Title:
超分子カルボプラチン誘導体、その製造方法、活性成分としてその誘導体を含有する薬学的組成物およびその使用
Document Type and Number:
Japanese Patent JP4235111
Kind Code:
B2
Abstract:
The present invention relates to a novel class of supermolecular carboplatin derivatives represented by general formula (I), wherein B is a polycarboxylic acid represented by general formula (II), wherein R1, R2 and n are defined as in the description. The present invention also relates to a process for preparing the same, pharmaceutical compositions containing the same as active ingredient and the use of the derivatives in the preparation of pharmaceutical compositions which are useful in treating various cellular cancers including hepatoma, stomach cancer, lung cancer and the like. The derivatives have stable cage-like chemical structures and constitutions in solid and in aqueous solution. The derivatives can not only kill cancer cells at a rate significantly higher than that by carboplatin, in particular, in the case of hepatoma cells, at a rate one to two times higher than that by carboplatin, but also produce little side effects such as vomit, baldness, decreases of leucocytes and platelets, and the like, which can be induced by administration of other chemotherapeutics. In the acute toxicity tests on mice, the lethal dose(LD50) of the present derivatives is about 300mg/kg and 260mg/kg body weight for a subcutaneous(sc) and an intraperitoneal(ip) administration, respectively. Therefore, the present derivatives are a novel class of cis-platium which can be widely used as anticancer agents.
Inventors:
King respect
Chui Kei
Wang Lei
King
Chui Kei
Wang Lei
King
Application Number:
JP2003547411A
Publication Date:
March 11, 2009
Filing Date:
November 30, 2001
Export Citation:
Assignee:
King respect
Chui Kei
Chui Kei
International Classes:
A61P35/00; C07C61/04; A61K31/282; C07C57/36; C07C59/245; C07C59/255; C07C59/265; C07F15/00
Foreign References:
| CN1311183A | ||||
| WO1993015729A1 |
Attorney, Agent or Firm:
Sota Asahina
Fumio Akiyama
Ryosuke Tamura
Koji Yashima
Fumio Akiyama
Ryosuke Tamura
Koji Yashima