C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 455/04 (2006.01) A61K 31/4745 (2006.01) A61P 31/04 (2006.01) A61P 31/06 (2006.01) C07D 455/00 (2006.01)
Patent
CA 2373291
The present invention relates to S-(-)-optically pure benzoquinolizine carboxylic acid of formula I: Image wherein X is OR1, and R1 is H, a cation, choline, an organic amine, a heterocyclic amine, a basic amino acid, an alkyl, an ester or an heterocyclylalkyl; or X is NHR2 and R2 is H or NHR2 is an amino acid residue; y is 0-3; z is 0 or moles of water; HB is an acid of an acid addition salt; and R3 is H, alkyl, aralkyl, alkanoyl, aminoalkanoyl, or an ester of gluconic, phosphoric or sulphuric acid; and their pharmaceutically acceptable salts, derivatives, pseudopolymorphs, and hydrates, substantially free of their R- (+) -isomers, to processes for their preparation and to pharmaceutical compositions thereof. The compounds have excellent antibacterial activity. The compounds and compositions can be used for the treatment of local and systemic bacterial infections, diseases and disorders caused by antibiotic-sensitive and antibiotic-resistant microbial strains, without the concomitant liability of adverse effects associated with the racemic mixture.
L'invention concerne des S-(-)- acides carboxyliques de benzoquinolizine optiquement purs de formule (I), y compris leurs sels pharmaceutiquement acceptables, dérivés, pseudopolymorphes et hydrates, sensiblement dépourvus de leurs R-(+)-isomères. L'invention concerne également des procédés relatifs à leur élaboration et des compositions pharmaceutiques renfermant un principe actif décrit dans l'invention. Les composés considérés ont une excellente activité antibactérienne. Les composés et les compositions en question peuvent être utilisés pour le traitement d'infections bactériennes locales et systémiques, de maladies et de troubles engendrés par des souches microbiennes sensibles et résistantes vis-à-vis des antibiotiques, sans risque concomitant d'effets préjudiciables associés au mélange racémique du principe actif décrit dans l'invention.
Agarwal S.k.
Chugh Y.
de Souza N.j.
Gupte S.v.
Khorakiwala H.f.
Smart & Biggar
Wockhardt Limited
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