C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 405/04 (2006.01) A61K 31/517 (2006.01) A61P 29/00 (2006.01)
Patent
CA 2659689
The present invention concerns novel amidines derivatives of 2-heteroaryl-quinazoline and quinolines of general formula (I), to a process for their preparation, to their pharmaceutical compositions and to the use of these compounds, salts and solvates thereof, along with the corresponding pharmaceutical compositions, for the treatment of pain and inflammatory disorders. Compounds of this invention are extremely potent analgesics, suitable for the treatment of both inflammatory and neuropathic pain. Particularly for the treatment of neuropathic pain the compounds of the invention have been proved largely superior to the standards currently in the clinical use. These compounds are not acting through inhibition of COX or NOS enzymes but are effective in inhibiting inflammatory cytokine production induced by inflammatory stimuli.
La présente invention concerne de nouveaux dérivés amidine de 2-hétéroaryl-quinazolines et de quinolines de formule générale (I), un procédé pour leur préparation, leurs compositions pharmaceutiques et l'utilisation de ces composés, de leurs sels et de leurs solvates, conjointement avec les compositions pharmaceutiques correspondantes, dans le traitement de la douleur et des troubles inflammatoires. Les composés de l'invention sont des analgésiques extrêmement puissants convenant au traitement de la douleur inflammatoire et neuropathique. Dans le traitement de la douleur neuropathique en particulier, les composés de l'invention se sont révélés largement supérieurs par rapport aux composés standard actuellement en usage clinique. Ces composés n'agissent pas par inhibition des enzymes COX ou NOS mais sont efficaces pour inhiber la production de cytokines inflammatoires induite par les stimuli inflammatoires.
Caselli Gianfranco
Fiorentino Teresa Simonetta
Giordani Antonio
Makovec Francesco
Mandelli Stefano
Macrae & Co.
Rottapharm S.p.a.
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