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Title:
QUINOLINECARBOXYLIC ACID DERIVATIVE
Document Type and Number:
Japanese Patent JPH0616678
Kind Code:
A
Abstract:

PURPOSE: To provide a new quinolinecarboxylic acid derivative useful for improving an infections disease caused by a Gram-positive bacterium including a methicillin-resistant Staphylococcus and a new quinolone-resistant and methicillin-resistant Staphylococcus.

CONSTITUTION: The derivative of formula I [Z is a (substituted) aromatic hetero group; R1 is H, an alkyl or a (substituted) phenyl; R2 is H, an alkyl, a halogen, etc.; R3 is H or an alkyl; R4 is H, an alkyl, hydroxy, etc.] and its pharmaceutically permissible salt, e.g. 6-fluoro-7-(4-pyridyl)-4-oxo-4H-[1,3]thiazeto[3,2- a]quinoline-3-carboxylic acid. The compound of formula I is obtained, e.g. by a cyclization reaction between a compound of formula II [R8 is an alkyl; Z0 is a (substituted) aromatic heterocyclic group] and a compound of formula III (D and E are each a halogen) in the presence of a deacidification agent (e.g. sodium carbonate) in an inert solvent at 0 to 120°C and, as necessary, a subsequent hydrolysis reaction.


Inventors:
MATSUOKA MASATO
MATSUDA MASATO
Application Number:
JP9548393A
Publication Date:
January 25, 1994
Filing Date:
March 30, 1993
Export Citation:
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Assignee:
NIPPON SHINYAKU CO LTD
International Classes:
A61K31/47; A61P31/04; C07D513/04; (IPC1-7): C07D513/04