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1. 发明申请

WO1997038727A1 MEDICAMENT COMPOSITE 审中-公开
标题翻译：药物组合物
公开(公告)号：WO1997038727A1
公开(公告)日：1997-10-23
申请号：PCT/JP1997001303
申请日：1997-04-15
申请人： ASAHI KASEI KOGYO KABUSHIKI KAISHA , SUGAWARA, Shuichi , KAJIKI, Masahiro , KURIYAMA, Hiroshi , KITAGUCHI, Nobuya
发明人： ASAHI KASEI KOGYO KABUSHIKI KAISHA
IPC分类号： A61K47/48
CPC分类号： A61K47/61 , A61K47/60
摘要： A composite of medicaments each having a hydroxyl group and represented by the following general formula: A-B-C, wherein A represents a carrier selected among saccharides each having a carboxyl group, polyethylene glycol, aliphatic carboxylic acids and their derivatives, B represents a spacer having amino and carboxyl groups in its molecule, and C represents a medicament having a hydroxyl group. In this case, the carrier A and the spacer B are bonded to each other through the amide linkage formed between the carboxyl group of the carrier A and the amino group of the spacer B, while the spacer B and the medicament C are bonded to each other through the ester bond formed between the carboxyl group of the spacer B and the hydroxyl group of the medicament C. The composite exhibits a surely controlled release rate of the medicament therefrom to increase the migration of the medicament to a target tissue and/or to enhance the efficacy of the medicament.
摘要翻译：具有羟基并由以下通式表示的药物复合物：ABC，其中A表示选自具有羧基的糖类，聚乙二醇，脂肪族羧酸及其衍生物的载体，B表示具有氨基和羧基分子，C代表具有羟基的药物。在这种情况下，载体A和间隔物B通过形成在载体A的羧基和间隔物B的氨基之间的酰胺键彼此键合，而隔离物B和药物C结合到每个另一个通过在间隔物B的羧基与药物C的羟基之间形成的酯键。复合材料表现出药物的可靠控制的释放速率，以增加药物向目标组织的迁移和/或增强药物的功效。

2. 发明申请

WO1994019376A1 POLYSACCHARIDE DERIVATIVE AND DRUG CARRIER 审中-公开
标题翻译：多糖衍生物和药物载体
公开(公告)号：WO1994019376A1
公开(公告)日：1994-09-01
申请号：PCT/JP1994000322
申请日：1994-02-28
申请人： DRUG DELIVERY SYSTEM INSTITUTE, LTD. , NOGUSA, Hideo , HAMANA, Hiroshi , YANO, Toshiro , KAJIKI, Masahiro , YAMAMOTO, Keiji , OKUNO, Satoshi , SUGAWARA, Shuichi , KASHIMA, Nobukazu , INOUE, Kazuhiro
发明人： DRUG DELIVERY SYSTEM INSTITUTE, LTD.
IPC分类号： C08B37/00
CPC分类号： C08B37/0063 , A61K47/65 , C08B37/00 , C08B37/0006
摘要： A novel polysaccharide derivative, and a drug carrier and a drug composite both comprising said derivative. The derivative is a carboxylated polysaccharide wherein a peptide chain composed of one to eight same or different amino acids is introduced into part or all of the carboxyl groups of the polysaccharide and wherein part or all of those amino or carboxyl groups of the peptide chain which do not participate in the above linkage to the carboxyl groups of the polysaccharide may be bonded to the carboxyl, amino or hydroxyl groups of another compound (e.g. a drug) through amide or ester bonds. The derivative can migrate to the tumor-bearing region so readily that it can efficiently send drugs which are problematic in the side effects or have limited persistence of the drug activity in the tumor-bearing region.
摘要翻译：一种新型多糖衍生物，以及包含所述衍生物的药物载体和药物复合物。该衍生物是一种羧化多糖，其中由一至八个相同或不同氨基酸组成的肽链被引入到多糖的部分或全部羧基中，并且其中肽链的那些氨基或羧基的部分或全部是不参与与多糖的羧基的上述键合可以通过酰胺或酯键与另一化合物（例如药物）的羧基，氨基或羟基键合。该衍生物可以很容易地迁移到含肿瘤的区域，以便能够有效地发送药物在副作用中有问题或在肿瘤负荷区域具有有限的药物活性持续性的药物。

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