Carrier polymers migrating into target organs and drug-containing polymers

Abstract

Polymers derived from polymers represented by Formula (A) (d is 20˜500; and Rs, which may be the same or different, represent each H, alkyl or benzyl) by substituting a part or all of the consisting peptide bonds by (1) hydrazino-Glu (Formula B), and saccharide-modified Glu (Formula C) or by (2) hydorazino-Glu (Formula B), and saccharide-modified Glu (Formula C), and drug bonded Glu (Formula D). These polymers, which are carriers optionally bonded to drugs capable of migrating into target organs (cells), are useful as medicines.

1 . A polymer wherein a part of or all of the consisting peptide bonds in the poly-L-glutamic acid of the formula (A)  
       
         
           
           
               
               
           
         
       
       (wherein, degree of polymerization d is 20˜500, R is hydrogen, C1˜6 alkyl or benzyl, with the proviso that each multiple R may be same or different.) are replaced with the group of the formula  
       
         
           
           
               
               
           
         
       
       (wherein  
       
         
           
           
               
               
           
         
       
       (wherein, G is a modified saccharide capable of connecting to hydrazine, m is 1 when  is a single bond and m is 0 when  is a double bond.)  
       (wherein, (1) group of the both formula (B) and (C) are essential substituents and when the number of replacement of group of the formula (C) is 2 or more, all the said group are the same.).  
     
     
         2 . A polymer wherein a part of or all of the consisting peptide bonds in the poly-L-glutamic acid of the formula (A)  
       
         
           
           
               
               
           
         
       
       (wherein, all the symbols are defined as in claim  1 .) are replaced with the group of the formula  
       
         
           
           
               
               
           
         
       
       (wherein,  
       
         
           
           
               
               
           
         
       
       is defined as  claim 1 ,  
       
         
           
           
               
               
           
         
       
       (wherein, D is drug, n is 1 when  is a single bond, or n is 0 when  is a double bond.)  
       (wherein, (1) group of the both formula (C) and (D) are essential substituents, (2) the number of replacement of group of the formula (C) or (D) is 2 or more, all the said group of the formula (C) or (D) are the same and (3) the number of replacement of group of the formula (B) may be 0.).  
     
     
         3 . A polymer according to  claim 1  or  2 , wherein  
       
         
           
           
               
               
           
         
       
       is  
       
         
           
           
               
               
           
         
       
       (in each Formula, Q is saccharide chain containing 1˜10 saccharide.).  
     
     
         4 . The polymer according to  claim 1  or  2 , wherein  
       
         
           
           
               
               
           
         
       
       is  
       
         
           
           
               
               
           
         
       
     
     
         5 . A polymer according to  claim 2 , wherein D is a drug which is unstable in an alkaline condition.  
     
     
         6 . A polymer according to  claim 2 , wherein D is a drug possessing keto group.  
     
     
         7 . A polymer according to  claim 2 , wherein D is PGEs.  
     
     
         8 . A polymer according to  claim 2 , wherein  
       
         
           
           
               
               
           
         
       
       is  
       
         
           
           
               
               
           
         
       
     
     
         9 . A polymer according to  claim 2 , wherein D is a drug possessing carboxyl group.  
     
     
         10 . A polymer according to  claim 2 , wherein  
       
         
           
           
               
               
           
         
       
       is