Mental complexes having an antineoplastic action, and medicament

Details Mental complexes having an antineoplastic action, and medicament Mental complexes having an antineoplastic action, and medicament

1983-04-29

1986-03-25

Sneed, Helen M. S.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Carbohydrate doai

556 40, A01N 5504, C07F 700, C07F 728, A61K 3132

Patent

active

045784019

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

The invention relates to metal complexes having an antineoplastic action and to medicaments containing these complexes.


PRIOR ART

A medicament which contains the complex compound cis-diamminodichloroplatinum(II) has recently been marketed as a chemotherapeutic agent against cancer. This compound, known by the International Nonproprietary Name (INN) of cisplatin has proved to be an extremely potent antitumoral agent, especially in the treatment of testicular tumors, and also, for example, of ovarian tumors and parvicellular bronchial carcinomas. The disadvantage of cisplatin is its relatively high toxicity. Its nephrotoxicity and its action leading to lasting damage to hearing are particularly serious. Renal damage and damage to hearing are found with considerable frequency after administration of only a single therapeutic dose. Besides the nephrotoxic and haematoxic action, the long-lasting severe nausea and the retching associated therewith are, above all, also extremely unpleasant for the patients.
Numerous other platinum complexes (German Offenlegungsschrift No. 2,445,418, German Offenlegungsschrift No. 2,837,237, German Offenlegungsschrift No. 2,626,559 and German Offenlegungsschrift No. 2,539,179) and complex compounds of other transition metals have recently been proposed as agents having a cytostatic action. In German Offenlegungsschrift No. 2,801,355, a brown amorphous complex which is obtained by reacting ascorbic acid with a titanium(III) compound and a copper (II) compound (in a molar ratio of 36:1:6) is said to have curative and prophylactic actions against, inter alia, leukemia. It has been reported that titanocene dichloride, zirconocene dichloride and hafnocene dichloride have an inhibiting action on ascitic Ehrlich tumors in mice [P.Kopf-Maier, B. Hesse and H. Kopf, J. Cancer Res. Clin. Oncol. 96, 43 (1980)].Dihalogenobis-(1,3-diketonato)-tin, -titanium, -zirconium and -hafnium compounds having an antineoplastic activity are described in European Laid-Open Application 49,486.


DESCRIPTION OF THE INVENTION

Surprisingly, it has now been found that the metal complexes of the general formula I M(OR.sup.4).sub.2-n X.sub.n (I) monosubstituted or polysubstituted by fluorine, chlorine, bromine, nitro, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or trifluoromethyl, monosubstituted or polysubstituted by fluorine, chlorine, bromine, nitro, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy or trifluoromethyl, hydroxyl, C.sub.1 -C.sub.3 -alkylamino or alkali metal sulfonato groups, or denotes C.sub.5 -C.sub.8 -cycloalkyl, which can be substituted by C.sub.1 -C.sub.5 -alkyl groups, hydroxyl or alkali metal sulfonato groups, hydrogen, and have an interesting cytostatic activity coupled with an advantageous therapeutic range, and are suitable as chemotherapeutic agents for the treatment of cancers. They are useful as chemotherapeutic agents with few side effects for the treatment of tumors, e.g. ovarian tumors, testicular tumors, carcinomas of the prostate, bronchial carcinomas, carcinomas of the urinary bladder, oesophagal carcinomas and other malignant neoplasias. Accordingly, the compounds are useful for alleviation of pain and suffering in connection with cancer therapy, remission, alleviation of symptoms and extension of life expectancy.
The invention thus relates to medicaments containing one or more metal complexes of the above general formula I, wherein M, R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, m and n have the abovementioned meanings, in particular for combating cancers.
Medicaments containing one or more metal complexes of the general formula I' M'(OR.sup.4').sub.2-n X'.sub.n (I') monosubstituted or polysubstituted by fluorine, chlorine, bromine, nitro, C.sub.1 -C.sub.2 -alkyl, C.sub.1 -C.sub.2 -alkoxy or trifluoromethyl, substituted by C.sub.1 -C.sub.2 -alkoxy, hydroxyl, C.sub.1 -C.sub.3 -alkylamino or alkali metal sulfonato groups, or denotes cyclohexyl, which can be substituted by C.sub.1 -C.sub.4 -alkyl groups, hydrogen, and are particularly preferred.
Medicaments

REFERENCES:
patent: 3334067 (1967-08-01), Weyenberg
Puri, Chemical Abstracts, vol. 58, No. 4, 3343h, 2/18/63.
Saxena, J. Chem. Soc. (A), 904-907, 1970.
Yamamoto, J.A.C.S., vol. 79, 4344-4348, 8/20/57.

Affiliated with

Also associated with

Rating

Mental complexes having an antineoplastic action, and medicament does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Mental complexes having an antineoplastic action, and medicament, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Mental complexes having an antineoplastic action, and medicament will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-631123