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    NEW PYROCATECHIN DERIVATIVES
    4.
    发明授权
    NEW PYROCATECHIN DERIVATIVES 有权
    新的吡咯并吡喃衍生物

    公开(公告)号：EP1904469B1

    公开(公告)日：2011-09-21

    申请号：EP06762514.5

    申请日：2006-07-10

    申请人： Novartis AG

    发明人： SEDELMEIER, Gottfried ,  NEBEL, Kurt ,  VEENSTRA, Siem, Jacob ,  ZERGENYI, Janos

    IPC分类号： C07D307/32 ,  C07C47/20

    CPC分类号： C07C69/96 ,  C07C45/676 ,  C07C45/71 ,  C07C49/84 ,  C07C68/06 ,  C07D307/33

    摘要： Pyrocatechin derivatives of formula I wherein R illustrates a group of formulae Ia, Ib, Ic or Id R1 is 4-halogen-but-2-enyl, R2 is lower alkyl or cycloalkyl, R3 is lower alkoxy and R4 is lower alkoxy lower alkoxy, or, where R is a group of formula (Ia), it is hydroxy, hydroxy lower alkoxy or a group of formula Ie R5 is reactive esterified hydroxy, R6 is azido and R7 is lower alkyl, lower alkenyl, cycloalkyl or aryl lower alkyl, and their salts, are valuable intermediates in the production of active ingredients for medicaments.

    摘要翻译： 其中R表示式Ia，Ib，Ic或Id的基团的式I的焦儿茶酚衍生物是4-卤素 - 丁-2-烯基，R2是低级烷基或环烷基，R3是低级烷氧基且R4是低级烷氧基低级烷氧基， 或者，其中R是式（Ia）基团，它是羟基，羟基低级烷氧基或式Ie基团，R5是反应性酯化羟基，R6是叠氮基，R7是低级烷基，低级链烯基，环烷基或芳基低级烷基， 和它们的盐是制备药物活性成分的有价值的中间体。

    NOVEL 2,3-DIOXO-1,2,3,4-TETRAHYDRO-QUINOYXALINYL DERIVATIVES
    9.
    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.