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    Methods for treating depression and other CNS disorders using enantiomerically enriched desmethyl-and didesmethyl-metabolites of citalopram
    1.
    发明申请
    Methods for treating depression and other CNS disorders using enantiomerically enriched desmethyl-and didesmethyl-metabolites of citalopram 审中-公开
    使用西酞普兰的对映体富集的脱甲基和二甲基 - 代谢物治疗抑郁症和其他CNS障碍的方法

    公开(公告)号：US20040266864A1

    公开(公告)日：2004-12-30

    申请号：US10842055

    申请日：2004-05-07

    Applicant: Sepracor Inc.

    Inventor： Larry R. Bush ,  Mark G. Currie ,  Q. Kevin Fang ,  Chris H. Senanayake

    IPC: C07D307/78 ,  A61K031/343

    CPC classification number: C07D307/87 ,  C07D317/20

    Abstract: This invention relates to novel compositions of matter containing enantiomerically enriched (null)-desmethylcitalopram, (null)-didesmethylcitalopram, or (null)-didesmethylcitalopram or mixtures thereof in optimal ratios. Contrary to prior teachings, the enantiomerically enriched citalopram metabolites disclosed herein possess potent serotonin reuptake inhibitory activity, with minimal inhibitory effects on the reuptake of other known monoamines, e.g., norepinephrine (NE) or dopamine (DA). The present invention also discloses methods for treating disorders, dysfunctions and diseases for which inhibition of serotonin reuptake is therapeutically beneficial. In particular, the present invention discloses a method for treating various forms of depression with pharmaceutical compositions described herein.

    Abstract translation: 本发明涉及以最佳比例含有对映体富集（ - ） - 去甲基西酞普兰，（+） - 二甲基西酞普兰或（ - ） - 二甲基西酞普兰或其混合物的物质的新型组合物。 与现有技术相反，本文公开的对映异构体富集的西酞普兰代谢物具有有效的5-羟色胺再摄取抑制活性，对其他已知的单胺例如去甲肾上腺素（NE）或多巴胺（DA）的再摄取具有最小的抑制作用。 本发明还公开了治疗疾病，功能障碍和5-羟色胺再摄取抑制治疗有益的疾病的方法。 特别地，本发明公开了一种用本文所述的药物组合物治疗各种形式的抑郁症的方法。

    Treatment of CNS disorders with trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine and its formamide
    3.
    发明申请
    Treatment of CNS disorders with trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine and its formamide 有权
    用反式4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺及其甲酰胺处理CNS病症

    公开(公告)号：US20040092605A1

    公开(公告)日：2004-05-13

    申请号：US10663173

    申请日：2003-09-16

    Applicant: Sepracor, Inc.

    Inventor： Thomas P. Jerussi ,  Qun Kevin Fang ,  Mark G. Currie

    IPC: A61K031/135 ,  C07C211/42

    CPC classification number: C07C211/42 ,  C07B2200/07 ,  C07C2602/10 ,  C07C2602/28

    Abstract: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-null4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-ylnullformamide, which are also useful.

    Abstract translation: 用（1R，4S） - 反式-4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺处理CNS病症; 和（1S，4R） - 反式-4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺。 还公开了制备4-（3,4-二氯苯基）-1,2,3,4-四氢-1-萘胺的方法。 该方法包括制备N- [4-（3,4-二氯苯基）-1,2,3,4-四氢萘-1-基]甲酰胺的全部四种异构体，它们也是有用的。

    D-amino acid oxidase inhibitors for learning and memory
    5.
    发明申请
    D-amino acid oxidase inhibitors for learning and memory 审中-公开
    用于学习和记忆的D-氨基酸氧化酶抑制剂

    公开(公告)号：US20030162825A1

    公开(公告)日：2003-08-28

    申请号：US10292368

    申请日：2002-11-12

    Applicant: SEPRACOR INC.

    Inventor： Donald L. Heefner ,  Mark G. Currie ,  Richard Filip Rossi JR. ,  Charles M. Zepp

    IPC: A61K031/473 ,  A61K031/404 ,  A61K031/401 ,  A61K031/34

    CPC classification number: A61K31/34 ,  A61K31/401 ,  A61K31/404 ,  A61K31/405 ,  A61K31/473

    Abstract: Methods and pharmaceutical compositions which inhibit the activity of D-amino acid oxidase (DAO) are disclosed. Inhibition of DAO improves memory, learning and cognition in individuals suffering from neurodegenerative diseases such as Alzheimer's, Huntington's or Parkinson's diseases; the methods and pharmaceutical compositions which inhibit the activity of DAO also improve cognitive dysfunctions associated with aging and improve catatonic schizophrenia. Several genera of heterocycle-2-carboxylic acids are disclosed as DAO inhibitors.

    Abstract translation: 公开了抑制D-氨基酸氧化酶（DAO）活性的方法和药物组合物。 抑制DAO改善患有阿尔茨海默病，亨廷顿病或帕金森病等神经退行性疾病的个体的记忆，学习和认知; 抑制DAO活性的方法和药物组合物也改善与老化相关的认知功能障碍并改善紧张型精神分裂症。 公开了几种杂环-2-羧酸作为DAO抑制剂。

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