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    Substituted pyrimidinyl-2-(diaza-bicyclo-alkyl)-pyrimidone derivatives
    2.
    发明公开
    Substituted pyrimidinyl-2-(diaza-bicyclo-alkyl)-pyrimidone derivatives 审中-公开
    取代基嘧啶基-2-（二氮杂 - 双环烷基） - 嘧啶酮

    公开(公告)号：EP1454910A1

    公开(公告)日：2004-09-08

    申请号：EP03290570.5

    申请日：2003-03-07

    申请人： SANOFI-SYNTHELABO ,  Mitsubishi Pharma Corporation

    发明人： Lochead, Alistair W. ,  Saady, Mourad ,  Slowinski, Franck ,  Yaiche, Philippe

    IPC分类号： C07D487/08 ,  A61K31/506 ,  A61P25/28 ,  A61P35/00

    CPC分类号： C07D487/08

    摘要： The invention relates to a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I) or a salt thereof:
    wherein:

    R1 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom;
    R2 represents a hydrogen atom, a C 1-6 alkyl group optionally substituted by 1 to 4 substituents selected from a halogen atom, a hydroxyl group or a C 1-4 alkoxy group; a C 1-2 perhalogenated alkyl group, a benzyl group, a phenethyl group, a benzyloxycarbonyl group, a C 1-4 alkoxy carbonyl group, a benzene ring, a naphthalene ring, a quinoline ring, a phthalazine ring, a 5,6,7,8-tetrahydronaphthalene ring, a pyridine ring, an indole ring, a pyrrole ring, a thiophene ring, a benzenesulfonyl group, a benzoyl group, a pyridazine ring, a furan ring or an imidazole ring; the benzyl group, the phenethyl group, the benzyloxycarbonyl group, the benzenesulfonyl group, the benzoyl group and the rings being optionally substituted by 1 to 4 substituents selected from a C 1-6 alkyl group, a benzene ring, a halogen atom, a C 1-2 perhalogenated alkyl group, a C 1-3 halogenated alkyl group, a hydroxyl group, a C 1-4 alkoxy group, a nitro, a cyano, an amino, a C 1-6 monoalkylamino group or a C 2-10 dialkylamino group;
    R3 represents a 2, 4 or 5-pyrimidine ring optionally substituted by a C 1-4 alkyl group, C 1-4 alkoxy group or a halogen atom;
    R4 represents a C 1-4 alkyl group optionally substituted by a hydroxyl group, a C 1-4 alkoxy group or a halogen atom and n represents 1 or 2.

    The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β, such as Alzheimer disease.

    摘要翻译： 本发明涉及由式（I）表示的2-（二氮杂双环烷基） - 嘧啶酮衍生物或其盐：其中：R1表示氢原子，C1-6烷基或卤素原子; R2表示氢原子，任选被1至4个选自卤素原子，羟基或C 1-4烷氧基的取代基取代的C 1-6烷基; C1-2全卤代烷基，苄基，苯乙基，苄氧基羰基，C1-4烷氧基羰基，苯环，萘环，喹啉环，酞嗪环，5,6,7 8-四氢萘环，吡啶环，吲哚环，吡咯环，噻吩环，苯磺酰基，苯甲酰基，哒嗪环，呋喃环或咪唑环; 苄基，苯乙基，苄氧基羰基，苯磺酰基，苯甲酰基和环任选被1〜4个选自C 1-6烷基，苯环，卤素原子，C1- 2个全卤代烷基，C1-3卤代烷基，羟基，C1-4烷氧基，硝基，氰基，氨基，C1-6单烷基氨基或C2-10二烷基氨基; R3表示任选被C 1-4烷基，C 1-4烷氧基或卤素原子取代的2,4或5-嘧啶环; R 4表示任选被羟基，C 1-4烷氧基或卤素原子取代的C 1-4烷基，n表示1或2.本发明还涉及包含所述衍生物或盐的药物 作为活性成分，其用于预防和/或治疗由GSK3β的异常活性如阿尔茨海默病引起的神经变性疾病。

    PHENOXYPROPANOLAMINES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE
    6.
    发明授权
    PHENOXYPROPANOLAMINES, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE 有权
    PHENOXYPROPANOLAMIN衍生物，生产和治疗用途

    公开(公告)号：EP1242404B1

    公开(公告)日：2004-07-07

    申请号：EP00988936.1

    申请日：2000-12-15

    申请人： SANOFI-SYNTHELABO

    发明人： BOVY, Philippe, R. ,  CECCHI, Roberto ,  VENIER, Olivier

    IPC分类号： C07D401/04 ,  A61K31/4545 ,  A61K31/4523 ,  A61P1/00 ,  C07D401/14 ,  C07D211/58

    CPC分类号： C07D401/04 ,  C07D401/14

    摘要： The invention concerns phenoxypropanolamines of formula (I) wherein: R1 represents a hydrogen, a -S(O)z-(C1-C4)Alk-R' group, R' being H, phenyl or (C1-C4) alkoxy), -NHSO2-(C1-C4) Alk, NHCO(C1-C4) Alk; m and n are each independently 0, 1 or 2; R2 and R3 represent independently a hydrogen, a (C5-C6) alkyl, (C3-C6) cycloalkyl, (C1-C4) alkoxy, hydroxy(C1-C4)alkyl, (C1-C4) alkoxy-(C1-C4)alkyl, mono-or di-(C1-C4)Alk-amino(C1-C4)alkyl, pyrrolidino-(C1-C4)alkyl, phenylamino, (C2-C4)alkenyl group, or an aromatic or heteroaromatic group substituted or not with a group R4; R2 and R3 can also together constitute a saturated or unsaturated cycle of 3 to 6 atoms capable of bearing a (C1-C4) alkyl, amino(C1-C4)alkyl, carbamoyl or benzyl substituent; R4 represents a hydrogen or a halogen, a -CO(C1-C4)Alk group or a -NHSO2-(C1-C4)Alk group; a (C1-C4)Alk group, a (C1-C4)alkoxy group, a halogen, -COOH, -COO(C1-C4)Alk, -CN, -CONR3R4, -NO2, -SO2NH2, -NHSO2(C1-C4)Alk; z is 1 or 2; and their salts and solvates. Said compounds have an agonist activity with respect to β-3 adrenergic receptors.

    DISPOSITIF POUR DISTRIBUER UN PRODUIT FLUIDE OU PULVERULENT A UNE DISTANCE PREDETERMINEE
    10.
    发明授权
    DISPOSITIF POUR DISTRIBUER UN PRODUIT FLUIDE OU PULVERULENT A UNE DISTANCE PREDETERMINEE 失效
    装置，使液体或粉末产品在一定的距离

    公开(公告)号：EP1009458B1

    公开(公告)日：2004-04-28

    申请号：EP98903081.2

    申请日：1998-01-19

    申请人： VALOIS S.A.S. ,  SANOFI-SYNTHELABO

    发明人： ARGHYRIS, Laurent ,  BEDOS, Michel

    IPC分类号： A61M11/00 ,  A61F9/00 ,  B05B15/08

    CPC分类号： B05B11/3091 ,  B05B11/0005 ,  B05B11/0027 ,  B05B15/68

    摘要： The invention concerns a device for spraying or dispensing a fluid or powdery product on a surface to be treated and/or an intake element (50), comprising: a dispensing member (1), including a dispensing opening (31), said dispensing member being associated with a reservoir (2 ) containing said product and being movable between an inoperative position and a dispensing position; and actuating means for moving said dispensing member (1) towards its dispensing position for delivering a dose of product: The invention is characterised in that the device further comprises: means for measuring distance (20) movable between an inoperative position and their useful position, and arranged in their useful position such that each time the device is used the dispensing opening (31) is located at a fixed predetermined distance from the surface to be treated and/or the intake element (50), the movement of said means for distance measuring (20) from their useful position towards their inoperative position bringing the said dispensing member (1) back towards its inoperative position.