Rottapharm Spa

Silvio Mazzari

Lucio C Rovati

Francesco Makovec

Antonio Giordani

Gianfranco Caselli

Simona Zanzola

Stefano Mandelli

Francesca Tarchino

Tiziana Piepoli

Ilario Verpilio

Teresa Simonetta Fiorentino

Lucio Claudio Rovati

The present invention is directed to novel 6-1H-imidazo-2-aryl and 2-heteroaryl quinazoline and quinoline of formula I, corresponding salts and solvates thereof, to a process for their preparation and to the use of this compounds and corresponding pharmaceutical composition for the treatment of pain and inflammatory related disorders. Compounds of the invention have been proven highly effective in the pharmacological treatment of both inflammatory and neuropathic pain, in addition to striking anti-inflammatory properties. Their effectiveness in interfering with COX-2 and inflammatory cytokines expressions and production, highlights them as interesting compounds also for the treatment of cancer in addition to several inflammatory diseases. 

6-1H-imidazo-quinazoline and quinolines derivatives, new potent analgesics and anti-inflammatory agents

The present invention is directed to novel 6-1H-imidazo-2-aryl and 2-heteroaryl quinazoline and quinoline of formula I, corresponding salts and solvates thereof, to a process for their preparation and to the use of this compounds and corresponding pharmaceutical composition for the treatment of pain and inflammatory related disorders. Compounds of the invention have been proven highly effective in the pharmacological treatment of both inflammatory and neuropathic pain, in addition to striking anti-inflammatory properties. Their effectiveness in interfering with COX-2 and inflammatory cytokines expressions and production, highlights them as interesting compounds also for the treatment of cancer in addition to several inflammatory diseases. Formula I: 

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. 

Amidine derivatives of 2-heteroaryl-quinazolines and quinolines; potent analgesics and anti-inflammatory agents

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Padua, Italy

Silvio Mazzari