Prodrugs of benzoquinolizine-2-carboxylic acid

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C514S290000, C546S079000

Reexamination Certificate

active

07868173

ABSTRACT:
The instant invention relates to novel prodrugs of optically pure benzoquinolizine-2-carboxylic acid and pharmaceutical compositions that include the prodrugs. In particular, the present invention relates to the sulfonic acid salts of L-alanine and L-valine prodrugs of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid. The compounds and compositions of the invention can be used to treat bacterial Gram-positive, Gram-negative and anaerobic infections, especially infections caused by resistant Gram-positive organism and Gram-negative organism, mycobacterial infections and emerging nosocomial pathogen infections.

REFERENCES:
patent: 0068229 (2000-11-01), None
patent: WO0209758 (2002-02-01), None
Berge et al, 1977, Pharmaceutical Salts.
Cabri Walter, et al, 2007 Polymorphism and Patent Market and Legal battles.
Berge et al., Pharmaceutical salts. Review article. J Pharm Sci. Jan. 1977;66(1):1-19. (Abstract).

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