IP Library Granted Patent US 7,186,414
Granted Patent B2
US 7,186,414 · App. 11/173,075 · Granted Mar 6, 2007

Compounds and compositions for delivering active agents

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Quick Facts
Patent No.
US 7,186,414
App. No.
11/173,075
Granted
Mar 6, 2007
Kind
B2
Abstract

Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Claims (96)

1. A compound comprising:

or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 wherein said salt is a sodium salt.

3. A composition comprising:

(A) at least one biologically active agent; and

(B) the compound of claim 1 .

4. The composition of claim 3 wherein said salt is a sodium salt.

5. The composition of claim 3 , wherein said biologically active agent comprises at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid.

6. The composition of claim 5 , wherein said biologically active agent comprises a protein, polypeptide or peptide.

7. The composition of claim 6 , wherein said biologically active agent comprises a mucopolysaccharide.

8. The composition of claim 3 , wherein said biologically active agent is selected from the group consisting of: growth hormone, growth hormone-releasing hormones, interferons, interleukin- 1, interleukin-2, insulin, insulin-like growth factor(IGF), heparin, calcitonin, erythropoietin (EPO), atrial naturetic factor, antigens, monoclonal antibodies, somatostatin, protease inhibitors, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, leutinizing-hormone-releasing-hormone, follicle stimulating hormone, glucocerebrosidase, thrombopoietin, filgrastim, prostaglandins, cyclosporin, vasopressin, cromolyn sodium, vancomycin, desferrioxamine (DFO), parathyroid hormone (PTH), antimicrobials, anti-fungal agents; analogs, fragments, mimetics and polyethylene glycol (PEG)-modified derivatives of these compounds; and any combination thereof.

9. The composition of claim 8 , wherein said biologically active agent comprises a growth hormone, interferon, insulin, heparin, cromolyn sodium, an antigen, an anti-microbial agent, calcitonin, parathyroid hormone, erythropoietin, and combinations thereof.

10. The composition of claim 9 , wherein said growth hormone comprises human growth hormones (hGH), recombinant human growth hormones (rhGH), bovine growth hormones, porcine growth hormones, or a combination thereof.

11. The composition of claim 8 , wherein said biologically active agent comprises interferon.

12. The composition of claim 8 , wherein said biologically active agent comprises insulin.

13. The composition of claim 8 , wherein said insulin comprises porcine insulin, bovine insulin, human insulin, and human recombinant insulin.

14. The composition of claim 8 , wherein said biologically active agent comprises heparin.

15. The composition of claim 14 , wherein said heparin comprises low molecular weight heparin, very low molecular weight heparin, ultra low molecular weight heparin, heparinoids, dermatans, chondroitins, or a combination thereof.

16. The composition of claim 15 , wherein said biologically active agent comprises low molecular weight heparin.

17. The composition of claim 8 , wherein said biologically active agent comprises cromolyn sodium.

18. The composition of claim 17 , wherein said cromolyn sodium comprises sodium chromoglycate, disodium chromoglycate or a combination thereof.

19. The composition of claim 8 , wherein said biologically active agent comprises an antigen.

20. The composition of claim 8 , wherein said biologically active agent comprises an anti-microbial agent.

21. The composition of claim 8 , wherein said biologically active agent comprises calcitonin.

22. The composition of claim 21 , wherein said calcitonin comprises salmon calcitonin, eel calcitonin, human calcitonin or a combination thereof.

23. The composition of claim 8 , wherein said biologically active agent comprises parathyroid hormone.

24. The composition of claim 8 , wherein said biologically active agent comprises erythropoietin.

25. A dosage unit form comprising

(A) a composition as defined in claim 3 ; 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.

26. The dosage unit of claim 25 wherein said salt of said compound is a sodium salt.

27. The dosage unit form of claim 25 , comprising a powder.

28. The dosage unit form of claim 25 comprising a tablet.

29. The dosage unit form of claim 25 comprising a capsule.

30. The dosage unit form of claim 25 comprising a liquid.

31. The dosage unit form of claim 25 , wherein said biologically active agent comprises at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid.

32. The dosage unit form of claim 25 , wherein said biologically active agent comprises a protein, polypeptide, peptide.

33. The dosage unit form of claim 25 , wherein said biologically active agent comprises a mucopolysaccharide.

34. The dosage unit form of claim 25 , wherein said dosing vehicle is selected from the group consisting of water, 1,2-propane diol, ethanol, olive oil or any combination thereof.

35. The dosage unit form of claim 25 , wherein said biologically active agent is selected from the group consisting of: growth hormone, growth hormone-releasing hormones, interferons, interleukin-1, interleukin-2, insulin, insulin-like growth factor(IGF), heparin, calcitonin, erythropoietin (EPO), atrial naturetic factor, antigens, monoclonal antibodies, somatostatin, protease inhibitors, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, leutinizing-hormone-releasing-hormone, follicle stimulating hormone, glucocerebrosidase, thrombopoietin, filgrastim, prostaglandins, cyclosporin, vasopressin, cromolyn sodium, vancomycin, desferrioxamine (DFO), parathyroid hormone (PTH), antimicrobials, anti-fungal agents; analogs, fragments, mimetics and polyethylene glycol (PEG)-modified derivatives of these compounds; and any combination thereof.

36. The dosage unit form of claim 35 , wherein said biologically active agent comprises a growth hormone, interferon, insulin, heparin, cromolyn sodium, an antigen, an anti-microbial agent, calcitonin, parathyroid hormone, erythropoietin, and combinations thereof.

37. The dosage unit form of claim 35 , wherein said growth hormone comprises human growth hormones (hGH), recombinant human growth hormones (rhGH), bovine growth hormones, porcine growth hormones, or a combination thereof.

38. The dosage unit form of claim 35 , wherein said biologically active agent comprises interferon.

39. The dosage unit form of claim 35 , wherein said biologically active agent comprises insulin.

40. The dosage unit form of claim 39 , wherein said insulin comprises porcine insulin, bovine insulin, human insulin, and human recombinant insulin.

41. The dosage unit form of claim 35 , wherein said biologically active agent comprises heparin.

42. The dosage unit form of claim 41 , wherein said heparin comprises low molecular weight heparin, very low molecular weight heparin, ultra low molecular weight heparin, heparinoids, dermatans, chondroitins, or a combination thereof.

43. The dosage unit form of claim 35 , wherein said biologically active agent comprises low molecular weight heparin.

44. The dosage unit form of claim 35 , wherein said biologically active agent comprises cromolyn sodium.

45. The composition of claim 44 , wherein said cromolyn sodium comprises sodium chromoglycate, disodium chromoglycate or a combination thereof.

46. The dosage unit form of claim 35 , wherein said biologically active agent comprises an antigen.

47. The dosage unit form of claim 35 , wherein said biologically active agent comprises an anti-microbial agent.

48. The dosage unit form of claim 35 , wherein said biologically active agent comprises calcitonin.

49. The dosage unit form of claim 35 , wherein said calcitonin comprises salmon calcitonin, eel calcitonin, human calcitonin or a combination thereof.

50. The dosage unit form of claim 35 , wherein said biologically active agent comprises parathyroid hormone.

51. The dosage unit form of claim 35 , wherein said biologically active agent comprises erythropoietin.

52. A method for administering a biologically-active agent to an animal, said method comprising administering to said animal the composition of claim 3 .

53. The method of claim 52 wherein said salt of said compound is a sodium salt.

54. The method of claim 52 , wherein said biologically-active agent is administered by a route which is: oral, intranasal, sublingual, intraduodenal, subcutaneous, buccal, intracolonic, rectal, vaginal, mucosal, pulmonary, transdermal, intradermal, parenteral, intravenous, intramuscular or intraocular.

55. The method of claim 54 , wherein said biologically-active agent is administered by oral route.

56. The method of claim 52 , wherein said biologically active agent comprises at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid.

57. The method of claim 52 , wherein said biologically active agent comprises a protein, a polypeptide, or a peptide.

58. The method of claim 52 , wherein said biologically active agent comprises a mucopolysaccharide.

59. The method of claim 52 , wherein said biologically active agent is selected from the group consisting of: growth hormone, growth hormone-releasing hormones, interferons, interleukin-1, interleukin-2, insulin, insulin-like growth factor(IGF), heparin, calcitonin, erythropoietin (EPO), atrial naturetic factor, antigens, monoclonal antibodies, somatostatin, protease inhibitors, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, leutinizing-hormone-releasing-hormone, follicle stimulating hormone, glucocerebrosidase, thrombopoietin, filgrastim, prostaglandins, cyclosporin, vasopressin, cromolyn sodium, vancomycin, desferrioxamine (DFO), parathyroid hormone (PTH), antimicrobials, anti-fungal agents; analogs, fragments, mimetics and polyethylene glycol (PEG)-modified derivatives of these compounds; and any combination thereof.

60. The method of claim 52 , wherein said biologically active agent comprises a growth hormone, interferon, insulin, heparin, cromolyn sodium, an antigen, an anti-microbial agent, calcitonin, parathyroid hormone, erythropoietin, and combinations thereof.

61. The method of claim 60 , wherein said growth hormone comprises human growth hormones (hGH), recombinant human growth hormones (rhGH), bovine growth hormones, porcine growth hormones, or a combination thereof.

62. The method of claim 52 , wherein said biologically active agent comprises interferon.

63. The method of claim 51 , wherein said biologically active agent comprises insulin.

64. The method of claim 63 , wherein said insulin comprises porcine insulin, bovine insulin, human insulin, and human recombinant insulin.

65. The method of claim 52 , wherein said biologically active agent comprises heparin.

66. The method of claim 65 , wherein said heparin comprises low molecular weight heparin, very low molecular weight heparin, ultra low molecular weight heparin, heparinoids, dermatans, chondroitins, or a combination thereof.

67. The method of claim 66 , wherein said biologically active agent comprises low molecular weight heparin.

68. The method of claim 52 , wherein said biologically active agent comprises cromolyn sodium.

69. The method of claim 68 , wherein said cromolyn sodium comprises sodium chromoglycate, disodium chromoglycate or a combination thereof.

70. The method of claim 52 , wherein said biologically active agent comprises an antigen.

71. The method of claim 52 , wherein said biologically active agent comprises an anti-microbial agent.

72. The method of claim 52 , wherein said biologically active agent comprises calcitonin.

73. The method of claim 52 , wherein said calcitonin comprises salmon calcitonin, eel calcitonin, human calcitonin or a combination thereof.

74. The method of claim 52 , wherein said biologically active agent comprises parathyroid hormone.

75. The method of claim 52 , wherein said biologically active agent comprises erythropoietin.

76. 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.

77. The method of claim 76 wherein said salt of said compound is a sodium salt.

78. The method of claim 76 , wherein said biologically active agent comprises at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid.

79. The method of claim 76 , wherein said biologically active agent comprises a protein, polypeptide, peptide.

80. The method of claim 76 , wherein said biologically active agent comprises a mucopolysaccharide.

81. The method of claim 76 , wherein said biologically active agent is selected from the group consisting of: growth hormone, growth hormone-releasing hormones, interferons, interleukin-1, interleukin-2, insulin, insulin-like growth factor(IGF), heparin, calcitonin, erythropoietin (EPO), atrial naturetic factor, antigens, monoclonal antibodies, somatostatin, protease inhibitors, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, leutinizing-hormone-releasing-hormone, follicle stimulating hormone, glucocerebrosidase, thrombopoietin, filgrastim, prostaglandins, cyclosporin, vasopressin, cromolyn sodium, vancomycin, desferrioxamine (DFO), parathyroid hormone (PTH), antimicrobials, anti-fungal agents; analogs, fragments, mimetics and polyethylene glycol (PEG)-modified derivatives of these compounds; and any combination thereof.

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 22, 2021
From: EMISPHERE TECHNOLOGIES, INC.
To: NOVO NORDISK NORTH AMERICA OPERATIONS A/S
Reel/Frame 056750/0169 →
SECURITY AGREEMENT Recorded Oct 3, 2005
From: EMISPHERE TECHNOLOGIES, INC.
To: MHR INSTITUTIONAL PARTNERS IIA LP
Reel/Frame 016617/0145 →