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    AZATRICYCLO[3.3.1.1] DECANE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    5.
    发明授权
    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：EP1068208B1

    公开(公告)日：2003-05-14

    申请号：EP99909806.4

    申请日：1999-03-03

    申请人： Targacept, Inc.

    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“分别为特征为具有大于0，小于0或0的σm值，Z'为除氢以外的取代基，j为0至5的整数的单独的取代基物种;以及波浪线 在结构中表示该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。

    AZASPIROALKENE AND AZAPIROALKANE COMPOUNDS WITH NICOTINIC CHOLINERGIC RECEPTOR ACTIVITY
    8.
    发明公开
    AZASPIROALKENE AND AZAPIROALKANE COMPOUNDS WITH NICOTINIC CHOLINERGIC RECEPTOR ACTIVITY 审中-公开
    AZASPIROALKEN-和AZASPIROALKANVERBINDUNGEN作用于烟碱型乙酰胆碱受体

    公开(公告)号：EP1802601A1

    公开(公告)日：2007-07-04

    申请号：EP05798620.0

    申请日：2005-09-19

    申请人： Targacept, Inc.

    发明人： BHATTI, Balwinder, Singh ,  BREINING, Scott, R. ,  HAMMOND, Philip, S. ,  KLUCIK, Jozef ,  XIAO, Yun-De

    IPC分类号： C07D401/04 ,  A61K31/438 ,  A61P25/04

    CPC分类号： C07D413/04 ,  C07D401/04

    摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are N-aryl or heteroaryl azaspiroalkene/alkane compounds, prodrugs or metabolites of these compounds, or pharmaceutically acceptable salts thereof. The aryl group can be a phenyl ring or 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 cholinergic 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 gastro-intestinal tract, and significant effects upon skeletal muscle).