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    AZATRICYCLO[3.3.1.1] DECANE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    4.
    发明公开
    AZATRICYCLO[3.3.1.1] DECANE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 有权
    AZATRICYCLO [3.3.1.1]癸烷衍生物和含有它们的药物组合物

    公开(公告)号：EP1068208A1

    公开(公告)日：2001-01-17

    申请号：EP99909806.4

    申请日：1999-03-03

    申请人： R.J. REYNOLDS TOBACCO COMPANY

    发明人： BENCHERIF, Merouane ,  LIPPIELLO, Patrick, Michael ,  CROOKS, Peter, Anthony ,  PARK, Haeil ,  BHATTI, Balwinder, Singh ,  CALDWELL, William, Scott ,  DULL, Gary, Maurice

    IPC分类号： C07D471/18 ,  A61K31/435

    CPC分类号： A61K31/444 ,  A61K31/439

    摘要： A pharmaceutical composition incorporating a nicotinic antagonist is provided. The composition is an effective amount of a compound of formula (I), wherein X' is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; X is nitrogen or carbon bonded to a substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; A, A' and A' are individually substituent species characterized as having a sigma m value greater than 0, less than 0 or 0; Z' is a substituent other than hydrogen; j is an integer from 0 to 5; and the wavy line in the structure indicates that the compound can exist in the form of an enantiomer or a diasteromer; Z' is hydrogen or a substituent other than hydrogen; Y is C=O, C(OH)R' or C-A, where R' is hydrogen or lower alkyl.

    摘要翻译： 提供了掺入烟碱拮抗剂的药物组合物。 该组合物是有效量的式（I）化合物，其中X'是氮或键合到特征为具有大于0，小于0或0的西格玛值的取代基物质的碳; X是键合到取代物上的氮或碳，其特征在于西格玛m值大于0，小于0或0; A，A'和A'分别是取代物种类，其特征在于西格玛m值大于0，小于0或0; Z'是除氢以外的取代基; j是从0到5的整数; 结构中的波浪线表明化合物可以以对映异构体或非对映异构体的形式存在; Z'是氢或除氢以外的取代基; Y是C = O，C（OH）R'或C-A，其中R'是氢或低级烷基。

    PHARMACEUTICAL COMPOSITIONS INCORPORATING ARYL SUBSTITUTED OLEFINIC AMINE COMPOUNDS
    6.
    发明公开
    PHARMACEUTICAL COMPOSITIONS INCORPORATING ARYL SUBSTITUTED OLEFINIC AMINE COMPOUNDS 失效
    药物组合物WHAT芳基取代的烯胺化合物

    公开(公告)号：EP0973743A1

    公开(公告)日：2000-01-26

    申请号：EP98905108.1

    申请日：1998-02-19

    申请人： R.J. REYNOLDS TOBACCO COMPANY

    发明人： CALDWELL, William, Scott ,  DULL, Gary, Maurice ,  DOBSON, Grayland, Page ,  MILLER, Craig, Harrison ,  BENCHERIF, Merouane ,  LIPPIELLO, Patrick, Michael

    IPC分类号： C07D213/64 ,  C07D213/61 ,  C07D213/38 ,  A61K31/44

    CPC分类号： C07D213/64 ,  C07D213/38 ,  C07D213/61

    摘要： Patients susceptible to or suffering from central nervous system disorders (e.g., Alzheimer's disease, Parkinson's disease, Tourette's syndrome, attention deficit disorder or schizophrenia) are treated by administering an effective amount of an aryl substituted olefinic amine compound of Formula (I): wherein X is C-R', C-OR', C-CH2-OR' wherein R' is selected from the group consisting of H, C1-C5 alkyl, an aromatic group containing species and alkyl-, halo-, or amino-substituted aromatic group containing species; E' is hydrogen or C1-C5 alkyl or halo substituted C1-C5 alkyl; E'' is C1-C5 alkyl or halo substituted C1-C5 alkyl; Z' and Z'' are each individually selected from the group consisting of hydrogen, C1-C5 alkyl, aryl rings, and can form a ring structure (a), A, A' and A'' are each individually selected from the group consisting of hydrogen, C1-C7 alkyl, and halo; m is 0 or 1; p is 0 or 1 with the proviso that when m or p is 0 then that E'' is hydrogen; and the wavy line in the structure represents a cis (Z) or trans (E) form of the compound. Exemplary compounds include (E)-N-methyl-4-[3-(benzyloxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-phenoxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-isopropoxypyridin)yl]-3-buten-1-amine, (E)-N-methyl-4-[3-(5-methoxymethylpyridin)yl]-3-buten-1-amine, and (E)-N-methyl-4-[3-(5-phenylpyridin)yl]-3-buten-1-amine.

    DEPOLARIZING SKELETAL MUSCLE RELAXANTS
    7.
    发明公开
    DEPOLARIZING SKELETAL MUSCLE RELAXANTS 失效
    去骨化肌骨骼肌松弛剂

    公开(公告)号：EP0804195A2

    公开(公告)日：1997-11-05

    申请号：EP95931029.0

    申请日：1995-08-29

    申请人： R.J. REYNOLDS TOBACCO COMPANY

    发明人： BENCHERIF, Merouane ,  LIPPIELLO, Patrick, Michael ,  CALDWELL, William, Scott

    IPC分类号： C07D401 ,  A61K31 ,  A61P21 ,  C07D453

    CPC分类号： A61K31/439 ,  A61K31/435 ,  A61K31/44 ,  A61K31/444 ,  A61K31/465

    摘要： Compounds such as 5-chloronicotine, 5-fluoronornicotine, anabaseine, 5-fluoroanabaseine, 2-acetoxymethylquinuclidine or 2-(3-pyridyl)-quinuclidine are useful as locally acting and highly selective muscle relaxants. Each compound, when administered intravenously, acts to bind to musculoskeletal nicotinic receptor sites in a reversible manner causing transient depolarization, and hence provides for reversible muscle relaxation to a patient during anesthesia.

    摘要翻译： 诸如5-氯烟碱，5-氟烟碱酸，香树碱，5-氟代香烟碱，2-乙酰氧基甲基奎宁环或2-（3-吡啶基） - 奎宁环的化合物可用作局部作用和高度选择性的肌肉松弛剂。 当静脉内给药时，每种化合物以可逆的方式与肌肉骨骼烟碱受体位点结合，引起短暂的去极化，并因此在麻醉期间为患者提供可逆的肌肉松弛。