Claims for Patent: 9,220,687

Summary for Patent: 9,220,687

Title:	Substituted diketopiperazine analogs for use as drug delivery agents
Abstract:	Disclosed are drug delivery systems for the delivery of small molecule and macromolecular drugs. More particularly, disclosed are substituted analogs of 3,6-di(alkyl-4 aminobutyl)-2,5-diketopiperazine (which may also be referred to DKP), their use in the formulation of both small molecule and macromolecular drugs including therapeutic, prophylactic and diagnostic agents, stabilizing agents and systems for their delivery.
Inventor(s):	Kraft; Kelly Sullivan (Hopewell Junction, NY)
Assignee:	MannKind Corporation (Valencia, CA)
Application Number:	14/536,168
Patent Claims:	1. A method for stabilizing an active agent comprising: spray drying a solution of an active agent molecule and a pharmaceutically acceptable salt of a substituted diketopiperazine to form a dry powder; wherein the pharmaceutically acceptable salt of a substituted diketopiperazine has the general structure of Formula A: ##STR00005## wherein R is an alkyl group of 1 to 10 carbons or hydrogen; X is an amide bond, an ester, a sulfone, a sulfoxide, an amine, or a ketone; and n or m represents an integer from 0 to 20, and Y is an amide, acid, hydroxyl, phenol, phosphonic acid, or thiol. 2. The method of claim 1 wherein R is hydrogen, n=3, m is C.dbd.C, X is --NHC(O)--, and Y is COOH. 3. The method of claim 1 wherein R is hydrogen, n=2, m is C.dbd.C, X is --NHC(O)--, and Y is COOH. 4. The method of claim 1 wherein R is an isopropyl, n=3, m is C.dbd.C, X is --NHC(O)--, and Y is COOH. 5. The method of claim 1 wherein the active agent is a peptide, protein, polypeptide, small molecule, or nucleic acid molecule. 6. The method of claim 5, wherein the active agent is selected from the group consisting of insulin, glucagon, glucagon like peptide 1 (GLP-1), calcitonin, parathyroid hormone 1-34, bioactive fragment of parathyroid hormone, octreotide, leuprolide, and RSV peptide, granulocyte colony stimulating factor (GM-CSF), peptide YY, oxyntomodulin, felbamate, cannabinoid antagonists and/or agonists, muscurinic antagonsits and/or agonistics, heparin, low molecular weight heparin, cromolyn, sildenafil, vardenafil, tadalafil, growth hormone, AZT, DDI, lamotrigine, chorionic gonadotropin releasing factor, luteinizing release hormone, .beta.-galactosidase, exendins 1-4, ghrelin, tryptin, and analogs and fragments thereof. 7. The method of claim 5, wherein the active agent is insulin or an insulin analog. 8. The method of claim 7 wherein the active agent is insulin. 9. The method of claim 8 wherein the insulin is human insulin. 10. The method of claim 5, wherein the active agent is GLP-1. 11. The method of claim 5, wherein the active agent is oxyntomodulin. 12. A method of delivering a stabilized active agent to a patient in need thereof, wherein the dry powder of claim 1 is delivered to the pulmonary system. 13. The method of claim 12, wherein the active agent is insulin or an insulin analog. 14. The method of claim 13 wherein the active agent is insulin. 15. The method of claim 14 wherein the insulin is human insulin. 16. The method of claim 12, wherein the active agent is GLP-1. 17. The method of claim 12, wherein the active agent is oxyntomodulin. 18. The method of claim 5 wherein the active agent is a GLP-1 analog. 19. The method of claim 12 wherein the active agent is a GLP-1 analog. 20. The method of claim 5 wherein the active agent is peptide YY. 21. The method of claim 12 wherein the active agent is peptide YY.

Details for Patent 9,220,687

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Ferring Pharmaceuticals Inc.	NOVAREL	chorionic gonadotropin	For Injection	017016	01/15/1974		2028-12-29
Ferring Pharmaceuticals Inc.	NOVAREL	chorionic gonadotropin	For Injection	017016	12/27/1984		2028-12-29
Ferring Pharmaceuticals Inc.	NOVAREL	chorionic gonadotropin	For Injection	017016	02/15/1985		2028-12-29
Ferring Pharmaceuticals Inc.	NOVAREL	chorionic gonadotropin	For Injection	017016	02/16/1990		2028-12-29
Bel-mar Laboratories, Inc.	CHORIONIC GONADOTROPIN	chorionic gonadotropin	Injection	017054	03/26/1974		2028-12-29
Fresenius Kabi Usa, Llc	CHORIONIC GONADOTROPIN	chorionic gonadotropin	For Injection	017067	03/05/1973		2028-12-29
Eli Lilly And Company	HUMULIN R U-100	insulin human	Injection	018780	10/28/1982		2028-12-29