Organic compounds -- part of the class 532-570 series – Organic compounds – Heavy metal containing
Reexamination Certificate
2007-08-21
2007-08-21
Nazario-Gonzalez, Porfirio (Department: 1621)
Organic compounds -- part of the class 532-570 series
Organic compounds
Heavy metal containing
C514S492000
Reexamination Certificate
active
10497081
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, R2and 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 300 mg/kg and 260 mg/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.
REFERENCES:
patent: 6699901 (2004-03-01), Yang et al.
Wong et al., 1999,“Current Status of Platinum-Based Antitumor Drugs”, Chem. Rev., 99: 2451-2466.
Go et al., 1999,“Review of the Comparative Pharmacology and Clinical Activity of Cisplatin and Carboplatin”, Journal of Clinical Oncology, vol. 17, No. 1: 409-422.
Qu Huisheng
Wang Jingzun
Wang Lei
Wang Ting
Morgan & Lewis & Bockius, LLP
Nazario-Gonzalez Porfirio
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