Rottapharm Spa

Rotta Research Laboratorium

Rotta Research Laboraturium S.p.a.

Rottapharm Biotech S.r.l.

Simona Zanzola

Lucio C Rovati

Francesco Makovec

Antonio Giordani

Roberto Artusi

Stefano Mandelli

Gianfranco Caselli

Ilario Verpilio

Francesca Tarchino

Silvio Mazzari

Lucio Claudio Rovati

Tiziana Piepoli

Marco Lanza

Teresa Simonetta Fiorentino

Massimo Maria D'amato

Ornella Letari

The present invention is directed to 6-(1H-imidazo-1-yl)-2-aryl and 2-heteroaryl quinazoline and quinolines derivatives, compounds of formula (I), their pharmaceutical acceptable salts and solvates and corresponding pharmaceutical compositions, that acts as Monoamine Oxidase (MAO) inhibitors and Imidazoline Receptor ligands: wherein: X is independently selected from &#x2014;CH group or a nitrogen atom (&#x2014;N), W is independently selected from an aryl group, an heteroaryl group, or a benzocondensed heteroaryl group such as 1,3-benzodioxole, benzofuran, 2,3-dihydrobenzofuran, benzothiophene, 2,3-dihydrobenzothiophene, indole, 2,3-dihydroindole, benzimidazole, benzoxazole, benzothiazole, 2H-3,4-dihydrobenzopyran, [1,4]-benzodioxine, 2,3-dihydro-[1,4]-benzodioxine (1,4-benzodioxan). Ris independently selected from hydrogen (&#x2014;H), C-Calkyl, hydroxymethyl (&#x2014;CHOH), aminomethyl (&#x2014;CHNH), alkylaminomethyl [CHNH(R)], or di-alkylaminomethyl [CHN(R)], trifluoromethyl (&#x2014;CF). Compounds of formula (I) elicited a pharmacological profile suitable for the clinical treatment of depression and related disorders, Parkinson disease, drug abuse, and morphine tolerance and dependence.

6-1H-imidazo-quinazoline and quinolines derivatives, new MAO inhibitors and imidazoline receptor ligands

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

Compounds which may be represented by the general formula (I) shown below and in which: Ris a group independently selected from among: CHO, &#x2014;COOH, &#x2014;CHOH Ris hydrogen or a linear or branched C-Calkyl group Ris hydrogen or a halogen group selected from among Cl and Br Ris a linear or branched C-Calkyl group and the pharmaceutically acceptable salts thereof such as the sodium or potassium salt. The compounds exhibit potent and selective All antagonist activity and are useful for the treatment of any disorders in which elevated synthesis of All or overexpression of the ATreceptor may play a primary pathological role, as in the case of arterial hypertension, congestive cardiac insufficiency, platelet aggregation and disorders associated therewith such as for example myocardial and cerebral infarction, renal ischaemia, venous and arterial thrombosis, peripheral vasculopathy, pulmonary hypertension, diabetes mellitus, diabetic neuropathy, glaucoma and diabetic retinopathy. 

Pyrrole derivatives with angiotensin II antagonist activity

Heterocyclic amidines with anti-inflammatory and analgesic activity that inhibit nitrogen oxide production, of formula (I): in which: and in which the substituents W, Y and X are combined to form 9- or 10-membered bicyclic heteroaromatic derivatives containing up to 2 hetero atoms in the same ring; and

Anti-inflammatory and analgesic heterocyclic amidines that inhibit nitrogen oxide (NO) production

Compounds which can be represented by the general formula (I) indicated below: and in which:

Benzamidine derivatives having anti-inflammatory and immunosuppressive activity

The invention describes compounds represented by the general formula (I) given below: in which:

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Milan, Italy

Simona Zanzola