Conjugate consisting of an active substance and a non-exogeneous native protein

Abstract

This invention relates to a conjugate which consists of an active substance and a native protein which is not regarded as exogenous and distinguishes itself in that an intracellularly cleavable linker is present between the active substance and the protein. In addition, this invention concerns a process for the preparation of such a conjugate and its use.

What is claimed is:  
     
         1 . A conjugate consisting of an active substance and a native protein which is not regarded as exogenous, characterized in that an intracellularly cleavable linker is present between the active substance and the protein.  
     
     
         2 . The conjugate according to    claim 1   , characterized in that the active substance is a compound usable for treating tumoral, infectious and/or autoimmune diseases.  
     
     
         3 . The conjugate according to    claim 2   , characterized in that the active substance is a chemotherapeutic agent and/or a photoactive compound.  
     
     
         4 . The conjugate according to    claim 3   , characterized in that the chemotherapeutic agent is an antibiotic.  
     
     
         5 . The conjugate according to    claim 3   , characterized in that the chemotherapeutic agent is an antimetabolite.  
     
     
         6 . The conjugate according to any one of    claims 1    to    5   , characterized in that several active substances are present.  
     
     
         7 . The conjugate according to any one of    claims 1    to    6   , characterized in that the linker comprises an azo group.  
     
     
         8 . The conjugate according to    claim 7   , characterized in that the linker has the following structure: 
       —Y—R—N═N— 
       wherein: 
 R is an aromatic compound, and  
 Y is a group selected from C(O), S(O) 2 , P(O)OH and As(O)H.  
 
     
     
         9 . The conjugate according to any one of    claims 1    to    8   , characterized in that the protein is albumin.  
     
     
         10 . The conjugate according to    claim 1   , namely the conjugate of FIG. 1.  
     
     
         11 . The conjugate according to    claim 1   , namely the conjugate of FIG. 2.  
     
     
         12 . The conjugate according to    claim 1   , namely the conjugate of FIG. 3.  
     
     
         13 . A process for the preparation of the conjugate according to    claim 7   , characterized in that the binding of the active substance via the linker to the protein comprises a diazotization of amino groups and/or an activation of acid groups.  
     
     
         14 . Use of the conjugate according to any one of    claims 1    to    12    for treating tumoral, infectious and/or auto-immune diseases.