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1. 发明授权

US07897647B2 Releasable polymeric conjugates based on aliphatic biodegradable linkers 失效
标题翻译：基于脂肪族可生物降解接头的可释放聚合物共轭物
公开(公告)号：US07897647B2
公开(公告)日：2011-03-01
申请号：US11502108
申请日：2006-08-09
申请人： Hong Zhao , Richard B. Greenwald , Annapurna Pendri
发明人： Hong Zhao , Richard B. Greenwald , Annapurna Pendri
IPC分类号： A01N33/08
CPC分类号： C07D333/34 , A61K38/00 , A61K47/60 , C07C271/16 , C07C271/20 , C07C271/22 , C07C317/28 , C07D207/452 , C07D277/16 , C07K14/43595
摘要： Activated polymeric bicine derivatives such as as well as conjugates made therewith are disclosed. Methods of making and using the bicine derivatives are also disclosed.
摘要翻译：公开了活性聚合物双金属衍生物，以及由其制备的缀合物。还公开了制备和使用双金属衍生物的方法。

2. 发明授权

US07273845B2 Polymeric prodrugs of vancomycin 失效
标题翻译：万古霉素的聚合物前药
公开(公告)号：US07273845B2
公开(公告)日：2007-09-25
申请号：US10705743
申请日：2003-11-11
申请人： Hong Zhao , Richard B. Greenwald
发明人： Hong Zhao , Richard B. Greenwald
IPC分类号： A61K38/16 , A61K38/14
CPC分类号： C07K9/008 , A61K38/00 , A61K47/60
摘要： Methods of preparing vancomycin-polymer conjugates are disclosed. In preferred aspects, polymer residues which are preferably releasable, are selectively attached to the sugar amino and/or N-methyl amino groups of vancomycin and related compounds. Vancomycin-polymer conjugates made by the methods and methods of treatment using the conjugates are also disclosed.
摘要翻译：公开了万古霉素 - 聚合物共轭物的制备方法。在优选的方面，优选可释放的聚合物残基选择性地连接到万古霉素和相关化合物的糖氨基和/或N-甲基氨基。还公开了通过使用共轭物的方法和方法制备的万古霉素 - 聚合物缀合物。

3. 发明申请

US20090221471A1 PRODRUGS OF VANCOMYCIN WITH HYDROLYSIS RESISTANT POLYMER LINKAGES 审中-公开
标题翻译：具有抗水解聚合物链接的VANCOMYCIN的产品
公开(公告)号：US20090221471A1
公开(公告)日：2009-09-03
申请号：US12275775
申请日：2008-11-21
申请人： Richard B. Greenwald , Hong Zhao
发明人： Richard B. Greenwald , Hong Zhao
IPC分类号： A61K38/14 , C07K9/00 , A61P31/04
CPC分类号： A61K47/641 , A61K47/60
摘要： Vancomycin-polymer conjugates are disclosed. In preferred aspects, polymer residues which are hydrolysis resistant in vitro, are selectively attached to the sugar amino and/or N-methyl amino groups of vancomycin and related compounds. Vancomycin-polymer conjugates made by the methods and methods of treatment using the conjugates are also disclosed.
摘要翻译：公开了万古霉素 - 聚合物共轭物。在优选的方面，体外耐水解的聚合物残基选择性地连接到万古霉素和相关化合物的糖氨基和/或N-甲基氨基上。还公开了通过使用共轭物的方法和方法制备的万古霉素 - 聚合物缀合物。

4. 发明授权

US07332164B2 Heterobifunctional polymeric bioconjugates 失效
标题翻译：异双功能聚合物生物共轭物
公开(公告)号：US07332164B2
公开(公告)日：2008-02-19
申请号：US10394393
申请日：2003-03-21
申请人： Richard B. Greenwald , Hong Zhao
发明人： Richard B. Greenwald , Hong Zhao
IPC分类号： A61K47/48 , A61K38/00
CPC分类号： A61K49/0041 , A61K47/60 , A61K49/0047
摘要： Heterobifunctional polymeric prodrug platforms for delivering biologically active compounds, including proteins, monoclonal antibodies and the like are disclosed. One preferred compound is Methods of making and using the compounds and conjugates described herein are also provided.
摘要翻译：公开了用于递送生物活性化合物（包括蛋白质，单克隆抗体等）的异双功能聚合物前药平台。一种优选的化合物是还提供制备和使用本文所述的化合物和缀合物的方法。

5. 发明授权

US06624142B2 Trimethyl lock based tetrapartate prodrugs 失效
标题翻译：基于三甲基锁的四聚物前药
公开(公告)号：US06624142B2
公开(公告)日：2003-09-23
申请号：US09852335
申请日：2001-05-09
申请人： Richard B. Greenwald , Hong Zhao
发明人： Richard B. Greenwald , Hong Zhao
IPC分类号： A61K31222
CPC分类号： C07C237/22 , A61K47/60 , C07B2200/11 , C07C271/16 , C07C271/22 , C07C271/48
摘要： The invention is directed primarily to compounds of Formula I: wherein: R1 is a polymeric residue; L1 is a bifunctional linking group; Y1 and Y2 are independently O, S or NR7; R2-7 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; D is a moiety that is a leaving group or a residue of a compound to be delivered into a cell; Z is selected from the group consisting of: a moiety that is actively transported into a target cell, a hydrophobic moiety, and combinations thereof; Ar is a moiety which when included in Formula (I) forms a multi-substituted aromatic hydrocarbon or a multi-substituted heterocyclic group; and (y) is a positive integer greater than or equal to 1. Methods of making and using the same are also disclosed.
摘要翻译：本发明主要针对式I化合物：其中：R1是无规残基; L1是双官能连接基团; Y 1和Y 2独立地是O，S或NR 7; R 2-7独立地选自氢，C1 C6烷基，C3-12支链烷基，C3-8环烷基，C1-6取代烷基，C3-8取代环烷基，芳基，取代芳基，芳烷基，C1-6杂烷基，取代C1-6杂烷基，C1-6烷氧基，苯氧基和C 1-6杂烷氧基; D是作为离开基团或待递送至细胞中的化合物的残基的部分; Z选自：主动转运入靶细胞的部分，疏水部分及其组合; Ar是当式（I）中包含时形成多取代芳族烃或多取代杂环基的部分; 和（y）是大于或等于1的正整数。还公开了制造和使用它们的方法。

6. 发明授权

US5965566A High molecular weight polymer-based prodrugs 失效
标题翻译：高分子量聚合物基前药
公开(公告)号：US5965566A
公开(公告)日：1999-10-12
申请号：US914927
申请日：1997-08-20
申请人： Richard B. Greenwald , Annapurna Pendri , Hong Zhao
发明人： Richard B. Greenwald , Annapurna Pendri , Hong Zhao
IPC分类号： A61K31/335 , A61K47/48 , C07D305/14 , C07D491/22 , C08G65/329 , A61K31/44
CPC分类号： A61K47/48215 , A61K31/335 , C07D305/14 , C08G65/329
摘要： The present invention is directed compositions of the formula: ##STR1## wherein: D is a residue of biologically active moiety;X is an electron withdrawing group;Y and Y' are independently O or S;(n) is zero (0) or a positive integer, preferably from 1 to about 12;wherein: R.sub.1 and R.sub.2 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls and substituted C.sub.1-6 alkyls;wherein: R.sub.3 is a substantially non-antigenic polymer, C.sub.1-12 straight or branched alkyl or substituted allyl, C.sub.5-8 cycloalkyl or substituted cycloalkyl, carboxyalkyl, carboalkoxy alkyl, dialkylaminoalkyl, phenylalkyl, phenylaryl or ##STR2## wherein: R.sub.4 and R.sub.5 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls, and substituted C.sub.1-6 alkyls or jointly form a cyclic C.sub.5 -C.sub.7 ring. In preferred embodiments, the prodrugs contain a polyethylene glycol having a molecular weight of at least about 20,000.
摘要翻译：本发明涉及下式的组合物：其中：D是生物活性部分的残基; X是吸电子基团; Y和Y'独立地为O或S; （n）为零（0）或正整数，优选1至约12; 其中：R 1和R 2独立地选自H，C 1-6烷基，芳基，取代的芳基，芳烷基，杂烷基，取代的杂烷基和取代的C 1-6烷基; 其中：R3是基本上非抗原性的聚合物，C1-12直链或支链烷基或取代的烯丙基，C5-8环烷基或取代的环烷基，羧基烷基，烷氧基烷基，二烷基氨基烷基，苯基烷基，苯基芳基或其中：R4和R5独立地选自由H，C 1-6烷基，芳基，取代的芳基，芳烷基，杂烷基，取代的杂烷基和取代的C 1-6烷基组成的基团或共同形成环状C 5 -C 7环。在优选的实施方案中，前药包含分子量为至少约20,000的聚乙二醇。

7. 发明授权

US07595304B2 Polymeric oligonucleotide prodrugs 失效
标题翻译：聚合寡核苷酸前药
公开(公告)号：US07595304B2
公开(公告)日：2009-09-29
申请号：US10822205
申请日：2004-04-09
申请人： Hong Zhao , Richard B. Greenwald
发明人： Hong Zhao , Richard B. Greenwald
IPC分类号： A61K31/70 , C07H21/04
CPC分类号： C07H19/10 , C07H19/20 , C07H21/00
摘要： Polymer conjugates containing nucleotides and/or oligonucleotides are disclosed.
摘要翻译：公开了含有核苷酸和/或寡核苷酸的聚合物缀合物。

8. 发明授权

US06824766B2 Biodegradable high molecular weight polymeric linkers and their conjugates 失效
标题翻译：可生物降解的高分子量聚合物接头及其共轭物
公开(公告)号：US06824766B2
公开(公告)日：2004-11-30
申请号：US09888072
申请日：2001-06-22
申请人： Richard B. Greenwald , Hong Zhao
发明人： Richard B. Greenwald , Hong Zhao
IPC分类号： A61K31785
CPC分类号： A61K47/60
摘要： The present invention includes polymeric transport systems corresponding to the formula: wherein: R31 is a linear or branched polymer residue; Y10 and Y11 are independently O, S, or NR40; X2 is O, S or NR41; R32-35, R37-41, R50 and R51 are independently selected among hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls and substituted C1-6 heteroalkyls; a, b and e are each independently selected positive integers; L is an amino acid residue or a bifunctional linker; X3 is wherein Y12 and Y13 are independently O, S, or NR41; Z is a bond, a moiety that is actively transported into a target cell, a hydrophobic moiety or combinations thereof; D1 and D2 are OH, a residue of a hydroxyl, a residue of an amine-containing moiety or a leaving group; and y1 and y2 are independently selected positive integers.
摘要翻译：本发明包括对应于下式的聚合物输送系统：其中：R 31是直链或支链聚合物残基; Y10和Y11独立地为O，S或NR40; X2是O，S或NR41; R32-35，R37-41，R50和R51独立地选自氢，C1-6烷基，C3-12支链烷基，C3-8环烷基，C1-6取代的烷基，C3-8取代的环烷基，芳基，取代的芳基，芳烷基，C 1-6杂烷基和取代的C 1-6杂烷基; a，b和e各自独立选择正整数; L是氨基酸残基或双功能连接体; X3中Y12和Y13独立地为O，S或NR41; Z是一个键，一个主要被运送到靶细胞中的部分，一个疏水部分或它们的组合; D1和D2是OH，羟基的残基，含胺部分的残基或离去基团; y1和y2是独立选择的正整数。

9. 发明授权

US06649778B1 Methods of preparing amino acid taxane derivatives and polymer conjugates containing the same 失效
标题翻译：制备氨基酸紫杉烷衍生物和含有它们的聚合物共轭物的方法
公开(公告)号：US06649778B1
公开(公告)日：2003-11-18
申请号：US10252024
申请日：2002-09-20
申请人： Hong Zhao , Richard B. Greenwald
发明人： Hong Zhao , Richard B. Greenwald
IPC分类号： C07D30514
CPC分类号： C07D409/12 , C07D305/14
摘要： Methods of preparing amino acid-substituted taxanes such as: using selected blocked amino acids are disclosed. After coupling of the blocked amino acid to the taxane, deprotection is carried out with about an equimolar amount of a secondary amine thus substantially avoiding base-catalyzed hydrolysis of amino acid from the taxane. The preferred amino acid-taxanes are useful as intermediates in the production of polymer conjugated therapeutic compositions or as part of pharmaceutically acceptable formulations.
摘要翻译：公开了制备氨基酸取代的紫杉烷的方法，例如：使用选择的封闭的氨基酸。在封闭的氨基酸与紫杉烷偶联之后，用约等摩尔量的仲胺进行脱保护，因此基本上避免了氨基酸从紫杉烷中的碱催化的水解。优选的氨基酸 - 紫杉烷可用作生产聚合物缀合的治疗组合物或作为药学上可接受的制剂的一部分的中间体。

10. 发明授权

US06608076B1 Camptothecin derivatives and polymeric conjugates thereof 失效
标题翻译：喜树碱衍生物及其聚合物共轭物
公开(公告)号：US06608076B1
公开(公告)日：2003-08-19
申请号：US10147168
申请日：2002-05-16
申请人： Richard B. Greenwald , Hong Zhao
发明人： Richard B. Greenwald , Hong Zhao
IPC分类号： A61K314745
CPC分类号： C07D471/14 , A61K47/55 , A61K47/60
摘要： Polymeric conjugates of camptothecin derivatives having increased circulating half-lives are disclosed. In preferred aspects, the E ring lactone of the camptothecin derivative is opened and functionalized to allow attachment of a polymer such as PEG in the 17- or 20-position thereof. A representative example of such compounds is Methods of preparing and using the same are also disclosed.
摘要翻译：公开了具有增加的循环半衰期的喜树碱衍生物的聚合物共轭物。在优选的方面，喜树碱衍生物的E环内酯被打开并官能化以允许聚合物如PEG在其17或20位的附着。这些化合物的代表性实例也是公开了制备和使用它们的方法。

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