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    Sub-type selective amides of diazabicycloalkanes
    2.
    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）。

    HETEROCYCLIC-CARBONYL-DIAZABICYCLOALKANES AS MODULATORS OF THE NEURONAL NICOTINIC ACETYLCHOLINE ALPHA 4 BETA 2, SUBTYPE RECEPTOR FOR THE TREATMENT OF CNS RELATED DISORDERS
    4.
    发明申请
    HETEROCYCLIC-CARBONYL-DIAZABICYCLOALKANES AS MODULATORS OF THE NEURONAL NICOTINIC ACETYLCHOLINE ALPHA 4 BETA 2, SUBTYPE RECEPTOR FOR THE TREATMENT OF CNS RELATED DISORDERS 审中-公开
    作为神经细胞性乙酰胆碱酯酶4β2的调节剂的杂环碳二亚氨基二醇，用于治疗CNS相关疾病的亚型受体

    公开(公告)号：US20100144700A1

    公开(公告)日：2010-06-10

    申请号：US12530997

    申请日：2008-03-12

    申请人： Philip S. Hammond ,  Anatoly A. Mazurov ,  Lan Miao ,  Yun-De Xiao ,  Balwinder Singh Bhatti ,  Jon-Paul Strachan ,  V. Srinivasa Murthy ,  David C. Kombo ,  Srinivisa Rao Akireddy

    发明人： Philip S. Hammond ,  Anatoly A. Mazurov ,  Lan Miao ,  Yun-De Xiao ,  Balwinder Singh Bhatti ,  Jon-Paul Strachan ,  V. Srinivasa Murthy ,  David C. Kombo ,  Srinivisa Rao Akireddy

    IPC分类号： A61K31/439 ,  C07D471/08 ,  C07D487/04 ,  C07D471/04 ,  A61K31/407 ,  A61K31/422 ,  A61K31/437 ,  A61K31/4353 ,  A61P25/00 ,  A61P25/28 ,  A61P25/18

    CPC分类号： C07D487/04 ,  C07D471/04 ,  C07D471/08

    摘要： A compound of Formula 1: A-C(O)-Cy, wherein A is a diazabicyclic core, containing 7, 8, or 9 ring atoms, and selected from the following: 2,6-diazabicyclo[3.2.0]heptane; 3,6-diazabicyclo[3.ZO]heptane; 2,7-diazabicyclo[4.2.0]octane; 3,7-diazabicyclo[4.2.0]octane; 3,8-diazabicyclo[4.2.0]octane; 2,7-diazabicyclo[3.3.0]octane; 2,7-diazbicyclo[4.3.0]nonane; 2,8-diazbicyclo[4.3.0]nonane; 3,7-diazabicyclo[4.3.0]nonane; 3,8-diazabicyclo[4.3.0]nonane; 3,9-diazabicyclo[4.3.0]nonane; 2,6-diazabicyclo[3.2.1]octane; 3,6-diazabicyclo[3.2.1]octane; wherein the diazabicycle is attached as a radical to the depicted carbonyl via either one of the two ring nitrogen atoms, such that the carbonyl forms an amide bond with the ring nitrogen; Cy is a heteroaryl group; The compounds exhibit selectivity for, and bind with high affinity to, neuronal nicotinic receptors of the α402 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 are believed to: (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, namely 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： 式1的化合物：A-C（O）-Cy，其中A是具有7,8或9个环原子的二氮杂双环核心，并且选自以下：2,6-二氮杂双环[3.2.0]庚烷; 3,6-二氮杂双环[3.ZO]庚烷; 2,7-二氮杂双环[4.2.0]辛烷; 3,7-二氮杂双环[4.2.0]辛烷; 3,8-二氮杂双环[4.2.0]辛烷; 2,7-二氮杂双环[3.3.0]辛烷; 2,7-二氮杂双环[4.3.0]壬烷; 2,8-二氮杂双环[4.3.0]壬烷; 3,7-二氮杂双环[4.3.0]壬烷; 3,8-二氮杂双环[4.3.0]壬烷; 3,9-二氮杂双环[4.3.0]壬烷; 2,6-二氮杂双环[3.2.1]辛烷; 3,6-二氮杂双环[3.2.1]辛烷; 其中所述二氮杂双环通过两个环氮原子中的任一个连接到所描绘的羰基上，使得羰基与环氮形成酰胺键; Cy是杂芳基; 该化合物对中枢神经系统（CNS）中α402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。 这些化合物被认为是：（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 影响如血压和心率显着升高，对胃肠道的显着负面影响，以及对骨骼肌的显着影响。

    Pharmaceutical Compositions and Methods for Relieving Pain and Treating Central Nervous System Disorders
    7.
    发明申请
    Pharmaceutical Compositions and Methods for Relieving Pain and Treating Central Nervous System Disorders 审中-公开
    减轻疼痛和治疗中枢性神经系统疾病的药物组合物和方法

    公开(公告)号：US20080242693A1

    公开(公告)日：2008-10-02

    申请号：US12123530

    申请日：2008-05-20

    申请人： Scott R. Breining ,  Balwinder S. Bhatti ,  Gregory D. Hawkins ,  Lan Miao ,  Anatoly Mazurov ,  Craig H. Miller

    发明人： Scott R. Breining ,  Balwinder S. Bhatti ,  Gregory D. Hawkins ,  Lan Miao ,  Anatoly Mazurov ,  Craig H. Miller

    IPC分类号： A61K31/439 ,  A61P25/30

    CPC分类号： C07D221/22 ,  C07D401/04

    摘要： Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas 1 or 2, as described herein. The compounds of Formulas 1 and 2 are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.

    摘要翻译： 特征在于正常神经递质释放（如多巴胺释放（如帕金森综合征，帕金森氏病，图雷特氏综合征，注意缺陷障碍或精神分裂症））改变的中枢神经系统疾病易患或患有疾病的患者是 通过施用如本文所述的式1或2的化合物进行治疗。 式1和式2化合物也可用于治疗疼痛，治疗药物成瘾，尼古丁成瘾和/或肥胖症。 该化合物可作为单独的立体异构体，外消旋混合物，非对映异构体等存在。