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33 条记录 (耗时 0.03 秒)

    1,2,3,4,5,6-Hexahydro-2,6-methano-3-benzazocin-10-ols
    5.
    发明授权
    1,2,3,4,5,6-Hexahydro-2,6-methano-3-benzazocin-10-ols 有权
    1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并吖庚因-10-ols

    公开(公告)号：US06455538B1

    公开(公告)日：2002-09-24

    申请号：US09523473

    申请日：2000-03-10

    申请人： Matthias Grauert ,  Adrian Carter ,  Wolf-Dietrich Bechtel ,  Thomas Weiser ,  Rainer Palluk ,  Uwe Pschorn

    发明人： Matthias Grauert ,  Adrian Carter ,  Wolf-Dietrich Bechtel ,  Thomas Weiser ,  Rainer Palluk ,  Uwe Pschorn

    IPC分类号： A61K31439

    CPC分类号： C07D221/26

    摘要： Compounds of general formula I wherein X is a single bond, —O—, C-C4-alkylene, or an alkylene bridge having 1 to 8 carbon atoms which may be branched or unbranched and optionally have one or two oxygen atom(s) anywhere in the bridge; R1 is hydrogen, methyl, ethyl, or phenyl; R2 is hydrogen or methyl; R3 is hydrogen, fluorine, chlorine, bromine, hydroxy, methyl, or methoxy; R4 is hydrogen, methyl, or ethyl; R5 is hydrogen, methyl, or ethyl; R6 is hydrogen, methyl, or ethyl; R7 is tert-butyl, cyclohexyl, phenyl optionally substituted by R9 and R10, which may be identical or different, or; R8 is hydrogen or C1-C4-alkyl; Z is oxygen, NH, or sulfur; R9 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; R10 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; optionally in the form of the individual optical isomers, mixtures of the individual enantiomers or racemates as well as in the form of the free bases or the corresponding acid addition salts with pharmaceutically acceptable acids.

    摘要翻译： 通式I的化合物，其中X是单键，-O-，C-C4-亚烷基或具有1至8个碳原子的亚烷基桥，其可以是支链或非支链的，并且任选地在一个或多个氧原子中具有一个或两个氧原子 桥梁 R1是氢，甲基，乙基或苯基; R2是氢或甲基; R3是氢，氟，氯，溴，羟基，甲基或甲氧基; R4是氢，甲基或乙基; R5是氢，甲基或乙基; R6是氢，甲基或乙基; R 7是叔丁基，环己基，任选被R 9和R 10取代的苯基，其可以相同或不同，或者R 8是氢或C 1 -C 4 - 烷基; Z是氧，NH或硫; R9是氢，甲基，氟，氯，溴或甲氧基; R 10为氢，甲基，氟，氯，溴或甲氧基; 任选以各种旋光异构体的形式，各个对映异构体或外消旋体的混合物，以及游离碱的形式或与药学上可接受的酸的相应的酸加成盐。

    Anticholinergics, processes for the preparation thereof, and pharmaceutical compositions
    7.
    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。

    Covalently coupled benzoylecgonine, egconine and ecgonidine derivatives
    8.
    发明授权
    Covalently coupled benzoylecgonine, egconine and ecgonidine derivatives 失效
    共价连接的苯并巴比妥，厄可宁和厄氨胍衍生物

    公开(公告)号：US06482831B1

    公开(公告)日：2002-11-19

    申请号：US09558534

    申请日：2000-04-26

    申请人： James E. Wynn ,  Lowell M. Somers

    发明人： James E. Wynn ,  Lowell M. Somers

    IPC分类号： A61K31439

    CPC分类号： C07D451/12 ,  A61K31/439 ,  C07D519/00

    摘要： The present invention relates to a novel class of covalently coupled benzoylecgonine, ecgonine and ecgonidine derivatives that are useful for alleviating the symptoms of immunoregulatory disorders, neuromuscular disorders, joint disorders, connective tissue disorders, circulatory disorders and pain. Accordingly, this invention also relates to pharmaceutical compositions and methods for their use.

    摘要翻译： 本发明涉及可用于缓解免疫调节障碍，神经肌肉疾病，关节疾病，结缔组织疾病，循环系统疾病和疼痛的症状的共价连接的苯并八氢大，嗪，厄古定和替康宁衍生物的新型。 因此，本发明还涉及其用途的药物组合物和方法。