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Generated: February 23, 2018

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Title: Compounds and compositions for delivering active agents
Abstract:Modified amino acid compounds useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.
Inventor(s): Leone-Bay; Andrea (Ridgefield, CT), Paton; Duncan R. (Purdys, NY), Ho; Koc-Kan (Mt. Kisco, NY), DeMorin; Frenel (Spring Valley, NY)
Assignee: Emisphere Technologies, Inc. (Tarrytown, NY)
Filing Date:Feb 06, 1997
Application Number:08/795,837
Claims:1. A composition comprising:

(A) at least one active agent; and

(B) a compound having the following formula ##STR7## or a salt thereof.

2. A composition as defined in claim 1, wherein said active agent is selected from the group consisting of a biologically active agent, a chemically active agent, or a combination thereof.

3. A composition as defined in claim 2, wherein said biologically active agent comprises at least one peptide, mucopolysaccharide, carbohydrate, or lipid.

4. The composition as defined in claim 3, wherein said biologically active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-II, insulin, heparin, low molecular weight heparin, calcitonin, erythropoietin, atrial naturetic factor, an antigen, a monoclonal antibody, samatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, cromolyn sodium, vancomycin, parathyroid hormone, desferrioxamine (DFO), or any combination thereof.

5. A composition as defined in claim 4, wherein said biologically active agent comprises an interferon, interleukin-II, insulin, heparin, low molecular weight heparin, calcitonin, oxytosin, vasopressin, vancomycin, DFO, parathyroid hormone, and combinations thereof.

6. A composition as defined in claim 2, wherein said biologically active agent comprises heparin.

7. A composition as defined in claim 1, wherein said biologically active agent comprises low molecular weight heparin.

8. A composition as defined in claim 1, wherein said carrier comprises a poly(amino acid).

9. A composition as defined in claim 1, wherein said carrier comprises a polypeptide.

10. A dosage unit form comprising:

(A) a composition as defined in claim 1; 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.

11. A dosage unit form as defined in claim 10, wherein said active agent is selected from the group consisting of a biologically active agent, a chemically active agent, or a combination thereof.

12. A dosage unit form as defined in claim 11, wherein said biologically active agent comprises at least one peptide, mucopolysaccharide, carbohydrate, or lipid.

13. The dosage unit form as defined in claim 12, wherein said biologically active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-II, insulin, heparin, low molecular weight heparin, calcitonin, erythropoietin, atrial naturetic factor, an antigen, a monoclonal antibody, samatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, cromolyn sodium, vancomycin, parathyroid hormone, desferrioxamine (DFO), or any combination thereof.

14. A dosage unit form as defined in claim 13, wherein said biologically active agent comprises an interferon, interleukin-II, insulin, heparin, low molecular weight heparin, calcitonin, oxytosin, vasopressin, vancomycin, DFO, parathyroid hormone, and combinations thereof.

15. A dosage unit form as defined in claim 10, wherein said biologically active agent comprises heparin.

16. A dosage unit form as defined in claim 10, wherein said biologically active agent comprises low molecular weight heparin.

17. A dosage unit form as defined in claim 10, comprising a tablet, a capsule, or a liquid.

18. A dosage unit form as defined in claim 17, wherein said dosing vehicle is selected from the group consisting of water, 1,2-propane diol, ethanol, or any combination thereof.

19. A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in claim 2.

20. A compound having the formula ##STR8## or a salt thereof.

21. A method for preparing a composition, said method comprising mixing:

(A) at least one active agent;

(B) at least one carrier compound as defined in claim 20; and

(C) optionally, a dosing vehicle.
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Covington
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