Pharmaceutical compounds, their preparation and use
    21.
    发明公开
    Pharmaceutical compounds, their preparation and use 失效
    药物化合物,它们的制备方法和它们的用途。

    公开(公告)号:EP0054924A2

    公开(公告)日:1982-06-30

    申请号:EP81110553.5

    申请日:1981-12-17

    发明人: Kneen, Geoffrey

    摘要: Compounds of formula
    wherein

    Y 1 is selected from hydroxyl, alkylamino, alkanoylamino,
    Y 2 , Y 3 and Y 4 are independently selected from hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, hydroxyl and benzyloxy; and
    Q 1 is either
    where
    Q 2 and Q 3 are independently selected from hydrogen and alkyl;
    X is selected from cyano, carboxyl, 5-tetrazolyl and alkylsulphonylcarbamoyl; and
    n is 0 or an integer selected from 1. 2. 3, 4, 5 and 6: salts of said compounds and, when X is carboxyl, esters and amides thereof,

    provided that

    when Y 1 is hydroxyl Y 2 , Y 3 and Y 4 are all hydrogen and Q 1 is either
    then X is alkylsulphonylcarbamoyl.

    These compounds are of value in medicine in the palliation of haemoglobinopathies, in particular sickle-cell anaemia and also in the palliation of pulmonary dysfunction, protection from the effects of hypoxia and the radio-sensitization of tumours. The invention is also directed to methods for the preparation of the ether compounds, to pharmaceutical formulations containing them and to the preparation of such formulations.

    摘要翻译: 式I的化合物... ... worin ... Y <1>选自羟基,烷基氨基,烷酰基氨基,Y <2>,Y <3>和Y <4>是unabhängig选自氢,卤素,烷基,烷氧基,三氟甲基 基,羟基和苄氧基; ......和Q <1>是... ...其中。Q <2>和Q <3>是unabhängig选自氢和烷基; ... X选自氰基,羧基,5-四唑基和alkylsulphonylcarbamoyl选择; 和... n是0或整数选择的氟利昂1,2,3,4,5和6; ...所述化合物和,当X是羧基,酯和酰胺的盐,...所提供的是...当Y <1>是羟基 ,Y <2>,Y <3>和Y <4>都是氢和Q <1>是... ...则X是alkylsulphonylcarbamoyl。 ... 这些化合物的在血红蛋白病的减轻医药价值,特别是镰状细胞贫血,因此,在肺功能障碍,保护从缺氧的影响和肿瘤的电波致敏缓和。 因此,本发明涉及用于所述醚化合物的制备方法,药物配方和灰含有它们的检索式蒸发散的制备。

    DÉRIVÉS DE LA 1-AMINO-PHTHALAZINE, LEUR PRÉPARATION, ET LEUR APPLICATION EN THÉRAPEUTIQUE
    24.
    发明公开
    DÉRIVÉS DE LA 1-AMINO-PHTHALAZINE, LEUR PRÉPARATION, ET LEUR APPLICATION EN THÉRAPEUTIQUE 有权
    1 AMINOPHTHALAZINDERIVATE,其制备方法及其食疗

    公开(公告)号:EP1737840A1

    公开(公告)日:2007-01-03

    申请号:EP05757289.3

    申请日:2005-04-13

    申请人: Sanofi-Aventis

    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.

    3-CYANO-2,4,5-TRIFLUOR-BENZOYLFLUORID UND ZWISCHENPRODUKTE ZU SEINER HERSTELLUNG
    26.
    发明授权
    3-CYANO-2,4,5-TRIFLUOR-BENZOYLFLUORID UND ZWISCHENPRODUKTE ZU SEINER HERSTELLUNG 失效
    3-氰基2,4,5-三氟苯甲酰及其生产中间产品

    公开(公告)号:EP0977729B1

    公开(公告)日:2002-03-13

    申请号:EP98919266.1

    申请日:1998-04-14

    申请人: BAYER AG

    摘要: The invention relates to 3-cyano-2,4,5-trifluoro-benzoyl fluoride and intermediate products for the production thereof and a method for the production of 3-cyano-2,4,5-trifluoro-benzoyl fluoride starting from 5-fluoro-1,3-xylol (VIII), which is chlorinated twice in the presence of a catalyst with ionic conditions in the nucleus to obtain 2,4-dichloro-5-fluoro-1,3-dymethylbenzol (VII), which is then chlorinated with radical conditions in the side chains to obtain 2,4-dichloro-5-fluoro-3-dichloromethyl-1-trichloromethyl benzol (VI), which is subsequently saponified by the optionally isolatable 2,4-dichloro-5-fluoro-3-dichloromethyl benzoic acid (V) to obtain 2,4-dichloro-5-fluoro-3-formyl-benzoic acid (IV) whose aldehyde group is converted to 2,4-dichloro-5-fluoro-3-N-hydroxyiminomethyl-benzoic acid (III), whereupon water is eliminated using an acid chloride while at the same time converting the carboxyl group into a chlorocarbonyl group to obtain nitrile 2,4-dichloro-3-cyano-5-fluoro-benzoyl-chloride (II), which is finally subjected to a fluorine/chlorine exchange.

    Smoking compositions containing a vanillin-release additive
    28.
    发明公开
    Smoking compositions containing a vanillin-release additive 失效
    香薰香草素。

    公开(公告)号:EP0514202A2

    公开(公告)日:1992-11-19

    申请号:EP92304427.5

    申请日:1992-05-15

    摘要: This invention provides smoking compositions which contain a vanillin carboxylate type flavorant-release additive.
    Under cigarette smoking conditions, a combustible filler and/or paper wrapper additive such as 5-carboxyethylvanillin pyrolyzes and releases ethylvanillin as a volatile flavorant component of the cigarette smoke.

    摘要翻译: 本发明提供含有香草醛羧酸盐型调味剂释放添加剂的吸烟组合物。 在吸烟条件下,可燃填料和/或纸包装添加剂如5-羧基乙基苯乙烯腈热解并释放乙烯基苯酚作为香烟烟雾的挥发性香料成分。