US2004005365A1PendingUtilityA1

Carcinostatic substance for compatible administration, process of administrating same and process of rapidly inspecting same

Priority: Nov 11, 1994Filed: Dec 17, 2002Published: Jan 8, 2004
Est. expiryNov 11, 2014(expired)· nominal 20-yr term from priority
A61P 35/00A61K 31/505A61K 31/555A61K 38/14A61K 31/70A61K 33/243
41
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Claims

Abstract

Disclosed herein are a process of compatibly administrating a carcinostatic substance with cis-oxalato (1R, 2R-diaminocyclohexane) Pt (II), or a certain platinum complex, and a carcinostatic substance which may be employed in the above process. The combination of the carcinostatic substance, for example, 6-fluorouracil and the above platinum complex in accordance with present invention promotes the anticancer property of the carcinostatic substance.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A process of compatibly administering a carcinostatic substance which comprises compatibly administering one or more compatible agents selected from a group consisting of cisplatin, carboplatin, 5-fluorouracil, tegaful, carmoful, doxifluridine, uracil, irinotecane, adriamycin, etoposide, mitomycin, mitoxantrone, and bleomycin with cis-oxalato (1R,2R-diaminocyclohexane) Pt (II).  
     
     
         2 . The process of compatibly administrating a carcinostatic substance as claimed in  claim 1 , therein the compatible agent is simultaneously administrated with the cis-oxalato (1R,2R-diaminocyclohexane) Pt (II).  
     
     
         3 . The process of compatibly administering a carcinostatic substance as claimed in  claim 2 , wherein the 5-fluorouracil is simultaneously administrated with the cis-oxalato (1R,2R-diaminocyclohexane) Pt (II).  
     
     
         4 . The process of compatibly administrating a carcinostatic substance as claimed in  claim 1 , wherein either of the compatible agent or the cis-oxalato (1R,2R-diaminocyclohexane) Pt (II) is subsequently added.  
     
     
         5 . A carcinostatic substance selected from a group consisting of cisplatin, carboplatin, 5-fluorouracil, tegaful, carmoful, doxifluridine, uracil, irinotecane, adriamycin, etoposide, mitomycin, mitoxantrone and bleomycin which can be compatibly administered with cis-oxalato (1R,2R-diaminocyclohexane) Pt (II).  
     
     
         6 . A mixed carcinostatic substance comprising one or more compatible agents selected from a group consisting of cisplatin, carboplatin, 5-fluorouracil, tegaful, carmoful, doxifluridine, uracil, irinotecane, adriamycin, etoposide, mitomycin, mitoxantrone, and bleomycin, and cis-oxalato (1R,2R-diaminocyclohexane) Pt (II) mixed with the compatible agent.  
     
     
         7 . A carcinostatic substance comprising cis-oxalato (1R,2R-diaminocyclohexane) Pt (II) and one or more compatible agents selected from a group consisting of cisplatin, carboplatin, 5-fluorouracil, tegaful, carmoful, doxifluridine, uracil, irinotecane, adriamycin, etoposide, mitomycin, mitoxantrone and bleomycin which are bonded to the cis-oxalato (1R,2R-diaminocyclohexane) Pt (II) by means of a coordination bond.  
     
     
         8 . A process of compatibly administrating a carcinostatic substance which comprises compatibly administrating one or more compatible agents selected from a group consisting of cisplatin, vincristin, carboplatin, 5-fluorouracil, tegaful, carmoful, doxifluridine, uracil, irinotecane, adriamycin, etoposide, mitomycin, mitoxantrone and bleomycin with a platinum complex having a Formula I [in this Formula, a Formula II is a diamine selected from a group consisting of 1,2-cycloalkane (C 6  to C 7 ) diamine (its stereostructure is cis-(R,S-), trans-d(1S,2S-) or trans-l(1R,2R-)) having a Formula III, 2′-aminomethylcyclohexylamine (its stereostructure is cis-l(R,R-), cis-d(S,S-), trans-l(R,S-) or trans-d(S,R-) having a Formula IV and 1,1-diaminomethylcyclohexane, 0-phenylenediamine, ethylenediamine or propyrenediamine having a Formula V, and a Formula VI is a ligand forming a five or six-membered ring coordinated to Pt(IV) in 0-0 coordination, and X is an aliphatic alkyl or an aromatic alkyl having C 1  to C 10 ].  
       
         
           
           
               
               
           
         
       
     
     
         9 . The process as claimed in  claim 8 , wherein the cisplatin or the vincristin is simultaneously administered with the platinum complex.  
     
     
         10 . A mixed carcinostatic substance comprising one or more compatible agents selected from a group consisting of cisplatin, vincristin, carboplatin, 6-fluorouracil, tegaful, carmoful, doxifluridine, uracil, irinotecane, adriamycin, etoposide, mitomycin, mitoxantrone and bleomycin, and a platinum complex having a Formula I [in this Formula, a Formula II is a diamine selected from a group consisting of 1,2-cycloalkane (C 6  to C 7 ) diamine (its stereostructure is cis-(R,S-), trans-d(1S,2S-) or trans-l(1R,2R-)) having a Formula III, 2-aminomethylcyclohexylamine (its stereostructure is cis-l(R,R-), cis-d(S,S-), trans-l(R,S-) or trans-d(S,R-)) having a Formula IV and 1,1-diaminomethylcyclohexane, 0-phenylenediamine, ethylenediamine or propyrenediamine having a Formula V, and a Formula VI is a ligand forming a five or six-membered ring coordinated to Pt(IV) in 0-0 coordination, and X is an aliphatic alkyl or an aromatic alkyl having C 1  to C 10 ] mixed with the compatible agent.  
       
         
           
           
               
               
           
         
       
     
     
         11 . A carcinostatic substance comprising a platinum complex having a Formula I [in this Formula, a Formula II is a diamine selected from a group consisting of 1,2-cycloalkane (C 6  to C 7 ) diamine {its stereostructure is cis-(R,S-), trans-d(1S,2S) or trans-l(1R,2R-)} having a Formula III, 2-aminomethylcyclohexylamine {its stereostructure is cis-l(R,R-), cis-d(S,S-), trans-l(R,S-) or trans-d(S,R-)} having a Formula IV and 1,1-diaminomethylcyclohexane, 0-phenylethylenediamine, ethylenediamine or propyrenediamine having a Formula V, and a Formula VI is a ligand forming a five or six-membered ring coordinated to Pt(IV) in 0-0 coordination, and X is an aliphatic alkyl or an aromatic alkyl having C 1  to C 10 ], and one or more compatible agents selected from a group consisting of cisplatin, vincristin, carboplatin, 5-fluorouracil, tegaful, carmoful, doxifluridine, uracil, irinotecane, adriamycin, etoposide, mitomycin, mitoxantrone and bleomycin coordinated to the platinum complex by means of chemical bonding.  
     
     
         12 . A process of observing cell division which comprises adding fluorescence dye to cells to be observed, bonding the fluorescence dye to each cell, and observing the cells with a microscope for clarifying the cell division condition.  
     
     
         13 . A process of rapidly inspecting a carcinostatic substance which comprises adding fluorescence dye and a carcinostatic substance to be inspected to a plurality of cancer cells which have been cultivated, continuing the cultivation, measuring the number of the cells in the division period appearing in the plurality of the cancer cells and inspecting the effect of the carcinostatic substance.  
     
     
         14 . The process as claimed in  claim 13 , wherein the fluorescence dye is 4′,6-diamidino-2-phenylindole-2HCl.

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