Claims for Patent: 7,977,506

Summary for Patent: 7,977,506

Title:	Compounds and compositions for delivering active agents
Abstract:	Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.
Inventor(s):	Boyd; Maria Aurora P. (Garrison, NY), Leone-Bay; Andrea (Ridgefield, CT), O\'Toole; Doris C. (Carmel, NY)
Assignee:	Emisphere Technologies, Inc. (Cedar Knolls, NJ)
Application Number:	11/557,589
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 7,977,506
Patent Claims:	1. A compound of the formula: ##STR00005## wherein R.sup.1 is --OH or --OCH.sub.3; R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are independently selected from hydrogen, halogen, --OH, --OCH.sub.3, C.sub.1-C.sub.4 alkyl, --NH.sub.2, --NH(CH.sub.3), --N(CH.sub.3).sub.2, or --NO.sub.2; m is 0; R.sup.6 is a phenyl substituted with --O--R.sup.7--COOH at the ortho, meta, or para position; R.sup.6 is optionally substituted with one or more members selected from halogen, --OH, --OCH.sub.3, C.sub.1-C.sub.4 alkyl, --NH.sub.2, NH(CH.sub.3), --N(CH.sub.3).sub.2, and --NO.sub.2; and R.sup.7 is C.sub.2-C.sub.12 linear alkyl, or C.sub.4-C.sub.12 branched alkyl, or a pharmaceutically acceptable salt thereof. 2. The compound of claim 1 wherein R.sup.1 is --OH. 3. The compound of claim 1 wherein said compound is selected from the group consisting of: ##STR00006## and pharmaceutically acceptable salts thereof. 4. The compound of claim 1 wherein said compound is ##STR00007## or a pharmaceutically acceptable salt thereof. 5. The compound of claim 4 wherein said compound is the disodium salt. 6. The compound of claim 1 wherein said compound is selected from the group consisting of: ##STR00008## and pharmaceutically acceptable salts thereof. 7. A composition comprising: (A) a biologically active agent; and (B) a compound as defined in claim 1. 8. A composition comprising: (A) a biologically active agent; and (B) a compound as defined in claim 4. 9. A composition comprising: (A) a biologically active agent; and (B) a compound as defined in claim 5. 10. The composition of claim 9, wherein the biologically active agent comprises at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid. 11. The composition of claim 10, wherein the biologically 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, growth hormone releasing factor; interferons, .alpha.-interferon, .beta.-interferon, .gamma.-interferon; interleukin, 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; 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. 12. The composition of claim 11, wherein the biologically active agent is insulin, unfractionated heparin, low molecular weight heparin, very low molecular weight heparin, ultra low molecular weight heparin, calcitonin, PTH, EPO, hGH or any combination thereof. 13. The composition of claim 12, wherein the biologically active agent is insulin. 14. A dosage unit form comprising: (A) the composition of claim 7; 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. 15. The dosage unit form of claim 14, wherein the biologically active agent comprises at least one protein, polypeptide, peptide, hormone, polysaccharide, mucopolysaccharide, carbohydrate, or lipid. 16. The dosage unit form of claim 15, wherein the biologically 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, growth hormone releasing factor; interferons, .alpha.-interferon, .beta.-interferon, .gamma.-interferon; interleukin, 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; thrombopoietin; filgrastim; prostaglandins; cyclosporin; vasopressin; cromolyn sodium; sodium chromoglycat; disodium chromoglycate; vancomycin; desferrioxamine; parathyroid hormone; fragments of parathyroid hormone; antimicrobials; anti-fungal agents; vitamins; and any combination thereof. 17. The dosage unit form of claim 16, wherein the biologically active agent is insulin, unfractionated heparin, low molecular weight heparin, very low molecular weight heparin, ultra low molecular weight heparin, calcitonin, PTH, EPO, hGH, or any combination thereof. 18. The dosage unit form of claim 17, wherein the active agent is insulin. 19. The dosage unit form of claim 14, wherein the dosage unit form is a tablet, a capsule, a powder, or a liquid. 20. The dosage unit form of claim 14, wherein the dosage unit form comprises a dosing vehicle selected from the group consisting of water, 25% aqueous propylene glycol, phosphate buffer, 1,2-propane diol, ethanol, and any combination thereof. 21. A method for administering a biologically-active agent to an animal in need of the agent, the method comprising administering to the animal the composition of claim 7. 22. A method for administering a biologically-active agent to an animal in need of the agent, the method comprising administering to the animal via the pulmonary route the composition of claim 9. 23. 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. 24. The compound of claim 1 wherein R.sup.7 is C.sub.2-C.sub.12 linear alkyl. 25. The compound of claim 1, wherein R.sup.1 is --OCH.sub.3.

Details for Patent 7,977,506

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		2039-03-29
Eli Lilly And Company	HUMULIN R U-500	insulin human	Injection	018780	12/29/2015		2039-03-29
Eli Lilly And Company	HUMULIN R U-100	insulin human	Injection	018780	08/06/1998		2039-03-29
Eli Lilly And Company	HUMULIN R U-500	insulin human	Injection	018780	03/31/1994		2039-03-29
Eli Lilly And Company	HUMULIN R U-100	insulin human	Injection	018780	05/25/2018		2039-03-29
Amgen, Inc.	NEUPOGEN	filgrastim	Injection	103353	02/20/1991		2039-03-29