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公开(公告)号：US20170281662A1
公开(公告)日：2017-10-05
申请号：US15627607
申请日：2017-06-20
申请人： International Business Machines Corporation , Agency For Science, Technology and Research , Universidad del PaÌs Vasco/Euskal Herriko Unibertsitatea
发明人： Julian M. W. Chan , Amanda C. Engler , James L. Hedrick , Haritz Sardon , Jeremy P. K. Tan , Yi Yan Yang
IPC分类号： A61K31/704 , A61K31/713 , A61K9/51
CPC分类号： A61K47/34 , A61K9/5146 , A61K31/704 , A61K31/713 , A61K38/00 , A61K38/16 , C08G64/0241 , C08G64/183 , C08L69/00
摘要： Nanoparticles comprise a drug, a first block polymer and a second block polymer. The first block polymer has a poly(ethylene oxide) (PEO) block and a polycarbonate block bearing a side chain aromatic nitrogen-containing heterocycle (N-heterocycle). The N-heterocycle can be in the form of a base, a hydrosalt of the base, a sulfobetaine adduct of the base, or a combination thereof. The second block polymer has a PEO block and a polycarbonate block bearing a side chain catechol group, which can be present as a catechol, oxidized form of a catechol, and/or a polymerized form of a catechol. The nanoparticles can be dispersed in water and are capable of controlled release of the drug.
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2.发明申请CATIONIC POLYMERS FOR ANTIMICROBIAL APPLICATIONS AND DELIVERY OF BIOACTIVE MATERIALS 有权用于抗生素应用和递送生物材料的阳离子聚合物公开(公告)号：US20140220093A1
公开(公告)日：2014-08-07
申请号：US14246045
申请日：2014-04-05
发明人： Daniel J. Coady , Amanda C. Engler , Kazuki Fukushima , James L. Hedrick , Jeremy P. K. Tan , Yi Yan Yang
IPC分类号： A01N37/44
CPC分类号： A01N37/44 , A01N33/12 , A61K48/0041 , C08G83/004 , C12N15/88 , A01N25/10 , A01N2300/00
摘要： A cationic star polymer is disclosed of the general formula (1): wherein w′ is a positive number greater than or equal to 3, I′ is a dendritic polyester core covalently linked to w′ independent peripheral linear cationic polymer chains P′. Each of the chains P′ comprises a cationic repeat unit comprising i) a backbone functional group selected from the group consisting of aliphatic carbonates, aliphatic esters, aliphatic carbamates, aliphatic ureas, aliphatic thiocarbamates, aliphatic dithiocarbonates, and combinations thereof, and ii) a side chain comprising a quaternary amine group. The quaternary amine group comprises a divalent methylene group directly covalently linked to i) a positive charged nitrogen and ii) an aromatic ring.
摘要翻译： 公开了通式（1）的阳离子星形聚合物：其中w'是大于或等于3的正数，I'是与w'独立的外部线性阳离子聚合物链P'共价连接的树枝状聚酯芯。 每个链P'包含阳离子重复单元，其包含i）选自脂族碳酸酯，脂族酯，脂族氨基甲酸酯，脂族脲，脂族硫代氨基甲酸酯，脂族二硫代碳酸酯及其组合的骨架官能团，和ii） 侧链包含季胺基。 季胺基包括与i）正电荷氮和ii）芳环直接共价连接的二价亚甲基。
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公开(公告)号：US20160081343A1
公开(公告)日：2016-03-24
申请号：US14960752
申请日：2015-12-07
CPC分类号： A01N47/06 , A01N43/72 , C07D273/01 , C08G64/0241 , C08G64/42
摘要： Eight-membered ring cyclic carbonates comprising a ring nitrogen at position 6 (1,3,6-dioxazocan-2-ones) were prepared by reaction of precursor diols with active carbonates. The ring nitrogen is linked to a pendant group Y′ via a methylene linking group. The cyclic carbonates undergo organocatalyzed ring opening polymerization to form an initial polycarbonate comprising a backbone tertiary amine group. Quaternization of the initial polycarbonates forms cationic polycarbonates comprising a positive-charged backbone quaternary nitrogen. The cationic polycarbonates can be potent antimicrobial agents.
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公开(公告)号：US09974303B2
公开(公告)日：2018-05-22
申请号：US14246045
申请日：2014-04-05
发明人： Daniel J. Coady , Amanda C. Engler , Kazuki Fukushima , James L. Hedrick , Jeremy P. K. Tan , Yi Yan Yang
CPC分类号： A01N37/44 , A01N33/12 , A61K48/0041 , C08G83/004 , C12N15/88 , A01N25/10 , A01N2300/00
摘要： A cationic star polymer is disclosed of the general formula (1): wherein w′ is a positive number greater than or equal to 3, I′ is a dendritic polyester core covalently linked to w′ independent peripheral linear cationic polymer chains P′. Each of the chains P′ comprises a cationic repeat unit comprising i) a backbone functional group selected from the group consisting of aliphatic carbonates, aliphatic esters, aliphatic carbamates, aliphatic ureas, aliphatic thiocarbamates, aliphatic dithiocarbonates, and combinations thereof, and ii) a side chain comprising a quaternary amine group. The quaternary amine group comprises a divalent methylene group directly covalently linked to i) a positive charged nitrogen and ii) an aromatic ring.
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公开(公告)号：US20140301968A1
公开(公告)日：2014-10-09
申请号：US13859048
申请日：2013-04-09
发明人： Daniel J. Coady , Richard A. Dipietro , Amanda C. Engler , James L. Hedrick , Victor W. L. Ng , Zhan-Yuin Ong , Jeremy P. K. Tan , Yi Yan Yang
IPC分类号： A01N47/06
CPC分类号： C08G63/64 , A01N33/12 , A01N43/50 , A01N57/34 , A61K9/0019 , A61K31/765 , A61K2800/54 , A61K2800/542 , A61K2800/5426 , C08G64/0233 , C08G64/0241 , C08G64/025 , C08G64/0258 , C08G64/0291 , C08G64/30 , A01N45/00
摘要： Antimicrobial cationic polymers having one or two cationic polycarbonate chains were prepared by organocatalyzed ring opening polymerization. One antimicrobial cationic polymer has a polymer chain consisting essentially of cationic carbonate repeat units linked to one or two end groups. The end groups can comprise a covalently bound form of biologically active compound such as cholesterol. Other antimicrobial cationic polymers have a random copolycarbonate chain comprising a minor mole fraction of hydrophobic repeat units bearing a covalently bound form of a vitamin E and/or vitamin D2. The cationic polymers exhibit high activity and selectivity against Gram-negative and Gram-positive microbes and fungi.
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公开(公告)号：US09622476B2
公开(公告)日：2017-04-18
申请号：US14960752
申请日：2015-12-07
IPC分类号： A01N47/06 , C07D273/01 , C08G64/02 , C08G64/42 , A01N43/72
CPC分类号： A01N47/06 , A01N43/72 , C07D273/01 , C08G64/0241 , C08G64/42
摘要： Eight-membered ring cyclic carbonates comprising a ring nitrogen at position 6 (1,3,6-dioxazocan-2-ones) were prepared by reaction of precursor diols with active carbonates. The ring nitrogen is linked to a pendant group Y′ via a methylene linking group. The cyclic carbonates undergo organocatalyzed ring opening polymerization to form an initial polycarbonate comprising a backbone tertiary amine group. Quaternization of the initial polycarbonates forms cationic polycarbonates comprising a positive-charged backbone quaternary nitrogen. The cationic polycarbonates can be potent antimicrobial agents.
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公开(公告)号：US20150157723A1
公开(公告)日：2015-06-11
申请号：US14097488
申请日：2013-12-05
申请人： International Business Machines Corporation , Universidad del Pais Vasco/Euskal Herriko Unibertsitatea , Agency For Science, Technology and Research
发明人： Julian M. W. Chan , Amanda C. Engler , James L. Hedrick , Xiyu Ke , Victor W.L. Ng , Haritz Sardon , Jeremy P. K. Tan , Yi Yan Yang
IPC分类号： A61K47/34 , A61K31/713 , A61K31/704 , A61K38/16
CPC分类号： A61K47/34 , A61K9/5146 , A61K31/704 , A61K31/713 , A61K38/00 , A61K38/16 , C08G64/0241 , C08G64/183 , C08L69/00
摘要： Nanoparticles comprise a drug, a first block polymer and a second block polymer. The first block polymer has a poly(ethylene oxide) (PEO) block and a polycarbonate block bearing a side chain aromatic nitrogen-containing heterocycle (N-heterocycle). The N-heterocycle can be in the form of a base, a hydrosalt of the base, a sulfobetaine adduct of the base, or a combination thereof. The second block polymer has a PEO block and a polycarbonate block bearing a side chain catechol group, which can be present as a catechol, oxidized form of a catechol, and/or a polymerized form of a catechol. The nanoparticles can be dispersed in water and are capable of controlled release of the drug.
摘要翻译： 纳米颗粒包含药物，第一嵌段聚合物和第二嵌段聚合物。 第一嵌段聚合物具有聚（环氧乙烷）（PEO）嵌段和带有侧链芳香族含氮杂环（N-杂环）的聚碳酸酯嵌段）。 N-杂环可以是碱的形式，碱的氢盐，碱的磺基甜菜碱加合物或其组合。 第二嵌段聚合物具有PEO嵌段和带有侧链儿茶酚基团的聚碳酸酯嵌段，其可以儿茶酚，氧化形式的儿茶酚和/或邻苯二酚的聚合形式存在。 纳米颗粒可以分散在水中并且能够控制释放药物。
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公开(公告)号：US09717797B2
公开(公告)日：2017-08-01
申请号：US14097488
申请日：2013-12-05
申请人： International Business Machines Corporation , Agency For Science, Technology and Research , Universidad del Pais Vasco/Euskal Herriko Unibertsitatea
发明人： Julian M. W. Chan , Amanda C. Engler , James L. Hedrick , Xiyu Ke , Victor W. L. Ng , Haritz Sardon , Jeremy P. K. Tan , Yi Yan Yang
IPC分类号： A61K9/00 , A61K47/34 , A61K31/704 , A61K31/713 , A61K9/51 , C08G64/02 , C08G64/18 , A61K38/16 , A61K38/00
CPC分类号： A61K47/34 , A61K9/5146 , A61K31/704 , A61K31/713 , A61K38/00 , A61K38/16 , C08G64/0241 , C08G64/183 , C08L69/00
摘要： Nanoparticles comprise a drug, a first block polymer and a second block polymer. The first block polymer has a poly(ethylene oxide) (PEO) block and a polycarbonate block bearing a side chain aromatic nitrogen-containing heterocycle (N-heterocycle). The N-heterocycle can be in the form of a base, a hydrosalt of the base, a sulfobetaine adduct of the base, or a combination thereof. The second block polymer has a PEO block and a polycarbonate block bearing a side chain catechol group, which can be present as a catechol, oxidized form of a catechol, and/or a polymerized form of a catechol. The nanoparticles can be dispersed in water and are capable of controlled release of the drug.
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公开(公告)号：US09631050B2
公开(公告)日：2017-04-25
申请号：US15154948
申请日：2016-05-14
发明人： Daniel J. Coady , Richard A. Dipietro , Amanda C. Engler , James L. Hedrick , Victor W. L. Ng , Zhan-Yuin Ong , Jeremy P. K. Tan , Yi Yan Yang
IPC分类号： A61K31/00 , C08G63/64 , A01N33/12 , A01N43/50 , A01N57/34 , A61K9/00 , A61K31/765 , A61K47/48
CPC分类号： C08G63/64 , A01N33/12 , A01N43/50 , A01N57/34 , A61K9/0019 , A61K31/765 , A61K2800/54 , A61K2800/542 , A61K2800/5426 , C08G64/0233 , C08G64/0241 , C08G64/025 , C08G64/0258 , C08G64/0291 , C08G64/30 , A01N45/00
摘要： Antimicrobial cationic polymers having one or two cationic polycarbonate chains were prepared by organocatalyzed ring opening polymerization. One antimicrobial cationic polymer has a polymer chain consisting essentially of cationic carbonate repeat units linked to one or two end groups. The end groups can comprise a covalently bound form of biologically active compound such as cholesterol. Other antimicrobial cationic polymers have a random copolycarbonate chain comprising a minor mole fraction of hydrophobic repeat units bearing a covalently bound form of a vitamin E and/or vitamin D2. The cationic polymers exhibit high activity and selectivity against Gram-negative and Gram-positive microbes and fungi.
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公开(公告)号：US09357772B2
公开(公告)日：2016-06-07
申请号：US13859048
申请日：2013-04-09
发明人： Daniel J. Coady , Richard A. Dipietro , Amanda C. Engler , James L. Hedrick , Victor W. L. Ng , Zhan-Yuin Ong , Jeremy P. K. Tan , Yi Yan Yang
CPC分类号： C08G63/64 , A01N33/12 , A01N43/50 , A01N57/34 , A61K9/0019 , A61K31/765 , A61K2800/54 , A61K2800/542 , A61K2800/5426 , C08G64/0233 , C08G64/0241 , C08G64/025 , C08G64/0258 , C08G64/0291 , C08G64/30 , A01N45/00
摘要： Antimicrobial cationic polymers having one or two cationic polycarbonate chains were prepared by organocatalyzed ring opening polymerization. One antimicrobial cationic polymer has a polymer chain consisting essentially of cationic carbonate repeat units linked to one or two end groups. The end groups can comprise a covalently bound form of biologically active compound such as cholesterol. Other antimicrobial cationic polymers have a random copolycarbonate chain comprising a minor mole fraction of hydrophobic repeat units bearing a covalently bound form of a vitamin E and/or vitamin D2. The cationic polymers exhibit high activity and selectivity against Gram-negative and Gram-positive microbes and fungi.
摘要翻译： 通过有机催化开环聚合制备具有一个或两个阳离子聚碳酸酯链的抗微生物阳离子聚合物。 一种抗微生物阳离子聚合物具有基本上由连接到一个或两个端基的阳离子碳酸酯重复单元组成的聚合物链。 末端基团可包含共价结合形式的生物活性化合物如胆固醇。 其它抗微生物阳离子聚合物具有无规共聚碳酸酯链，其包含具有共价结合形式的维生素E和/或维生素D2的疏水重复单元的较小摩尔分数。 阳离子聚合物对革兰氏阴性和革兰氏阳性微生物和真菌表现出高活性和选择性。
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