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    DÉRIVÉS DE LA 1-AMINO-PHTHALAZINE, LEUR PRÉPARATION, ET LEUR APPLICATION EN THÉRAPEUTIQUE
    4.
    发明授权
    DÉRIVÉS DE LA 1-AMINO-PHTHALAZINE, LEUR PRÉPARATION, ET LEUR APPLICATION EN THÉRAPEUTIQUE 有权
    1-AMINOPHTHALAZINDERIVATE，DEREN HERSTELLUNG UND DEREN THERAPEUTISCHE VERWENDUNG

    公开(公告)号：EP1737840B1

    公开(公告)日：2007-09-12

    申请号：EP05757289.3

    申请日：2005-04-13

    申请人： Sanofi-Aventis

    发明人： AUGEREAU, Jean Michel ,  GESLIN, Michel ,  COURTEMANCHE, Gilles

    IPC分类号： C07D401/12 ,  C07D239/32 ,  C07D239/34 ,  C07C65/30 ,  C07C65/32 ,  A61K31/502

    CPC分类号： C07D333/22 ,  C07D213/50 ,  C07D237/30 ,  C07D237/32 ,  C07D317/54 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/14 ,  C07D417/14 ,  C07D451/04

    摘要： The invention relates to 1-amino-phthalazine derivatives of general formula (I), wherein A, B = possibly substituted C1-4-alkylene; L = a simple bond or C1-2-alkylene, possibly substituted -CH=CH-, or -C=C- or cycloprop-1,2--diyl; R1 = possibly substituted aryl or heteroaryl; R2, R3 = H, C1-3-alkyl, C1-3-fluoralkyl or R2 et R3 forming together with a bearing them carbon atom, a cycloprop-1,1-diyl; R4 = H, C1-5-alkyl, C1-3-fluoralkyl, C3-6-cycloalkyl, C3-6-cycloalkyl-C1-3-alkylene, C1-3-alkyl-O-C1-3-alkylene, HO-C1-3-alkylene, C1-3-alkyl-X-C1-3-alkylene, wherein X = S, SO or S02; or R4 = RaRbN-C1-3-alkylene, aryl, aryl-C1-3-alkylene, aryl-O-, aryl-O-C1-3-alkylene, aryl-C1-3-alkylene-O-C1-3-alkylene, heteroaryl or heteroaryl-C1-3-alkylene; R5 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, HO-C1-3-alkylene, -CN, C1-3-alkyl-X-, wherein X = S, SO or SO2; or R5 = RaRbN-, RaRbN-C1-3-alkylene, aryl, aryl-C1-3-alkylene, aryl-O- or heteroaryl; R6 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, -CN, RaRbN-, RaRbN-C1-3-alkylene, aryl or heteroaryl ; R7 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, HO-C1-3--alkylene, -CN, C1-3-alkyl-X-, wherein X = S, SO or SO2; or R7, = RaRbN-, RaRbN-C1-3--alkylene, ReRbNC(O)-, C1-3-alkyl-C(O)-, aryl, aryl-0- or heteroaryl ; R8 = H, halogen, C1-5-alkyl, C1-5-alkoxy, C1-3-fluoroalkoxy ; in the form of base or acid additional salt and in the form of a hydrate or solvent. A method for preparing and using the inventive derivatives for therapeutically purpose is also disclosed.

    摘要翻译： 通式（I）的1-氨基 - 酞嗪衍生物，其中取代基如本文所定义。 还公开了制备这种化合物的方法，用于这种方法的中间体和使用式（I）化合物的医疗处理。

    PROCEDE DE PREPARATION DE 3-CARBOXY-4-HYDROXYBENZALDEHYDES ET DERIVES
    5.
    发明授权
    PROCEDE DE PREPARATION DE 3-CARBOXY-4-HYDROXYBENZALDEHYDES ET DERIVES 失效
    用于生产3-羧基-4-羟基 - 苯甲醛及其衍生物

    公开(公告)号：EP0773919B1

    公开(公告)日：2000-09-20

    申请号：EP96917543.9

    申请日：1996-05-24

    申请人： RHODIA CHIMIE

    发明人： METIVIER, Pascal

    IPC分类号： C07C65/30 ,  C07C51/255

    CPC分类号： C07C45/676 ,  C07C45/38 ,  C07C51/255 ,  C07C47/575 ,  C07C47/58 ,  C07C65/30

    摘要： The object of the invention is a method for preparing 3-carboxy-4-hydroxybenzaldehydes and derivatives thereof from phenol compounds bearing formyl and/or hydroxymethyl groups in positions 2 and 4. Another object of the invention is the production of 4-hydroxybenzaldehydes from 3-carboxy-4-hydroxybenzaldehydes, and particularly the production of 3-methoxy-4-hydroxybenzaldehyde and 3-ethoxy-4-hydroxybenzaldehyde, known as 'vanillin' and 'ethyl vanillin' respectively. The method for preparing 3-carboxy-4-hydroxybenzaldehyde is characterised in that the group in position 2 of the phenol compound bearing formyl and/or hydroxymethyl groups in positions 2 and 4 is selectively oxidised to a carboxylic group, and optionally a hydroxymethyl group in position 4 to a formyl group. By thereafter decarboxylating the 3-carboxy-4-hydroxybenzaldehyde, a 4-hydroxybenzaldehyde is obtained.