PRODRUGS OF ANTIBIOTIC 7-ACYLAMINO-3-HETEROARYLTHIO-3-CEPHEM CARBOXYLIC ACID Russian patent published in 2006 - IPC C07D501/59 A61K31/546 A61P31/04

Abstract RU 2279435 C2

FIELD: organic chemistry, antibiotics, pharmacy.

SUBSTANCE: invention relates to compound of the formula: wherein R'¹ means hydrogen atom; R'² represents acyl group but with exception of glycyl that is cleaved by mammalian enzyme. Also, invention describes (7R)-7-[(Z)-2-(2-amino-5-chlorothiazol-4-yl)-2-(hydroxyimino)acetamido]-3-{3-[2-N-(L)-aspartylaminoethylthiomethyl]pyrid-4-ylthio}-3-cephem-4-carboxylic acid of the formula: or its pharmaceutically acceptable salt and pharmaceutical composition used in treatment or prophylaxis of bacterial infection and comprising the effective amount of one or more of indicated compounds. The claimed prodrugs show the enhanced solubility in water at neutral or near to neutral pH value as compared with the parent compounds.

EFFECT: improved and valuable properties of prodrugs.

15 cl

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RU 2 279 435 C2

Authors

Ehkker Skott Dzh.

Cho Aehsop

Glinka Tomas V.

Kolkins Trevor

Li Ving Dzh.

Dates

2006-07-10—Published

2001-03-20—Filed