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    Anticholinergics, processes for the preparation thereof, and pharmaceutical compositions
    1.
    发明授权
    Anticholinergics, processes for the preparation thereof, and pharmaceutical compositions 有权
    抗胆碱能药，其制备方法和药物组合物

    公开(公告)号：US06696462B2

    公开(公告)日：2004-02-24

    申请号：US10345911

    申请日：2003-01-16

    申请人： Christian Eickmeier ,  Sabine Germeyer ,  Matthias Grauert ,  Sabine Pestel ,  Michael P. Pieper ,  Georg Speck ,  Steffen Breitfelder

    发明人： Christian Eickmeier ,  Sabine Germeyer ,  Matthias Grauert ,  Sabine Pestel ,  Michael P. Pieper ,  Georg Speck ,  Steffen Breitfelder

    IPC分类号： A61K31439

    CPC分类号： C07D451/06 ,  C07D451/10

    摘要： A compound of formula 1 wherein: X- is an anion with a single negative charge; A and B, which are identical or different, are each —O—, —S—, —NH—, —CH2—, —CH═CH—, or —N(C1-C4-alkyl)—; R is hydrogen, hydroxy, —C1-C4-alkyl, —C1-C4-alkyloxy, —C1-C4-alkylene-halogen, —0—C1-C4-alkylene-halogen, —C1-C4-alkylene-OH, —CF3, —CHF2, —C1-C4-alkylene-C1-C4-alkyloxy, —0—COC1-C4-alkyl, —0—COC1-C4-alkylene-halogen, —C1-C4-alkylene-C3-C6-cycloalkyl, —0—COCF3, or halogen; R1 and R2, which are identical or different, are each —C1-C5-alkyl, which is optionally substituted by —C3-C6-cycloalkyl, hydroxy, or halogen, or R1 and R2 together are a —C3-C5-alkylene bridge; R3, R4, R3′, and R4′, which are identical or different, are each hydrogen, C1-C4-alkyl, C1-C4-alkyloxy, hydroxy, —CF3, —CHF2, —CN, —NO2, or halogen; RX and RX′, which are identical or different, are each hydrogen, C1-C4-alkyl, C1-C4-alkyloxy, hydroxy, —CF3, —CHF2, —CN, —NO2, or halogen, or RX and RX′ together are a single bond or a bridging group selected from —O—, —S—, —NH—, —CH2—, —CH2—CH2—, —N(C1-C4-alkyl)—, —CH(C1-C4-alkyl)—, and —C(C1-C4-alkyl)2—, or a pharmacologically acceptable acid addition salt thereof, processes for preparing, them and their use in pharmaceutical compositions.

    摘要翻译： 式1的化合物，其中X 1是具有单个负电荷的阴离子; A和B相同或不同，各自为-O - ， - S - ， - NH-， - CH 2 - ， - CH = CH-或-N（C 1 -C 4 - 烷基） - ; R是氢，羟基，-C 1 -C 4 - 烷基，-C 1 -C 4 - 烷氧基，-C 1 -C 4 - 亚烷基 - 卤素，-O-C 1 -C 4 - 亚烷基 - 卤素，-C 1 -C 4 - 亚烷基-OH，-CF 3，-CHF 2，-C 1 -C 4 - 亚烷基-C 1 -C 4 - 烷氧基，-O-CCl-C 4 - 烷基，-O-CCl- - 卤素，-C 1 -C 4 - 亚烷基-C 3 -C 6 - 环烷基，-O-COCF 3或卤素; R 1和R 2各自为-C 1 -C 5 - 烷基， 任选被-C 3 -C 6 - 环烷基，羟基或卤素取代，或R 1和R 2一起是-C 3 -C 5亚烷基桥; R 3，R 4，R 3' R 1，R 2，R 3，R 4，R 4，R 4，R 4，R 4， X，R 1，R 2，R 2，R 2，R 2，R 3，R 3，R 3，R 3，R 3， X>和R X'一起是单键 或选自-O - ， - S - ， - NH - ， - CH 2 - ， - CH 2 -CH 2 - ， - N（C 1 -C 4 - 烷基） - ， - CH（C 1 -C 4烷基） 和-C（C 1 -C 4 - 烷基）2-或其药理学上可接受的酸加成盐，用于制备它们及其在药物组合物中的用途。