Platinum(II) complex and malignant tumor treatment agent

Details Platinum(II) complex and malignant tumor treatment agent Platinum(II) complex and malignant tumor treatment agent

1996-01-29

1997-04-01

Nazario-Gonzalez, Porfirio

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heavy metal containing doai

549210, 549212, 549297, 556137, A61K 3128, C07F 1500

Patent

active

056166133

DESCRIPTION:

BRIEF SUMMARY
This application was filed under 35 U.S.C. .sctn.371 as a request for U.S. examination of International application No. PCT/JP95/0075 filed on Apr. 10, 1995.
1. Technical Field
The present invention relates to a novel platinum(II) complex and to an agent for treating malignant tumors which contains it as effective component.
2. Background Art
A number of platinum(II) complexes with antitumor activity have been reported, including cis-diamminedichloroplatinum(II) complex (cisplatin) (for example, Japanese Unexamined Patent Publication Nos. 1-311089 and 2-45494).
However, although cisplatin and carboplatin have been known to be very effective against testicular carcinoma and the like, there have been problems of resistance to and thus lowered potency of cisplatin and carboplatin when they are readministered to recurrent patients.
In addition, most of the hitherto known complexes have had disadvantages such as low solubility, either making it impossible to employ intravenous administration which is the method of administration for platinum complexes (for example, cyclobutane-1,1-dicarboxylate, Japanese Unexamined Patent Publication No. 60-10952), or giving them poor stability in aqueous solutions (for example, trimellitic acid, J. P. Andrelius et al., Proceedings of the Fifth International Symposium on Other Metal Compounds in Cancer Chemotherapy, 450 (1987)). The platinum complex described in Japanese Unexamined Patent Publication No. 5-178873 is soluble enough for intravenous administration, but when the hydrophobicity of its substituents increases, the water-solubility of the platinum complex is reduced.


DISCLOSURE OF THE INVENTION

It is an object of the present invention to overcome the above-mentioned disadvantages of the prior art by providing an agent for treating malignant tumors which is based on the discovery of a complex with antitumor activity which has an effect against cisplatin-resistant carcinoma, which is soluble enough for intravenous administration, and which is stable in aqueous solution.
The aforementioned object is achieved by the following invention.
That is, the present invention relates to a novel platinum(II) complex represented by the following general formula (A) ##STR2## in which R.sub.1 represents a lower hydrocarbon radical of 1 to 3 carbon atoms, R.sub.2 and R.sub.3 each independently represent a hydrogen atom or a lower hydrocarbon radical of 1 to 3 carbon atoms, or R.sub.2 and R.sub.3 together may form --(CH.sub.2).sub.4 --or --(CH.sub.2).sub.5 --, Y and Z each independently represent an ammonia molecule or a monodentate amine of 1 to 7 carbon atoms or X and Y together may form a bidentate diamine of 2 to 10 carbon atoms, and X.sup.- represents an inorganic acid anion or an organic carboxylate anion, as well as an agent for treating malignant tumors which contains the compound as an effective component.


BEST MODE FOR CARRYING OUT THE INVENTION

In the compound of formula (A), the lower hydrocarbon radical of 1 to 3 carbon atoms is preferably an alkyl or alkenyl radical, and may specifically be methyl, ethyl, propyl, vinyl, isopropyl, allyl or isopropenyl, with methyl being particularly preferred.
The moiety, ##STR3## bonded to the platinum in formula (A) exhibits a tautomerism represented by ##STR4##
When Y and Z are amines with one nitrogen atom, they are preferably amines having a hydrocarbon radical of 1 to 10 carbon atoms. Specific examples thereof include n-propylamine, iso-propylamine, n-butylamine, n-hexylamine, n-octylamine, cyclopropylamine, cyclobutylamine, cyclopentylamine and cyclohexylamine.
Examples of the bidentate diamine formed by Y and Z together include unsubstituted and substituted 1,2-diaminoethane, unsubstituted and substituted 1,3-diaminopropane, unsubstituted and substituted 1,4-diaminobutane and unsubstituted and substituted 2-aminomethylpyridine. The substituents on these diamines are preferably radicals composed of carbon and hydrogen or of carbon, hydrogen and oxygen, and have 1 to 10 carbon atoms.
Preferred examples of substituted 1,2-diamino

REFERENCES:
"The Pharmaceutical Stabilization of the Clinical Anticancer Drug Dach-Platinum-TMA (NSC271674)" P.J. Andrulis, Jr. et al, Proceedings of the Fifth International Symposium on Platinum and Other Metal Coordination Compounds in Cancer Chemotherapy Abano, Padua, Italy-Jun. 29-Jul. 2, 1987, pp. 450-455.

Affiliated with

Also associated with

Rating

Platinum(II) complex and malignant tumor treatment agent does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Platinum(II) complex and malignant tumor treatment agent, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Platinum(II) complex and malignant tumor treatment agent will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-539428