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109 条记录 (耗时 0.037 秒)

    Process for the preparation of compounds capable of activating cholinergic receptors
    8.
    发明公开
    Process for the preparation of compounds capable of activating cholinergic receptors 审中-公开
    Verfahren zur Herstellung von zur Aktivierung cholinerger Rezeptoren geeigneter Verbindungen

    公开(公告)号：EP2253616A1

    公开(公告)日：2010-11-24

    申请号：EP10075370.6

    申请日：2003-10-01

    申请人： Targacept, Inc.

    发明人： Caldwell, Wiliams S ,  Dull, Gary M ,  Wagner, Jered M

    IPC分类号： C07D213/38 ,  C07D239/26

    CPC分类号： C07D239/26 ,  A61K31/44 ,  A61K31/505 ,  C07D213/38 ,  C07D213/61 ,  C07D213/65 ,  C07D213/73 ,  C07D403/06

    摘要： The present invention provides a method for synthesizing a compound of formula

    or a pharmaceutically acceptable salt thereof, wherein
    each of A, A I , and A" is H;
    X is COR I ;
    R' is C 1-5 alkyl;
    X I is N;
    mis1;
    n is 1;
    each of E', E", E III , E IV , and E V is H;
    E VI is C 1-5 alkyl; and
    each of Z I and Z II individually is H or C 1-5 alkyl;

    or comprising coupling of a halo-substituted pyridine with an olefin containing protected amine functionality.

    摘要翻译： 本发明提供了一种用于合成式或其药学上可接受的盐的方法，其中A，AI和A“各自为H; X为COR I; R'为C 1-5烷基; XI为N; mis1; n为1; E'，E“，E III，E IV和EV各为H; E VI为C 1-5烷基; Z I和Z II各自为H或C 1-5烷基; 或包括卤素取代的吡啶与含有保护的胺官能团的烯烃的偶联。

    N-ARYL DIAZASPIRACYCLIC COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF
    9.
    发明授权
    N-ARYL DIAZASPIRACYCLIC COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF 有权
    N-芳基化合物DIAZASPIROZYKLISCHE，其用途和方法及其生产

    公开(公告)号：EP1519939B1

    公开(公告)日：2009-12-09

    申请号：EP03739358.4

    申请日：2003-06-27

    申请人： Targacept, Inc.

    发明人： BHATTI, Balwinder, S. ,  MILLER, Craig, H. ,  SCHMITT, Jeffrey, D.

    IPC分类号： C07D487/10 ,  C07D471/10 ,  A61K31/40 ,  A61K31/435

    CPC分类号： C07D487/20 ,  C07D453/02 ,  C07D471/10 ,  C07D471/20 ,  C07D487/10

    摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryldiazaspirocyclic compounds, bridged analogs of N-heteroaryl diazaspirocyclic compounds, or prodrugs or metabolites of these compounds. The aryl group can be a five or six-membered heterocyclic ring (heteroaryl). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly those disorders characterized by dysfunction of nicotinic choligernic neurotransmission, including disorders involving neuromodulation of neurotransmitter release, such as dopamine release. CNS disorders, which are characterized by an alteration in normal neurotransmitter release, are another example of disorders that can be treated and/or prevented. The compounds and compositions can also be used to alleviate pain. The compounds can: ( I ) alter the number of nicotinic cholinergic receptors of the brain of the patient, ( ii ) exhibit neuroprotective effects and ( iii ) when employed in effective amounts, not result in appreciable adverse side effects (e.g. side effects such as significant increases in blood pressure and heart rate, significant negative effects upon the gastrointestinal tract, and significant effects upon skeletal muscle).