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1.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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2.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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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：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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