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1.发明授权公开(公告)号：US07579324B2
公开(公告)日：2009-08-25
申请号：US10367105
申请日：2003-02-14
申请人： Michael Burnet , Jan-Hinrich Guse , Hans-Jurgen Gutke , Albert Beck , Georgia Tsotsou , Irina Droste-Borel , Jeannette Reichert , Kattie Luyten , Maximilian Busch , Michael Wolff , Moussa Khobzaoui , Simona Margutti , Thomas Meindl , Gene Kim , Laurence Barker
发明人： Michael Burnet , Jan-Hinrich Guse , Hans-Jurgen Gutke , Albert Beck , Georgia Tsotsou , Irina Droste-Borel , Jeannette Reichert , Kattie Luyten , Maximilian Busch , Michael Wolff , Moussa Khobzaoui , Simona Margutti , Thomas Meindl , Gene Kim , Laurence Barker
CPC分类号： A61K49/0004 , A61K47/54 , A61K47/545 , A61K47/549
摘要： This invention features a compound of the following formula: T-(-L-C)m, T is a transportophore, L is a bond or a linker having a molecular weight up to 240 dalton, C is a non-antibiotic therapeutic agent, and m is 1, 2, 3, 4, 5, 6, 7, or 8, in which the transportophore has an immune selectivity ratio of at least 2, the transportophore is covalently bonded to the non-antibiotic therapeutic agent via the bond or the linker, and the compound has an immune selectivity ratio of at least 2.
摘要翻译： 本发明的特征在于下列化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？> T - （ - LC）m，<？in-line-formula description =“ T是一个转运载体，L是分子量高达240道尔顿的键或接头，C是非抗生素治疗剂，m是1,2,3 ，4,5,6,7或8，其中转运载体具有至少2的免疫选择性比，转运载体通过键或接头与非抗生素治疗剂共价结合，并且该化合物具有 免疫选择性比至少为2。
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2.发明申请Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof 审中-公开生物活性化合物的缀合物，其制备和使用方法，其制剂和药物应用公开(公告)号：US20050171342A1
公开(公告)日：2005-08-04
申请号：US10504787
申请日：2003-02-14
申请人： Michael Burnet , Jan-Hinrich Guse , Hans-Jurgen Gutke , Albert Beck , Georgia Tsotsou , Irina Droste-Borel , Jeannette Reichert , Kattie Luyten , Maximilian Busch , Michael Wolff , Moussa Khobzaoui , Simona Margutti , Thomas Meindl , Gene Kim , Laurent Barker
发明人： Michael Burnet , Jan-Hinrich Guse , Hans-Jurgen Gutke , Albert Beck , Georgia Tsotsou , Irina Droste-Borel , Jeannette Reichert , Kattie Luyten , Maximilian Busch , Michael Wolff , Moussa Khobzaoui , Simona Margutti , Thomas Meindl , Gene Kim , Laurent Barker
CPC分类号： A61K49/0004 , A61K47/54 , A61K47/545 , A61K47/549
摘要： This invention features a compound of the following formula: T-(-L-C)m, T is a transportophore, L is a bond or a linker having a molecular weight up to 240 dalton, C is a non-antibiotic therapeutic agent, and m is 1, 2, 3, 4, 5, 6, 7, or 8, in which the transportophore has an immune selectivity ratio of at least 2, the transportophore is covalently bonded to the non-antibiotic therapeutic agent via the bond or the linker, and the compound has an immune selectivity ratio of at least 2.
摘要翻译： 本发明的特征在于下式的化合物：<？in-line-formula description =“In-line Formulas”end =“lead”？> T - （ - LC） -line-formula description =“In-line Formulas”end =“tail”？> T是转运载体，L是分子量高达240道尔顿的键或接头，C是非抗生素治疗剂， m是1,2,3,4,5,6,7或8，其中转运蛋白具有至少2的免疫选择性比，所述转运载体通过所述键或所述非抗生素治疗剂共价结合， 接头，并且化合物的免疫选择性比至少为2。
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3.发明申请公开(公告)号：US20090093014A1
公开(公告)日：2009-04-09
申请号：US12157937
申请日：2008-06-12
申请人： Michael Burnet , Jan-Hinrich Guse , Gene Kim , Albert Beck , Georgia Tsotsou , Irina Droste-Borel , Laurence Barker , Michael Wolff , Hans-Jurgen Gutke
发明人： Michael Burnet , Jan-Hinrich Guse , Gene Kim , Albert Beck , Georgia Tsotsou , Irina Droste-Borel , Laurence Barker , Michael Wolff , Hans-Jurgen Gutke
CPC分类号： B82Y5/00 , A61K47/552 , A61K47/556 , A61K47/67 , A61K49/0004 , G01N33/5047 , G01N33/5094
摘要： This invention features a method of identifying a compound useful for enhancing efficacy of a therapeutic agent. The method includes incubating a compound in blood cells; separating immune cells from erythrocytic cells; and determining the ratio of the concentration of the compound in the immune cells to the concentration of the compound in the erythrocytic cells; wherein the compound comprises a transportophore and a therapeutic agent, in which the transportophore is covalently bonded to the therapeutic agent via a bond or a linker.
摘要翻译： 本发明的特征在于鉴定可用于增强治疗剂功效的化合物的方法。 该方法包括在血细胞中孵育化合物; 将免疫细胞与红细胞分离; 并测定免疫细胞中化合物的浓度与红细胞中化合物浓度之比; 其中所述化合物包含转运载体和治疗剂，其中所述转运载体通过键或接头共价键合到所述治疗剂。
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4.发明授权公开(公告)号：US08357506B2
公开(公告)日：2013-01-22
申请号：US12157937
申请日：2008-06-12
申请人： Michael Burnet , Jan-Hinrich Guse , Gene Kim , Albert Beck , Georgia Tsotsou , Irina Droste-Borel , Laurence Barker , Michael Wolff , Hans-Jurgen Gutke
发明人： Michael Burnet , Jan-Hinrich Guse , Gene Kim , Albert Beck , Georgia Tsotsou , Irina Droste-Borel , Laurence Barker , Michael Wolff , Hans-Jurgen Gutke
IPC分类号： C12Q1/02
CPC分类号： B82Y5/00 , A61K47/552 , A61K47/556 , A61K47/67 , A61K49/0004 , G01N33/5047 , G01N33/5094
摘要： This invention features a method of identifying a compound useful for enhancing efficacy of a therapeutic agent. The method includes incubating a compound in blood cells; separating immune cells from erythrocytic cells; and determining the ratio of the concentration of the compound in the immune cells to the concentration of the compound in the erythrocytic cells; wherein the compound comprises a transportophore and a therapeutic agent, in which the transportophore is covalently bonded to the therapeutic agent via a bond or a linker.
摘要翻译： 本发明的特征在于鉴定可用于增强治疗剂功效的化合物的方法。 该方法包括在血细胞中孵育化合物; 将免疫细胞与红细胞分离; 并测定免疫细胞中化合物的浓度与红细胞中化合物浓度之比; 其中所述化合物包含转运载体和治疗剂，其中所述转运载体通过键或接头共价键合到所述治疗剂。
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5.发明申请Conjugates of biologically active compounds, methods for their preparation and use, formulation and pharmaceutical applications thereof 审中-公开生物活性化合物的缀合物，其制备和使用方法，其制剂和药物应用公开(公告)号：US20080145343A1
公开(公告)日：2008-06-19
申请号：US11895295
申请日：2007-08-23
申请人： Michael Burnet , Jan-Hinrich Guse , Gene Kim , Hans-Jurgen Gutke , Albert Beck , Georgia Tsotsou , Irina Droste-Borel , Laurence Barker , Michael Wolf
发明人： Michael Burnet , Jan-Hinrich Guse , Gene Kim , Hans-Jurgen Gutke , Albert Beck , Georgia Tsotsou , Irina Droste-Borel , Laurence Barker , Michael Wolf
CPC分类号： B82Y5/00 , A61K47/552 , A61K47/556 , A61K47/67 , A61K49/0004 , G01N33/5047 , G01N33/5094
摘要： This invention features a method of identifying a compound useful for enhancing efficacy of a therapeutic agent. The method includes incubating a compound in blood cells; separating immune cells from erythrocytic cells; and determining the ratio of the concentration of the compound in the immune cells to the concentration of the compound in the erythrocytic cells; wherein the compound comprises a transportophore and a therapeutic agent, in which the transportophore is covalently bonded to the therapeutic agent via a bond or a linker.
摘要翻译： 本发明的特征在于鉴定可用于增强治疗剂功效的化合物的方法。 该方法包括在血细胞中孵育化合物; 将免疫细胞与红细胞分离; 并测定免疫细胞中化合物的浓度与红细胞中化合物浓度之比; 其中所述化合物包含转运载体和治疗剂，其中所述转运载体通过键或接头共价键合到所述治疗剂。
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公开(公告)号：US20060099660A1
公开(公告)日：2006-05-11
申请号：US10504786
申请日：2003-02-14
申请人： Michael Burnet , Jan-Hinrich Guse , Gene Kim , Albert Beck , Georgia Tsotsou , Irina Droste-Borel , Laurence Barker , Michael Wolff
发明人： Michael Burnet , Jan-Hinrich Guse , Gene Kim , Albert Beck , Georgia Tsotsou , Irina Droste-Borel , Laurence Barker , Michael Wolff
IPC分类号： G01N33/555
CPC分类号： B82Y5/00 , A61K47/552 , A61K47/556 , A61K47/67 , A61K49/0004 , G01N33/5047 , G01N33/5094
摘要： This invention features a method of identifying a compound useful for enhancing efficacy of a therapeutic agent. The method includes incubating a compound in blood cells; separating immune cells from erythrocytic cells; and determining the ratio of the concentration of the compound in the immune cells to the concentration of the compound in the erythrocytic cells; wherein the compound comprises a transportophore and a therapeutic agent, in which the transportophore is covalently bonded to the therapeutic agent via a bond or a linker.
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公开(公告)号：US20110028417A1
公开(公告)日：2011-02-03
申请号：US12847740
申请日：2010-07-30
IPC分类号： A61K31/7052 , C07H17/00 , A61P31/12 , A61P31/04 , A61P9/00 , A61P3/00 , A61P37/00 , A61P29/00
CPC分类号： C07H17/08
摘要： The invention features novel macrocyclic compounds, methods of making the compounds, pharmaceutical compositions including the compounds, and methods of treatment using the compounds.
摘要翻译： 本发明的特征在于新颖的大环化合物，制备化合物的方法，包括该化合物的药物组合物以及使用该化合物的治疗方法。
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公开(公告)号：US07767797B1
公开(公告)日：2010-08-03
申请号：US11241514
申请日：2005-09-30
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： The invention features novel macrocyclic compounds, methods of making the compounds, pharmaceutical compositions including the compounds, and methods of treatment using the compounds.
摘要翻译： 本发明的特征在于新颖的大环化合物，制备化合物的方法，包括该化合物的药物组合物以及使用该化合物的治疗方法。
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公开(公告)号：US08461120B2
公开(公告)日：2013-06-11
申请号：US12847740
申请日：2010-07-30
CPC分类号： C07H17/08
摘要： The invention features novel macrocyclic compounds, methods of making the compounds, pharmaceutical compositions including the compounds, and methods of treatment using the compounds.
摘要翻译： 本发明的特征在于新颖的大环化合物，制备化合物的方法，包括该化合物的药物组合物以及使用该化合物的治疗方法。
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公开(公告)号：US07271154B2
公开(公告)日：2007-09-18
申请号：US10367104
申请日：2003-02-14
申请人： Michael Burnet , Jan-Hinrich Guse , Gene Kim
发明人： Michael Burnet , Jan-Hinrich Guse , Gene Kim
IPC分类号： C07H17/08 , A61K31/335
CPC分类号： C07D273/00 , A61K31/7048 , A61K47/552 , C07D267/00 , C07D413/14 , C07D499/00 , C07H17/08
摘要： This invention features a compound of the following formula: wherein T is a transportophore, L is a bond or linker, and C is an antibiotic therapeutic agent, the transportophore is covalently bonded to the antibiotic therapeutic agent via the bond or the linker, and the transportophore is an azithromycin derivative or crown ether derivative.
摘要翻译： 本发明的特征在于下式的化合物：其中T是转运载体，L是一个键或连接体，C是抗生素治疗剂，转运载体通过键或连接体与抗生素治疗剂共价结合， 转运蛋白是阿奇霉素衍生物或冠醚衍生物。
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