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Title:
SUPERMOLECULAR CARBOPLATINUM DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITION CONTAINING THEM AS ACTIVE INGREDIENT AND APPLICATIONS OF THE COMPOSITIONS
Document Type and Number:
WIPO Patent Application WO/2003/045962
Kind Code:
A1
Abstract:
The present invention relates to a novol class of supermolecules carboplatinum derivatives represented by general formula (I), wherein B is a polycarboxylic represented by general formula (II), wherein (R1) and (R2) and (n) is defined as in the description. This invention also relates to method of preparing the same, relates to pharmaceutical composition containing the same as active principle and the use of the derivatives in the preparation of pharmaceutical compositions which are useful in treating several cellular cancers including hepatoma, stomach cancer, lung cancer, etc. The derivatives have stable cage-like chemical structures and constituitions in solid and in aqeous solution. The derivatives can not only induce the fatality of several cancer cells at a rate significantly higher than that by carboplatinum, in particular, on hapatoma cells, at a rate one to two times higher than that by carboplatinum, but also produce little side effects such as vomit, baldness, decreases of leucocytes and platelets, which can be resulted by administration of other chemotherapeutics. The acute doxity dose LD50 of the present derivatives is about 300mg/kg and 260mg/kg weight body for a subcutaneous and a intraperitoneal administration respectively. Therefore, the novol class of cis-platium of the present derivatives have a wide prospective of application as anticancer agents.

Inventors:
WANG JINGZUN (CN)
QU HUISHENG (CN)
WANG LEI (CN)
WANG TING (CN)
Application Number:
PCT/CN2001/001595
Publication Date:
June 05, 2003
Filing Date:
November 30, 2001
Export Citation:
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Assignee:
WANG JINGZUN (CN)
QU HUISHENG (CN)
WANG LEI (CN)
WANG TING (CN)
International Classes:
A61P35/00; A61K31/282; C07C57/36; C07C59/245; C07C59/255; C07C59/265; C07C61/04; C07F15/00; (IPC1-7): C07F15/00; A61K31/282
Foreign References:
CN1311183A2001-09-05
CN1118252A1996-03-13
Other References:
See also references of EP 1473298A4
Attorney, Agent or Firm:
Beijing, Zhongzi Law Office (Tower C Jiancai Building 11A Sanlihe Road Haidian District Beijing 7, CN)
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