US2005171002A1PendingUtilityA1

Polyoxyalkylene compound and method for making

Priority: Feb 3, 2004Filed: Feb 3, 2004Published: Aug 4, 2005
Est. expiryFeb 3, 2024(expired)· nominal 20-yr term from priority
C07C 229/16C07C 251/24C07C 229/14
46
PatentIndex Score
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Claims

Abstract

A process for forming a conjugate of a polyoxyalkylene polymer (such as polyethylene glycol) with a compound containing an amine group(s) and/or a sulfide group(s) by reacting the compound with an acrylate terminated polyoxyalkylene (such as polyethylene glycol terminate at one end with acrlyate or methacrylate and terminated at the other end with a methoxy group). The reaction is believed to be a Michael addition. When the compound contains primary amine groups (such as the surface primary amine groups of a PAMAM dendrimer), it is usually desirable to convert the primary amine groups to secondary amine groups before the reaction with the acrylate terminated polyoxyalkylene.

Claims

exact text as granted — not AI-modified
1 . A compound corresponding to the formula:  
       
         
           
           
               
               
           
         
         where R 1  is an organic radical  
         where R 2  is H or an organic radical  
         where R 3  is H or an organic radical  
         where R 4  is a polyoxyalkylene radical and where R 5  is an organic radical or H.  
       
     
     
         2 . The compound of  claim 1 , wherein R 1  is derived from a dendrimer.  
     
     
         3 . The compound of  claim 1 , wherein R 1  is selected from the group consisting of a group derived from a peptide or a protein.  
     
     
         4 . The compound of  claim 1 , wherein R 4  is derived from polyethylene glycol.  
     
     
         5 . The compound of  claim 2 , wherein R 2  is derived from a cyclodextrin, wherein R 3  is H, wherein R 4  is derived from polyethylene glycol and wherein R 5  is CH 3 .  
     
     
         6 . The compound of  claim 3 , wherein R 2  is derived from a cyclodextrin, wherein R 3  is H, wherein R 4  is derived from polyethylene glycol and wherein R 5  is CH 3 .  
     
     
         7 . The compound of  claim 3 , wherein R 2  is H, wherein R 3  is H, wherein R 4  is derived from polyethylene glycol and wherein R 5  is CH 3 .  
     
     
         8 . A compound corresponding to the formula:  
       
         
           
           
               
               
           
         
         where R 6  is an organic radical  
         where R 7  is H or an organic radical  
         where R 8  is a polyoxyalkylene radical  
         and where R 9  is an organic radical or H.  
       
     
     
         9 . The compound of  claim 8 , wherein R 6  is selected from the group consisting of a group derived from a peptide or a protein.  
     
     
         10 . The compound of  claim 8 , wherein R 6  is derived from polyethylene glycol.  
     
     
         11 . The compound of  claim 9 , wherein R 7  is H, wherein R 8  is derived from polyethylene glycol and wherein R 9  is CH 3 .  
     
     
         12 . A method for preparing a compound corresponding to the formula:  
       
         
           
           
               
               
           
         
         where R 1  is an organic radical  
         where R 2  is H or an organic radical  
         where R 3  is H or an organic radical  
         where R 4  is a polyoxyalkylene radical  
         and where R 5  is an organic radical or H, comprising the step of: reacting A with B, wherein A is R 1 —N—R 2  and wherein  
         
           
             
             
                 
                 
             
           
         
       
     
     
         13 . The process of  claim 12 , wherein R 1  is derived from a dendrimer.  
     
     
         14 . The process of  claim 12 , wherein R 1  is selected from the group consisting of a group derived from a peptide or a protein.  
     
     
         15 . The process of  claim 12 , wherein R 4  is derived from polyethylene glycol.  
     
     
         16 . The process of  claim 13 , wherein R 2  is derived from a cyclodextrin, wherein R 3  is H, wherein R 4  is derived from polyethylene glycol and wherein R 5  is CH 3 .  
     
     
         17 . The process of  claim 14 , wherein R 2  is derived from a cyclodextrin, wherein R 3  is H, wherein R 4  is derived from polyethylene glycol and wherein R 5  is CH 3 .  
     
     
         18 . The process of  claim 14 , wherein R 2  is H, wherein R 3  is H, wherein R 4  is derived from polyethylene glycol and wherein R 5  is CH 3 .  
     
     
         19 . A method for preparing a compound corresponding to the formula:  
       
         
           
           
               
               
           
         
         where R 6  is an organic radical  
         where R 7  is H or an organic radical  
         where R 8  is a polyoxyalkylene radical  
         and where R 9  is an organic radical or H, comprising the step of: reacting D with E, wherein D is R 6 —S and wherein E is  
         
           
             
             
                 
                 
             
           
         
       
     
     
         20 . The compound of  claim 19 , wherein R 6  is selected from the group consisting of a group derived from a peptide or a protein.  
     
     
         21 . The compound of  claim 19 , wherein R 8  is derived from polyethylene glycol.  
     
     
         22 . The compound of  claim 20 , wherein R 7  is H, wherein R 8  is derived from polyethylene glycol and wherein R 9  is CH 3 .

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