Process to obtain new mixed copper aminoacidate complexes from phenylate phenathrolines to be used as anticancerigenic agents

Abstract

This invention refers to a process to obtain new mixed copper aminoacidates complexes from phenanthrolines of an aromatic type to be used as anticancerigenic agents preferably with a therapeutic use for the treatment of liquid and solid cancerigenic tumors such as leukemia. The complexes obtained are of the [Cu (N-N) (N-O)]± NO 3 type in which the N-N ligand corresponds to 4, 7-diphenyl-1, 10 phenanthroline and the N-O ligand preferably corresponds to one of the aminoacidates such as glycinate, alaninate, isoleucinate, leucinate, serinate and valinate. The process is characterized because it includes the following steps: making an aqueous solution based on an aliphatic alcohol and 4,7-diphenyl-1, 10 phehanthrolin react with a copper complex preferably Cu NO 3 5H 2 O at room temperature, and immediately after making the obtained product react in an aqueous aminoacidate solution adjusting a slightly alkaline pH.

What is claimed is: 
     
       1. A process for preparing an aromatic copper aminoacidate complex from a phenylate phenanthroline useful as an anticancerigenic agent and having the formula [Cu (N-N) (N-O)].sup.± NO 3 , where the N-N ligand is a diimine compound comprising 4,7-diphenyl-1,10-phenanthroline and the N-O ligand is an aminoacidate ion selected from the group consisting of glycinate, alaninate, isoleucinate, leucinate, serinate, and valinate, comprising the steps of preparing a first aqueous solution containing from 30% to 35% by weight of Cu (NO 3 ) 2 .5H 2  O, preparing a second aqueo-ethanolic solution containing from 50% to 55% by weight of the diimine compound, combining the first and second aqueous solutions together in a reactor at room temperature to form a reaction medium and obtain a copper complex of the diimine compound while maintaining an acid pH of between 5 and 7, adding to the medium an aqueous solution containing from 10% to 15% by weight of the aminoacidate ion, and thereafter keeping the reaction medium slightly alkaline to obtain an aromatic copper aminoacidate complex selected from the group consisting of: [Cu (4,7diphenyl-1,10-phenanthroline) (alaninate)].sup.± NO 3  ;   [Cu (4,7diphenyl-1,10-phenanthroline) (glycinate)].sup.± NO 3  ;   [Cu (4,7diphenyl-1,10-phenanthroline) (isoleucinate)].sup.± NO 3  ;   [Cu (4,7diphenyl-1,10-phenanthroline) (leucinate)].sup.± NO 3  ;   [Cu (4,7diphenyl-1,10-phenanthroline) (serinate)].sup.± NO 3  ; and   [Cu (4,7diphenyl-1,10-phenanthroline) (valinate)].sup.± NO 3 .   
     
     
       2. The process of claim 1, wherein the copper complex of the diimine compound is of the [Cu (N-N)].sup.± NO 3  type, the first and second solutions being brought into contact in the reactor for approximately 5 minutes at room temperature to yield said copper complex. 
     
     
       3. The process of claim 1, wherein the aqueous solution contains from 12% to 15% by weight of the aminoacidate ion and the reaction medium is kept slightly alkaline after addition of the aminoacidate ion containing aqueous solution with an aqueous-ammonical solution. 
     
     
       4. The process of claim 1, 2, or 3, wherein the aromatic copper aminoacidate complex obtained is passed through a millipore filter, slightly heated and distilled in vacuum to eliminate raw materials and secondary products, and then sterilized to obtain a pure complex. 
     
     
       5. A process for treating a subject suffering from liquid or solid cancerigenic tumors which comprises administering to said subject a therapeutic effective amount of one or more of said aromatic copper aminoacidate complexes produced by the process of claim 1, 2 or 3. .Iadd. 
     
     
       6.  A copper amino acidate diimine nitrate compound selected from the group consisting of: [Cu (4,7diphenyl-1,10-phenanthroline) (alaninate)]NO 3  ;   [Cu (4,7diphenyl-1,10-phenanthroline) (glycinate)]NO 3  ;   [Cu (4,7diphenyl-1,10-phenanthroline) (isoleucinate)]NO 3  ;   [Cu (4,7diphenyl-1,10-phenanthroline) (leucinate)]NO 3  ;   [Cu (4,7diphenyl-1,10-phenanthroline) (serinate)]NO 3  ; and   [Cu (4,7diphenyl-1,10-phenanthroline) (valinate)]NO 3 . .Iaddend..Iadd.7. A composition for the treatment of liquid and solid cancerigenic tumors comprising an effective amount of at least one copper amino acidate diimine nitrate compound of claim 6 and acceptable carrier. .Iaddend.