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公开(公告)号：EP0916348B1
公开(公告)日：2004-08-18
申请号：EP97924325.0
申请日：1997-06-05
发明人： INOUE, Kazuhiro, Daiichi Pharmaceutical Co., Ltd. , SUSAKI, Hiroshi, Daiichi Pharmaceutical Co., Ltd. , IKEDA, Masahiro, Daiichi Pharmaceutical Co., Ltd. , KUGA, Hiroshi, Daiichi Pharmaceutical Co., Ltd. , KUMAZAWA, Eiji, Daiichi Pharmaceutical Co., Ltd. , TOGO, Akiko, Daiichi Pharmaceutical Co., Ltd.
IPC分类号： A61K47/48
CPC分类号： A61K47/61
摘要： Drug complexes wherein a carboxy (C1-4)alkyldextran polyalcohol, which has been treated under such conditions as to allow the substantially complete formation of the polyalcohol, is bonded to the residue of a medicinal compound such as an antitumor agent via a spacer consisting of one amino acid or a spacer consisting of two to eight amino acids bonded to each other via peptide bonds. The complexes are excellent in the tumor site selectivity and thus can exhibit a high antitumor effect with relieved expression of toxicity.
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公开(公告)号：EP0916348A1
公开(公告)日：1999-05-19
申请号：EP97924325.0
申请日：1997-06-05
发明人： INOUE, Kazuhiro, Daiichi Pharmaceutical Co., Ltd. , SUSAKI, Hiroshi, Daiichi Pharmaceutical Co., Ltd. , IKEDA, Masahiro, Daiichi Pharmaceutical Co., Ltd. , KUGA, Hiroshi, Daiichi Pharmaceutical Co., Ltd. , KUMAZAWA, Eiji, Daiichi Pharmaceutical Co., Ltd. , TOGO, Akiko, Daiichi Pharmaceutical Co., Ltd.
IPC分类号： A61K47/48
CPC分类号： A61K47/61
摘要： A drug complex characterized in that a residue of a drug compound such as antineoplastic agents and a carboxy(C 1-4 )alkyldextran polyalcohol obtained by treating a dextran under conditions that enable substantially complete polyalcoholization are bound to each other by means of a spacer comprising an amino acid or a spacer comprising peptide-bonded 2 to 8 amino acids. Said complex is characterized in that it has excellent selectivity to tumorous sites so as to exhibit high antineoplastic activity and also achieves reduced appearance of toxicity.
摘要翻译： 一种药物复合物，其特征在于通过在基本上完成多元醇化的条件下处理葡聚糖而得到的抗肿瘤剂和羧基（C1-4）烷基葡聚糖多元醇等药物化合物的残基彼此通过包含 氨基酸或包含肽键合2至8个氨基酸的间隔区。 所述复合物的特征在于它对肿瘤部位具有优异的选择性，从而显示出高抗肿瘤活性并且还实现了降低的毒性表现。
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