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1.发明申请Mixtures Of Calcitonin Drug-Oligomer Conjugates And Methods Of Use In Pain Treatment 审中-公开降钙素药物低聚物缀合物的混合物及其在疼痛治疗中的应用公开(公告)号：US20070213262A1
公开(公告)日：2007-09-13
申请号：US10562478
申请日：2004-05-27
申请人： Gordana Kosutic , Nnochiri Ekwuribe , Christopher H. Price , Christopher Price , Aslam Andsari , Amy Odenbaugh
发明人： Gordana Kosutic , Nnochiri Ekwuribe , Christopher H. Price , Christopher Price , Aslam Andsari , Amy Odenbaugh
IPC分类号： A61K38/17
CPC分类号： A61K38/23 , A61K51/02 , A61K51/0402 , A61K51/0406 , A61K51/0489 , A61K51/0491 , A61K51/10 , A61K51/1241
摘要： A mixture of conjugates in which each conjugate in the mixture comprises a calcitonin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may lower serum calcium levels in a subject by 10, 15 or even 20 percent or more. Moreover, the mixture may be more effective at surviving an in vitro model of intestinal digestion than non-conjugated calcitonin. Furthermore, the mixture may exhibit a higher bioavailability than non-conjugated calcitonin. The compositions of this invention are useful in the treatment of various bone disorders and pain.
摘要翻译： 公开了混合物的混合物，其中混合物中的每个偶联物包含与包含聚亚烷基二醇部分的低聚物偶联的降钙素药物。 该混合物可使受试者中的血清钙水平降低10,15或甚至20％或更多。 此外，混合物在存活肠内消化的体外模型时可能比非共轭降钙素更有效。 此外，该混合物可能表现出比非共轭降钙素更高的生物利用度。 本发明的组合物可用于治疗各种骨病和疼痛。
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2.发明申请Mixtures Of Calcitonin Drug-Oligomer Conjugates And Methods Of Use In Pain Treatment 审中-公开降钙素药物低聚物缀合物的混合物及其在疼痛治疗中的应用公开(公告)号：US20090281023A9
公开(公告)日：2009-11-12
申请号：US10562478
申请日：2004-05-27
IPC分类号： A61K38/17
CPC分类号： A61K38/23 , A61K51/02 , A61K51/0402 , A61K51/0406 , A61K51/0489 , A61K51/0491 , A61K51/10 , A61K51/1241
摘要： A mixture of conjugates in which each conjugate in the mixture comprises a calcitonin drug coupled to an oligomer that includes a polyalkylene glycol moiety is disclosed. The mixture may lower serum calcium levels in a subject by 10, 15 or even 20 percent or more. Moreover, the mixture may be more effective at surviving an in vitro model of intestinal digestion than non-conjugated calcitonin. Furthermore, the mixture may exhibit a higher bioavailability than non-conjugated calcitonin. The compositions of this invention are useful in the treatment of various bone disorders and pain.
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降钙素药物。 该混合物可使受试者中的血清钙水平降低10,15或甚至20％或更多。 此外，混合物在存活肠内消化的体外模型时可能比非共轭降钙素更有效。 此外，该混合物可能表现出比非共轭降钙素更高的生物利用度。 本发明的组合物可用于治疗各种骨病和疼痛。
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3.发明申请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：US20050059799A1
公开(公告)日：2005-03-17
申请号：US10977973
申请日：2004-10-29
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)b—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聚合物的基本上单分散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：R 1（OC 2 H 4）b O - X +（I） 1>是H或亲脂性部分; n为1至25; 并且X +是具有式II结构的化合物的基本上单分散的混合物：R 2（OC 2 H 4）m-OM（II）其中R 2是H或亲油部分; 并且m为1至25，在足以提供包含聚乙二醇部分并且具有式III结构的基本单分散混合物的条件下：R 2（OC 2 H 4）m + n -OR 1（III）。 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：US20060293219A1
公开(公告)日：2006-12-28
申请号：US11424295
申请日：2006-06-15
申请人： Nnochiri Ekwuribe , Christopher Price , James Still , Jennifer Filbey , Aslam Ansari , Amy Odenbaugh , Balasingam Radhakrishnan
发明人： Nnochiri Ekwuribe , Christopher Price , James Still , Jennifer Filbey , Aslam Ansari , Amy Odenbaugh , Balasingam Radhakrishnan
IPC分类号： A61K38/28
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：US20060199759A1
公开(公告)日：2006-09-07
申请号：US11417586
申请日：2006-05-04
申请人： Nnochiri Ekwuribe , Christopher Price , Aslam Ansari , Balasingam Radhakrishnan , Amy Odenbaugh
发明人： Nnochiri Ekwuribe , Christopher Price , Aslam Ansari , Balasingam Radhakrishnan , Amy 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.
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公开(公告)号：US20060100137A1
公开(公告)日：2006-05-11
申请号：US11314309
申请日：2005-12-21
申请人： Nnochiri Ekwuribe , Christopher Price , James Still , Jennifer Filbey , Aslam Ansari , Amy Odenbaugh , Balasingam Radhakrishnan
发明人： Nnochiri Ekwuribe , Christopher Price , James Still , Jennifer Filbey , Aslam Ansari , Amy 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.
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7.发明申请Aryl carbamate oligomers for hydroilyzable prodrugs and prodrugs comprising same 有权用于可水解前体药物的氨基甲酸酯低聚物和包含其的前体药物公开(公告)号：US20060167234A1
公开(公告)日：2006-07-27
申请号：US10525290
申请日：2004-05-06
申请人： Nnochiri Ekwuribe , Amy Odenbaugh
发明人： Nnochiri Ekwuribe , Amy Odenbaugh
CPC分类号： C07C235/48 , C07C41/16 , C07C41/26 , C07C43/23 , C07C45/673 , C07C45/71 , C07C47/575 , C07C49/84 , C07C271/22 , C07C271/28 , C07K7/02 , C07K7/06 , C07C43/2055
摘要： The present invention provides a compound having a formula: where R1 is selected from the group consisting of alkyl, CH2(OC2H4)OCH3, and —(OC2H4)OCH3; n is 0-4; Olig is an oligomer having a formula: -L-O-PAGR●R2]q where L is a optional linker moiety selected from the group consisting of —CH2O—, —CH2OX—, —OX—, —C(O)—, —C(O)X, —NH—, —NHC(O)—, —XNHC(O)—, —NHC(O)X—, —C(O)NH—, —C(O)NHX—, and where X is alky1-6 or is not present, Y is N or O or is not present, and R3 is alkyl1-6; PAG is a linear or branched polyalkylene glycol moiety; R2 is an alkyl1-22 capping moiety if X is present or alkyl2-22 if X is not present; and q is a number from 1 to the maximum number of branches on PAG; and m is 1-5.
摘要翻译： 本发明提供具有下式的化合物：其中R 1选自烷基，CH 2（OC 2 H 4） OCH 3，和 - （OC 2 H 4 H）OCH 3; n为0-4; Olig是具有下式的低聚物：<？in-line-formula description =“In-line Formulas”end =“lead”？> - LO-PAGR●R＆lt; 2＆ 其中L是选自-CH 2 O 2的任选的接头部分，其中L是选自-CH 2 - ，-O - ， - C（O） - ， - C（O）X，-NH-，-NHC（O） - ， - N - （O） -NHC（O）X - ， - C（O）NH - ， - C（O）NHX-，其中X是烷基，或不存在，Y是N或O或 不存在，R 3是烷基1-6。 PAG是直链或支链的聚亚烷基二醇部分; 如果X不存在，则R 2是烷基封端的封端部分，如果不存在X则为烷基2-22。 q是PAG上从1到最大分支数的数字; m为1-5。
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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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9.发明授权公开(公告)号：US07119074B2
公开(公告)日：2006-10-10
申请号：US10808044
申请日：2004-03-24
IPC分类号： A61K31/704
CPC分类号： A61K47/60
摘要： The present invention provides amphiphilic prodrugs comprising a therapeutic compound conjugated to an PEG-oligomer/polymer and methods for using said prodrugs to enable oral drug delivery and/or delivery of drugs across the blood brain barrier into the central nervous system.
摘要翻译： 本发明提供了包含与PEG-低聚物/聚合物缀合的治疗化合物的两亲前药，以及使用所述前体药物以使药物能够穿过血脑屏障进入中枢神经系统的口服药物递送和/或递送的方法。
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公开(公告)号：US06713454B1
公开(公告)日：2004-03-30
申请号：US09474915
申请日：1999-12-31
IPC分类号： A61K31704
CPC分类号： A61K47/60
摘要： The present invention provides amphiphilic prodrugs comprising a therapeutic compound conjugated to an PEG-oligomer/polymer and methods for using said prodrugs to enable oral drug delivery and/or delivery of drugs across the blood brain barrier into the central nervous system.
摘要翻译： 本发明提供了包含与PEG-低聚物/聚合物缀合的治疗化合物的两亲前药，以及使用所述前体药物以使药物能够穿过血脑屏障进入中枢神经系统的口服药物递送和/或递送的方法。
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