Antigenic substance inductor, vaccine precursor, vaccine, antibody, neutralizing antibody, antitoxin, idiotype antibody and/or anti-idiotype antibody which is induced by its idiotype antibody

Abstract

This invention provides antigen substance inductors which produce highly selective and/or specific vaccine precursor, vaccine, antibody (including idiotype antibody), neutralizing antibody, antitoxin. This invention is to produce and/or manufacture highly selective and/or specific vaccine precursor, vaccine, antibody (including idiotype antibody), neutralizing antibody, antitoxin by quantum thermodynamic and chemical control of molecular functions and morphogenesis, inducing non-functional complex macromolecules which form organism and/or non-organism and which become to be substance with fundamental structure more closed to an induction of the functions, utilizing the fundamental structure of molecule which is indicated in Formula 3-a as a representative molecule. Moreover, by those produced substances, this invention is to produce and/or manufacture antimicrobial agent, antiviral agent, neutralizing antibody, antitoxin, antitumor agent, anti-protozoa agent (malaria, spirochaeta et. al), molecular discriminating agent, antibody as labeled compounds, histocompatible accelerator on tissues or organs, immuno-response accelerator or immuno-response controller, complement chain reaction accelerator.

1 . An antigenic substance inductor represented by the Formula 1-a:  
       
         
           
           
               
               
           
         
         (wherein  
         (i) R1, R2, R3, R4, R5 and R6 represent independently hydrogen atom; halogen atom; C1-C6 alkyl group; amidino group; C3-C8 cycloalkyl group; C1-C6 alkoxy C1-C6 alkyl group; aryl group; allyl group; aralkyl group in which one or more C1-C6 alkyl groups are bound to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene ring; C1-C6 alkylene group; benzoyl group; cinnamyl group; cinnamoyl group or furoyl group;  
         (ii) A represents hydrogen atom or  
         
           
             
             
                 
                 
             
           
         
         (wherein 
 R7 represents C1-C6 alkyl group; sulfide group or phosphate group;  
 R8 and R9 represent independently hydrogen atom; halogen atom; straight or branched C1-C6 alkyl group; aryl group; allyl group; aralkyl group in which one or more C1-C6 alkyl groups are bound to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene ring; C1-C6 alkylene group; benzoyl group; cinnamyl group; cinnamoyl group or furoyl group;  
 
         (iii) one or more of R1, R2, R3 and R4, and/or one or more of R5 and R6 may be substituted or non-substituted cyclopentyl group; substituted or non-substituted cyclohexyl group; or substituted or non-substituted naphthyl group;  
         (iv) R5 and R6 may form a ring by binding with another condensation polycyclic hydrocarbon compound or heterocyclic compound;  
         (v) one or more of R3, R4, R5 and R6 may be substituted by one or more of substituents selected from the group consisting of halogen atom, cyano group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, C1-C6 alkyl group, C1-C6 alkoxy group, C1-C7 alkoxy carbonyl group, aryl group, C3-C6 cycloalkyl group, C1-C6 acylamino group, C1-C6 acyloxy group, C2-C6 alkenyl group, C1-C6 trihalogenoalkyl group, C1-C6 alkylamino group, and C1-C6 dialkylamino group;  
         (vi) R2 and/or R5 may be substituted by one or more substituents selected from the group consisting of halogen atom, C1-C6 alkyl group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, protected or non-protected C1-C6 alkylamino group, protected or non-protected C1-C6 aminoalkyl group, protected or non-protected C1-C6 alkylamino C1-C6 alkyl group, protected or non-protected hydroxyalkyl group, and C3-C6 cycloalkylamino group;  
         (vii) when one or more of R3, R4, R5 and R6 are alkyl groups, terminal end(s) of the alkyl group(s) may be substituted by C3-C8 cycloalkyl group).  
       
     
     
         2 . The antigenic substance inductor according to  claim 1 , wherein 
 said aryl group in (i), (ii) and (v) is phenyl, tollyl, xylyl or naphthyl group;    said substituted cyclopentyl group in (iii) is cyclopentylamino group or cyclopentylcarbinol group, said substituted cyclohexyl group in (iii) is cyclohexylamino group, cyclohexylaldehyde group or cyclohexyl acetic acid group, and said substituted naphthyl group in (iii) is naphthylamino group or naphthylamino sulfonic acid group; and    said condensation polycyclic hydrocarbon compound in (iv) is pentalene, indene, naphthalene, azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthrene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-cyclopentacyclooctene or benzocyclooctene, and said heterocyclic compound is furan, thiophene, pyrrole, γ-pyran, γ-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole or quinoline.    
     
     
         3 . An antigenic substance inductor represented by the Formula 1-b:  
       
         
           
           
               
               
           
         
         (wherein  
         (i) R1, R2, R3, R4, R5, R6, R10 and R11 represent independently hydrogen atom; halogen atom; C1-C6 alkyl group; amidino group; C3-C8 cycloalkyl group; C1-C6 alkoxy C1-C6 alkyl group; aryl group; allyl group; aralkyl group in which one or more C1-C6 alkyl groups are bound to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene ring; C1-C6 alkylene group; benzoyl group; cinnamyl group; cinnamoyl group or furoyl group;  
         (ii) A represents hydrogen atom or  
         
           
             
             
                 
                 
             
           
         
         (wherein 
 R7 represents C1-C6 alkyl group; sulfide group or phosphate group;  
 R8 and R9 represent independently hydrogen atom; halogen atom; straight or branched C1-C6 alkyl group; aryl group; allyl group; aralkyl group in which one or more C1-C6 alkyl groups are bound to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene ring; C1-C6 alkylene group; benzoyl group; cinnamyl group; cinnamoyl group or furoyl group;  
 
         (iii) one or more of R1, R2, R3 and R4, and/or one or more of R5, R6, R10 and R11 may be substituted or non-substituted cyclopentyl group; substituted or non-substituted cyclohexyl group; or substituted or non-substituted naphthyl group;  
         (iv) R5, R6, R10 and R11 may form a ring by binding with another condensation polycyclic hydrocarbon compound or heterocyclic compound;  
         (v) one or more of R3, R4, R5, R6, R10 and R11 may be substituted by one or more of substituents selected from the group consisting of halogen atom, cyano group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, C1-C6 alkyl group, C1-C6 alkoxy group, C1-C7 alkoxy carbonyl group, aryl group, C3-C6 cycloalkyl group, C1-C6 acylanmino group, C1-C6 acyloxy group, C2-C6 alkenyl group, C1-C6 trihalogenoalkyl group, C1-C6 alkylamino group, and C1-C6 dialkylamino group;  
         (vi) R2 and/or R5 may be substituted by one or more substituents selected from the group consisting of halogen atom, C1-C6 alkyl group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, protected or non-protected C1-C6 alkylamino group, protected or non-protected C1-C6 aminoalkyl group, protected or non-protected C1-C6 alkylamino C1-C6 alkyl group, protected or non-protected hydroxyalkyl group, and C3-C6 cycloalkylamino group;  
         (vii) when one or more of R3, R4, R5, R6, R10 and R11 are alkyl groups, terminal end(s) of the alkyl group(s) may be substituted by C3-C8 cycloalkyl group).  
       
     
     
         4 . The antigenic substance inductor according to  claim 3 , wherein 
 said aryl group in (i), (ii) and (v) is phenyl, tollyl, xylyl or naphthyl group;    said substituted cyclopentyl group in (iii) is cyclopentylamino group or cyclopentylcarbinol group, said substituted cyclohexyl group in (iii) is cyclohexylamino group, cyclohexylaldehyde group or cyclohexyl acetic acid group, and said substituted naphthyl group in (iii) is naphthylamino sulfonic acid group; and    said condensation polycyclic hydrocarbon compound in (iv) is pentalene, indene, naphthalene, azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthrene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-cyclopentacyclooctene or benzocyclooctene, and said heterocyclic compound is furan, thiophene, pyrrole, γ-pyran, γ-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole or quinoline.    
     
     
         5 . An antigenic substance inductor represented by the Formula 2:  
       
         
           
           
               
               
           
         
         (wherein  
         (i) R1, R2, R3, R4, R5 and R6 represent independently hydrogen atom; halogen atom; C1-C6 alkyl group; amidino group; C3-C8 cycloalkyl group; C1-C6 alkoxy C1-C6 alkyl group; aryl group; allyl group; aralkyl group in which one or more C1-C6 alkyl groups are bound to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene ring; C1-C6 alkylene group; benzoyl group; cinnamyl group; cinnamoyl group or furoyl group;  
         (ii) one or more of R1, R2, R3 and R4, and/or one or more of R5 and R6 may be substituted or non-substituted cyclopentyl group; substituted or non-substituted cyclohexyl group; or substituted or non-substituted naphthyl group;  
         (iii) R5 and R6 may form a ring by binding with another condensation polycyclic hydrocarbon compound or heterocyclic compound;  
         (iv) one or more of R3, R4, R5 and R6 may be substituted by one or more of substituents selected from the group consisting of halogen atom, cyano group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, C1-C6 alkyl group, C1-C6 alkoxy group, C1-C7 alkoxy carbonyl group, aryl group, C3-C6 cycloalkyl group, C1-C6 acylamino group, C1-C6 acyloxy group, C2-C6 alkenyl group, C1-C6 trihalogenoalkyl group, C1-C6 alkylamino group, and C1-C6 dialkylamino group;  
         (v) R2 and/or R5 may be substituted by one or more substituents selected from the group consisting of halogen atom, C1-C6 alkyl group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, protected or non-protected C1-C6 alkylamino group, protected or non-protected C1-C6 aminoalkyl group, protected or non-protected C1-C6 alkylamino C1-C6 alkyl group, protected or non-protected hydroxyalkyl group, and C3-C6 cycloalkylamino group;  
         (vi) when one or more of R3, R4, R5 and R6 are alkyl groups, terminal end(s) of the alkyl group(s) may be substituted by C3-C8 cycloalkyl group).  
       
     
     
         6 . The antigenic substance inductor according to  claim 5 , wherein 
 said aryl group in (i) and (iv) is phenyl, tollyl, xylyl or naphthyl group;    said substituted cyclopentyl group in (ii) is cyclopentylamino group or cyclopentylcarbinol group, said substituted cyclohexyl group in (ii) is cyclohexylamino group, cyclohexylaldehyde group or cyclohexyl acetic acid group, and said substituted naphthyl group in (ii) is naphthylamino group or naphthylamino sulfonic acid group; and    said condensation polycyclic hydrocarbon compound in (iii) is pentalene, indene, naphthalene, azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthrene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-cyclopentacyclooctene or benzocyclooctene, and said heterocyclic compound is furan, thiophene, pyrrole, γ-pyran, γ-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole or quinoline.    
     
     
         7 . An antigenic substance inductor represented by the Formula 3-a:  
       
         
           
           
               
               
           
         
         (wherein  
         (i) R3, R4, R5 and R6 represent independently hydrogen atom; halogen atom; C1-C6 alkyl group; amidino group; C3-C8 cycloalkyl group; C1-C6 alkoxy C1-C6 alkyl group; aryl group; allyl group; aralkyl group in which one or more C1-C6 alkyl groups are bound to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene ring; C1-C6 alkylene group; benzoyl group; cinnamyl group; cinnamoyl group or furoyl group;  
         (ii) one or more of R3 and R4, and/or one or more of R5 and R6 may be substituted or non-substituted cyclopentyl group; substituted or non-substituted cyclohexyl group; or substituted or non-substituted naphthyl group;  
         (iii) R5 and R6 may form a ring by binding with another condensation polycyclic hydrocarbon compound or heterocyclic compound;  
         (iv) one or more of R3, R4, R5 and R6 may be substituted by one or more of substituents selected from the group consisting of halogen atom, cyano group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, C1-C6 alkyl group, C1-C6 alkoxy group, C1-C7 alkoxy carbonyl group, aryl group, C3-C6 cycloalkyl group, C1-C6 acylamino group, C1-C6 acyloxy group, C2-C6 alkenyl group, C1-C6 trihalogenoalkyl group, C1-C6 alkylamino group, and C1-C6 dialkylamino group;  
         (v) R5 may be substituted by one or more substituents selected from the group consisting of halogen atom, C1-C6 alkyl group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, protected or non-protected C1-C6 alkylamino group, protected or non-protected C1-C6 aminoalkyl group, protected or non-protected C1-C6 alkylamino C1-C6 alkyl group, protected or non-protected hydroxyalkyl group, and C3-C6 cycloalkylamino group;  
         (vi) when one or more of R3, R4, R5 and R6 are alkyl groups, terminal end(s) of the alkyl group(s) may be substituted by C3-C8 cycloalkyl group).  
       
     
     
         8 . The antigenic substance inductor according to  claim 7 , wherein 
 said aryl group in (i) and (iv) is phenyl, tollyl, xylyl or naphthyl group;    said substituted cyclopentyl group in (ii) is cyclopentylamino group or cyclopentylcarbinol group, said substituted cyclohexyl group in (ii) is cyclohexylamino group, cyclohexylaldehyde group or cyclohexyl acetic acid group, and said substituted naphthyl group in (ii) is naphthylamino group or naphthylamino sulfonic acid group; and    said condensation polycyclic hydrocarbon compound in (iii) is pentalene, indene, naphthalene, azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthrene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-cyclopentacyclooctene or benzocyclooctene, and said heterocyclic compound is furan, thiophene, pyrrole, γ-pyran, γ-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole or quinoline.    
     
     
         9 . The antigenic substance inductor according to  claim 7 , wherein R3, R4, R5 and R6 represent hydrogen atoms.  
     
     
         10 . An antigenic substance inductor represented by the Formula 3-b:  
       
         
           
           
               
               
           
         
         (wherein  
         (i) R3, R4, R5 and R6 represent independently hydrogen atom; halogen atom; C1-C6 alkyl group; amidino group; C3-C8 cycloalkyl group; C1-C6 alkoxy C1-C6 alkyl group; aryl group; allyl group; aralkyl group in which one or more C1-C6 alkyl groups are bound to an aromatic ring selected from the group consisting of benzene, naphthalene and anthracene ring; C1-C6 alkylene group; benzoyl group; cinnamyl group; cinnamoyl group or furoyl group;  
         (ii) one or more of R3 and R4, and/or one or more of R5 and R6 may be substituted or non-substituted cyclopentyl group; substituted or non-substituted cyclohexyl group; or substituted or non-substituted naphthyl group;  
         (iii) R5 and R6 may form a ring by binding with another condensation polycyclic hydrocarbon compound or heterocyclic compound;  
         (iv) one or more of R3, R4, R5 and R6 may be substituted by one or more of substituents selected from the group consisting of halogen atom, cyano group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, C1-C6 alkyl group, C1-C6 alkoxy group, C1-C7 alkoxy carbonyl group, aryl group, C3-C6 cycloalkyl group, C1-C6 acylamino group, C1-C6 acyloxy group, C2-C6 alkenyl group, C1-C6 trihalogenoalkyl group, C1-C6 alkylamino group, and C1-C6 dialkylamino group;  
         (v) R5 may be substituted by one or more substituents selected from the group consisting of halogen atom, C1-C6 alkyl group, protected or non-protected carboxyl group, protected or non-protected hydroxyl group, protected or non-protected amino group, protected or non-protected C1-C6 alkylamino group, protected or non-protected C1-C6 aminoalkyl group, protected or non-protected C1-C6 alkylamino C1-C6 alkyl group, protected or non-protected hydroxyalkyl group, and C3-C6 cycloalkylamino group;  
         (vi) when one or more of R3, R4, R5 and R6 are alkyl groups, terminal end(s) of the alkyl group(s) may be substituted by C3-C8 cycloalkyl group).  
       
     
     
         11 . The antigenic substance inductor according to  claim 10 , wherein 
 said aryl group in (i) and (iv) is phenyl, tollyl, xylyl or naphthyl group;    said substituted cyclopentyl group in (ii) is cyclopentylamino group or cyclopentylcarbinol group, said substituted cyclohexyl group in (ii) is cyclohexylamino group, cyclohexylaldehyde group or cyclohexyl acetic acid group, and said substituted naphthyl group in (ii) is naphthylamino group or naphthylamino sulfonic acid group; and    said condensation polycyclic hydrocarbon compound in (iii) is pentalene, indene, naphthalene, azulene, heptalene, biphenylene, indacene, acenaphthylene, fluorene, phenalene, phenanthrene, anthracene, pentacene, hexacene, dibenzophenanthrene, 1H-cyclopentacyclooctene or benzocyclooctene, and said heterocyclic compound is furan, thiophene, pyrrole, γ-pyran, γ-thiopyran, pyridine, thiazole, imidazole pyrimidine, indole or quinoline.    
     
     
         12 . A vaccine precursor or vaccine which was manufactured or produced by using the antigenic substance inductor according to any one of claims  1 - 11 .  
     
     
         13 . An antibody or neutralizing antibody which was manufactured or produced by using the antigenic substance inductor according to any one of claims  1 - 11 .  
     
     
         14 . An antitoxin which was manufactured or produced by using the antigenic substance inductor according to any one of claims  1 - 11 .  
     
     
         15 . Idiotype antibody which was manufactured or produced by using the antigenic substance inductor according to any one of claims  1 - 11 .  
     
     
         16 . A vaccine precursor or vaccine which was manufactured or produced by using the idiotype antibody inducer according to  claim 15 .  
     
     
         17 . An antibody, neutralizing antibody or antitoxin which was manufactured or produced by using the idiotype antibody inducer according to  claim 15 .  
     
     
         18 . The vaccine precursor, vaccine, antibody, neutralizing antibody, antitoxin, idiotype antibody or anti-idiotype antibody, (which is modified by an artificial antibody to a macromolecule (such as peptides, proteins, lipids, glycoproteins and polysaccharides so on) that is not an organism), induced by the idiotype antibody according to any one of claims  12 - 17 .  
     
     
         19 . The antigenic substance inductor, vaccine precursor, vaccine, antibody, neutralizing antibody, antitoxin or idiotype antibody according to any one of claims  12 - 17 , which is an antimicrobial agent.  
     
     
         20 . The antigenic substance inductor, vaccine precursor, vaccine, antibody, neutralizing antibody, antitoxin or idiotype antibody according to any one of claims  12 - 17 , which is an antiviral agent.  
     
     
         21 . The antigenic substance inductor, vaccine precursor, vaccine, antibody, neutralizing antibody, antitoxin or idiotype antibody according to any one of claims  12 - 17 , which is an antitumor agent.  
     
     
         22 . The antigenic substance inductor, vaccine precursor, vaccine, antibody, neutralizing antibody, antitoxin or idiotype antibody according to any one of claims  12 - 17 , which is an anti-protozoa agent (malaria, spirochaeta et. al).  
     
     
         23 . The antibody or idiotype antibody according to  claim 13  or  15 , which is a molecular discriminating agent.  
     
     
         24 . The antibody or idiotype antibody according to  claim 13  or  15 , which is a labeled compound that has a labeled substance or that has substrate including compounds being capable to demonstrate effector site.  
     
     
         25 . The antibody or idiotype antibody according to  claim 13  or  15 , which is a histocompatible accelerator on homologous tissues or organs.  
     
     
         26 . The antibody or idiotype antibody according to  claim 13  or  15 , which is a histocompatible accelerator on heterogeneous tissues or organs.  
     
     
         27 . The antibody or idiotype antibody according to  claim 13  or  15 , which is an immuno-response accelerator or immuno-response controller.  
     
     
         28 . The antibody or idiotype antibody according to  claim 13  or  15 , which is a complement-linkage reaction accelerator.