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11.发明授权Substantially monodispersed mixtures of polymers having polyethylene glycol moieties 有权具有聚乙二醇部分的聚合物的基本单分散混合物公开(公告)号：US07119162B2
公开(公告)日：2006-10-10
申请号：US10977973
申请日：2004-10-29
IPC分类号： C08G65/34
CPC分类号： C08G65/334 , C08L71/02 , C08L71/00
摘要： Methods of synthesizing a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties include: reacting a substantially monodispersed mixture of compounds having the structure of Formula I: R1(OC2H4)n—O−X+ (I) wherein R1 is H or a lipophilic moiety; n is from 1 to 25; and X+ is a positive ion, with a substantially monodispersed mixture of compounds having the structure of Formula II: R2(OC2H4)m—OMs (II) wherein R2 is H or a lipophilic moiety; and m is from 1 to 25, under conditions sufficient to provide a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties and having the structure of Formula III: R2(OC2H4)m+n—OR1 . (III) Substantially monodispersed mixtures of polymers comprising polyethylene glycol moieties are also disclosed.
摘要翻译： 合成基本上单分散的包含聚乙二醇部分的聚合物的混合物的方法包括：使具有式I结构的化合物的基本上单分散的混合物：<？in-line-formula description =“In-Line Formulas”end =“lead” （O 2 H 4） （I）<？in-line-formula description =“In-line formula”end =“tail”？>其中R 1是H或亲油部分; n为1至25; 并且X + +是正离子，其具有具有式II结构的化合物的基本上单分散的混合物：<？in-line-formula description =“In-line Formulas”end =“lead”？ （II）H 2 -OMs（II）＆lt;＆lt;＆lt;＆lt; 2-in-line-formula description =“In-line Formulas”end =“tail”？>其中R 2是H或亲脂性部分; 且m为1至25，在足以提供包含聚乙二醇部分并且具有式III结构的基本上单分散的聚合物混合物的条件下：<？在线公式描述=“在线公式”末端=“铅 （○2 H 4）m + n - 或 - 1个/ SUP>。 （III）<？in-line-formula description =“In-line Formulas”end =“tail”？>还公开了包含聚乙二醇部分的聚合物的基本上单分散的混合物。
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公开(公告)号：US06956051B1
公开(公告)日：2005-10-18
申请号：US09429798
申请日：1999-10-29
申请人： Nnochiri N. Ekwuribe , Balasingam Rhadakrishnan , Christopher H. Price , Wes Anderson Jr. , Aslam M. Ansari
发明人： Nnochiri N. Ekwuribe , Balasingam Rhadakrishnan , Christopher H. Price , Wes Anderson Jr. , Aslam M. Ansari
IPC分类号： A61K38/00 , A61K38/04 , A61K38/11 , A61K38/21 , A61K38/22 , A61K38/26 , A61K38/27 , A61K38/36 , A61K38/46 , A61K38/48 , A61K39/395 , A61K45/00 , A61K47/48 , A61P5/02 , A61P5/10 , A61P5/14 , A61P5/18 , A61P29/00 , A61P43/00 , C07K14/70 , C07K17/00
CPC分类号： A61K47/60
摘要： The present invention relates to amphiphilic drug-oligomer conjugates capable of traversing the blood-brain barrier (“BBB”) and to methods of making and using such conjugates. An amphiphilic drug-oligomer conjugates comprise a therapeutic compound conjugated to an oligomer, wherein the oligomer comprises a lipophilic moiety coupled to a hydrophilic moiety. The conjugates of the invention further comprise therapeutic agents such as proteins, peptides, nucleosides, nucleotides, antiviral agents, antineoplastic agents, antibiotics, etc., and prodrugs, precursors, derivatives and intermediates thereof, chemically coupled to amphiphilic oligomers.
摘要翻译： 本发明涉及能够穿过血脑屏障（“BBB”）的两亲药物 - 低聚物缀合物以及制备和使用这种缀合物的方法。 两亲药物 - 低聚物缀合物包含与低聚物缀合的治疗化合物，其中所述寡聚物包含与亲水部分偶联的亲脂性部分。 本发明的缀合物还包含治疗剂，例如蛋白质，肽，核苷，核苷酸，抗病毒剂，抗肿瘤剂，抗生素等，以及与两亲寡聚物化学偶联的前药，前体，衍生物和中间体。
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13.发明授权Methods for delivering therapeutics across blood-barrier and for altering receptor binding affinity 失效通过血液屏障递送治疗剂和改变受体结合亲和力的方法公开(公告)号：US06943148B1
公开(公告)日：2005-09-13
申请号：US09430735
申请日：1999-10-29
申请人： Nnochiri N. Ekwuribe , Balasingam Rhadakrishnan , Christopher H. Price , Wes Anderson Jr. , Adam M. Ansari
发明人： Nnochiri N. Ekwuribe , Balasingam Rhadakrishnan , Christopher H. Price , Wes Anderson Jr. , Adam M. Ansari
IPC分类号： A61K38/00 , A61K38/04 , A61K38/11 , A61K38/21 , A61K38/22 , A61K38/26 , A61K38/27 , A61K38/36 , A61K38/46 , A61K38/48 , A61K39/395 , A61K45/00 , A61K47/48 , A61P5/02 , A61P5/10 , A61P5/14 , A61P5/18 , A61P29/00 , A61P43/00 , C07K14/70 , C07K17/00 , A61K38/08
CPC分类号： A61K47/60
摘要： The present invention relates to amphiphilic drug-oligomer conjugates capable of traversing the blood-brain barrier (“BBB”) and to methods of making and using such conjugates. An amphiphilic drug-oligomer conjugates comprise a therapeutic compound conjugated to an oligomer, wherein the oligomer comprises a lipophilic moiety coupled to a hydrophilic moiety. The conjugates of the invention further comprise therapeutic agents such as proteins, peptides, nucleosides, nucleotides, antiviral agents, antineoplastic agents, antibiotics, etc., and prodrugs, precursors, derivatives and intermediates thereof, chemically coupled to amphiphilic oligomers.
摘要翻译： 本发明涉及能够穿过血脑屏障（“BBB”）的两亲药物 - 低聚物缀合物以及制备和使用这种缀合物的方法。 两亲药物 - 低聚物缀合物包含与低聚物缀合的治疗化合物，其中所述寡聚物包含与亲水部分偶联的亲脂性部分。 本发明的缀合物还包含治疗剂，例如蛋白质，肽，核苷，核苷酸，抗病毒剂，抗肿瘤剂，抗生素等，以及与两亲寡聚物化学偶联的前药，前体，衍生物和中间体。
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14.发明授权Mixtures of drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same 有权包含聚亚烷基二醇的药物 - 低聚物共轭物的混合物，其用途及其制备方法公开(公告)号：US06858580B2
公开(公告)日：2005-02-22
申请号：US09873797
申请日：2001-06-04
IPC分类号： A61K38/00 , A61K38/22 , A61K39/385 , A61K47/34 , A61K47/48 , A61P5/00 , A61P43/00 , C07K1/107 , A61K38/02 , A61K38/17 , C07K1/113 , C07K2/00
CPC分类号： A61K39/385 , A61K47/60 , A61K2039/6093 , C07K1/1077
摘要： A non-polydispersed mixture of conjugates in which each conjugate in the mixture comprises a drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may exhibit higher in vivo activity than a polydispersed mixture of similar conjugates. The mixture may be more effective at surviving an in vitro model of intestinal digestion than polydispersed mixtures of similar conjugates. The mixture may result in less inter-subject variability than polydispersed mixtures of similar conjugates.
摘要翻译： 公开了一种缀合物的非多分散混合物，其中混合物中的每个缀合物包含与包含聚亚烷基二醇部分的低聚物偶联的药物。 该混合物可以表现出比类似共轭物的多分散混合物更高的体内活性。 与类似共轭物的多分散混合物相比，该混合物在存活肠内消化的体外模型时可能更有效。 与相似共轭物的多分散混合物相比，混合物可能导致较少的受试者间变异性。
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15.发明授权Substantiallymonodispersed mixtures of polymers having polyethylene glycol moieties 有权具有聚乙二醇部分的聚合物的主要单分散混合物公开(公告)号：US06815530B2
公开(公告)日：2004-11-09
申请号：US10367047
申请日：2003-02-14
IPC分类号： C08G6534
CPC分类号： C08G65/334 , C08L71/02 , C08L71/00
摘要： Methods of synthesizing a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties include: reacting a substantially monodispersed mixture of compounds having the structure of Formula I: R1(OC2H4)n—O−X+ (I) wherein R1 is H or a lipophilic moiety; n is from 1 to 25; and X+ is a positive ion, with a substantially monodispersed mixture of compounds having the structure of Formula II: R2(OC2H4)m—OMS (II) wherein R2 is H or a lipophilic moiety; and m is from 1 to 25, under conditions sufficient to provide a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties and having the structure of Formula III: R2(OC2H4)m+n—OR1 (III). Substantially monodispersed mixtures of polymers comprising polyethylene glycol moieties are also disclosed.
摘要翻译： 合成包含聚乙二醇部分的基本上单分散的聚合物混合物的方法包括：使具有式I结构的化合物的基本上单分散的混合物：其中R 1为H或亲油部分; n为1至25; 并且X +是正离子，其具有具有式II结构的化合物的基本上单分散的混合物：其中R 2是H或亲脂性部分; 并且m为1至25，在足以提供包含聚乙二醇部分并具有式III结构的聚合物的基本单分散混合物的条件下：还公开了包含聚乙二醇部分的聚合物的基本上单分散的混合物。
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16.发明授权Mixtures of insulin drug-oligomer conjugates comprising polyalkylene glycol, uses thereof, and methods of making same 有权包含聚亚烷基二醇的胰岛素药物 - 低聚物缀合物的混合物，其用途及其制备方法公开(公告)号：US07470663B2
公开(公告)日：2008-12-30
申请号：US11417586
申请日：2006-05-04
申请人： Nnochiri N. Ekwuribe , Christopher H. Price , Aslam M. Ansari , Balasingam Radhakrishnan , Amy L. Odenbaugh
发明人： Nnochiri N. Ekwuribe , Christopher H. Price , Aslam M. Ansari , Balasingam Radhakrishnan , Amy L. Odenbaugh
摘要： A mixture of conjugates in which each conjugate in the mixture comprises an insulin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may exhibit higher in vivo activity than a polydispersed mixture of similar conjugates. The mixture may also be more effective at surviving an in vitro model of intestinal digestion than polydispersed mixtures of similar conjugates. The mixture may also result in less inter-subject variability than polydispersed mixtures of similar conjugates.
摘要翻译： 公开了混合物的混合物，其中混合物中的每个缀合物包含与包含聚亚烷基二醇部分的低聚物偶联的胰岛素药物。 该混合物可以表现出比类似共轭物的多分散混合物更高的体内活性。 与类似共轭物的多分散混合物相比，混合物在存活肠内消化的体外模型时也可能更有效。 与相似缀合物的多分散混合物相比，混合物还可导致较少的受试者间变异性。
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公开(公告)号：US07381702B2
公开(公告)日：2008-06-03
申请号：US11424295
申请日：2006-06-15
申请人： Nnochiri N. Ekwuribe , Christopher H. Price , James Gordon Still , Jennifer Ann Filbey , Aslam M. Ansari , Amy L. Odenbaugh , Balasingam Radhakrishnan
发明人： Nnochiri N. Ekwuribe , Christopher H. Price , James Gordon Still , Jennifer Ann Filbey , Aslam M. Ansari , Amy L. Odenbaugh , Balasingam Radhakrishnan
CPC分类号： C07K14/62 , A61K38/28 , A61K47/542 , A61K47/60
摘要： Methods of treating diabetes mellitus in a patient in need of such treatment include administering an effective amount of an insulin drug to the patient in order to treat diabetes mellitus in the patient. Methods according to the present invention may “activate” the liver, potentially restoring normal glucose homeostasis to individuals suffering from diabetes mellitus.
摘要翻译： 在需要这种治疗的患者中治疗糖尿病的方法包括向患者施用有效量的胰岛素药物以治疗患者的糖尿病。 根据本发明的方法可以“激活”肝脏，潜在地恢复患有糖尿病的个体的正常葡萄糖体内平衡。
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公开(公告)号：US06541508B2
公开(公告)日：2003-04-01
申请号：US09802739
申请日：2001-03-09
IPC分类号： A61K31337
CPC分类号： A61K31/704 , A61K31/335 , A61K31/70 , A61K33/24 , A61K45/06 , A61K47/60 , Y02A50/411 , A61K2300/00
摘要： Taxane prodrugs comprise a taxane joined by a hydrolyzable bond to one or more oligomers that comprise a polyethylene glycol moiety. The oligomer preferably further comprises a salt-forming moiety.
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公开(公告)号：US06380405B1
公开(公告)日：2002-04-30
申请号：US09476974
申请日：1999-12-31
IPC分类号： C07D30514
CPC分类号： A61K33/24 , A61K45/06 , A61K47/60 , Y02A50/411 , A61K2300/00
摘要： The present invention generally provides taxane prodrugs comprising at least one taxane joined by hydrolyzable bond(s) to one or more polyethylene glycol oligomer(s) selected from the group consisting of a straight or branched polyethylene glycol oligomer having from 1 to 25 polyethylene glycol units and optionally comprising a salt-forming moiety. The polyethylene glycol oligomer preferably comprises a salt-forming moiety, which is preferably selected from the group consisting of ammonium and carboxylate.
摘要翻译： 本发明通常提供紫杉烷前药，其包含至少一种紫杉烷类，其通过可水解键连接到一种或多种选自具有1至25个聚乙二醇单元的直链或支链聚乙二醇低聚物的聚乙二醇低聚物 并且任选地包含成盐部分。 聚乙二醇低聚物优选包含成盐部分，其优选选自铵和羧酸盐。
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20.发明授权Methods of synthesizing substantially monodispersed mixtures of polymers having polyethylene glycol moieties 有权合成具有聚乙二醇部分的聚合物的基本单分散混合物的方法公开(公告)号：US06835802B2
公开(公告)日：2004-12-28
申请号：US09873731
申请日：2001-06-04
IPC分类号： C08G6534
CPC分类号： C08G65/334 , C08L71/02 , C08L71/00
摘要： Methods of synthesizing a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties include: reacting a substantially monodispersed mixture of compounds having the structure of Formula I: R1(OC2H4)n—O−X+ (I) wherein R1 is H or a lipophilic moiety; n is from 1 to 25; and X+ is a positive ion, with a substantially monodispersed mixture of compounds having the structure of Formula II: R2(OC2H4)m—OMs (II) wherein R2 is H or a lipophilic moiety; and m is from 1 to 25, under conditions sufficient to provide a substantially monodispersed mixture of polymers comprising polyethylene glycol moieties and having the structure of Formula III: R2(OC2H4)m+n—OR1 (III).
摘要翻译： 合成包含聚乙二醇部分的基本上单分散的聚合物混合物的方法包括：使具有式I结构的化合物的基本上单分散的混合物：其中R 1为H或亲油部分; n为1至25; 并且X +是正离子，其具有具有式II结构的化合物的基本上单分散的混合物：其中R 2是H或亲脂性部分; 并且m为1至25，在足以提供包含聚乙二醇部分并具有式III结构的聚合物的基本上单分散混合物的条件下：
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