Claims for Patent: 9,458,089

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.

Details for Patent 9,458,089

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Eli Lilly And Company	HUMULIN R U-100	insulin human	Injection	018780	10/28/1982		2032-08-23
Eli Lilly And Company	HUMULIN R U-500	insulin human	Injection	018780	12/29/2015		2032-08-23
Eli Lilly And Company	HUMULIN R U-100	insulin human	Injection	018780	08/06/1998		2032-08-23