IP Library Granted Patent US 7,351,741
Granted Patent B2
US 7,351,741 · App. 10/312,703 · Granted Apr 1, 2008

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 7,351,741
App. No.
10/312,703
Granted
Apr 1, 2008
Kind
B2
Abstract

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

Claims (70)

1. A compound of the formula

or a salt thereof.

2. A composition comprising:

(A) at least one active agent; and

(B) a compound having the formula

a salt thereof, or a mixture 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 is at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid.

5. The composition of claim 2 , wherein the active agent is selected from the group consisting of:

growth hormones, human growth hormones, recombinant human growth hormones, bovine growth hormones, porcine growth hormones, growth hormone-releasing hormones, 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 (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, parathyroid hormone, fragments of parathyroid hormone, antimicrobials, anti-fungal agents, vitamins; and any combination thereof.

6. The composition of claim 2 , wherein the active agent is insulin, human growth hormone, interferon, cromolyn sodium or combinations thereof.

7. The composition of claim 2 , wherein the active agent is insulin.

8. The composition of claim 2 , wherein the active agent is interferon.

9. 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.

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

11. The dosage unit form of claim 10 , wherein the biologically active agent is a protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid.

12. The dosage unit form of claim 9 , wherein the active agent is selected from the group consisting of:

growth hormones, human growth hormones, recombinant human growth hormones, bovine growth hormones, porcine growth hormones, growth hormone-releasing hormones, 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 heparmn, ultra low molecular weight heparmn, 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, thrombopoietin, filgrastim, prostaglandins, cyclosporin, vasopressin, cromolyn sodium, sodium chromoglycate, disodium chromoglycate, vancomycin, desferrioxamine, parathyroid hormone, fragments of parathyroid hormone, antimicrobials, anti-fungal agents, vitamins; and any combination thereof.

13. The dosage unit form of claim 9 , wherein the active agent is insulin, human growth hormone, interferon, cromolyn sodium or combinations thereof.

14. The dosage unit form of claim 9 , wherein the active agent is insulin.

15. The dosage unit form of claim 9 , wherein the active agent is interferon.

16. The dosage unit form of claim 9 , wherein the dosage unit form is in the form of a tablet, a capsule, a particle, a powder, a sachet, or a liquid.

17. The dosage unit form of claim 9 , wherein the dosing vehicle is a liquid selected from the group consisting of water, 25% aqueous propylene glycol, phosphate buffer, 1,2-propane diol, ethanol, and any combination thereof.

18. 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.

19. Anhydrous sodium 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate.

20. A composition comprising:

(a) at least one active agent; and

(b) the anhydrous compound of claim 19 .

21. The composition of claim 20 , wherein the active agent is insulin.

22. A solid oral dosage form comprising:

(A) the composition of claim 21 ; 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.

23. Sodium 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate isopropanol solvate.

24. A composition comprising:

(a) at least one active agent; and

(b)the compound of claim 23 .

25. The composition of claim 24 , wherein the active agent is insulin.

26. A solid oral dosage form comprising:

(A) the composition of claim 25 ; 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.

27. A pharmaceutical composition comprising:

(A) insulin; and

(B) a compound having the formula

or a salt thereof.

Assignments (4)
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 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 25, 2003
From: WEIDNER, JOHN J.; VARIANO, BRUCE F.; MAJURU, SHINGAI; BHANDARKAR, SATEJ; BAY, WILLIAM E.; SHIELDS, LYNN
To: EMISPHERE TECHNOLOGIES, INC.
Reel/Frame 014391/0806 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 25, 2003
From: WEIDNER, JOHN J.; VARIANO, BRUCE F.; MAJURU, SHINGAI; BHANDARKAR, SATEJ; BAY, WILLIAM E.; SHIELDS, LYNN
To: EMISPHERE TECHNOLOGIES, INC.
Reel/Frame 014397/0835 →