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1317 条记录 (耗时 0.019 秒)

    1-[(2'-SUBSTITUTED)-PIPERAZIN-1'-YL]-ISOQUINOLINES AS NOREPINEPHRINE TRANSPORTER INHIBITOR THERAPEUTICS AND POSITRON EMISSION TOMOGRAPHY IMAGING AGENTS
    92.
    发明申请
    1-[(2'-SUBSTITUTED)-PIPERAZIN-1'-YL]-ISOQUINOLINES AS NOREPINEPHRINE TRANSPORTER INHIBITOR THERAPEUTICS AND POSITRON EMISSION TOMOGRAPHY IMAGING AGENTS 审中-公开
    1 - [（2'-取代的） - 哌嗪-1'-基] - 异喹啉作为肾上腺素转运蛋白抑制剂治疗剂和排泄物成像成像剂

    公开(公告)号：WO2008115593A1

    公开(公告)日：2008-09-25

    申请号：PCT/US2008/003792

    申请日：2008-03-21

    申请人： THE UNIVERSITY OF MONTANA ,  GERDES, John, M. ,  BOLSTAD, David, B. ,  BRADEN, Michael, R. ,  BARANY, August, W.

    发明人： GERDES, John, M. ,  BOLSTAD, David, B. ,  BRADEN, Michael, R. ,  BARANY, August, W.

    IPC分类号： A61K31/496 ,  C07D401/04 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30

    CPC分类号： C07D401/04

    摘要： Racemic mixtures and enantiomerically pure forms of novel 1-[(2'- substituted)-piperazin-1'-yl]-isoquinolines are norepinephrine (NE) transporter (NET) inhibitor compounds. Compounds of the invention are considered therapeutic agents for central nervous system (CNS) diseases and disorders, without limitation, including neurodegeneration, anxiety, depression, attention deficit disorders, drug dependency, and post traumatic stress disorder. Examples of the chemical syntheses of the compounds of the invention are provided. The isoquinoline compounds of the invention competitively bind at NET at nanomolar concentrations. The isoquinoline agents of the invention bind selectively to NET over other competitive transporter targets and receptor binding sites, including those of serotonin and dopamine, amongst others. The chemical syntheses of the invention are suitable for labeling with radionuclide atoms. Radiolabeled forms of the novel 1-[(2'-substituted)-piperazin-1'- yl]-isoquinoline comoundss are positron emission tomography and single photon emission tomography imaging tracers. Methods of in vivo imaging with the tracers within various subjects and tissues therein, including regions of the brain, are provided. Imaging methods with the tracers in combination other NET inhibitor agents are provided. The imaging methods within subjects allow quantitative detection of NET, determinations of NET distributions, and measures of tracer interactions at NET in the presence or absence of non-radioactive NET agents. The tracer imaging methods are suitable to locate, diagnose, identify, evaluate, detect or quantitate NET, or abnormalities of NET, or NE abnormalities; that are associated with various CNS diseases and disorders.

    摘要翻译： 外消旋混合物和对映体纯形式的新的1 - [（2'-取代的） - 哌嗪-1'-基] - 异喹啉是去甲肾上腺素（NE）转运蛋白（NET）抑制剂化合物。 本发明的化合物被认为是中枢神经系统（CNS）疾病和病症的治疗剂，但不限于，包括神经变性，焦虑，抑郁，注意力缺陷障碍，药物依赖性和创伤后应激障碍。 提供了本发明化合物的化学合成的实例。 本发明的异喹啉化合物在NET下以纳摩尔浓度竞争结合。 本发明的异喹啉试剂与其它竞争性转运靶标和受体结合位点选择性结合，包括血清素和多巴胺等。 本发明的化学合成适用于用放射性核素原子标记。 新颖的1 - [（2'-取代的） - 哌嗪-1'-基] - 异喹啉的放射标记形式是正电子发射断层扫描和单光子发射层析成像示踪剂。 提供了使用包括脑区域在内的各种受试者和组织内的示踪剂进行体内成像的方法。 提供与其他NET抑制剂组合的示踪剂的成像方法。 受试者中的成像方法允许NET的定量检测，NET分布的确定，以及在存在或不存在非放射性NET剂的情况下NET的示踪剂相互作用的测量。 示踪成像方法适用于定位，诊断，识别，评估，检测或定量NET，或NET异常或NE异常; 这与各种CNS疾病和疾病有关。

    COMPOUNDS WITH A COMBINATION OF CANNABINOID-CB1 ANTAGONISM AND ACETYLCHOLINESTERASE INHIBITION
    93.
    发明申请
    COMPOUNDS WITH A COMBINATION OF CANNABINOID-CB1 ANTAGONISM AND ACETYLCHOLINESTERASE INHIBITION 审中-公开
    具有CANNABINOID-CB1拮抗剂和乙酰胆碱酯酶抑制剂的组合的化合物

    公开(公告)号：WO2008074816A1

    公开(公告)日：2008-06-26

    申请号：PCT/EP2007/064169

    申请日：2007-12-19

    申请人： SOLVAY PHARMACEUTICALS B.V. ,  LANGE, Josephus H.M. ,  KRUSE, Cornelis G. ,  SHADID, Belal

    发明人： LANGE, Josephus H.M. ,  KRUSE, Cornelis G. ,  SHADID, Belal

    IPC分类号： C07D401/12 ,  A61K31/473 ,  A61P25/28 ,  A61P25/30 ,  A61P25/24

    CPC分类号： C07D401/12

    摘要： Thisinvention concerns compounds with a combination of cannabinoid-CB 1 antagonism and cholinesterase inhibition, to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly for treating Alzheimer's disease, cognitive disorders, memory disorders, dementia, attention deficits, traumatic brain injury, drug dependence, addiction and substance abuse. In particular the invention relates to compounds of the general Formula (1) wherein the symbols have the meanings given in the specification.

    摘要翻译： 本发明涉及具有大麻素-CB 1拮抗剂和胆碱酯酶抑制的组合的化合物，含有这些化合物的药物组合物，制备该化合物的方法，制备用于其合成的新中间体的方法和 制备组合物。 本发明还涉及这些化合物和组合物，特别是用于治疗阿尔茨海默病，认知障碍，记忆障碍，痴呆，注意力缺陷，创伤性脑损伤，药物依赖，成瘾和药物滥用的用途。 具体而言，本发明涉及通式（1）的化合物，其中符号具有说明书中给出的含义。

    HETEROCYCLIC FXR BINDING COMPOUNDS
    98.
    发明申请
    HETEROCYCLIC FXR BINDING COMPOUNDS 审中-公开
    杂环FXR结合化合物

    公开(公告)号：WO2008025539A1

    公开(公告)日：2008-03-06

    申请号：PCT/EP2007/007556

    申请日：2007-08-29

    申请人： PHENEX PHARMACEUTICALS AG ,  KREMOSER, Claus ,  DEUSCHLE, Ulrich ,  ABEL, Ulrich ,  SCHULZ, Andreas

    发明人： KREMOSER, Claus ,  DEUSCHLE, Ulrich ,  ABEL, Ulrich ,  SCHULZ, Andreas

    IPC分类号： C07D413/12 ,  A61K31/4155 ,  A61P3/10 ,  A61P29/00 ,  A61P25/30

    CPC分类号： C07D413/12

    摘要： The present invention relates to compounds of formula (I) which bind to the NRl H4 receptor (FXR) and act as agonists or partial agonists of the NRl H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds, and an enantiomer, diasterecmer, tautomer, solvate or pharmaceutically acceptable salt thereof, wherein X is (a) or (b) or (c) or (d), and the rest of the variables are as specified in claim 1.

    摘要翻译： 本发明涉及结合NR1H4受体（FXR）并作为NR1H4受体（FXR）的激动剂或部分激动剂的式（I）化合物。 本发明还涉及该化合物在制备用于通过所述化合物与所述核受体结合而治疗疾病和/或病症的药物的用途，以及用于合成所述化合物的方法，以及对映体， 非对映体，互变异构体，溶剂合物或其药学上可接受的盐，其中X为（a）或（b）或（c）或（d），其余变量如权利要求1所述。

    METHODS AND COMPOSITIONS FOR THE TREATMENT OF BRAIN REWARD SYSTEM DISORDERS BY COMBINATION THERAPY
    100.
    发明申请
    METHODS AND COMPOSITIONS FOR THE TREATMENT OF BRAIN REWARD SYSTEM DISORDERS BY COMBINATION THERAPY 审中-公开
    通过组合治疗治疗脑卒中系统疾病的方法和组合

    公开(公告)号：WO2007056300A3

    公开(公告)日：2008-01-17

    申请号：PCT/US2006043221

    申请日：2006-11-03

    申请人： ALKERMES INC ,  DEAN REGINALD L III ,  DEAVER DANIEL ,  EHRICH ELLIOT

    发明人： DEAN REGINALD L III ,  DEAVER DANIEL ,  EHRICH ELLIOT

    IPC分类号： A61K31/485 ,  A61K31/13 ,  A61K31/197 ,  A61K31/416 ,  A61K31/496 ,  A61P25/30 ,  A61P25/32 ,  A61P25/36

    CPC分类号： A61K45/06 ,  A61K31/4745 ,  A61K31/485 ,  A61K2300/00

    摘要： The present invention is directed to a combination treatment of an opioid antagonist e.g., naltrexone and a second compound selected from the group consisting of a GABA B agonist, an NMDA antagonist, a serotonin antagonist, and a cannabinoid antagonist is the key to the successful treatment of a brain reward system disorder. A brain reward system, include but are not limited, to pathological gambling, compulsive alcohol consumption, compulsive over-eating and obesity, compulsive smoking, and drug addiction. The compounds and methods of the present invention effectively reduce the cravings, withdrawal symptoms and negative drug side effects associated with a monotherapy. As such, patient compliance is greatly increased, thereby decreasing relapse of a brain reward system disorder.

    摘要翻译： 本发明涉及阿片样物质拮抗剂的组合治疗，例如纳曲酮和选自GABA B激动剂，NMDA拮抗剂，5-羟色胺拮抗剂和大麻素拮抗剂的第二化合物是成功治疗的关键 的脑回报系统障碍。 大脑奖励制度包括但不限于病理赌博，强迫性酒精消费，强迫性过度饮食和肥胖，强迫性吸烟和吸毒成瘾。 本发明的化合物和方法有效地减少与单一疗法相关的渴望，戒断症状和药物副作用。 因此，患者顺应性大大增加，从而减少脑回报系统障碍的复发。