US2003144503A1PendingUtilityA1

Substituted liposaccharides useful in the treatment and prevention of endotoxemia

Priority: Jun 5, 1995Filed: May 13, 2002Published: Jul 31, 2003
Est. expiryJun 5, 2015(expired)· nominal 20-yr term from priority
A61P 7/02A61P 9/10A61P 9/02A61P 31/04A61P 29/00A61P 31/00C07H 15/04A61K 9/0073C07H 3/04A61P 1/16A61P 13/12C07H 11/00C07H 15/12A61P 11/00C07H 15/00C07H 17/00C07H 5/04
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Claims

Abstract

Novel substituted liposaccharides useful as in the prophylactic and affirmative treatment of endotoxemia including sepsis, septicemia and various forms of septic shock and methods of using these agents are provided. Also provided are methods of preparing these agents and intermediates useful therein.

Claims

exact text as granted — not AI-modified
1 . The compound of the formula:  
       
         
           
           
               
               
           
         
       
       wherein R 2  is a straight chained or branched C5 to C15 alkyl group.  
     
     
         2 . A compound having the formula:  
       
         
           
           
               
               
           
         
       
       wherein R 2  is a straight chained or branched C5 to C15 alkyl group.  
     
     
         3 . A compound having the formula:  
       
         
           
           
               
               
           
         
       
       wherein R 2  is a straight chained or branched C5 to C15 alkyl group; and R 1  is selected from the group consisting of:  
       
         
           
           
               
               
           
         
       
       wherein each J, K and Q, independently, is straight or branched C1 to C15 alkyl; L is O, NH or CH 2 ; M is O or NH; and G is NH, O, S, SO or SO 2 .  
     
     
         4 . The compound of  claim 1 ,  2  or  3 , wherein R 2  is C8 is C15 straight or branched alkyl group.  
     
     
         5 . The compound of  claim 1 ,  2  or  3 , wherein R 2  is C9 is C12 straight or branched alkyl group.  
     
     
         6 . The compound of  claim 1 ,  2  or  3 , wherein R 2  is C10 straight or branched alkyl group.  
     
     
         7 . The compound of  claim 3 , wherein R 1  is selected from the group consisting of:  
       
         
           
           
               
               
           
         
       
       where each J, K and Q, independently, is straight or branched C1 to C15 alkyl.  
     
     
         8 . The compound of  claim 3 , wherein R 1  is  
       
         
           
           
               
               
           
         
       
     
     
         9 . A compound having the formula:  
       
         
           
           
               
               
           
         
       
       wherein R 4  is selected from the group consisting of straight or branched C4 to C15 alkyl, and  
       
         
           
           
               
               
           
         
       
       where each U and V, independently, is straight or branched C2 to C15 alkyl and W is hydrogen or straight or branched C1 to C5 alkyl.  
     
     
         10 . A compound having the formula:  
       
         
           
           
               
               
           
         
       
       wherein R 4  is selected from the group consisting of straight or branched C4 to C15 alkyl, and  
       
         
           
           
               
               
           
         
       
       where each U and V, independently, is straight or branched C2 to C15 alkyl and W is hydrogen or straight or branched C1 to C5 alkyl; and 
 R A  is R 5  or R 5 —O—CH 2 —, where R 5  is selected from the group consisting of hydrogen, —J′, —J′—OH, —J′—O—K′, —J′—O—K′—OH, and —J′—O—PO(OH) 2 , where each J′ and K′, independently, is straight or branched C1 to C15 alkyl.  
 
     
     
         11 . A compound having the formula:  
       
         
           
           
               
               
           
         
       
       wherein R 4  is selected from the group consisting of straight or branched C4 to C15 alkyl, and  
       
         
           
           
               
               
           
         
       
       where each U and V, independently, is straight or branched C2 to C15 alkyl and W is hydrogen or straight or branched C1 to C5 alkyl; and 
 R A  is R 5  or R 5 —O—CH 2 —, where R 5  is selected from the group consisting of hydrogen, —J′, —J′—OH, —J′—O—K′, —J′—O—K′—OH, and —J′—O—PO(OH) 2 , where each J′ and K′, independently, is straight or branched C1 to C15 alkyl.  
 
     
     
         12 . The compound of  claim 10  or  11 , wherein R 5  is methyl.  
     
     
         13 . The compound of  claim 9 ,  10  or  11 , wherein R 4  is

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