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    NOVEL 2,3-DIOXO-1,2,3,4-TETRAHYDRO-QUINOYXALINYL DERIVATIVES
    33.
    发明公开
    NOVEL 2,3-DIOXO-1,2,3,4-TETRAHYDRO-QUINOYXALINYL DERIVATIVES 失效
    2,3-DIOXO-1,2,3,4-四氢 - 二氢喹啉衍生物

    公开(公告)号：EP0853617A1

    公开(公告)日：1998-07-22

    申请号：EP96929275.0

    申请日：1996-08-19

    申请人： Novartis AG

    发明人： ACKLIN, Pierre ,  ALLGEIER, Hans ,  AUBERSON, Yves ,  BIOLLAZ, Michel ,  MORETTI, Robert ,  OFNER, Silvio ,  VEENSTRA, Siem, Jacob

    IPC分类号： A61K31 ,  A61P25 ,  A61P43 ,  C07D241 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409 ,  C07D413 ,  C07D417 ,  C07D491 ,  C07F9

    CPC分类号： C07D401/06 ,  C07D241/44 ,  C07D401/12 ,  C07D417/12 ,  C07F9/650994

    摘要： 2,3-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-R¿7? (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 R¿7? 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.

    2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL-SULFONAMIDE DERIVATIVES
    35.
    发明公开
    2,4-DIOXO-1,4-DIHYDRO-2H-QUINAZOLIN-3-YL-SULFONAMIDE DERIVATIVES 审中-公开
    2,4-二氧代-1,4-二氢-2H-CHINAZOLIN -3- YL-SULFONAMIDDERIVATE

    公开(公告)号：EP2571865A1

    公开(公告)日：2013-03-27

    申请号：EP11719840.8

    申请日：2011-05-18

    申请人： Novartis AG

    发明人： AUBERSON, Yves ,  CARCACHE, David ,  LERCHNER, Andreas ,  NOZULAK, Joachim

    IPC分类号： C07D403/04 ,  C07D405/04 ,  A61P25/08 ,  A61K31/517

    CPC分类号： C07D403/04 ,  C07D239/96 ,  C07D405/04

    摘要： The invention relates to a 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivative being (A) a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; or (B) a compound selected from a certain group of 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivatives disclosed in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them. In a first aspect, the invention provides prodrugs of AMPA receptor antagonists which potentially useful in the treatment of a wide range of disorders, particularly epilepsy.

    SUBSTITUIERTE AMINOALKANPHOSPHONSÄUREN
    36.
    发明公开
    SUBSTITUIERTE AMINOALKANPHOSPHONSÄUREN 失效
    SUBSTITUIERTEAMINOALKANPHOSPHONSÄUREN

    公开(公告)号：EP0934326A1

    公开(公告)日：1999-08-11

    申请号：EP97946755.0

    申请日：1997-10-22

    申请人： Novartis AG

    发明人： ACKLIN, Pierre ,  ALLGEIER, Hans ,  AUBERSON, Yves ,  OFNER, Silvio ,  VEENSTRA, Siem, Jacob

    IPC分类号： A61K31 ,  A61P9 ,  A61P25 ,  A61P43 ,  C07F9

    CPC分类号： C07F9/650994

    摘要： Compounds have the formula (I), in which R1 stands for hydroxy or an aliphatic, araliphatic or aromatic radical; X stands for a bivalent aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical; R2 stands for hydrogen or an aliphatic or araliphatic radical; alk stands for lower alkylidene; and R3, R4 and R5 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro. These compounds and their salts may be used for treating pathological conditions which respond to the blocking of exciter amino acid receptors, and for producing pharmaceutical compositions.

    摘要翻译： 化合物具有式（I），其中R 1代表羟基或脂族，芳脂族或芳族基团; X代表二价脂族，脂环族，脂环族 - 脂族，芳脂族，杂芳脂族或芳族基团; R2代表氢或脂族或芳脂族基团; alk代表低级亚烷基; 并且R3，R4和R5独立地表示氢，低级烷基，卤素，三氟甲基，氰基或硝基。 这些化合物及其盐可用于治疗对激动剂氨基酸受体的阻断作出反应的病理状态，并用于制备药物组合物。