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    Nicotinic acetylcholine receptor sub-type selective amides of diazabicycloalkanes
    1.
    发明授权
    Nicotinic acetylcholine receptor sub-type selective amides of diazabicycloalkanes 有权
    烟碱乙酰胆碱受体亚型二氮杂双环烷烃选择性酰胺

    公开(公告)号：US08859609B2

    公开(公告)日：2014-10-14

    申请号：US13342635

    申请日：2012-01-03

    申请人： Anatoly Mazurov ,  Lan Miao ,  Yunde Xiao

    发明人： Anatoly Mazurov ,  Lan Miao ,  Yunde Xiao

    IPC分类号： A61K31/40 ,  C07D471/08 ,  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 heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 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).

    摘要翻译： 公开了化合物，包括该化合物的药物组合物，及其制备和使用方法。 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α4和bgr2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）改变患者脑部烟碱性胆碱能受体的数量，（ii）显示出神经保护作用，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）。

    Sub-type selective amides of diazabicycloalkanes
    4.
    发明授权
    Sub-type selective amides of diazabicycloalkanes 失效
    二氮杂双环烷烃的亚型选择性酰胺

    公开(公告)号：US08268860B2

    公开(公告)日：2012-09-18

    申请号：US12723790

    申请日：2010-03-15

    申请人： Anatoly A. Mazurov ,  Lan Miao ,  Yun-De Xiao ,  Philip S. Hammond ,  Craig H. Miller ,  Srinivisa Rao Akireddy ,  V. Srinivasa Murthy ,  Regina C. Whitaker ,  Scott R. Breining ,  Matt S. Melvin

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

    IPC分类号： A61K43/42 ,  A01N31/44

    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 heteroaryl carboxylic acids and certain diazabicycloalkanes. The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α4β2 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).

    摘要翻译： 公开了化合物，包括该化合物的药物组合物，及其制备和使用方法。 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α4和bgr2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）改变患者脑部烟碱性胆碱能受体的数量，（ii）显示神经保护作用，和（iii）当以有效量使用时，不会产生明显的副作用（例如副作用 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）。

    3-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof
    6.
    发明授权
    3-substituted-2(arylalkyl)-1-azabicycloalkanes and methods of use thereof 有权

    公开(公告)号：US08143272B2

    公开(公告)日：2012-03-27

    申请号：US12636269

    申请日：2009-12-11

    申请人： Anatoly A. Mazurov ,  Lan Miao

    发明人： Anatoly A. Mazurov ,  Lan Miao

    IPC分类号： A01N43/90 ,  A61K31/519

    CPC分类号： C07D471/08 ,  A61K51/0455 ,  C07D453/02 ,  C07D487/08

    摘要： The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the α7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission. Methods for preventing or treating conditions and disorders, including central nervous system (CNS) disorders, which are characterized by an alteration in normal neurotransmission, are also disclosed. Also disclosed are methods for treating inflammation, autoimmune disorders, pain and excess neovascularization, such as that associated with tumor growth.

    N-aryl diazaspirocyclic compounds and methods of preparation and use thereof
    10.
    发明授权
    N-aryl diazaspirocyclic compounds and methods of preparation and use thereof 失效
    N-芳基二氮杂环辛烷化合物及其制备方法及用途

    公开(公告)号：US07923559B2

    公开(公告)日：2011-04-12

    申请号：US12042778

    申请日：2008-03-05

    申请人： Balwinder S. Bhatti ,  Craig Harrison Miller ,  Jeffrey Daniel Schmitt

    发明人： Balwinder S. Bhatti ,  Craig Harrison Miller ,  Jeffrey Daniel Schmitt

    IPC分类号： C07D211/02 ,  A61K31/44

    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-aryl diazaspirocyclic 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 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).

    摘要翻译： 公开了化合物，包括该化合物的药物组合物，及其制备和使用方法。 化合物是N-芳基二氮杂螺环化合物，N-杂芳基二氮杂螺环化合物的桥连类似物，或这些化合物的前药或代谢物。 芳基可以是五元或六元杂环（杂芳基）。 化合物和组合物可用于治疗和/或预防各种各样的病症或病症，特别是以烟碱型胆碱能神经传递功能障碍为特征的疾病，包括涉及神经递质释放神经调节的疾病，如多巴胺释放。 其特征在于正常神经递质释放的改变的CNS疾病是可以治疗和/或预防的疾病的另一个例子。 化合物和组合物也可用于缓解疼痛。 化合物可以：（i）改变患者脑部烟碱性胆碱能受体的数量，（ii）表现出神经保护作用，和（iii）当以有效量使用时，不会产生明显的不利副作用（例如副作用 因为血压和心率的显着增加，对胃肠道的显着的负面影响以及对骨骼肌的显着影响）。