公开(公告)号：EP0916348A4

公开(公告)日：2000-11-29

申请号：EP97924325

申请日：1997-06-05

申请人： DAIICHI SEIYAKU CO ,  DRUG DELIVERY SYSTEM INST LTD

发明人： INOUE KAZUHIRO ,  SUSAKI HIROSHI ,  IKEDA MASAHIRO ,  KUGA HIROSHI ,  KUMAZAWA EIJI ,  TOGO AKIKO

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.

公开(公告)号：EP1155702A4

公开(公告)日：2004-12-15

申请号：EP99952805

申请日：1999-10-29

申请人： DAIICHI SEIYAKU CO

发明人： SUSAKI HIROSHI ,  INOUE KAZUHIRO ,  KUGA HIROSHI ,  IKEDA MASAHIRO ,  SHIOSE YOSHINOBU ,  KORENAGA HIROSHI

IPC分类号： A61K31/4745 ,  A61K47/48 ,  C08B37/02 ,  C07D491/22 ,  C08B37/00

CPC分类号： A61K31/4745 ,  A61K47/61 ,  A61K47/65 ,  C08B37/0021

摘要： A method for assaying a DDS compound containing a saccharide compound-modified carboxy C1-4 alkyldextran polyalcohol and a drug compound residue bonded to this carboxy C1-4 alkyldextran polyalcohol, or a DDS compound wherein a polymer carrier is bonded to a drug compound residue via a spacer containing 2 to 8 amino acids bonded together via peptide bonds, which involves the step of assaying a hydrolysate obtained by treating the DDS compound with peptidase.

公开(公告)号：EP1080732A4

公开(公告)日：2004-08-25

申请号：EP99919664

申请日：1999-05-21

申请人： DAIICHI SEIYAKU CO

发明人： SUSAKI HIROSHI ,  INOUE KAZUHIRO ,  KUGA HIROSHI

IPC分类号： A61K47/48 ,  A61K9/00 ,  A61K31/47 ,  A61K47/36 ,  C07D491/22

CPC分类号： A61K47/62 ,  A61K47/56 ,  A61K47/61 ,  A61K47/65

摘要： Drug composites useful as DDS compounds, which are represented by the general formula: A-R-NH-Y-CH2-O-CO-Q (wherein A is a polymer serving as a carrier for a drug; R is a spacer comprising one amino acid molecule or one comprising 2 to 8 amino acid molecules bound to each other through peptide linkage; Y is optionally substituted phenylene; and Q is a residue of a drug compound such as an antitumor agent). The composites permit the speedy and regioselective release of drug compounds such as antitumor or anti-inflammatory agents, thus exhibiting expected drug effects without fail.

摘要翻译： 用作DDS化合物的药物复合物，其由下式表示：A-R-NH-Y-CH 2 -O-CO-Q，其中A是作为药物载体的聚合物; R是间隔基，其中所述间隔基是氨基酸或包含2-8个氨基酸的寡肽; Y是可以被取代的亚苯基; Q是药物化合物的残留物，例如抗肿瘤剂。 该复合物提供了药物化合物例如抗肿瘤药或抗炎药物的快速和局部选择性释放，并确实显示预期的疗效。