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    • 22. 发明专利
    • ES2217324T3
    • 2004-11-01
    • ES96929275
    • 1996-08-19
    • NOVARTIS AG
    • ACKLIN PIERREALLGEIER HANSAUBERSON YVESBIOLLAZ MICHELMORETTI ROBERTOFNER SILVIO
    • A61K20060101A61K31/00A61K31/495A61K31/498A61K31/502A61K31/505A61K31/506A61K31/535A61K31/5355A61K31/5375A61K31/5377A61K31/55A61K31/662A61P25/28A61P43/00C07D20060101C07D241/44C07D401/06C07D401/12C07D403/06C07D403/12C07D405/12C07D409/06C07D413/06C07D417/06C07D417/12C07D491/113C07F9/6509
    • PCT No. PCT/EP96/03644 Sec. 371 Date Feb. 27, 1998 Sec. 102(e) Date Feb. 27, 1998 PCT Filed Aug. 19, 1996 PCT Pub. No. WO97/08155 PCT Pub. Date Mar. 6, 19972,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), wherein one of the radicals R1, and R2 is a group R5 and the other is a group of formula -CH(R6)-alk-R7 (Ia), -alk-CH(R6-R7 (Ib), -alk-N(R8)-X-R7 (Ic), -alk-N+(R8)(R9)-X-R7A- (Id), -alk-O-X-R7 (Ie) or -alk-S-X-R7 (If), R3, R4 and R5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R7 is hydrogen; an aliphatic, cycloaliphatic or heterocycloaliphatic radical; cyano; acyl derived from carbonic acid or from a semiester or semiamide of carbonic acid, from sulfuric acid or from an aliphatic or aromatic sulfonic acid or from phosphoric acid or from a phosphonic acid ester; amino that is unsubtituted or aliphatically or araliphatically substituted and/or substituted by aliphatic, araliphatic or aromatic acyl; or an aromatic or heteroaromatic radical, R8 is hydrogen; an aliphatic or araliphatic radical; or acyl derived from an aliphatic or araliphatic carboxylic acid or from an aliphatic or araliphatic semiester of carbonic acid, or R7 and R8, together with X and the nitrogen atom bonding R8 and X, form an unsubstitued or substituted mono- or di-azaxycloalkyl, azoxacycloalkyl, azathiacycloalkyl or optionally oxidised thiacycloalkyl radical bonded via a nitrogen atom, or an unsubstituted or substituted, optionally partially hxdrogenated aryl or heteroaryl radical, R9 is an aliphatic or araliphatic radical, or R7, R8 and R9 together with X and the nitrogen atom bonding R8, R9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A- being the anion of a protonic acid, alk is lower alkylene, and X (unless, together with R7 and R8 and the nitrogen atom bonding R8 and X or together with the nitrogen atom bonding R8, R9 and X, it forms part of one of the mentioned ring systems) is a divalent aliphatic, cycloaliphatic or araliphatic radical or a direct bond, and the pharmaceutically acceptable salts thereof can be used in the preparation of a medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor.
    • 23. 发明专利
    • NOVEL 2,3-DIOXO-1,2,3,4-TETRAHYDRO-QUINOYXALINYL DERIVATIVES
    • SI0853617T1
    • 2004-08-31
    • SI9630678
    • 1996-08-19
    • NOVARTIS AG
    • ACKLIN PIERREALLGEIER HANSAUBERSON YVESBIOLLAZ MICHELMORETTI ROBERTOFNER SILVIOVEENSTRA SIEM JACOB
    • A61K20060101A61K31/00A61K31/495A61K31/498A61K31/502A61K31/505A61K31/506A61K31/535A61K31/5355A61K31/5375A61K31/5377A61K31/55A61K31/662A61P25/28A61P43/00C07D20060101C07D241/44C07D401/06C07D401/12C07D403/06C07D403/12C07D405/12C07D409/06C07D413/06C07D417/06C07D417/12C07D491/113C07F9/6509
    • PCT No. PCT/EP96/03644 Sec. 371 Date Feb. 27, 1998 Sec. 102(e) Date Feb. 27, 1998 PCT Filed Aug. 19, 1996 PCT Pub. No. WO97/08155 PCT Pub. Date Mar. 6, 19972,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), wherein one of the radicals R1, and R2 is a group R5 and the other is a group of formula -CH(R6)-alk-R7 (Ia), -alk-CH(R6-R7 (Ib), -alk-N(R8)-X-R7 (Ic), -alk-N+(R8)(R9)-X-R7A- (Id), -alk-O-X-R7 (Ie) or -alk-S-X-R7 (If), R3, R4 and R5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R7 is hydrogen; an aliphatic, cycloaliphatic or heterocycloaliphatic radical; cyano; acyl derived from carbonic acid or from a semiester or semiamide of carbonic acid, from sulfuric acid or from an aliphatic or aromatic sulfonic acid or from phosphoric acid or from a phosphonic acid ester; amino that is unsubtituted or aliphatically or araliphatically substituted and/or substituted by aliphatic, araliphatic or aromatic acyl; or an aromatic or heteroaromatic radical, R8 is hydrogen; an aliphatic or araliphatic radical; or acyl derived from an aliphatic or araliphatic carboxylic acid or from an aliphatic or araliphatic semiester of carbonic acid, or R7 and R8, together with X and the nitrogen atom bonding R8 and X, form an unsubstitued or substituted mono- or di-azaxycloalkyl, azoxacycloalkyl, azathiacycloalkyl or optionally oxidised thiacycloalkyl radical bonded via a nitrogen atom, or an unsubstituted or substituted, optionally partially hxdrogenated aryl or heteroaryl radical, R9 is an aliphatic or araliphatic radical, or R7, R8 and R9 together with X and the nitrogen atom bonding R8, R9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A- being the anion of a protonic acid, alk is lower alkylene, and X (unless, together with R7 and R8 and the nitrogen atom bonding R8 and X or together with the nitrogen atom bonding R8, R9 and X, it forms part of one of the mentioned ring systems) is a divalent aliphatic, cycloaliphatic or araliphatic radical or a direct bond, and the pharmaceutically acceptable salts thereof can be used in the preparation of a medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor.
    • 25. 发明专利
    • DE69631774D1
    • 2004-04-08
    • DE69631774
    • 1996-08-19
    • NOVARTIS AG
    • ACKLIN PIERREALLGEIER HANSAUBERSON YVESBIOLLAZ MICHELMORETTI ROBERTOFNER SILVIOVEENSTRA JACOB
    • A61K20060101A61K31/00A61K31/495A61K31/498A61K31/502A61K31/505A61K31/506A61K31/535A61K31/5355A61K31/5375A61K31/5377A61K31/55A61K31/662A61P25/28A61P43/00C07D20060101C07D241/44C07D401/06C07D401/12C07D403/06C07D403/12C07D405/12C07D409/06C07D413/06C07D417/06C07D417/12C07D491/113C07F9/6509
    • PCT No. PCT/EP96/03644 Sec. 371 Date Feb. 27, 1998 Sec. 102(e) Date Feb. 27, 1998 PCT Filed Aug. 19, 1996 PCT Pub. No. WO97/08155 PCT Pub. Date Mar. 6, 19972,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), wherein one of the radicals R1, and R2 is a group R5 and the other is a group of formula -CH(R6)-alk-R7 (Ia), -alk-CH(R6-R7 (Ib), -alk-N(R8)-X-R7 (Ic), -alk-N+(R8)(R9)-X-R7A- (Id), -alk-O-X-R7 (Ie) or -alk-S-X-R7 (If), R3, R4 and R5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R7 is hydrogen; an aliphatic, cycloaliphatic or heterocycloaliphatic radical; cyano; acyl derived from carbonic acid or from a semiester or semiamide of carbonic acid, from sulfuric acid or from an aliphatic or aromatic sulfonic acid or from phosphoric acid or from a phosphonic acid ester; amino that is unsubtituted or aliphatically or araliphatically substituted and/or substituted by aliphatic, araliphatic or aromatic acyl; or an aromatic or heteroaromatic radical, R8 is hydrogen; an aliphatic or araliphatic radical; or acyl derived from an aliphatic or araliphatic carboxylic acid or from an aliphatic or araliphatic semiester of carbonic acid, or R7 and R8, together with X and the nitrogen atom bonding R8 and X, form an unsubstitued or substituted mono- or di-azaxycloalkyl, azoxacycloalkyl, azathiacycloalkyl or optionally oxidised thiacycloalkyl radical bonded via a nitrogen atom, or an unsubstituted or substituted, optionally partially hxdrogenated aryl or heteroaryl radical, R9 is an aliphatic or araliphatic radical, or R7, R8 and R9 together with X and the nitrogen atom bonding R8, R9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A- being the anion of a protonic acid, alk is lower alkylene, and X (unless, together with R7 and R8 and the nitrogen atom bonding R8 and X or together with the nitrogen atom bonding R8, R9 and X, it forms part of one of the mentioned ring systems) is a divalent aliphatic, cycloaliphatic or araliphatic radical or a direct bond, and the pharmaceutically acceptable salts thereof can be used in the preparation of a medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor.