IP Library Granted Patent US 6,846,844
Granted Patent B2
US 6,846,844 · App. 10/362,066 · Granted Jan 25, 2005

Compounds and compositions for delivering active agents

View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 6,846,844
App. No.
10/362,066
Granted
Jan 25, 2005
Kind
B2
Abstract

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

Claims (49)

1. A compound selected from the group consisting of compounds:

and salts thereof.

2. A composition comprising:

(A) a biologically active agent; and

(B) at least one compound of claim 1 .

3. The composition of claim 2 , wherein the biologically active agent comprises at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid.

4. The composition of claim 2 , wherein the biologically active agent is selected from the group consisting of: growth hormones, human growth hormones recombinant human growth hormones (rhGH), bovine growth hormones, porcine growth hormones, growth hormone releasing hormones, growth hormone releasing factor, interferons, α-interferon, β-interferon, γ-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, postaglandins, 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.

5. The composition of claim 2 , wherein the biologically active agent comprises insulin, heparin, calcitonin, parathyroid hormone, erythropoietin, human growth hormone, or combinations thereof.

6. The composition of claim 2 , wherein the biologically active agent comprises recombinant human growth hormones.

7. The composition of claim 2 , wherein the biologically active agent comprises parathyroid hormone.

8. The composition of claim 2 , wherein the biologically active agent comprises insulin.

9. The composition of claim 2 , wherein the biologically active agent comprises heparin.

10. The composition of claim 2 , wherein the biologically active agent comprises calcitonin.

11. The composition of claim 2 , wherein the biologically active agent comprises interferon.

12. A dosage unit form comprising:

(A) the composition of claim 2 ; and

(B) (a) an excipient

(b) a dilutent

(c) a disintegrant,

(d) a lubricant,

(e) a plasticizer,

(f) a colorant,

(g) a dosing vehicle, or

(h) any combination thereof.

13. The dosage unit form of claim 12 , wherein the biologically active agent comprises at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid.

14. The dosage unit form of claim 12 , 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, growth hormone releasing factor, interferons, α-interferon, β-interferon, γ-interferon, interleukin- 1, interleukin-2, insulin, porcine insulin, bovine insulin, human insulin, human recombinant insulin, insulin-like growth factor, insulin-like growth factor-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, atrial naturetic factor, antigens, monoclonal antibodies, somatostatin, protease inhibitors, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, leutinizing-hormone-releasing-hormone, follicle stimulating hormone, glucocerebrosidase, thrombopoeitin, filgrastim, postaglandins, cyclosporin, vasopressin, cromolyn sodium, sodium chromoglycate, disodium chromoglycate, vancomycin, desferrioxamine, parathyroid hormone, fragments of PTH, antimicrobials, anti-fungal agents, vitamins; analogs, fragments, mimetics and polyethylene glycol-modified derivatives of these compounds; and any combination thereof.

15. The dosage unit form of claim 12 , wherein the biologically active agent comprises insulin, heparin, calcitonin, parathyroid hormone, erythropoietin, human growth hormone, or combinations thereof.

16. The dosage unit form of claim 12 , wherein the biologically active agent comprises recombinant human growth hormone.

17. The dosage unit form of claim 12 , wherein the biologically active agent comprises parathyroid hormone.

18. The dosage unit form of claim 12 , wherein the biologically active agent comprises insulin.

19. The dosage unit form of claim 12 , wherein the biologically active agent comprises heparin.

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

21. The dosage unit form of claim 12 , wherein the biologically active agent comprises interferon.

22. The dosage unit form of claim 12 , wherein the dosage unit form comprises a dosing vehicle comprising a tablet, a capsule, a powder, or a liquid.

23. The dosage unit form of claim 12 , wherein the dosing vehicle is a liquid selected from the group consisting or water, 1,2-propane diol, ethanol, and any combination.

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

25. A method for preparing a composition comprising mixing:

(A) at least one biologically active agent;

(B) the compound of claim 1 ; and

(C) optionally, a dosing vehicle.

26. A compound having the formula:

or a salt thereof, wherein

R 1 , R 2 , R 3 , and R 4 are independently H, —OH, halogen, C 1 -C 4 alkoxy, C 1 -C 4 alkyl, C 2 -C 4 alkenyl, C 2 -C 4 alkynyl, or aryl;

R 1 , R 2 , R 3 , and R 4 are optionally substituted with halogen, —OH, C 1 -C 4 alkoxy, or alkyl; and

R 5 is a C 2 -C 16 branched alkylene, optionally substituted with halogen.

27. A composition comprising:

(A) a biologically active agent; and

(B) at least one compound of claim 26 .

Assignments (3)
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 Sep 28, 2005
From: EMISPHERE TECHNOLOGIES, INC.
To: MHR INSTITUTIONAL PARTNERS IIA LP
Reel/Frame 016593/0703 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 7, 2003
From: TANG, PINGWAH
To: EMISPHERE TECHNOLOGIES, INC.
Reel/Frame 014135/0193 →