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Last Updated: October 13, 2019

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Claims for Patent: 9,458,089

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Summary for Patent: 9,458,089
Title:Phenoxy alkyl diethanolamine and diisopropanolamine compounds for delivering active agents
Abstract: The present invention relates to particular phenoxy alkyl diethanolamine and diisopropanolamine compounds for delivering biologically active agents to a target. These compounds are well suited for forming non-covalent mixtures with active agents for oral, intracolonic, pulmonary, and other routes of administration to animals.
Inventor(s): Mustata; Gabriela (Roseland, NJ), Pan; Dahua (Roseland, NJ), Gschneidner; David (Roseland, NJ)
Assignee: Emisphere Technologies, Inc. (Roseland, NJ)
Application Number:14/423,319
Patent Claims:1. A compound selected from ##STR00009## and salts thereof.

2. The compound of claim 1, wherein the compound is ##STR00010## or a salt thereof.

3. The compound of claim 1, wherein the compound is ##STR00011## or a salt thereof.

4. The compound of claim 1, wherein the compound is ##STR00012## or a salt thereof.

5. The compound of claim 1, wherein the compound is ##STR00013## or a salt thereof.

6. The compound of claim 1, wherein the compound is ##STR00014## or a salt thereof.

7. A pharmaceutical composition comprising: (A) a biologically active agent; and (B) a compound of claim 1.

8. The pharmaceutical composition of claim 7, wherein the biologically active agent comprises at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid, and any combination thereof.

9. The pharmaceutical composition of claim 7, wherein the biologically active agent is selected from the group consisting of: triptans, BIBN-4096BS, 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, .alpha.-interferon, .beta.-interferon, .gamma.-interferon, interleukin-1, interleukin-2, insulin, porcine insulin, bovine insulin, human insulin, human recombinant insulin, insulin-like growth factor (TGF), 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, thrombopoeitin, 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.

10. The pharmaceutical composition of claim 7, wherein the biologically active agent comprises a triptan, insulin, BIBN-4096BS, calcitonin, parathyroid hormone, erythropoietin, growth hormones and any combination thereof.

11. A dosage unit form comprising: (A) a pharmaceutical composition of claim 7; and (B) at least one of (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.

12. A method for administering a biologically active agent to an animal in need of the agent, the method comprising administering orally to the animal a pharmaceutical composition of claim 7.

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

14. A compound selected from ##STR00015## and pharmaceutically acceptable salts thereof.

15. The pharmaceutical composition of claim 7, wherein the biologically active agent is selected from the group consisting of: BIBN-4096BS, 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, .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, thrombopoeitin, 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.

16. The pharmaceutical composition of claim 7, wherein the biologically active agent comprises insulin, BIBN-4096BS, calcitonin, parathyroid hormone, erythropoietin, growth hormones and any combination thereof.

17. A pharmaceutical composition comprising: (A) a biologically active agent; and (B) a compound of claim 14; wherein the biologically active agent is selected the group consisting of: BIBN-4096BS, 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, .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, thrombopoeitin, 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.

18. The pharmaceutical composition of claim 17, wherein the biologically active agent is selected from the group consisting of insulin, BIBN-4096BS, calcitonin, parathyroid hormone, erythropoietin, growth hormones and any combination thereof.

19. The compound of claim 14, wherein the compound is ##STR00016## or a pharmaceutically acceptable salt thereof.

20. A pharmaceutical composition comprising: (A) a biologically active agent; and (B) the compound of claim 19.

21. A method for administering a biologically active agent to an animal in need of the agent, the method comprising administering orally to the animal a pharmaceutical composition of claim 20.

Summary for Patent:   See Pricing

PCT Information
PCT FiledAugust 22, 2013PCT Application Number:PCT/US2013/056221
PCT Publication Date:February 27, 2014PCT Publication Number:WO2014/031874

Details for Patent 9,458,089

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Amgen NEUPOGEN filgrastim VIAL 103353 001 1991-02-20   See Pricing Emisphere Technologies, Inc. (Roseland, NJ) 2032-08-23 RX search
Amgen NEUPOGEN filgrastim VIAL 103353 002 1991-02-20   See Pricing Emisphere Technologies, Inc. (Roseland, NJ) 2032-08-23 RX search
Amgen NEUPOGEN filgrastim SYRINGE 103353 003 1991-02-20   See Pricing Emisphere Technologies, Inc. (Roseland, NJ) 2032-08-23 RX search
Amgen NEUPOGEN filgrastim SYRINGE 103353 004 1991-02-20   See Pricing Emisphere Technologies, Inc. (Roseland, NJ) 2032-08-23 RX search
Nps Pharms Inc NATPARA parathyroid hormone INJECTABLE;INJECTION 125511 001 2015-01-23   See Pricing Emisphere Technologies, Inc. (Roseland, NJ) 2032-08-23 RX Orphan search
Nps Pharms Inc NATPARA parathyroid hormone INJECTABLE;INJECTION 125511 002 2015-01-23   See Pricing Emisphere Technologies, Inc. (Roseland, NJ) 2032-08-23 RX Orphan search
Nps Pharms Inc NATPARA parathyroid hormone INJECTABLE;INJECTION 125511 003 2015-01-23   See Pricing Emisphere Technologies, Inc. (Roseland, NJ) 2032-08-23 RX Orphan search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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