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    Arylpiperazines having activity at the serotonin 1A receptor
    5.
    发明申请
    Arylpiperazines having activity at the serotonin 1A receptor 失效
    具有5-羟色胺1A受体活性的芳基哌嗪

    公开(公告)号：US20020169170A1

    公开(公告)日：2002-11-14

    申请号：US10022045

    申请日：2001-12-18

    发明人： Alexander Glenn Godfrey ,  Daniel Timothy Kohlman ,  John Cunningham O' Toole ,  Yao-Chang Xu ,  Tony Yantao Zhang

    IPC分类号： A61K031/495 ,  A61K031/496

    CPC分类号： C07D295/088 ,  A61K31/495 ,  A61K31/496 ,  C07C45/004 ,  C07C45/29 ,  C07C45/40 ,  C07C45/515 ,  C07C45/59 ,  C07C45/68 ,  C07C49/563 ,  C07C49/577 ,  C07C49/583 ,  C07C49/86 ,  C07D213/74 ,  C07D295/104 ,  C07D295/108

    摘要： A method for potentiating the action of a serotonin reuptake inhibitor in increasing the availability of serotonin, norepinephrin and dopamine in the brain, comprising administering to a patient in need of such treatment a serotonin reuptake inhibitor in combination with an effective amount of a compound of the formula 1 wherein Arnull is a mono or bicyclic aryl or heteroaryl radical substituted with one to three substituents selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkyl halo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R1 is hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio; R2 is phenyl, naphthyl or (C3-C12)cycloalkyl substituted with one or two substituents selected from the group consisting of hydrogen (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkyl halo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R3 is selected from the group consisting of hydrogen (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; X is null(CnullO)null, nullCHOHnull or nullCH2null; or a pharmaceutically acceptable salt, racemate, optical isomer or solvate thereof.

    摘要翻译： 一种用于增强5-羟色胺再摄取抑制剂在增加脑中5-羟色胺，去甲肾上腺素和多巴胺的可利用性的作用的方法，包括向需要这种治疗的患者施用5-羟色胺再摄取抑制剂与有效量的 其中Ar'是被一至三个选自氢，（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷硫基，（C 2 -C 6）烷基， -C 6）烯基，（C 2 -C 6）炔基，（C 1 -C 6）烷基卤，（C 3 -C 8）环烷基，（C 3 -C 8）环烯基或卤素; R1是氢，（C1-C6）烷基，（C1-C6）烷氧基，（C1-C6）烷硫基; R2是被一个或两个选自氢（C1-C6）烷基，（C1-C6）烷氧基，（C1-C6）烷硫基，（C2-C6）烷基）取代基取代的苯基，萘基或（C3-C12） ）烯基，（C 2 -C 6）炔基，（C 1 -C 6）烷基卤，（C 3 -C 8）环烷基，（C 3 -C 8）环烯基或卤素; R 3选自氢（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，（C 1 -C 6）烷硫基，（C 2 -C 6）烯基，（C 2 -C 6）炔基，（C 1 -C 6）烷基卤素 ，（C 3 -C 8）环烷基，（C 3 -C 8）环烯基或卤素; X是 - （C = O） - ， - CHOH-或-CH 2 - ; 或其药学上可接受的盐，外消旋物，旋光异构体或溶剂合物

    Process for the preparation of ketones and novel insecticides produced therefrom
    9.
    发明授权
    Process for the preparation of ketones and novel insecticides produced therefrom 失效
    用于制备由其制备的酮和新型杀虫剂的方法

    公开(公告)号：US4829091A

    公开(公告)日：1989-05-09

    申请号：US55265

    申请日：1987-05-27

    申请人： Frank D. Mills ,  Richard T. Brown ,  Giles D. Mills, Jr

    发明人： Frank D. Mills ,  Richard T. Brown ,  Giles D. Mills, Jr

    IPC分类号： A01N35/02 ,  A01N43/08 ,  C07C45/67 ,  C07C49/577 ,  C07D307/42

    CPC分类号： C07C45/676 ,  A01N35/02 ,  A01N43/08 ,  C07C49/577 ,  C07D307/42

    摘要： An improved method for the decarbalkoxylation of alkylated .beta.-keto esters to obtain high yields of ketones. In accordane with the method, decarbalkoxylation of alkylated .beta.-keto esters is accomplished by heating the esters in the presence of dilute aqueous alkali and an effective amount of a phase-transfer agent. The method produces commercially practical yields of ketone in a manner which is facile, economical and environmentally safe. Novel methylene-linked pyrethroid ketones produced from the improved method exhibit insecticidal activity against various agricultural pests.

    摘要翻译： 烷基化β-酮酯的脱烷基氧化的改进方法，以获得高产率的酮。 根据该方法，烷基化β-酮酯的脱烷基氧化通过在稀碱水溶液和有效量的相转移剂的存在下加热酯来实现。 该方法以便利，经济和环境安全的方式产生商业上实用的酮产率。 由改进的方法生产的新型亚甲基联结的拟除虫菊酯对各种农业害虫具有杀虫活性。