US2004068013A1PendingUtilityA1

Compounds and compositions for delivering active agents

63
Assignee: EMISPHERE TECH INCPriority: Apr 22, 1993Filed: Oct 1, 2003Published: Apr 8, 2004
Est. expiryApr 22, 2013(expired)· nominal 20-yr term from priority
A61K 31/727A61K 9/1617A61K 9/1641A61K 31/16A61K 38/212A61K 38/23A61K 38/25A61K 38/27A61K 47/183C07C 229/42C07C 233/48C07C 233/55C07C 233/63C07C 233/82C07C 233/87C07C 235/26C07C 235/38C07C 235/64C07C 235/78C07C 235/84C07C 237/22C07C 279/14C07K 1/1077C07K 5/06043C07C 2601/02C07C 2601/08C07C 2601/14C07C 2601/18
63
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Claims

Abstract

Modified amino acid compounds useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A compound selected from the group consisting of  
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
       or salts thereof.  
     
     
         2 . A poly amino acid comprising at least one compound selected from the group consisting of  
       
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
         
           
           
               
               
           
         
       
       or salts thereof.  
     
     
         3 . A poly amino acid as defined in  claim 2 , comprising a peptide.  
     
     
         4 . A composition comprising 
 a. an active agent; and    b. a compound as defined in  claim 1 .    
     
     
         5 . A composition comprising 
 a. an active agent; and    b. a poly amino acid as defined in  claim 2 .    
     
     
         6 . A composition as defined in  claim 5 , wherein said poly amino acid comprises a peptide.  
     
     
         7 . A composition as defined in  claim 4 , wherein said active agent comprises a biologically active agent.  
     
     
         8 . A composition as defined in  claim 7 , wherein said biologically-active agent is selected from the group consisting of a peptide, a mucopoly-saccharide, a carbohydrate, a lipid, a pesticide, or any combination thereof.  
     
     
         9 . A composition as defined in  claim 8 , wherein said biologically-active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-II, insulin, heparin, calcitonin, erythropoietin, atrial naturetic factor, an antigen, a monoclonal antibody, somatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, cromolyn sodium, vancomycin, desferrioxamine (DFO), or any combination thereof.  
     
     
         10 . A composition as defined in  claim 5 , wherein said active agent comprises a biologically active agent.  
     
     
         11 . A composition as defined in  claim 10 , wherein said biologically-active agent is selected from the group consisting of a peptide, a mucopoly-saccharide, a carbohydrate, a lipid, a pesticide, or any combination thereof.  
     
     
         12 . A composition as defined in  claim 11 , wherein said biologically-active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-II, insulin, heparin, calcitonin, erythropoietin, atrial naturetic factor, an antigen, a monoclonal antibody, somatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, cromolyn sodium, vancomycin, desferrioxamine (DFO), or any combination thereof.  
     
     
         13 . A composition as defined in  claim 6 , wherein said active agent comprises a biologically active agent.  
     
     
         14 . A composition as defined in  claim 13 , wherein said biologically-active agent is selected from the group consisting of a peptide, a mucopoly-saccharide, a carbohydrate, a lipid, a pesticide, or any combination thereof.  
     
     
         15 . A composition as defined in  claim 14 , wherein said biologically-active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-II, insulin, heparin, calcitonin, erythropoietin, atrial naturetic factor, an antigen, a monoclonal antibody, somatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, cromolyn sodium, vancomycin, desferrioxamine (DFO), or any combination thereof.  
     
     
         16 . A dosage unit form comprising 
 (A) a composition according to  claim 4;  and    (B) (a) an excipient, 
 (b) a diluent,  
 (c) a disintegrant,  
 (d) a lubricant,  
 (e) a plasticizer,  
 (f) a colorant,  
 (g) a dosing vehicle, or  
 (h) any combination thereof.  
   
     
     
         17 . A dosage unit form according to  claim 16 , comprising a tablet, a capsule, or a liquid.  
     
     
         18 . A dosage unit form comprising 
 (A) a composition according to  claim 5;  and    (B) (a) an excipient, 
 (b) a diluent,  
 (c) a disintegrant,  
 (d) a lubricant,  
 (e) a plasticizer,  
 (f) a colorant,  
 (g) a dosing vehicle, or  
 (h) any combination thereof.  
   
     
     
         19 . A dosage unit form according to  claim 18 , comprising a tablet, a capsule, or a liquid.  
     
     
         20 . A dosage unit form comprising 
 (A) a composition according to  claim 6;  and    (B) (a) an excipient, 
 (b) a diluent,  
 (c) a disintegrant,  
 (d) a lubricant,  
 (e) a plasticizer,  
 (f) a colorant,  
 (g) a dosing vehicle, or  
 (h) any combination thereof.  
   
     
     
         21 . A dosage unit form according to  claim 20 , comprising a tablet, a capsule, or a liquid.  
     
     
         22 . A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in  claim 4 .  
     
     
         23 . A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in  claim 5 .  
     
     
         24 . A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in  claim 6 .  
     
     
         25 . A method for preparing a composition, said method comprising mixing: 
 (A) at least one biologically-active agent;    (B) at least one compound as defined in  claim 1;  and    (C) optionally a dosing vehicle    
     
     
         26 . A method for preparing a composition, said method comprising mixing: 
 (A) at least one biologically-active agent;    (B) at least one poly amino acid as defined in  claim 2;  and    (C) optionally a dosing vehicle    
     
     
         27 . A method for preparing a composition, said method comprising mixing: 
 (A) at least one biologically-active agent;    (B) at least one peptide as defined in  claim 3;  and    (C) optionally a dosing vehicle.

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