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    Amides of diazabicycloalkanes selective for nicotinic acetylcholine receptor sub-types
    2.
    发明公开
    Amides of diazabicycloalkanes selective for nicotinic acetylcholine receptor sub-types 有权
    酰胺二氮杂双环链烷酸脱乙酰壳多糖

    公开(公告)号：EP2284171A1

    公开(公告)日：2011-02-16

    申请号：EP10075738.4

    申请日：2007-11-01

    申请人： Targacept, Inc.

    发明人： Mazurov, Anatoly ,  Miao, Lan ,  Xiao, Yun-de ,  Hammond, Philip S. ,  Miller, Craig H. ,  Akireddy, Srinivasa Rao ,  Murthy, V Srinivasa ,  Whitaker, Regina C. ,  Breining, Scott R. ,  Melvin, Matt S.

    IPC分类号： C07D471/08 ,  A61P25/00 ,  A61K31/407 ,  C07D487/04

    CPC分类号： C07D487/04 ,  C07D471/08

    摘要： Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are amide compounds which can be prepared from certain heteroraryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the a4ss2 subtype in the central nervous system (CNS). The compounds and compositions can be used to treat and/or prevent a wide variety of conditions or disorders, particularly CNS disorders. 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).
    Formula I:

    wherein n has the value of 0 or 1, and
    Cy is a heteroaryl group chosen from the group of 2-furanyl, 3-furanyl, 2-oxazolyl, 4-oxazolyl, 5-oxazolyl, 3-isoxazolyl, 4-isoxazolyl, 5-isoxazolyl, 1,3,4-oxadiazol-2-yl, 1,2,4-oxadiazol-3-yl, 1,2,4-oxadiazol-5-yl, 2-thiazolyl, 4-thiazolyl, 5-thiazolyl, 3-isothiazolyl, 4-isothiazolyl, 5-isothiazolyl, 1,3,4-thiadiazol-2-yl, 1,2,4-thiadiazol-3-yl, 1,2,4-thiadiazol-5-yl and 4-pyridinyl.

    摘要翻译： 公开了化合物，包括该化合物的药物组合物，及其制备方法和用途。 这些化合物是可以由某些杂芳基羧酸和某些二氮杂双环烷烃制备的酰胺化合物。 该化合物对中枢神经系统（CNS）中a4ss2亚型的神经元烟碱受体表现出选择性并且以高亲和力结合。 化合物和组合物可用于治疗和/或预防多种病症或病症，特别是CNS疾病。 化合物可以：（i）改变患者脑部烟碱型胆碱能受体的数量，（ii）表现出神经保护作用，和（iii）当以有效量使用时，不会产生明显的不良副作用 因为血压和心率的显着增加，对胃肠道的显着的负面影响和对骨骼肌的显着影响）。 式I：其中n具有0或1的值，Cy是选自2-呋喃基，3-呋喃基，2-恶唑基，4-恶唑基，5-恶唑基，3-异恶唑基，4-恶唑基， 异恶唑基，5-异恶唑基，1,3,4-恶二唑-2-基，1,2,4-恶二唑-3-基，1,2,4-恶二唑-5-基，2-噻唑基，4-噻唑基， 5-噻唑基，3-异噻唑基，4-异噻唑基，5-异噻唑基，1,3,4-噻二唑-2-基，1,2,4-噻二唑-3-基，1,2,4-噻二唑-5-基， 吡啶基和4-吡啶基。