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Last Updated: August 4, 2020

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Claims for Patent: 7,138,546

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Summary for Patent: 7,138,546
Title:Compounds and compositions for delivering active agents
Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.
Inventor(s): Tang; Pingwah (Elmsford, NY)
Assignee: Emisphere Technologies, Inc. (Tarrytown, NY)
Application Number:10/362,067
Patent Claims:1. A compound selected from the group consisting of: ##STR00003## and salts thereof.

2. A composition comprising: (A) an active agent; and (B) a compound selected from the group consisting of ##STR00004## and salts thereof, and mixtures thereof.

3. The composition of claim 2, wherein the active agent is selected from the group consisting of a biologically active agent, a chemically active agent, and a combination thereof.

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

5. The composition of claim 3, wherein the biologically active agent is selected from the group consisting of: growth hormones, human growth hormones (hGH), recombinant human growth hormones (rhGH), bovine growth hormones, porcine growth hormones, growth hormone-releasing hormones, interferons, .alpha.-interferon, .beta.-interferon, .gamma.-interferon, interleukin- 1, interleukin-2, insulin, porcine insulin, bovine insulin, human insulin, human recombinant insulin, insulin-like growth factor (IGF), IGF-1, heparin, unfractionated heparin, heparinoids, dermatans, chondroitins, low molecular weight heparin, very low molecular weight heparin, ultra low molecular weight heparin, calcitonin, salmon calcitonin, eel calcitonin, human 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, sodium chromoglycate, disodium chromoglycate, vancomycin, desferrioxamine (DFO), parathyroid hormone (PTH), fragments of PTH, antimicrobials, anti-fungal agents, vitamins; analogs, fragments, mimetics and polyethylene glycol (PEG)-modified derivatives of these compounds; and any combination thereof.

6. The composition of claim 3, wherein the biologically active agent comprises salmon calcitonin, heparin, low molecular weight heparin, hGH or combinations thereof.

7. The composition of claim 3, wherein the biologically active agent comprises salmon calcitonin.

8. A dosage unit form comprising: (A) the composition of claim 2; 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.

9. The dosage unit form of claim 8, wherein the active agent is selected from the group consisting of a biologically active agent, a chemically active agent, and a combination thereof.

10. The dosage unit form of claim 9, wherein the biologically active agent comprises at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid.

11. The dosage unit form of claim 10, wherein the biologically active agent is selected from the group consisting of: growth hormones, human growth hormones (hGH), recombinant human growth hormones (rhGH), bovine growth hormones, porcine growth hormones, growth hormone-releasing hormones, interferons, .alpha.-interferon, .beta.-interferon, .gamma.-interferon, interleukin-1, interleukin-2, insulin, porcine insulin, bovine insulin, human insulin, human recombinant insulin, insulin-like growth factor(JGF), IGF-1, heparin, unfractionated heparin, hepannoids, dermatans, chondroitins, low molecular weight heparin, very low molecular weight heparin, ultra low molecular weight heparin, calcitonin, salmon calcitonin, eel calcitonin, human 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, sodium chromoglycate, disodium chromoglycate, vancomycin, desferrioxamine (DFO), parathyroid hormone (PTH), fragments of PTH, antimicrobials, anti-fungal agents, vitamins; analogs, fragments, mimetics and polyethylene glycol (PEG)-modified derivatives of these compounds; and any combination thereof.

12. The dosage unit form of claim 10, wherein the biologically active agent comprises salmon calcitonin.

13. The dosage unit form of claim 8, wherein the dosage unit form is in the form of a tablet, a capsule, a particle, a powder, a sachet, or a liquid.

14. The dosage unit form of claim 8, wherein the dosing vehicle is a liquid selected from the group consisting of water, aqueous propylene glycol, phosphate buffer, 1,2-propane diol, ethanol, and any combination thereof.

15. A method for administering an active agent to an animal in need of the agent, the method comprising administering orally to the animal the composition of claim 2.

16. A method for preparing a composition comprising mixing: (A) at least one active agent; (B) the compound of claim 1; and (C) optionally, a dosing vehicle.

17. A composition comprising: (A) an active agent; and (B) a compound selected from the group consisting of compounds of the formula: ##STR00005## and salts thereof; wherein: R.sup.1 R.sup.4 are independently H, --OH, halogen, C.sub.1 C.sub.4 alkoxy, C.sub.1 C.sub.4 alkyl, C.sub.2 C.sub.4 alkenyl, C.sub.2 C.sub.4 alkynyl, or aryl; R.sup.1 R.sup.4 are optionally substituted with halogen, -OH, C.sub.1 C.sub.4 alkoxy, or C.sub.1 C.sub.4 alkyl; R.sup.5 is a C.sub.1 C.sub.4 alkylene optionally substituted with a C.sub.1 C.sub.4 alkyl group; R.sup.7 is H, or C.sub.1 C.sub.4 alkyl, or aryl; and R.sup.7 is optionally substituted with halogen or --OH, and mixtures thereof.

18. The composition of claim 17, wherein the active agent comprises at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid.

19. A compound of the formula: ##STR00006## or a salt thereof wherein: R.sup.1 R.sup.4 are independently H, --OH, halogen, C.sub.1 C.sub.4 alkoxy, C.sub.1 C.sub.4 alkyl, C.sub.2 C.sub.4 alkenyl, C.sub.2 C.sub.4 alkynyl, or aryl; R.sup.1 R.sup.4 are optionally substituted with halogen, --OH, C.sub.1 C.sub.4 alkoxy, or C1 C.sub.4 alkyl; R.sup.5 is a C.sub.1 C.sub.4 alkylene optionally substituted with a C.sub.1 C.sub.4 alkyl group; and R.sup.7 is a hydroxy substituted aryl.

20. A composition comprising: (A) an active agent; and (B) a compound selected from the compounds of claim 19 and mixtures thereof.

21. The composition of claim 20, wherein the active agent comprises at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid.

22. A method of administering a growth hormone comprising orally administering a composition comprising: (a) a growth hormone; and (b) a compound of claim 1.

23. A method of administering an interferon comprising orally administering a composition comprising: (a) an interferon; and (b) a compound of claim 1.

24. A method of administering interleuken-1 comprising orally administering a composition comprising: (a) interleuken-1; and (b) a compound of claim 1.

25. A method of administering interleuken-2 comprising orally administering a composition comprising: (a) interleuken-2; and (b) a compound of claim 1.

26. A method of administering heparin comprising orally administering a composition comprising: (a) heparin; and (b) a compound of claim 1.

27. A method of administering calcitonin comprising orally administering a composition comprising: (a) calcitonin; and (b) a compound of claim 1.

28. A method of administering erythropoietin comprising orally administering a composition comprising: (a) erythropoietin; and (b) a compound of claim 1.

29. A method of administering a monoclonal antibody comprising orally administering a composition comprising: (a) a monoclonal antibody; and (b) a compound of claim 1.

30. A method of administering a somatostatin comprising orally administering a composition comprising: (a) a somatostatin; and (b) a compound of claim 1.

31. A method of administering a protease inhibitor comprising orally administering a composition comprising: (a) a protease inhibitor; and (b) a compound of claim 1.

32. A method of administering a ganadotropin releasing hormone comprising orally administering a composition comprising: (a) a ganadotropin releasing hormone; and (b) a compound of claim 1.

33. A method of administering a leutinizing-hormone-releasing hormone comprising orally administering a composition comprising: (a) a leutinizing-hormone-releasing hormone; and (b) a compound of claim 1.

34. A method of administering a follicle stimulating hormone comprising orally administering a composition comprising: (a) a follicle stimulating hormone; and (b) a compound of claim 1.

35. A method of administering a bisphosphonate comprising orally administering a composition comprising: (a) a bisphosphonate; and (b) a compound of claim 1.

36. The method of claim 35, wherein the bisphosphonate is alendronate.

37. A method for administering an active agent to an animal in need of the agent, the method comprising orally administering to the animal a composition comprising the active agent and a compound of the formula: ##STR00007## or a salt thereof, wherein: R.sup.1 R.sup.4 are independently H, --OH, halogen, C.sub.1 C.sub.4 alkoxy, C.sub.1 C.sub.4 alkyl, C.sub.2 C.sub.4 alkenyl, C.sub.2 C.sub.4 alkynyl, or aryl; R.sup.1 R.sup.4 are optionally substituted with halogen, --OH, C.sub.1 C.sub.4 alkoxy, or C.sub.1 C.sub.4 alkyl; R.sup.5 is a C.sub.1 C.sub.4 alkylene optionally substituted with a C.sub.1 C.sub.4 alkyl group; R.sup.7 is H or C.sub.2 C.sub.4 alkyl; and R.sup.7 is optionally substituted with halogen or --OH.

38. The method of claim 37, wherein the active agent comprises at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid.

Summary for Patent:   Start Trial

PCT Information
PCT FiledAugust 16, 2001PCT Application Number:PCT/US01/25679
PCT Publication Date:February 28, 2002PCT Publication Number:WO02/16309

Details for Patent 7,138,546

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Lilly HUMULIN R insulin recombinant human INJECTABLE;INJECTION 018780 001 1982-12-02   Start Trial Emisphere Technologies, Inc. (Tarrytown, NY) 2020-08-18 RX search
Lilly HUMULIN R KWIKPEN insulin human SOLUTION;SUBCUTANEOUS 018780 002 1982-12-02   Start Trial Emisphere Technologies, Inc. (Tarrytown, NY) 2020-08-18 RX search
Lilly HUMULIN R insulin human SOLUTION;SUBCUTANEOUS 018780 004 1982-12-02   Start Trial Emisphere Technologies, Inc. (Tarrytown, NY) 2020-08-18 RX search
Lilly HUMULIN R PEN insulin recombinant human INJECTABLE;INJECTION 018780 005 1982-12-02   Start Trial Emisphere Technologies, Inc. (Tarrytown, NY) 2020-08-18 RX search
Amgen NEUPOGEN filgrastim VIAL 103353 001 1991-02-20   Start Trial Emisphere Technologies, Inc. (Tarrytown, NY) 2020-08-18 RX search
Amgen NEUPOGEN filgrastim VIAL 103353 002 1991-02-20   Start Trial Emisphere Technologies, Inc. (Tarrytown, NY) 2020-08-18 RX search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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