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Last Updated: April 26, 2024

Claims for Patent: 7,803,791

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Summary for Patent: 7,803,791

Title:	Method for producing albumin conjugates containing gyrase inhibitors
Abstract:	The present invention is directed to a Gyrase inhibitor-protein conjugate; in particular a Gyrase inhibitor-albumin conjugate. The present invention further provides methods of the treatment of inflammatory conditions and tumors. Methods of making and producing a Gyrase inhibitor-protein conjugate are also disclosed.
Inventor(s):	Sinn; Hannsjorg (Wiesloch, DE), Mulbaier; Marcel (Heidelberg, DE)
Assignee:	Albupharm Heidelberg GmbH & Co. KG (Heidelberg, DE)
Application Number:	11/795,721
Patent Claims:	1. A Gyrase inhibitor-albumin conjugate comprising a gyrase inhibitor and an albumin, wherein the molar ratio of the gyrase inhibitor to the albumin is 2:1 to 0.1:1 wherein the conjugate is obtained by reacting the gyrase inhibitor and the albumin in the presence of N-(3-dimethylaminopropyl)-N'-ethyl-carbonyldiimide in an organic solvent, and wherein the gyrase inhibitor compound comprises a carboxylic acid group which links the gyrase inhibitor via an amide bond to the albumin, wherein the gyrase inhibitor is selected from the group consisting of quinolone carboxylic acid derivatives, 1,8-naphtyridine derivatives, pyridopyrimidine carboxylic acid derivatives and cinnolone carboxylic acid derivatives, wherein said quinolone carboxylic acid derivative selected from the group consisting of ciprofloxacin, enoxacin, norfloxacin, ofloxacin, oxolinic acid, sparfloxacin, pefloxacin, fleroxacin, temafloxacin, lomifloxacin, ibafloxacin, marbofloxacin, danofloxacin, moxifloxacin, nadifloxacin, enrofloxacin, sarafloxacin and gatifloxacin; wherein said 1,8-naphtyridine derivative is a nalidixic acid; wherein said pyridopyrimidine carboxylic acid derivative selected from the group consisting of pipemidic acid and piromidic acid; and wherein said cinnolone carboxylic acid derivative selected from the group consisting of rosoxacin and cinoxacin. 2. The Gyrase inhibitor-albumin conjugate according to claim 1, wherein the albumin is a human serum albumin. 3. The Gyrase inhibitor-albumin conjugate according to claim 1, wherein the albumin is present in a native form. 4. The Gyrase inhibitor-albumin conjugate according to claim 1 wherein the gyrase inhibitor is covalently coupled to the albumin. 5. The Gyrase inhibitor-albumin conjugate according to claim 4, wherein the covalent coupling is cleavable under pathological conditions. 6. The Gyrase inhibitor-albumin conjugate according to claim 5, wherein the cleavage takes place enzymatically. 7. The Gyrase inhibitor-albumin conjugate according to claim 1, wherein the albumin is present in its natural form. 8. The Gyrase inhibitor-albumin conjugate according to claim 1, wherein the gyrase inhibitor is selected from the group consisting of norfloxacin, enoxacin and ciprofloxacin. 9. The Gyrase inhibitor-albumin conjugate according to claim 8, wherein the gyrase inhibitor is norfloxacin. 10. The Gyrase inhibitor-albumin conjugate according to claim 1, wherein the gyrase inhibitor has a molecular weight of <2000 Da. 11. The Gyrase inhibitor-albumin conjugate according to claim 10, wherein the molar ratio of the gyrase inhibitor to protein is 1.1:1 to 0.5:1. 12. The Gyrase inhibitor-albumin conjugate according to claim 11, wherein the molar ratio of the gyrase inhibitor to the albumin is 1.1:1 to 0.9:1. 13. A Pharmaceutical preparation comprising a gyrase inhibitor-albumin conjugate according to claim 1 as the active substance.

Details for Patent 7,803,791

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Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Grifols Therapeutics Llc	ALBUKED, PLASBUMIN-20, PLASBUMIN-25, PLASBUMIN-5	albumin (human)	For Injection	101138	10/21/1942	⤷ Try a Trial	2025-01-21
Baxalta Us Inc.	BUMINATE, FLEXBUMIN	albumin (human)	Injection	101452	03/03/1954	⤷ Try a Trial	2025-01-21
Csl Behring Ag	ALBURX	albumin (human)	Injection	102366	07/23/1976	⤷ Try a Trial	2025-01-21
Grifols Biologicals Llc	ALBUTEIN	albumin (human)	Injection	102478	08/15/1978	⤷ Try a Trial	2025-01-21
Instituto Grifols, S.a.	HUMAN ALBUMIN GRIFOLS	albumin (human)	Injection	103352	02/17/1995	⤷ Try a Trial	2025-01-21
Instituto Grifols, S.a.	HUMAN ALBUMIN GRIFOLS	albumin (human)	Injection	103352	06/11/2003	⤷ Try a Trial	2025-01-21
Csl Behring Llc	ALBUMINAR, ALBUMINAR-20, ALBUMINAR-25, ALBUMINAR-5	albumin (human)	Injection	103955	03/17/2000	⤷ Try a Trial	2025-01-21
>Applicant	>Tradename	>Biologic Ingredient	>Dosage Form	>BLA	>Approval Date	>Patent No.	>Expiredate

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