Compounds and compositions for delivering active agents

Abstract

The present invention provides delivery agent compounds, compositions containing delivery agent compounds and an active agent and methods for delivering active agents, such as biologically or chemically active agents.

What is claimed is: 
     
       1. A delivery agent compound selected from the group consisting of: 
       
         
           
           
               
               
           
         
       
       and pharmaceutically acceptable salts thereof. 
     
     
       2. The delivery agent compound of  claim 1 , wherein the delivery agent is 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
       3. The A delivery agent compound selected from the group consisting of  claim 1 , wherein the delivery agent is 
       
         
           
           
               
               
           
         
       
       or aand pharmaceutically acceptable saltsalts thereof. 
     
     
       4. The delivery agent compound of  claim 1 , wherein the delivery agent is 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
       5. The delivery agent compound of  claim 1 , wherein the delivery agent is 
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof. 
     
     
       6. A pharmaceutical composition comprising
 (A) a therapeutically effective amount of a biologically active agent; 
 (B) at least one compound selected from the group consisting of 
 
       
         
           
           
               
               
           
         
         and pharmaceutically acceptable salts thereof according to claim 3, and 
         (C) a pharmaceutically acceptable excipient, 
         wherein the biologically active agent is selected from recombinant human growth hormone (rhGH), human growth hormone, bovine growth hormone, porcine growth hormone, BIBN-4096BS, growth hormone releasing factor, interferons, interleukin-1, interleukin-2, insulin, insulin-like growth factor (IGF), heparin, heparinoids, dermatans, chondroitins, calcitonin, erythropoietin (EPO), atrial naturetic factor, CPHPC, monoclonal antibodies, somatostatin, octreotide, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, leutinizing-hormone releasing-hormone, follicle stimulating hormone, glucocerebrosidase, thrombopoeitin, filgrastim, GM-CSF5, prostaglandins, cyclosporin, vasopressin, cromolyn sodium, sodium chromoglycate, disodium chromoglycate, vancomycin, gallium nitrate, glucagon, DPP-4 inhibitors, peptide YY, desferoxamine (DFO), parathyroid hormone (PTH), glucagon-like peptide 1 (GLP-I) (GLP-1), argatroban; and any combination thereof. 
       
     
     
       7. The pharmaceutical composition of  claim 6 , wherein the biologically active agent is selected from the group consisting of insulin, leutenizing-hormone releasing hormone, GLP-1, heparin, recombinant human growth hormone, argatroban, and any combination thereof. 
     
     
       8. The pharmaceutical composition of  claim 6 , wherein the biologically active agent is argatroban. 
     
     
       9. The pharmaceutical composition of  claim 6 , wherein the biologically active agent is insulin. 
     
     
       10. The pharmaceutical composition of  claim 6 , wherein the biologically active agent is human growth hormone. 
     
     
       11. The pharmaceutical composition of  claim 6 , wherein the growth hormone biologically active agent is human growth hormone, recombinant human growth hormone (rhGH), bovine growth hormone or porcine growth hormone. 
     
     
       12. The pharmaceutical composition of  claim 6 , wherein the calcitonin is salmon calcitonin, eel calcitonin or human calcitonin. 
     
     
       13. The pharmaceutical composition of  claim 6 , wherein the insulin is porcine insulin, bovine insulin, human insulin or human recombinant insulin. 
     
     
       14. The pharmaceutical composition of  claim 6 , wherein the heparin is unfractionated heparin, low molecular weight heparin, very low molecular weight heparin or ultra low molecular weight heparin. 
     
     
       15. The pharmaceutical composition of  claim 6 , wherein the insulin-like growth factor is IGF-I. 
     
     
       16. A dosage unit form comprising a pharmaceutical composition of  claim 6 . 
     
     
       17. The dosage unit form of  claim 16 , wherein the dosage unit form is a tablet or capsule. 
     
     
       18. A pharmaceutical composition comprising
 (A) a therapeutically effective amount of a biologically active agent; 
 
       
         
           
           
               
               
           
         
       
       and pharmaceutically acceptable salts thereof; and
 (C) a pharmaceutically acceptable excipient; 
 
       wherein the biologically active agent is selected from calcitonin, insulin, GLP-1, heparin, argatroban, and any combination thereof. 
     
     
       19. A pharmaceutical composition comprising
 (A) a therapeutically effective amount of a biologically active agent; 
 (B) a compound selected from: 
 
       
         
           
           
               
               
           
         
       
       and pharmaceutically acceptable salts thereof; and
 (C) a pharmaceutically acceptable excipient; 
 
       wherein the biologically active agent is selected from calcitonin, insulin, GLP-1, heparin, argatroban; and any combination thereof. 
     
     
       20. A pharmaceutical composition comprising
 (A) a therapeutically effective amount of a biologically active agent; 
 (B) a compound selected from: 
 
       
         
           
           
               
               
           
         
       
       and pharmaceutically acceptable salts thereof; and
 (C) a pharmaceutically acceptable excipient; 
 wherein the biologically active agent is selected from BIBN-4096BS, growth hormone releasing factor, interferons, interleukin-1, interleukin-2, insulin, insulin-like growth factor (IGF), heparin, heparinoids, dermatans, chondroitins, calcitonin, erythropoietin (EPO), atrial naturetic factor, CPHPC, monoclonal antibodies, somatostatin, octreotide, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, leutinizing-hormone releasing-hormone, follicle stimulating hormone, glucocerebrosidase, thrombopoeitin, filgrastim, GM-CSF5, prostaglandins, cyclosporin, vasopressin, cromolyn sodium, sodium chromoglycate, disodium chromoglycate, vancomycin, gallium nitrate, glucagon, DPP-4 inhibitors, peptide YY, desferoxamine (DFO), parathyroid hormone (PTH), glucagon-like peptide 1 (GLP-I) (GLP-1), argatroban; and any combination thereof. 
 
     
     
       21. A pharmaceutical composition comprising
 (A) a therapeutically effective amount of a biologically active agent; 
 (B) a compound selected from: 
 
       
         
           
           
               
               
           
         
       
       and pharmaceutically acceptable salts thereof; and
 (C) a pharmaceutically acceptable excipient; 
 wherein the biologically active agent is selected from BIBN-4096BS, growth hormone releasing factor, interferons, interleukin-1, interleukin-2, insulin, insulin-like growth factor (IGF), heparin, heparinoids, dermatans, chondroitins, calcitonin, erythropoietin (EPO), atrial naturetic factor, CPHPC, monoclonal antibodies, somatostatin, octreotide, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, leutinizing-hormone releasing-hormone, follicle stimulating hormone, glucocerebrosidase, thrombopoeitin, filgrastim, GM-CSF5, prostaglandins, cyclosporin, vasopressin, cromolyn sodium, sodium chromoglycate, disodium chromoglycate, vancomycin, gallium nitrate, glucagon, DPP-4 inhibitors, peptide YY, desferoxamine (DFO), parathyroid hormone (PTH), glucagon-like peptide 1 (GLP-I) (GLP-1), argatroban; and any combination thereof. 
 
     
     
       22. The composition according to  claim 20 , wherein the biologically active agent is selected from calcitonin, insulin, PTH, GLP-1, heparin, argatroban; and any combination thereof. 
     
     
       23. The composition according to  claim 21 , wherein the biologically active agent is selected from calcitonin, insulin, PTH, GLP-1, heparin, argatroban; and any combination thereof. 
     
     
       24. A method for administering a biologically active agent comprising orally administering to a human a pharmaceutical composition comprising:
 (A) a therapeutically effective amount of a biologically active agent wherein the biologically active agent is a polypeptide;   (B) a compound selected from   
       
         
           
           
               
               
           
         
       
       and pharmaceutically acceptable salts thereof; and
 (C) a pharmaceutically acceptable excipient. 
 
     
     
       25. The method of claim 24, wherein compound (B) is selected from 
       
         
           
           
               
               
           
         
       
       and pharmaceutically acceptable salts thereof. 
     
     
       26. The method of claim 24, wherein compound (B) is selected from 
       
         
           
           
               
               
           
         
       
       and pharmaceutically acceptable salts thereof. 
     
     
       27. The method of claim 24, wherein the polypeptide is GLP-1. 
     
     
       28. The method of claim 25, wherein the polypeptide is GLP-1. 
     
     
       29. The method of claim 26, wherein the polypeptide is GLP-1. 
     
     
       30. The composition of claim 18, wherein the biologically active agent is insulin, heparin, or any combination thereof. 
     
     
       31. The composition of claim 19, wherein the biologically active agent is insulin, heparin, or any combination thereof. 
     
     
       32. The method of claim 24, wherein the biologically active agent is insulin, peptide YY, human growth hormone, heparin, luteinizing hormone-releasing hormone, or any combination thereof.