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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. 发明授权

US06177087B1 Non-antigenic amine derived polymers and polymer conjugates 失效
标题翻译：非抗原胺衍生的聚合物和聚合物共轭物
公开(公告)号：US06177087B1
公开(公告)日：2001-01-23
申请号：US09184910
申请日：1998-11-03
申请人： Richard B. Greenwald , Anthony Martinez , Annapurna Pendri
发明人： Richard B. Greenwald , Anthony Martinez , Annapurna Pendri
IPC分类号： A61K4500
CPC分类号： C08G65/3331 , A61K47/60 , C07K14/805 , C08G65/329 , C08G65/33303 , Y10S526/936 , Y10S530/815
摘要： Substantially non-antigenic polymers containing pI and/or pH optimum modulating moieties are disclosed. The polymers are useful as intermediates for synthesis of amine-based polymers and in the formation of activated polymers for conjugation with nucleophiles. Conjugates and methods of preparation and treatment with the conjugates are also disclosed.
摘要翻译：公开了含有pI和/或pH最佳调节部分的基本非抗原性聚合物。聚合物可用作合成基于胺的聚合物的中间体和用于与亲核试剂缀合的活化聚合物的形成。还公开了共轭物的共轭物和制备和处理方法。

4. 发明授权

US6011042A Acyl polymeric derivatives of aromatic hydroxyl-containing compounds 失效
标题翻译：芳香族含羟基化合物的酰基聚合衍生物
公开(公告)号：US6011042A
公开(公告)日：2000-01-04
申请号：US948872
申请日：1997-10-10
申请人： Richard B. Greenwald , Annapurna Pendri , Yun H. Choe
发明人： Richard B. Greenwald , Annapurna Pendri , Yun H. Choe
IPC分类号： C07D519/00 , A61K31/33 , C07D491/22
CPC分类号： C07D519/00
摘要： The present invention is directed to conjugates such as polymeric prodrugs of aromatic, hydroxyl-containing compounds and methods of making and using the same. These polymeric prodrugs are preferably esters of hydroxyl-containing aromatic compounds and are formed by reacting a desired aromatic, hydroxyl-containing compound with a substantially non-antigenic polymer so as to produce a transport form having an ester linkage between the aromatic compound and the polymer. Preferred aromatic hydroxyl-containing compositions include 10- and 11-hydroxycamptothecin derivatives. Methods of treatment are also disclosed.
摘要翻译：本发明涉及诸如芳香族，含羟基化合物的聚合前体药物的共轭物，以及制备和使用它们的方法。这些聚合前药优选为含羟基的芳族化合物的酯，并且通过使所需的含芳族羟基的化合物与基本上非抗原性的聚合物反应形成，以产生在芳族化合物和聚合物之间具有酯键的转运体。优选的含芳族羟基的组合物包括10-和11-羟基喜树碱衍生物。还公开了治疗方法。

5. 发明授权

US5880131A 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：US5880131A
公开(公告)日：1999-03-09
申请号：US537207
申请日：1995-09-29
申请人： Richard B. Greenwald , Annapurna Pendri
发明人： Richard B. Greenwald , Annapurna Pendri
IPC分类号： A61K31/335 , A61K47/48 , C07D305/14 , C07D491/22 , A61K31/44
CPC分类号： A61K31/335 , C07D305/14
摘要： High molecular weight, water-soluble prodrugs of the formula: ##STR1## wherein: D is a biologically active moiety;M is X or Q;X is an electron withdrawing group;Q is a moiety containing a free electron pair positioned five or six atoms from Y';Y and Y' are oxygen or sulfur;R is a polyalkylene oxide; andZ is OH, C.sub.1-4 all moieties or ##STR2## are disclosed. In preferred embodiments, the prodrugs contain a polyethylene glycol having a molecular weight of at least about 20,000.
摘要翻译：具有下式的高分子量的水溶性前药：其中：D是生物活性部分; M为X或Q; X是吸电子基团; Q是含有自由电子对的部分，其位于Y'的5或6个原子上; Y和Y'是氧或硫; R是聚环氧烷; 并且Z是OH，C1-4所有部分或。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。

6. 发明授权

US5605976A Method of preparing polyalkylene oxide carboxylic acids 失效
标题翻译：聚环氧烷羧酸的制备方法
公开(公告)号：US5605976A
公开(公告)日：1997-02-25
申请号：US440732
申请日：1995-05-15
申请人： Anthony J. Martinez , Richard B. Greenwald
发明人： Anthony J. Martinez , Richard B. Greenwald
IPC分类号： A61K47/48 , C08G65/32 , C08G65/329 , C08G65/332 , C08G65/333 , C08G65/337 , C08G65/338
CPC分类号： A61K47/48215 , C08G65/329 , C08G65/3322 , C08G65/33396 , C08G65/337 , C08G65/338
摘要： The present invention is directed to methods of preparing high purity polyalkylene oxide carboxylic acids. The methods include reacting a polyalkylene oxide such as polyethylene glycol with a t-butyl haloacetate in the presence of a base followed by treatment with an acid such as trifluoroacetic acid. The resultant polymer carboxylic acids are of sufficient purity so that expensive and time consuming purification steps required for pharmaceutical grade polymers are avoided.
摘要翻译：本发明涉及制备高纯度聚环氧烷羧酸的方法。所述方法包括在碱的存在下使聚环氧烷如聚乙二醇与卤代乙酸叔丁酯反应，然后用酸如三氟乙酸处理。得到的聚合物羧酸具有足够的纯度，因此避免了医药级聚合物所需的昂贵且耗时的纯化步骤。

7. 发明授权

US5567422A Azlactone activated polyalkylene oxides conjugated to biologically active nucleophiles 失效
标题翻译：与生物活性亲核试剂缀合的吖内酯活化聚环氧烷
公开(公告)号：US5567422A
公开(公告)日：1996-10-22
申请号：US220307
申请日：1994-03-30
申请人： Richard B. Greenwald
发明人： Richard B. Greenwald
IPC分类号： A61K47/48 , C08G65/329 , C08G65/332 , A61K31/77
CPC分类号： A61K47/48215 , C08G65/329 , C08G65/332 , Y10S530/815
摘要： Water-soluble azlactone activated polyalkylene oxides having improved hydrolytic stability and conjugates of the azlactone activated polyalkylene oxides with biologically active nucleophiles are disclosed. Methods of forming and conjugating the activated polyalkylene oxides with biologically active nucleophiles are also disclosed.
摘要翻译：公开了具有改善的水解稳定性的水溶性吖内酯活化聚环氧烷和吖内酯活化聚环氧烷与生物活性亲核试剂的共轭物。还公开了活化的聚环氧烷与生物活性亲核试剂的形成和共轭的方法。

8. 发明授权

US4056539A Naphthalide indicator dyes 失效
标题翻译：萘指示剂染料
公开(公告)号：US4056539A
公开(公告)日：1977-11-01
申请号：US669190
申请日：1976-03-22
申请人： Richard B. Greenwald
发明人： Richard B. Greenwald
IPC分类号： C07C37/20 , C07D209/08 , C07D311/92 , G03C8/48 , C07D209/18
CPC分类号： C07D311/92 , C07C37/20 , C07D209/08 , G03C8/48
摘要： This invention relates to indole (na) phthalide indicator dyes substituted with a particular class of hydrogen bonding groups, such as, perhaloalkyl carbinols. These dyes are useful as optical filter agents in photographic processes to protect a selectivity exposed photosensitive material from further exposure during processing in the presence of incident light.
摘要翻译：本发明涉及用特定类型的氢键基取代的吲哚（na）二苯酞指示剂染料，例如全卤烷基甲醇。这些染料在摄影过程中可用作光学过滤剂，以在入射光的存在下保护曝光的感光材料免于进一步曝光。

9. 发明授权

US4010168A Naphthalide indicator dyes 失效
标题翻译：萘指示剂染料
公开(公告)号：US4010168A
公开(公告)日：1977-03-01
申请号：US520247
申请日：1974-11-04
申请人： Richard B. Greenwald
发明人： Richard B. Greenwald
IPC分类号： C09B11/08 , C09B11/26 , G03C8/48 , C07D305/14
CPC分类号： G03C8/48 , C09B11/08 , C09B11/26
摘要： This invention relates to 1-naphthol (na)phthalide indicator dyes substituted with a particular class of hydrogen bonding groups, such as, perhaloalkyl carbinols. These dyes are useful as optical filter agents in photographic processes to protect a selectively exposed photosensitive material from further exposure during processing in the presence of incident light.
摘要翻译：本发明涉及用特定类型的氢键基团如全卤代烷基甲醇取代的1-萘酚（na）二苯酞指示剂染料。这些染料可用作照相过程中的滤光剂，以在入射光的存在下保护选择性曝光的感光材料免于进一步曝光。

10. 发明授权

US3976647A N-(lower alkyl sulfonyl-methyl sulfonyl)-piperazines 失效
标题翻译： N-（低级烷基磺酰基 - 甲基磺酰基） - 哌嗪
公开(公告)号：US3976647A
公开(公告)日：1976-08-24
申请号：US564166
申请日：1975-04-01
申请人： Richard B. Greenwald
发明人： Richard B. Greenwald
IPC分类号： C07D295/26 , C07D295/18
CPC分类号： C07D295/26
摘要： This application is directed to compounds of the formula ##EQU1## wherein R.sup.1 is lower alkyl; R.sup.2 is hydrogen, lower alkyl or ##EQU2## wherein m is a whole number 2 to 5, n is a whole number 1 to 4 and Y is hydrogen, --OH or --COOR wherein R is hydrogen or lower alkyl; and X is ##EQU3## wherein R.sup.3 is hydrogen or ##EQU4## wherein n and Y have the same meaning given above, R.sup.4 is ##EQU5## wherein n and Y have the same meaning given above and R.sup.5 is lower alkyl. These compounds are useful as silver halide solvents in photography.
摘要翻译：本申请涉及式R2 | R1-SO2-CH-SO2-X的化合物，其中R1是低级烷基; R2是氢，低级烷基或-CH2）mS-CH2）nY其中m是整数2至5，n是整数1至4，Y是氢，-OH或-COOR，其中R是氢或低级烷基并且X是R 4 -NN-R 3或-N + N AN RLE R 5，其中R 3是氢或-CH 2）n Y其中n和Y具有与上述相同的含义，R 4是-CH 2）n Y其中n和Y具有与上述相同，R5为低级烷基。这些化合物在摄影中可用作卤化银溶剂。

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