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29 条记录 (耗时 0.031 秒)

    Pyridone-fused azabicyclic- or cytisine derivatives, their preparation and their use in addiction therapy
    1.
    发明授权
    Pyridone-fused azabicyclic- or cytisine derivatives, their preparation and their use in addiction therapy 失效
    吡啶酮稠合的氮杂双环或星果苷衍生物，其制备及其在成瘾治疗中的应用

    公开(公告)号：US06630467B2

    公开(公告)日：2003-10-07

    申请号：US09783443

    申请日：2001-02-14

    申请人： Brian T. O'Neill

    发明人： Brian T. O'Neill

    IPC分类号： A61K314375

    CPC分类号： C07D471/18

    摘要： Pyridone-fused azabicyclic compounds of the formula and their pharmaceutically acceptable salts and prodrugs, wherein R1, R2 and R3 are defined below, intermediates and methods for their preparation. Compositions and methods for using compounds of the formula I in the treatment of neurological and mental disorders related to a decrease in cholinergic function such as nicotine addiction, Huntington's Chorea, tardive dyskinesia, hyperkinesia, mania, dyslexia, schizophrenia, analgesia, attention deficit disorder (ADD), multi-infarct demetia, age related cognitive decline, epilepsy, neurological and mental disorders related to a decrease in cholinergic function, senile dementia of the Alzheimer's type, Parkinson's disease, attention deficit hyperactivity disorder (ADHD), anxiety, obesity, Tourette's Syndrome and ulcerative colitis.

    摘要翻译： 具有下式定义的吡啶酮稠合的氮杂双环化合物及其药学上可接受的盐和前药，其中R 1，R 2和R 3定义如下，其中间体及其制备方法。 使用式I化合物的组合物和方法用于治疗与胆碱能功能降低相关的神经和精神障碍，例如尼古丁成瘾，亨廷顿氏舞蹈病，迟发性运动障碍，运动迟缓，躁狂症，阅读障碍，精神分裂症，镇痛，注意力缺陷障碍（ ADD），多发性脑梗塞，与年龄相关的认知衰退，癫痫，与胆碱能功能下降有关的神经和精神障碍，阿尔茨海默氏型老年痴呆，帕金森病，注意力缺陷多动障碍（ADHD），焦虑，肥胖，Tourette's 综合征和溃疡性结肠炎。

    Process for the preparation of meso 2,5-dihaloadipates
    6.
    发明授权
    Process for the preparation of meso 2,5-dihaloadipates 失效
    内消旋2,5-二卤代己酸酯的制备方法

    公开(公告)号：US4736059A

    公开(公告)日：1988-04-05

    申请号：US82703

    申请日：1987-08-07

    申请人： Brian T. O'Neill ,  Harry A. Watson, Jr.

    发明人： Brian T. O'Neill ,  Harry A. Watson, Jr.

    IPC分类号： C07C67/52 ,  C07C67/14 ,  C07C69/44

    CPC分类号： C07C67/14

    摘要： The present process produces the meso dialkyl 2,5-dihaloadipate from a mixture of the racemic dialkyl 2,5-dihaloadipate and meso 2,5-dihaloadipate. In the disclosed process, a 2,5-dihaloadipoyl halide is formed under conditions which result in the formation of an acidic compound. The 2,5-dihaloadipoyl halide is then esterified under conditions wherein the ester of the dihaloadipoyl halide is allowed to remain in contact with the acidic compound, thus allowing the racemic diester to epimerize in the presence of the acidic compound to the meso form and then the meso diester spontaneously crystallizes. In the last stage, the meso diester produced is removed.

    Diazabicyclic compounds useful in the treatment of CNS and other disorders
    7.
    发明授权
    Diazabicyclic compounds useful in the treatment of CNS and other disorders 失效
    可用于治疗CNS和其他疾病的二氮杂双环化合物

    公开(公告)号：US07442694B2

    公开(公告)日：2008-10-28

    申请号：US10657738

    申请日：2003-09-08

    申请人： Jotham W. Coe ,  Christopher J. O'Donnell ,  Brian T. O'Neill ,  Lawrence A. Vincent

    发明人： Jotham W. Coe ,  Christopher J. O'Donnell ,  Brian T. O'Neill ,  Lawrence A. Vincent

    IPC分类号： C07D487/08 ,  A61K31/495

    CPC分类号： C07D487/08

    摘要： The present invention relates to a compounds of formula I: wherein A, B, D, E and F are defined herein; that are useful in treating central nervous system (CNS) diseases, disorders and conditions, such as but not limited to nicotine addiction, schizophrenia, depression, Alzheimer's disease, Parkinson's disease and ADHD. The present invention further comprises pharmaceutical compositions containing such compounds and methods of treatment comprising the use of such compounds.

    摘要翻译： 本发明涉及式I化合物：其中A，B，D，E和F如本文所定义; 可用于治疗中枢神经系统（CNS）疾病，疾病和病症，例如但不限于尼古丁成瘾，精神分裂症，抑郁症，阿尔茨海默病，帕金森病和ADHD。 本发明还包含含有这些化合物的药物组合物和包括使用这些化合物的治疗方法。

    Benzimidazole derivatives having dopaminergic activity
    8.
    发明授权
    Benzimidazole derivatives having dopaminergic activity 失效
    具有多巴胺能活性的苯并咪唑衍生物

    公开(公告)号：US5889010A

    公开(公告)日：1999-03-30

    申请号：US793032

    申请日：1997-01-31

    申请人： William S. Faraci ,  Anton F. J. Fliri ,  Brian T. O'Neill ,  Mark A. Sanner ,  Stevin H. Zorn

    发明人： William S. Faraci ,  Anton F. J. Fliri ,  Brian T. O'Neill ,  Mark A. Sanner ,  Stevin H. Zorn

    IPC分类号： C07D235/06 ,  C07D235/08 ,  C07D235/26 ,  A01N43/60 ,  C07D403/00

    CPC分类号： C07D235/06 ,  C07D235/08 ,  C07D235/26

    摘要： Pharmaceutically active benzimidazole derivatives are disclosed comprising compounds of the formula: ##STR1## particularly wherein X is nitrogen, R.sup.1 is phenyl or heteroaryl, and one of R.sup.2 or R.sup.3 is hydroxy. Said compounds have D4 dopaminergic receptor binding activity and consequently are useful as active ingredients in pharmaceutical compositions and methods of treatment for sleep disorders, sexual disorders, gastrointestinal disorders, psychosis, affective psychosis, nonorganic psychosis, personality disorders, psychiatric mood disorders, conduct and impulse disorders, schizophrenic and schizoaffective disorders, polydipsia, bipolar disorders, dysphoric mania, anxiety and related disorders, obesity, emesis, bacterial infections of the CNS, learning disorders, memory disorders, Parkinson's disease, depression, extrapyramidal side effects from neuroleptic agents, neuroleptic malignant syndrome, hypothalamic pituitary disorders, ocular disorders, congestive heart failure, chemical dependencies, vascular and cardiovascular disorders, dystonia, tardive dyskinesia, Gilles De La Tourette's syndrome and other hyperkinesias, dementia, ischemia, Parkinson's disease, akathesia and other movement disorders, hypertension and diseases caused by a hyperactive immune system such as allergies and inflammation in a mammal.

    摘要翻译： PCT No.PCT / IB95 / 00378 Sec。 371日期1997年1月31日 102（e）日期1997年1月31日PCT提交1995年5月18日PCT公布。 公开号WO96 / 04250 PCT 日期：1996年2月15日公开了药物活性苯并咪唑衍生物，其包括下式的化合物：其中X是氮，R 1是苯基或杂芳基，R 2或R 3之一是羟基。 所述化合物具有D4多巴胺能受体结合活性，因此可用作药物组合物和治疗睡眠障碍，性障碍，胃肠道疾病，精神病，情感性精神病，无机精神病，人格障碍，精神病情绪障碍，行为和冲动的活性成分 障碍，精神分裂症和分裂情感障碍，多饮，双相情感障碍，焦虑症和相关疾病，肥胖症，呕吐，CNS的细菌感染，学习障碍，记忆障碍，帕金森病，抑郁症，精神分裂症药物的锥体外系副作用，精神安定药物恶性 综合征，下丘脑垂体障碍，眼部疾病，充血性心力衰竭，化学依赖性，血管和心血管疾病，肌张力障碍，迟发性运动障碍，Gilles De La Tourette综合征和其他运动过度，痴呆，局部缺血，帕金森病，感染等运动 异位症，高血压和由哺乳动物过敏和炎症等过度活动的免疫系统引起的疾病。