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US 8,299,085 B2Granted
Quinazoline derivatives
AssigneeNovartis AG
InventorsHans Allgeier, Wolfgang Froestl, Manuel Koller, Henri Mattes, Joachim Nozulak, Silvio Ofner, David Orain, Vittorio Rasetti, Johanne Renaud, Nicolas Soldermann, Philipp Floersheim
Life of this patent
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Abstract
The present invention relates to 1H-Quinazoline-2,4-dione derivatives of formula(I) wherein the substituents are defined as in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them.
Claims6
Compounds of the formula (I)
- wherein G is in the 6-position and R1 is in the 7-position of the benzpyrimidin-dione;
- G is NR3R4;
- R3 and R4 together with the adjacent nitrogen atom form a mono- or polycyclic aromatic 5- to 10-membered heteroaryl residue being attached via this nitrogen ring atom and containing one or more hetero ring atoms;
- wherein said residue is unsubstituted or substituted by substituents selected from halogen, nitro, cyano, formyl, carboxamido, hydroxyl, amino, (C1-C4)-alkylamino, di-(C1-C4)-alkylamino, (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4) -alkoxycarbonyl, (C1-C4)-alkanesulfonyl, (C1-C4)-alkyl-carbonyl, (C1-C4)-alkoxycarbonylamino, (C1-C4) -alkylcarbonylamino, aryl, (C1-C8)-alkyl-alkyl, substituted by aryl, aryloxy-(C1-C8)-alkyl, aminocarbonyl-(C1-C8) mono-(C1-C8)-alkyl-aminocarbonyl-(C1-C8)-alkyl, di-(C1-C8)-alkyl-aminocarbonyl-(C1-C8)-alkyl and morpholinocarbonyl-(C1-C8)-alkyl,
- wherein the aryl groups are selected from phenyl, naphthyl and a mono- or polycyclic aromatic 5- to 10-membered heteroaryl containing one or more hetero ring atoms, and wherein the aryl groups themselves are unsubstituted or substituted by substituents selected from halogen, nitro, cyano, formyl, carboxamido, hydroxyl, amino, (C1-C4)-alkylamino, di-(C1-C4)-alkylamino, (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-alkoxycarbonyl, (C1-C4)- alkanesulfonyl, (C1-C4)-alkyl-carbonyl, (C1-C4)-alkoxycarbonylamino and (C1-C4)-alkylcarbonylamino;
- or R3 and R4 together with the adjacent nitrogen atom form a mono- or polycyclic saturated or partially unsaturated heterocyclyl residue containing three to ten ring atoms being attached via this nitrogen ring atom and wherein one or more of the ring atoms are hetero atoms;
- wherein said residue is unsubstituted or substituted by substituents selected from halogen, nitro, cyano, formyl, carboxamido, hydroxyl, amino, (C1-C4)-alkylamino, di-(C1-C4)-alkylamino, (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-alkoxycarbonyl, (C1-C4)-alkanesulfonyl, (C1-C4)-alkyl-carbonyl, (C1-C4)-alkoxycarbonylamino, (C1-C4)-alkylcarbonylamino, aryl, (C1-C8)-alkyl substituted by aryl, aryloxy-(C1-C8)-alkyl, aminocarbonyl-(C1-C8) -alkyl, mono-(C1-C8)-alkyl -aminocarbonyl-(C1-C8)-alkyl, di-(C1-C8)-alkyl-aminocarbonyl-(C1-C8)-alkyl and morpholinocarbonyl-(C1-C8)-alkyl,
- wherein the aryl groups are selected from phenyl, naphthyl and a mono- or polycyclic aromatic 5- to 10-membered heteroaryl containing one or more hetero ring atoms, and wherein the aryl groups themselves are unsubstituted or substituted by substituents selected from halogen, nitro, cyano, formyl, carboxamido, hydroxyl, amino, (C1-C4)-alkylamino, di-(C1-C4)-alkylamino, (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-alkoxycarbonyl, (C1-C4)- alkanesulfonyl, (C1-C4)- alkyl-carbonyl, (C1-C4)-alkoxycarbonylamino and (C1-C4)-alkylcarbonylamino;
- R1 is nitro or trifluoromethyl;
- R2 is (C1-C8)-alkyl, aryl or (C1-C8)-alkyl substituted by aryl,
- wherein the aryl groups are selected from phenyl, naphthyl and a mono- or polycyclic aromatic 5- to 10-membered heteroaryl containing one or more hetero ring atoms, and wherein the aryl groups themselves are unsubstituted or substituted by substituents selected from halogen, nitro, cyano, formyl, carboxamido, hydroxyl, amino, (C1-C4)-alkylamino, di-(C1-C4)-alkylamino, (C1-C4)-alkyl, (C1-C4)-alkoxy, (C1-C4)-alkoxycarbonyl, (C1-C4)- alkanesulfonyl, (C1-C4)- alkyl-carbonyl, (C1-C4)-alkoxycarbonylamino and (C1-C4)-alkylcarbonylamino;
- and their physiologically acceptable salts.
9 more elements
Dependencies are inferred from the claim text.