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1. 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。

2. 发明授权

US5730990A Non-antigenic amine derived polymers and polymer conjugates 失效
公开(公告)号：US5730990A
公开(公告)日：1998-03-24
申请号：US465403
申请日：1995-06-05
申请人： Richard B. Greenwald , Anthony Martinez , Annapurna Pendri
发明人： Richard B. Greenwald , Anthony Martinez , Annapurna Pendri
IPC分类号： A61K31/335 , A61K31/495 , A61K38/00 , A61K38/43 , A61K39/44 , A61K47/48 , C07K14/805 , C07K16/00 , C07K17/14 , C08F8/30 , C08F20/54 , C08F26/10 , C08G65/32 , C08G65/329 , C08G65/333 , A61K45/00 , A61K31/74 , C08G63/48 , C08G63/91
CPC分类号： A61K47/48215 , C07K14/805 , C08G65/329 , C08G65/33303 , C08G65/3331 , 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.

3. 发明授权

US5902588A 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：US5902588A
公开(公告)日：1999-05-11
申请号：US974532
申请日：1997-11-19
申请人： Richard B. Greenwald , Anthony Martinez , Annapurna Pendri
发明人： Richard B. Greenwald , Anthony Martinez , Annapurna Pendri
IPC分类号： A61K31/335 , A61K31/495 , A61K38/00 , A61K38/43 , A61K39/44 , A61K47/48 , C07K14/805 , C07K16/00 , C07K17/14 , C08F8/30 , C08F20/54 , C08F26/10 , C08G65/32 , C08G65/329 , C08G65/333 , A61K45/00 , C08F110/02
CPC分类号： A61K47/48215 , C07K14/805 , C08G65/329 , C08G65/33303 , C08G65/3331 , 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

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。

5. 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。

6. 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。

7. 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。

8. 发明授权

US06638499B2 Terminally-branched polymeric linkers and polymeric conjugates containing the same 失效
标题翻译：末端支化的聚合物接头和含有它们的聚合物共轭物
公开(公告)号：US06638499B2
公开(公告)日：2003-10-28
申请号：US10067930
申请日：2002-02-06
申请人： Anthony J. Martinez , Annapurna Pendri , Richard B. Greenwald , Yun H. Choe
发明人： Anthony J. Martinez , Annapurna Pendri , Richard B. Greenwald , Yun H. Choe
IPC分类号： A61K31785
CPC分类号： C07D491/22 , A61K47/60 , C07H15/252 , C08F283/00
摘要： The present invention is directed to polymeric-prodrug transport forms of the formula: wherein: E1-4 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, C1-6 heteroalkoxy, and at least one of E1-4 includes a B moiety, wherein B is a leaving group, OH, a residue of a hydroxyl-or amino-containing moiety or wherein J1 is the same as J, or another member of the group defining J and E5 is the same as E1-4, or another member of the group defining E1-4, Y1-2 are independently O, S or NR9; M is a heteroatom selected from either X or Q; wherein X is an electron withdrawing group and Q is a moiety containing a free electron pair positioned three to six atoms from C(═Y2); R2-5 and R7-9 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 heteroakoxy; (m1) and (m2) are independently zero or one; (n1), (n2), (p1), (p2) and (q) are independently zero or a positive integer, Z is an electron withdrawing group; and R1 is a polymeric residue. which is optionally capped with a moiety of the formula:
摘要翻译：本发明涉及下式的聚合物 - 前药转运形式：其中：E1-4独立地选自氢，C 1-6烷基，C 3-12支链烷基，C 3-8环烷基，C 1-6取代的烷基，C 3-8取代的环烷基，芳基，取代的芳基，芳烷基，C 1-6杂烷基，取代的C 1-6杂烷基，C 1-6烷氧基，苯氧基，C 1-6杂烷氧基，E1-4中的至少一个包括B部分其中B是离去基团，OH，含羟基或氨基的部分的残基或其中J 1与J相同，或者定义J和E5的基团的另一个成员与E1-4相同或另一个成员定义E1-4的基团，Y1-2独立地为O，S或NR9; M为选自X或Q的杂原子; 其中X是吸电子基团，Q是含有从C（= Y2）定位为三至六个原子的自由电子对的部分; R2-5和R7-9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，C1-6杂烷基，取代的C1-6杂烷基，C1-6烷氧基，苯氧基和C1 -6杂芳氧基;（m1）和（m2）分别为零或一;（n1），（n2），（p1），（p2）和（q）分别为零或正整数，Z为吸电子基团 ; 并且R 1是聚合物残基，其任选地被下式的部分封端：

9. 发明授权

US06395266B1 Terminally-branched polymeric linkers and polymeric conjugates containing the same 失效
标题翻译：末端支化的聚合物接头和含有它们的聚合物共轭物
公开(公告)号：US06395266B1
公开(公告)日：2002-05-28
申请号：US09293624
申请日：1999-04-16
申请人： Anthony J. Martinez , Annapurna Pendri , Richard B. Greenwald , Yun H. Choe
发明人： Anthony J. Martinez , Annapurna Pendri , Richard B. Greenwald , Yun H. Choe
IPC分类号： A61K31785
CPC分类号： C07D491/22 , A61K47/60 , C07H15/252 , C08F283/00
摘要： The present invention is directed to polymeric-prodrug transport forms of the formula: wherein: E1-4 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, C1-6 heteroalkoxy, and at least one of E1-4 includes a B moiety, wherein B is a leaving group, OH, a residue of a hydroxyl-or amino-containing moiety or wherein J1 is the same as J, or another member of the group defining J and E5 is the same as E1-4, or another member of the group defining E1-4; Y1-2 are independently O, S or NR9; M is a heteroatom selected from either X or Q; wherein X is an electron withdrawing group and Q is a moiety containing a free electron pair positioned three to six atoms from C(=Y2); R2-5 and R7-9 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, C1-16 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; (m1) and (m2) are independently zero or one; (n1), (n2), (p1), (p2) and (q) are independently zero or a positive integer, Z is an electron withdrawing group; and R1 is a polymeric residue. which is optionally capped with a moiety of the formula:
摘要翻译：本发明涉及下式的聚合物 - 前药转运形式：其中：E1-4独立地选自氢，C 1-6烷基，C 3-12支链烷基，C 3-8环烷基，C 1-6取代的烷基，C 3-8取代的环烷基，芳基，取代的芳基，芳烷基，C 1-6杂烷基，取代的C 1-6杂烷基，C 1-6烷氧基，苯氧基，C 1-6杂烷氧基，E1-4中的至少一个包括B部分其中B是离去基团，OH，含羟基或氨基的部分的残基或其中J 1与J相同，或者定义J和E5的基团的另一个成员与E1-4相同或另一个成员定义E1-4的基团; Y1-2独立地为O，S或NR9; M为选自X或Q的杂原子; 其中X是吸电子基团，Q是含有从C（= Y2）定位为三至六个原子的自由电子对的部分; R2-5和R7-9独立地选自氢，C1-6烷基，C3-12支链烷基，C3-8环烷基，C1-6取代烷基，C3-8取代环烷基，芳基，取代芳基，芳烷基，C1-16杂烷基，取代C1-6杂烷基，C1-6烷氧基，苯氧基和C1 -6杂烷氧基;（m1）和（m2）独立为零或一;（n1），（n2），（p1），（p2）和（q）独立为零或正整数，Z为吸电子基团 ; 并且R 1是聚合物残基，其任选地被下式的部分封端：

10. 发明授权

US06251382B1 Biodegradable high molecular weight polymeric linkers and their conjugates 有权
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：US06251382B1
公开(公告)日：2001-06-26
申请号：US09293557
申请日：1999-04-15
申请人： Richard B. Greenwald , Anthony J. Martinez , Yun H. Choe , Annapurna Pendri
发明人： Richard B. Greenwald , Anthony J. Martinez , Yun H. Choe , Annapurna Pendri
IPC分类号： A61K4748
CPC分类号： A61K47/60
摘要： Polymeric compounds of the formula: (D)n—M—(R1)m (I) wherein (m) and (n) independently selected positive integers, preferably from about 1 to about 6 each; D is a residue of a biologically active moiety; M is a multifunctional linker/spacer moiety; and R1 is a polymer residue are disclosed. Methods of preparing the same and methods of treatment using the same are also included as part of the present invention.
摘要翻译：下式的聚合化合物：其中（m）和（n）独立选择的正整数，优选约1至约6; D是生物活性部分的残基; M是多官能连接体/间隔子部分; 并且R 1是聚合物残基。制备方法和使用该方法的方法也包括在本发明的一部分中。

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