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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）。

    Use of anhydrovinblastine
    3.
    发明授权
    Use of anhydrovinblastine 失效
    使用脱氢长春花碱

    公开(公告)号：US6011041A

    公开(公告)日：2000-01-04

    申请号：US690195

    申请日：1996-07-26

    申请人： Bruce Schmidt ,  James Kutney ,  Lawrence Mayer

    发明人： Bruce Schmidt ,  James Kutney ,  Lawrence Mayer

    IPC分类号： C07D519/04 ,  A61K31/33 ,  A61K31/485 ,  A61K43/42

    CPC分类号： C07D519/04 ,  Y10S514/908

    摘要： The present invention is particularly directed to the use of a derivative of vinblastine, 3',4'-anhydrovinblastine (AHVB), which differs from vinblastine in that it possesses a double bond at the 3',4' position of the caranthine nucleus rather than the hydroxyl group that is present in the parent structure, as an antineoplastic agent in the therapeutic treatment of cancer. Specifically, the treatment of lymphoma with 3',4'-anhydrovinblastine is disclosed.

    摘要翻译： 本发明特别涉及长春碱，3'，4'-脱氢长春碱（AHVB）的衍生物，其与长春花碱不同，因为它在黄嘌呤核的3'，4'位具有双键，而不是 比在母体结构中存在的羟基作为癌症治疗性治疗中的抗肿瘤剂。 具体地，公开了用3'，4'-脱氢长春花碱治疗淋巴瘤。