Method for producing albumin conjugates containing gyrase inhibitors

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.