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107 条记录 (耗时 0.04 秒)

    1,4-piperazine derivatives
    75.
    发明授权
    1,4-piperazine derivatives 失效
    1,4-哌嗪衍生物

    公开(公告)号：US06255302B1

    公开(公告)日：2001-07-03

    申请号：US09459793

    申请日：1999-12-13

    申请人： Michael G. Kelly ,  Yvette L. Palmer

    发明人： Michael G. Kelly ,  Yvette L. Palmer

    IPC分类号： C07D40106

    CPC分类号： C07D401/06 ,  C07D211/26 ,  C07D401/12

    摘要： Compounds of the formula are useful for the treatment of disorder of the central nervous system including anxiety, depression, panic, alcohol and drug addiction, sexual dysfunction, sleep disorders, cognitive disorders, Alzheimer's disease and Parkinson's disease.

    摘要翻译： 该化合物可用于治疗中枢神经系统疾病，包括焦虑，抑郁，恐慌，酒精和药物成瘾，性功能障碍，睡眠障碍，认知障碍，阿尔茨海默病和帕金森病。

    Diazole derivatives as serotonergic agents
    76.
    发明授权
    Diazole derivatives as serotonergic agents 失效
    二唑衍生物作为血清素能药剂

    公开(公告)号：US06239134B1

    公开(公告)日：2001-05-29

    申请号：US09515049

    申请日：2000-02-25

    申请人： Annmarie L. Sabb ,  Robert L. Vogel ,  Michael G. Kelly ,  Yvette L. Palmer ,  Wayne E. Childers

    发明人： Annmarie L. Sabb ,  Robert L. Vogel ,  Michael G. Kelly ,  Yvette L. Palmer ,  Wayne E. Childers

    IPC分类号： A61K31496

    CPC分类号： C07D285/10 ,  C07D417/12

    摘要： The present invention provides compounds of the general formula (1): wherein: two atoms of X, Y, or Z are nitrogen and the third atom is sulfur or oxygen; R is H, halogen, OH, SH, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 thioalkyl, phenoxy, thiophenoxy, phenyl or substituted phenyl; A is C, CH, or N; R1 is aryl, heteroaryl, or cycloalkyl groups, optionally substituted by from 1 to 3 substituents selected from C1-C6 alkyl, C1-C6 alkoxy; CF3, Cl, Br, F, CN, or CO2CH3; R2is H or alkyl R3 is C1-C6 alkyl, optionally substituted aryl, optionally substituted 5- or 6-membered heteroaryl, C3 to C8 cycloalkyl optionally substituted by C1-C6 alkyl, or a 3 to 8-membered heterocyclic ring containing one or more heteroatoms selected from O, S or N; or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions and methods of treating central nervous system disorders using these compounds.

    摘要翻译： 本发明提供通式（1）的化合物：其中X，Y或Z的两个原子是氮，第三个原子是硫或氧; R是H，卤素，OH，SH，C 1 -C 6烷基， C 1 -C 6烷氧基，C 1 -C 6硫代烷基，苯氧基，硫代苯氧基，苯基或取代的苯基; A是C，CH或N; R 1是芳基，杂芳基或环烷基，任选地被1至3个选自C1- C6烷基，C1-C6烷氧基; CF 3，Cl，Br，F，CN或CO 2 CH 3; R 2为H或烷基R 3为C 1 -C 6烷基，任选取代的芳基，任选取代的5或6元杂芳基，任选被C 1 -C 6烷基取代的C 3至C 8环烷基， 含有一个或多个选自O，S或N的杂原子的3至8元杂环; 或其药学上可接受的盐，以及使用这些化合物治疗中枢神经系统疾病的药物组合物和方法。

    Arylpiperidine and aryl-1,2,5,6-tetra-hydropyridine urea derivatives
    77.
    发明授权
    Arylpiperidine and aryl-1,2,5,6-tetra-hydropyridine urea derivatives 失效
    芳基哌啶和芳基-1,2,5,6-四氢吡啶脲衍生物

    公开(公告)号：US06239126B1

    公开(公告)日：2001-05-29

    申请号：US09459791

    申请日：1999-12-13

    申请人： Michael G. Kelly ,  Gan Zhang

    发明人： Michael G. Kelly ,  Gan Zhang

    IPC分类号： A01N4300

    CPC分类号： C07D211/22 ,  C07D211/70

    摘要： Compounds of the formula are useful for the treatment of disorder of the central nervous system including anxiety, depression, panic, alcohol and drug addiction, sexual dysfunction, sleep disorders, migraine, obesity, cognitive disorders and neurodegenerative diseases.

    摘要翻译： 该化合物可用于治疗中枢神经系统疾病，包括焦虑，抑郁，恐慌，酒精和药物成瘾，性功能障碍，睡眠障碍，偏头痛，肥胖症，认知障碍和神经变性疾病。

    Oxazole derivatives as serotonin-1A receptor agonists
    78.
    发明授权
    Oxazole derivatives as serotonin-1A receptor agonists 失效
    恶唑衍生物作为血清素-1A受体激动剂

    公开(公告)号：US6057340A

    公开(公告)日：2000-05-02

    申请号：US243589

    申请日：1999-02-03

    申请人： Michael G. Kelly ,  Lynne P. Greenblatt ,  Frances C. Nelson

    发明人： Michael G. Kelly ,  Lynne P. Greenblatt ,  Frances C. Nelson

    IPC分类号： C07D413/06 ,  C07D471/04 ,  A61K31/445 ,  C07D401/06

    CPC分类号： C07D413/06 ,  C07D471/04

    摘要： This invention provides compounds of Formula 1 having the structure ##STR1## wherein: R.sub.1 is hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, benzyloxy, trifluoromethyl, chloro, bromo, or fluoro;a dashed line indicates an optional bond,X is NR.sub.4, or no atom;R.sub.2 is alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, cycloalkylalkyl wherein the cycloalkyl moiety is 3-8 carbon atoms and the alkyl moiety is 1-6 carbon atoms, aryl of 5-12 carbon atoms, or arylalkyl of 6-12 carbon atoms;R.sub.3 is aryl of 5-12 carbon atoms, arylalkyl of 6-12 carbon atoms, or heteroaryl of 5-12 atoms;R.sub.4 is hydrogen or alkyl of 1-6 carbon atoms;or a pharmaceutically acceptable salt thereof, which are useful in the treatment of psychosis (e.g. schizophrenia), anxiety, depression and related CNS disorders and other conditions such as the treatment of alcohol and drug withdrawal, sexual dysfunction and memory deficits associated with Alzheimer's disease and other dementias.

    摘要翻译： 本发明提供具有以下结构的式1化合物：其中：R 1是氢，1-6个碳原子的烷基，1-6个碳原子的烷氧基，苄氧基，三氟甲基，氯，溴或氟; 虚线表示任选的键，X为NR4或无原子; R2是1-6个碳原子的烷基，3-8个碳原子的环烷基，环烷基烷基，其中环烷基部分是3-8个碳原子，烷基部分是1-6个碳原子，5-12个碳原子的芳基或芳烷基 6-12个碳原子; R3是5-12个碳原子的芳基，6-12个碳原子的芳基烷基或5-12个原子的杂芳基; R4是氢或1-6个碳原子的烷基; 其可用于治疗精神病（例如精神分裂症），焦虑症，抑郁症和相关的中枢神经系统疾病以及其他病症，例如治疗酒精和药物戒断，与阿尔茨海默病相关的性功能障碍和记忆缺陷，以及 其他痴呆症