公开(公告)号：EP2014306A3

公开(公告)日：2012-08-15

申请号：EP08009119.2

申请日：2008-05-16

申请人： Taiwan Hopax Chems. Mfg. Co., Ltd

发明人： Wei, I-Chien ,  Yang, David J. ,  Yu, Dong-Fang

IPC分类号： A61K47/48

CPC分类号： A61K47/4823 ,  A61K31/282 ,  A61K33/24 ,  A61K47/61

摘要： The current disclosure, in one embodiment, includes a polysaccharide conjugate. This conjugate has a polysaccharide and at least one monomeric amino acid having an O-group covalently bound to the polysaccharide. The conjugate also has at least one metal conjugated by the O-group of the amino acid. According to another embodiment, the disclosure provides a method of synthesizing a polysaccharide conjugate by covalently bonding a monomeric amino acid having an O-group to a polysaccharide and by conjugating a metal to the O-group to form a polysaccharide conjugate. According to a third embodiment, the disclosure relates to a method of killing a cancer cell by administering to the cell an effective amount of a polysaccharide conjugate. This conjugate has a polysaccharide and at least one monomeric amino acid having an O-group covalently bound to the polysaccharide. The conjugate also has at least one metal conjugated by the O-group of the amino acid.

摘要翻译： 在一个实施方案中，本发明包括多糖缀合物。 该缀合物具有多糖和至少一种与多糖共价结合的O-基团的单体氨基酸。 缀合物还具有至少一种由氨基酸的O-基缀合的金属。 根据另一个实施方案，本公开提供了通过将具有O-基团的单体氨基酸共价键合到多糖并通过将金属与O基团缀合以形成多糖缀合物来合成多糖缀合物的方法。 根据第三实施方案，本公开涉及通过向细胞施用有效量的多糖缀合物来杀死癌细胞的方法。 该缀合物具有多糖和至少一种与多糖共价结合的O-基团的单体氨基酸。 缀合物还具有至少一种由氨基酸的O-基缀合的金属。

公开(公告)号：EP1698351B1

公开(公告)日：2017-06-07

申请号：EP06004026.8

申请日：2006-02-28

申请人： Taiwan Hopax Chems. Mfg. Co., Ltd. ,  Board of Regents, The University of Texas System

发明人： Wei, I-Chien ,  Yang, David J. ,  Yu, Dong-Fang

IPC分类号： A61K51/08 ,  A61K31/505 ,  A61K31/66

CPC分类号： A61K31/505 ,  A61K31/66 ,  A61K51/025

摘要： The invention includes glycopeptides having a glycoside and a peptide covalently bound through an amide bond. The glycopeptides may also include a diagnostic or therapeutic agent bound to the glycopeptide. A metal, such as a radionuclide, may also be chelated to the glycopeptide. Specific embodiments of the invention relate to glycopeptides made of chitosan covalently bound to a poly(amino acid) such as poly(glutamic acid) or poly(aspartic acid). Diagnostic agents conjugated to the glycopeptide may facilitate imaging. Specific therapeutic agents that may be conjugated to the glycopeptide include anticancer drugs, rheumatoid arthritis drugs, anticoagulants, anti-angiogenesis drugs, apoptosis drugs, osteoporosis drugs, steroids, and anti-inflammatory drugs. Some agents, such as radionuclides, may have both diagnostic and therapeutic effects. The glycopeptides may be made by combining a glycoside and a peptide in the presence of a carbodiimide and an acid group activator to form an amide bond between the glycoside and the peptide.

摘要翻译： 本发明包括具有糖苷和通过酰胺键共价结合的肽的糖肽。 糖肽还可以包括与糖肽结合的诊断或治疗剂。 诸如放射性核素的金属也可以与糖肽螯合。 本发明的具体实施方案涉及由聚（氨基酸）如聚（谷氨酸）或聚（天冬氨酸）共价结合的脱乙酰壳多糖制成的糖肽。 与糖肽缀合的诊断剂可以促进成像。 可以与糖肽结合的具体治疗剂包括抗癌药物，类风湿关节炎药物，抗凝血剂，抗血管生成药物，凋亡药物，骨质疏松症药物，类固醇和抗炎药物。 一些药剂如放射性核素可能具有诊断和治疗作用。 糖肽可以通过在碳二亚胺和酸基活化剂的存在下结合糖苷和肽来在糖苷和肽之间形成酰胺键来制备。

公开(公告)号：EP1698351A3

公开(公告)日：2006-12-27

申请号：EP06004026.8

申请日：2006-02-28

申请人： Taiwan Hopax Chems. Mfg. Co., Ltd ,  Board of Regents, The University of Texas System

发明人： Wei, I-Chien ,  Yang, David J. ,  Yu, Dong-Fang

IPC分类号： A61K51/08 ,  A61K31/505 ,  A61K31/66

CPC分类号： A61K31/505 ,  A61K31/66 ,  A61K51/025

摘要： The invention includes glycopeptides having a glycoside and a peptide covalently bound through an amide bond. The glycopeptides may also include a diagnostic or therapeutic agent bound to the glycopeptide. A metal, such as a radionuclide, may also be chelated to the glycopeptide. Specific embodiments of the invention relate to glycopeptides made of chitosan covalently bound to a poly(amino acid) such as poly(glutamic acid) or poly(aspartic acid). Diagnostic agents conjugated to the glycopeptide may facilitate imaging. Specific therapeutic agents that may be conjugated to the glycopeptide include anticancer drugs, rheumatoid arthritis drugs, anticoagulants, anti-angiogenesis drugs, apoptosis drugs, osteoporosis drugs, steroids, and anti-inflammatory drugs. Some agents, such as radionuclides, may have both diagnostic and therapeutic effects. The glycopeptides may be made by combining a glycoside and a peptide in the presence of a carbodiimide and an acid group activator to form an amide bond between the glycoside and the peptide.

摘要翻译： 本发明包括具有糖苷和通过酰胺键共价结合的肽的糖肽。 糖肽还可以包括与糖肽结合的诊断或治疗剂。 诸如放射性核素的金属也可以与糖肽螯合。 本发明的具体实施方案涉及由聚（氨基酸）如聚（谷氨酸）或聚（天冬氨酸）共价结合的脱乙酰壳多糖制成的糖肽。 与糖肽缀合的诊断剂可以促进成像。 可以与糖肽结合的具体治疗剂包括抗癌药物，类风湿关节炎药物，抗凝血剂，抗血管生成药物，凋亡药物，骨质疏松症药物，类固醇和抗炎药物。 一些药剂如放射性核素可能具有诊断和治疗作用。 糖肽可以通过在碳二亚胺和酸基活化剂的存在下结合糖苷和肽来在糖苷和肽之间形成酰胺键来制备。

公开(公告)号：EP2014306B1

公开(公告)日：2015-02-25

申请号：EP08009119.2

申请日：2008-05-16

申请人： Taiwan Hopax Chems. Mfg. Co., Ltd.

发明人： Wei, I-Chien ,  Yang, David J. ,  Yu, Dong-Fang

IPC分类号： A61K47/48

CPC分类号： A61K47/4823 ,  A61K31/282 ,  A61K33/24 ,  A61K47/61

公开(公告)号：EP2014306A2

公开(公告)日：2009-01-14

申请号：EP08009119.2

申请日：2008-05-16

申请人： Taiwan Hopax Chems. Mfg. Co., Ltd

发明人： Wei, I-Chien ,  Yang, David J. ,  Yu, Dong-Fang

IPC分类号： A61K47/48

CPC分类号： A61K47/4823 ,  A61K31/282 ,  A61K33/24 ,  A61K47/61

摘要： The current disclosure, in one embodiment, includes a polysaccharide conjugate. This conjugate has a polysaccharide and at least one monomeric amino acid having an O-group covalently bound to the polysaccharide. The conjugate also has at least one metal conjugated by the O-group of the amino acid. According to another embodiment, the disclosure provides a method of synthesizing a polysaccharide conjugate by covalently bonding a monomeric amino acid having an O-group to a polysaccharide and by conjugating a metal to the O-group to form a polysaccharide conjugate. According to a third embodiment, the disclosure relates to a method of killing a cancer cell by administering to the cell an effective amount of a polysaccharide conjugate. This conjugate has a polysaccharide and at least one monomeric amino acid having an O-group covalently bound to the polysaccharide. The conjugate also has at least one metal conjugated by the O-group of the amino acid.

公开(公告)号：EP1698351A2

公开(公告)日：2006-09-06

申请号：EP06004026.8

申请日：2006-02-28

申请人： Taiwan Hopax Chems. Mfg. Co., Ltd ,  Board of Regents, The University of Texas System

发明人： Wei, I-Chien ,  Yang, David J. ,  Yu, Dong-Fang

IPC分类号： A61K51/08 ,  A61K31/505 ,  A61K31/66

CPC分类号： A61K31/505 ,  A61K31/66 ,  A61K51/025

摘要： The invention includes glycopeptides having a glycoside and a peptide covalently bound through an amide bond. The glycopeptides may also include a diagnostic or therapeutic agent bound to the glycopeptide. A metal, such as a radionuclide, may also be chelated to the glycopeptide. Specific embodiments of the invention relate to glycopeptides made of chitosan covalently bound to a poly(amino acid) such as poly(glutamic acid) or poly(aspartic acid). Diagnostic agents conjugated to the glycopeptide may facilitate imaging. Specific therapeutic agents that may be conjugated to the glycopeptide include anticancer drugs, rheumatoid arthritis drugs, anticoagulants, anti-angiogenesis drugs, apoptosis drugs, osteoporosis drugs, steroids, and anti-inflammatory drugs. Some agents, such as radionuclides, may have both diagnostic and therapeutic effects. The glycopeptides may be made by combining a glycoside and a peptide in the presence of a carbodiimide and an acid group activator to form an amide bond between the glycoside and the peptide.

摘要翻译： 本发明包括具有通过酰胺键共价结合的糖苷和肽的糖肽。 糖肽还可以包括与糖肽结合的诊断剂或治疗剂。 金属如放射性核素也可以与糖肽螯合。 本发明的具体实施方案涉及由共价结合至聚（氨基酸）如聚（谷氨酸）或聚（天冬氨酸）的壳聚糖制成的糖肽。 与糖肽缀合的诊断剂可以促进成像。 可以与糖肽缀合的特定治疗剂包括抗癌药物，类风湿性关节炎药物，抗凝血剂，抗血管生成药物，凋亡药物，骨质疏松药物，类固醇和抗炎药物。 一些药物，如放射性核素，可能同时具有诊断和治疗作用。 糖肽可以通过在碳二亚胺和酸基活化剂存在下将糖苷和肽结合以在糖苷和肽之间形成酰胺键来制备。