I) or (II)) and methods of preparing the lipidoids. A described lipidoid includes R—C(═O)—O— moieties (where R is a lipid moiety), which may be hydrolyzed into non-toxic fatty acids. Also provided are compositions including a described lipidoid and an agent (e.g., polynucleotide, small molecule, peptide, or protein). The present disclosure also provides methods, kits, and uses that involve the lipidoids or compositions for delivering an agent to a subject, tissue, or cell and/or for treating and/or preventing a range of diseases, such as genetic diseases, proliferative diseases, hematological diseases, neurological diseases, immunological diseases, gastrointestinal diseases, respiratory diseases, painful conditions, psychiatric disorders, and metabolic disorders.
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14.发明授权Amino acid-, peptide-and polypeptide-lipids, isomers, compositions, and uses thereof 有权氨基酸，肽和多肽 - 脂质，异构体，组合物及其用途公开(公告)号：US09512073B2
公开(公告)日：2016-12-06
申请号：US13662002
申请日：2012-10-26
Applicant: Massachusetts Institute of Technology
Inventor： Yizhou Dong , Kevin Thomas Love , Robert S. Langer , Daniel Griffith Anderson , Delai Chen , Yi Chen , Arturo Jose Vegas , Akinleye C. Alabi , Yunlong Zhang
IPC: A61K31/535 , C07C229/00 , C07C323/58 , C07D233/64 , C07D403/06 , C07D241/08 , C07C229/12 , C07C229/22 , C07C229/26 , C07D487/06 , C07D207/16 , C07D209/20 , C12N15/87 , C07C229/24 , C07C279/14 , C07D209/24 , C07D265/32 , C07D413/06 , C07D487/04 , C12Q1/02 , G01N33/15 , C07C271/22 , C07C229/36 , C07C237/08 , C07C237/12 , C12N15/88
CPC classification number: 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
Abstract: 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.
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公开(公告)号：US09101666B2
公开(公告)日：2015-08-11
申请号：US14029552
申请日：2013-09-17
Applicant: Massachusetts Institute of Technology
Inventor： Robert S. Langer , David M. Lynn , David A. Putnam , Mansoor M. Amiji , Daniel Griffith Anderson
CPC classification number: A61K47/34 , A61K9/5146 , A61K31/711 , A61K31/713 , A61K47/59 , A61K47/593 , A61K47/6929 , B82Y5/00 , C08G63/685 , C08G73/02 , C08G73/0273 , C08G73/06 , C08G73/0611 , C08G73/0616 , C12N15/88
Abstract: Poly(β-amino esters) prepared from the conjugate addition of bis(secondary amines) or primary amines to a bis(acrylate ester) are described. Methods of preparing these polymers from commercially available starting materials are also provided. These tertiary amine-containing polymers are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the poly(amine) nature of these polymers, they are particularly suited for the delivery of polynucleotides. Nanoparticles containing polymer/polynucleotide complexes have been prepared. The inventive polymers may also be used to encapsulate other agents to be delivered. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
Abstract translation: 描述了从双（仲胺）或伯胺向双（丙烯酸酯）共轭加成制备的聚（＆（bgr。 - 氨基酯））。 还提供了从市售的原料制备这些聚合物的方法。 这些含叔胺的聚合物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。 鉴于这些聚合物的聚（胺）性质，它们特别适用于递送多核苷酸。 已经制备了含有聚合物/多核苷酸复合物的纳米颗粒。 本发明的聚合物也可以用于包封待递送的其它试剂。 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。
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Patent Agency Ranking
公开(公告)号：US20140161830A1
公开(公告)日：2014-06-12
申请号：US14089603
申请日：2013-11-25
Applicant: Massachusetts Institute of Technology
Inventor： Daniel Griffith Anderson , Kathryn Ann Whitehead , Joseph R. Dorkin , Arturo Jose Vegas , Yunlong Zhang
IPC: C07C229/26 , A61K31/4965 , A61K31/445 , A61K31/40 , A61K31/357 , A61K31/24 , A61K31/225 , C07D487/04 , C07D295/15 , C07D211/34 , C07D207/09 , C07D319/16 , C07C229/34 , C07C229/28 , C07C229/24 , A61K45/06 , C07D241/04 , A61K31/4985
CPC classification number: A61K47/22 , A61K9/1272 , A61K9/5123 , A61K31/225 , A61K31/357 , A61K31/40 , A61K31/445 , A61K31/495 , A61K31/4985 , A61K31/573 , A61K31/704 , A61K31/713 , A61K45/06 , A61K47/18 , A61K47/542 , A61K47/543 , A61K47/6925 , C07C225/06 , C07C229/12 , C07C229/14 , C07C229/24 , C07C229/26 , C07C229/28 , C07C229/34 , C07C2601/14 , C07D207/09 , C07D211/14 , C07D211/26 , C07D211/34 , C07D241/04 , C07D295/13 , C07D295/15 , C07D295/16 , C07D319/16 , C07D319/18 , C07D487/04 , C12N15/111 , C12N15/1137 , C12N15/88 , C12N2310/14 , C12N2320/32 , A61K2300/00
Abstract: Provided herein are lipidoids that may be prepared from the conjugate addition of alkylamines to acrylates. In some embodiments, provided lipidoids are biodegradable and may be used in a variety of drug delivery systems. Given the amino moiety of the lipidoids, they are well-suited for the delivery of polynucleotides, in addition to other agents. Nanoparticles containing the inventive lipidoids and polynucleotides have been prepared and have been shown to be effective in delivering siRNA.
Abstract translation: 本文提供的是可以通过将烷基胺偶联加成丙烯酸酯制备的类脂。 在一些实施方案中，提供的类脂质是可生物降解的并且可以用于多种药物递送系统中。 考虑到类固醇的氨基部分，除了其它药剂之外，它们非常适合于递送多核苷酸。 已经制备了含有本发明的类脂和多核苷酸的纳米颗粒，并且已显示其在递送siRNA方面是有效的。
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公开(公告)号：US20230061974A1
公开(公告)日：2023-03-02
申请号：US17939528
申请日：2022-09-07
Applicant: Massachusetts Institute of Technology
IPC: A61K47/18 , A61K9/19 , A61K31/7088 , A61K9/00 , C12N15/88 , C08G73/02 , A61K9/12 , A61K47/32 , A61K47/34 , C08G63/685
Abstract: Provided herein are branched poly(beta-amino esters) (PBAE) useful as vehicles for the delivery of therapeutic agents, such as nucleic acids. The disclosed polymers form stable compositions, and are suitable for the delivery of therapeutic agents via nebulization. Compositions of the disclosed polymers are capable of delivering therapeutic agents such as mRNA to lung epithelial cells.
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公开(公告)号：US11464860B2
公开(公告)日：2022-10-11
申请号：US16170318
申请日：2018-10-25
Applicant: Massachusetts Institute of Technology
IPC: A61K47/18 , A61K9/19 , A61K31/7088 , A61K9/00 , C12N15/88 , C08G73/02 , A61K9/12 , A61K47/32 , A61K47/34 , C08G63/685 , A61P11/00 , A61K31/7105 , A61K31/711
Abstract: Provided herein are branched poly(beta-amino esters) (PBAE) useful as vehicles for the delivery of therapeutic agents, such as nucleic acids. The disclosed polymers form stable compositions, and are suitable for the delivery of therapeutic agents via nebulization. Compositions of the disclosed polymers are capable of delivering therapeutic agents such as mRNA to lung epithelial cells.
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公开(公告)号：US20220204654A1
公开(公告)日：2022-06-30
申请号：US17602558
申请日：2020-04-24
Applicant: Massachusetts Institute of Technology
Inventor： Chandrabali Bhattacharya , Robert S. Langer , Daniel Griffith Anderson , Arijit Basu
Abstract: Provided herein are new cyclodextrin-based compounds, and pharmaceutically acceptable salts, stereoisomers, and isotopically labeled derivatives thereof, which are capable of binding sugars (e.g., glucose). The compounds provided herein may be conjugated to agents or tags (e.g., therapeutic agents such as insulin) to form conjugates. In another aspect, also provided herein are pharmaceutical compositions comprising the compounds and conjugates described herein. The compounds and conjugates described herein are capable of binding glucose; therefore, provided herein are methods of sensing or detecting glucose comprising contacting glucose with the compound or conjugate. In another aspect, also provided herein are methods of treating a disease (e.g., a metabolic disorder, such as diabetes) in a subject comprising administering to the subject a compound, conjugate, or composition provided herein.
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公开(公告)号：US11041069B2
公开(公告)日：2021-06-22
申请号：US16179698
申请日：2018-11-02
Inventor： Umberto Capasso Palmiero , James C. Kaczmarek , Daniel Griffith Anderson , Davide Moscatelli
Abstract: Disclosed are methods, compositions, reagents, systems, and kits to prepare and utilize poly (β-amino ester) (PBAE) polymers, which are synthesized via Michael addition reactions of diacrylates and amines disclosed herein. Various embodiments utilize lactones and lactone derivatives to generate the diacrylate compounds. The PBAE polymers are shown to be effective biodegradable carriers for the delivery of an agent such as an organic molecule, inorganic molecule, nucleic acid, protein, peptide, polynucleotide, targeting agent, an isotopically labeled chemical compound, vaccine, or an immunological agent.
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