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1.发明申请VITAMIN FUNCTIONALIZED GEL-FORMING BLOCK COPOLYMERS FOR BIOMEDICAL APPLICATIONS 有权维生素功能化凝胶形成用于生物医学应用的嵌段共聚物公开(公告)号：US20150231257A1
公开(公告)日：2015-08-20
申请号：US14697878
申请日：2015-04-28
IPC分类号： A61K47/34 , C08G65/331 , A61K31/65 , A61K31/765 , A61K31/4196
CPC分类号： C08G64/183 , A61K9/0024 , A61K9/06 , A61K31/355 , A61K31/592 , A61K31/593 , A61K47/34 , A61K47/551 , A61K47/60 , A61K2039/505 , A61K2039/54 , A61P35/00 , C07K16/32 , C07K2317/24 , C07K2317/73 , C07K2317/76 , C07K2317/90 , C08G65/3318 , C08G2210/00 , Y02A50/473
摘要： Gel-forming block copolymers were prepared comprising i) a central hydrophilic block consisting essentially of a divalent poly(ethylene oxide) chain and ii) two peripheral monocarbonate or polycarbonate hydrophobic blocks. The hydrophobic blocks comprise one or more vitamin-bearing subunits. The vitamin-bearing subunits comprise a carbonate backbone portion and a side chain comprising a covalently bound form of a vitamin. The gel-forming block copolymers can be used to prepare various biodegradable and/or biocompatible hydrogel and organogel drug compositions, in particular antimicrobial and/or anti-tumor drug compositions. The hydrogel compositions can be suitable for depot injections. Synergistic enhancement of toxicity to microbes was observed with compositions comprising an antimicrobial cationic polymer and an antimicrobial compound.
摘要翻译： 制备凝胶形成嵌段共聚物，其包括：i）主要由二价聚（环氧乙烷）链和ii）两个周边单碳酸酯或聚碳酸酯疏水嵌段组成的中心亲水嵌段。 疏水性嵌段包含一种或多种含有维生素的亚基。 含维生素的亚基包含碳酸酯主链部分和包含共价结合形式的维生素的侧链。 凝胶形成嵌段共聚物可用于制备各种可生物降解和/或生物相容的水凝胶和有机凝胶药物组合物，特别是抗微生物和/或抗肿瘤药物组合物。 水凝胶组合物可适用于贮存注射。 用包含抗微生物阳离子聚合物和抗微生物化合物的组合物观察到对微生物的毒性的协同增强。
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2.发明授权Vitamin functionalized gel-forming block copolymers for biomedical applications 有权用于生物医学应用的维生素官能化凝胶形成嵌段共聚物公开(公告)号：US09040034B2
公开(公告)日：2015-05-26
申请号：US13859062
申请日：2013-04-09
CPC分类号： C08G64/183 , A61K9/0024 , A61K9/06 , A61K31/355 , A61K31/592 , A61K31/593 , A61K47/34 , A61K47/551 , A61K47/60 , A61K2039/505 , A61K2039/54 , A61P35/00 , C07K16/32 , C07K2317/24 , C07K2317/73 , C07K2317/76 , C07K2317/90 , C08G65/3318 , C08G2210/00 , Y02A50/473
摘要： Gel-forming block copolymers were prepared comprising i) a central hydrophilic block consisting essentially of a divalent poly(ethylene oxide) chain and ii) two peripheral monocarbonate or polycarbonate hydrophobic blocks. The hydrophobic blocks comprise one or more vitamin-bearing subunits. The vitamin-bearing subunits comprise a carbonate backbone portion and a side chain comprising a covalently bound form of a vitamin. The gel-forming block copolymers can be used to prepare various biodegradable and/or biocompatible hydrogel and organogel drug compositions, in particular antimicrobial and/or anti-tumor drug compositions. The hydrogel compositions can be suitable for depot injections. Synergistic enhancement of toxicity to microbes was observed with compositions comprising an antimicrobial cationic polymer and an antimicrobial compound.
摘要翻译： 制备凝胶形成嵌段共聚物，其包括：i）主要由二价聚（环氧乙烷）链和ii）两个周边单碳酸酯或聚碳酸酯疏水嵌段组成的中心亲水嵌段。 疏水性嵌段包含一种或多种含有维生素的亚基。 含维生素的亚基包含碳酸酯主链部分和包含共价结合形式的维生素的侧链。 凝胶形成嵌段共聚物可用于制备各种可生物降解和/或生物相容的水凝胶和有机凝胶药物组合物，特别是抗微生物和/或抗肿瘤药物组合物。 水凝胶组合物可适用于贮存注射。 用包含抗微生物阳离子聚合物和抗微生物化合物的组合物观察到对微生物的毒性的协同增强。
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公开(公告)号：US09987369B2
公开(公告)日：2018-06-05
申请号：US15340795
申请日：2016-11-01
发明人： Wei Cheng , Mareva B. Fevre , James L. Hedrick , Nor Lizawati Ibrahim , Ashlynn L. Z. Lee , Victor W. L. Ng , Robert J. Ono , Chuan Yang , Yi Yan Yang
IPC分类号： A61K39/395 , A61K31/65 , A61K31/4196 , A61K45/06 , A61K9/00 , A61K9/06 , A61K31/592 , A61K31/355 , C08G64/18 , C07K16/32 , A61K47/48 , A61K31/455
CPC分类号： A61K47/6903 , A61K9/0014 , A61K9/0024 , A61K9/06 , A61K31/355 , A61K31/4196 , A61K31/455 , A61K31/592 , A61K31/65 , A61K39/39558 , A61K45/06 , A61K47/22 , A61K47/34 , A61K47/48192 , A61K47/48784 , A61K47/59 , C07K16/32 , C08G64/183 , C08G2210/00
摘要： Gel-forming block copolymers were prepared comprising i) a central hydrophilic block consisting essentially of a divalent poly(ethylene oxide) chain and ii) two peripheral monocarbonate or polycarbonate hydrophobic blocks linked to the central block by linking groups bearing one or more hydrogen bond forming *—N(H)—* groups. The hydrophobic blocks comprise one or more vitamin-bearing subunits. The gel-forming block copolymers can be used to prepare various biodegradable and/or biocompatible hydrogel and organogel drug compositions, in particular antimicrobial and/or anti-tumor drug compositions. The hydrogel compositions have utility in depot injections for drug delivery. The hydrogen bonding *—N(H)—* group(s) provide longer in vivo lifetime of the hydrogel before degradation and a more prolonged and controlled release rate of a hydrophobic drug compared to similar hydrogels prepared from poly(ethylene glycol).
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公开(公告)号：US20140301967A1
公开(公告)日：2014-10-09
申请号：US13859037
申请日：2013-04-09
发明人： Willy Chin , Daniel J. Coady , Richard A. Dipietro , Amanda C. Engler , James L. Hedrick , Ashlynn L. Z. Lee , Victor W. L. Ng , Zhan-Yuin Ong , Yi Yan Yang
IPC分类号： A61K31/785 , A61K31/80
CPC分类号： A61K31/785 , A01N33/12 , A61K31/80 , C08G64/0241 , Y02A50/473 , A01N25/10
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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公开(公告)号：US09999633B2
公开(公告)日：2018-06-19
申请号：US13859037
申请日：2013-04-09
发明人： Willy Chin , Daniel J. Coady , Amanda C. Engler , James L. Hedrick , Ashlynn L. Z. Lee , Victor W. L. Ng , Zhan-Yuin Ong , Yi Yan Yang
IPC分类号： A61K31/785 , A61K31/80 , C08G64/02 , A01N33/12
CPC分类号： A61K31/785 , A01N33/12 , A61K31/80 , C08G64/0241 , Y02A50/473 , A01N25/10
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：US09511146B2
公开(公告)日：2016-12-06
申请号：US14697878
申请日：2015-04-28
IPC分类号： A61K47/34 , A61K31/765 , A61K31/4196 , A61K31/65 , C08G65/331
CPC分类号： C08G64/183 , A61K9/0024 , A61K9/06 , A61K31/355 , A61K31/592 , A61K31/593 , A61K47/34 , A61K47/551 , A61K47/60 , A61K2039/505 , A61K2039/54 , A61P35/00 , C07K16/32 , C07K2317/24 , C07K2317/73 , C07K2317/76 , C07K2317/90 , C08G65/3318 , C08G2210/00 , Y02A50/473
摘要： Gel-forming block copolymers were prepared comprising i) a central hydrophilic block consisting essentially of a divalent poly(ethylene oxide) chain and ii) two peripheral monocarbonate or polycarbonate hydrophobic blocks. The hydrophobic blocks comprise one or more vitamin-bearing subunits. The vitamin-bearing subunits comprise a carbonate backbone portion and a side chain comprising a covalently bound form of a vitamin. The gel-forming block copolymers can be used to prepare various biodegradable and/or biocompatible hydrogel and organogel drug compositions, in particular antimicrobial and/or anti-tumor drug compositions. The hydrogel compositions can be suitable for depot injections. Synergistic enhancement of toxicity to microbes was observed with compositions comprising an antimicrobial cationic polymer and an antimicrobial compound.
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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：US20180228835A1
公开(公告)日：2018-08-16
申请号：US15954776
申请日：2018-04-17
发明人： Willy Chin , Daniel J. Coady , Richard A. Dipietro , Amanda C. Engler , James L. Hedrick , Ashlynn L. Z. Lee , Victor W. L. Ng , Zhan-Yuin Ong , Yi Yan Yang
IPC分类号： A61K31/785 , C08G64/02 , A01N25/10 , A01N33/12 , A61K31/80
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：US09951179B2
公开(公告)日：2018-04-24
申请号：US15436955
申请日：2017-02-20
发明人： Mareva B. Fevre , James L. Hedrick , Victor W. L. Ng , Robert J. Ono , Shrinivas Venkataraman , Yi Yan Yang
IPC分类号： C07D273/01 , C08G64/02 , C07D323/00 , C08G64/30 , A01N47/06 , A01N43/72
CPC分类号： C07D323/00 , A01N47/06 , C07D273/01 , C08G64/0241 , C08G64/30
摘要： Eight-membered ring cyclic carbonates having an oxygen or an acylated nitrogen at position 6 were prepared by reaction of precursor diols with ethyl chloroformate. The cyclic carbonates undergo organocatalyzed ring opening polymerization. In one instance, the initial polymer formed comprises a carbonate repeat unit having a Boc-protected nitrogen in the polymer backbone. Deprotecting the nitrogen with acid forms a cationic carbonate repeat unit having a positive charged secondary ammonium nitrogen in the polymer backbone.
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10.发明申请VITAMIN FUNCTIONALIZED GEL-FORMING BLOCK COPOLYMERS FOR BIOMEDICAL APPLICATIONS 有权维生素功能化凝胶形成用于生物医学应用的嵌段共聚物公开(公告)号：US20170051105A1
公开(公告)日：2017-02-23
申请号：US15343537
申请日：2016-11-04
CPC分类号： C08G64/183 , A61K9/0024 , A61K9/06 , A61K31/355 , A61K31/592 , A61K31/593 , A61K47/34 , A61K47/551 , A61K47/60 , A61K2039/505 , A61K2039/54 , A61P35/00 , C07K16/32 , C07K2317/24 , C07K2317/73 , C07K2317/76 , C07K2317/90 , C08G65/3318 , C08G2210/00 , Y02A50/473
摘要： Gel-forming block copolymers were prepared comprising i) a central hydrophilic block consisting essentially of a divalent poly(ethylene oxide) chain and ii) two peripheral monocarbonate or polycarbonate hydrophobic blocks. The hydrophobic blocks comprise one or more vitamin-bearing subunits. The vitamin-bearing subunits comprise a carbonate backbone portion and a side chain comprising a covalently bound form of a vitamin. The gel-forming block copolymers can be used to prepare various biodegradable and/or biocompatible hydrogel and organogel drug compositions, in particular antimicrobial and/or anti-tumor drug compositions. The hydrogel compositions can be suitable for depot injections. Synergistic enhancement of toxicity to microbes was observed with compositions comprising an antimicrobial cationic polymer and an antimicrobial compound.
摘要翻译： 制备凝胶形成嵌段共聚物，其包括：i）主要由二价聚（环氧乙烷）链和ii）两个周边单碳酸酯或聚碳酸酯疏水嵌段组成的中心亲水嵌段。 疏水性嵌段包含一种或多种含有维生素的亚基。 含维生素的亚基包含碳酸酯主链部分和包含共价结合形式的维生素的侧链。 凝胶形成嵌段共聚物可用于制备各种可生物降解和/或生物相容的水凝胶和有机凝胶药物组合物，特别是抗微生物和/或抗肿瘤药物组合物。 水凝胶组合物可适用于贮存注射。 用包含抗微生物阳离子聚合物和抗微生物化合物的组合物观察到对微生物的毒性的协同增强。
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