Tripeptide derivatives with central nervous system activity and
preparation thereof
    1.
    发明授权
    Tripeptide derivatives with central nervous system activity and preparation thereof 失效
    具有中枢神经系统活性的三肽衍生物及其制备方法

    公开(公告)号:US4018912A

    公开(公告)日:1977-04-19

    申请号:US599450

    申请日:1975-07-28

    CPC分类号: C07K5/0823 Y02P20/55

    摘要: The tripeptide derivatives of formula 1H--L--Pro--N(R.sup.1)CH(R.sup.2)CO--Y--R.sup.3 (1)in which R.sup.1 is hydrogen, lower alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each are lower alkyl, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is amino, lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino and Y is one of the amino acid residues Gly or D-Ala with the proviso that when R.sup.1 is NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are as defined herein and R.sup.2 and Y are as defined herein, R.sup.3 is lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino, and a method for their preparation are disclosed. The tripeptide derivatives of formula 1 possess central nervous system activity and methods for their use are given.

    摘要翻译: 式1的HL-Pro-N(R1)CH(R2)CO-Y-R3(1)的三肽衍生物,其中R 1是氢,低级烷基或NR 4 R 5,其中R 4和R 5各自是低级烷基,R 2是氢或更低 烷基,R3是氨基,低级烷基氨基,二(低级)烷基氨基或氨基(低级)烷基氨基,Y是氨基酸残基Gly或D-Ala之一,条件是当R 1是NR 4 R 5时,其中R 4和R 5如本文所定义 并且R 2和Y如本文所定义,R 3是低级烷基氨基,二(低级)烷基氨基或氨基(低级)烷基氨基,并且公开了其制备方法。 式1的三肽衍生物具有中枢神经系统活性,并给出了其使用方法。

    Method and apparatus for the generation of voltage pulses
    2.
    发明授权
    Method and apparatus for the generation of voltage pulses 失效
    用于产生电压脉冲的方法和装置

    公开(公告)号:US4939443A

    公开(公告)日:1990-07-03

    申请号:US295633

    申请日:1989-01-10

    IPC分类号: H02M1/08 H02M3/155 H03K4/06

    CPC分类号: H02M1/08 H03K4/06

    摘要: The present invention relates to a method and apparatus for the generation of voltage pulses for controlling the switching operation in switching power supplies. A voltage increase of a pulse generator is respectively started when reaching a first, lower threshold (A). Resetting of the voltage increase is carried out in free-running mode, when the voltage increase reaches a second (D) or a third (C) threshold lying between the first (A) and the second (D) one. In sync mode, the pulse edges occurring in the synchronization signal (V.sub.sync) effect resetting of the voltage increase. The advantages of the invention lie in the fact that the switching current, occurring at the change form free-running mode to sync mode due to the frequency difference, is minimized and that the generator operates reliably.

    摘要翻译: 本发明涉及一种用于产生用于控制开关电源中的开关操作的电压脉冲的方法和装置。 当达到第一,下阈值(A)时,分别开始脉冲发生器的电压增加。 当电压增加达到第一(A)和第二(D)之间的第二(D)或第三(C)阈值时,在自由运行模式下进行升压的复位。 在同步模式下,同步信号(Vsync)中出现的脉冲边沿会影响电压升高的复位。 本发明的优点在于,由于频率差异而以自由运行模式转变为同步模式而发生的开关电流被最小化,并且发电机可靠地运行。

    Derivatives of imidazolidin-2-ones and -2-thiones
    3.
    发明授权
    Derivatives of imidazolidin-2-ones and -2-thiones 失效
    咪唑烷-2-酮衍生物和2,3-噻二唑的衍生物

    公开(公告)号:US3979380A

    公开(公告)日:1976-09-07

    申请号:US585019

    申请日:1975-06-09

    CPC分类号: C07D235/02

    摘要: There are disclosed herein derivatives of imidazolidin-2-ones and -2-thiones of the formula I ##SPC1##and their acid addition salts with pharmacologically acceptable acids, in which R.sup.1 is hydrogen or lower alkyl; R.sup.2 is lower alkyl, nitrothiazolyl, or nitrofuryl; or R.sup.1 and R.sup.2 together with the nitrogen to which they are attached are a heterocyclic group containing 4-6 carbon atoms, or 4 carbon atoms and an additional nitrogen atom which may optionally be substituted with a lower alkyl group, or 4 carbon atoms and an oxygen atom, R.sup.3 is hydrogen or lower alkyl; R.sup.4 is lower alkyl or aralkyl, or R.sup.3 and R.sup.4 together with the carbon atom 5 of the imidazolidine ring to which they are attached are a carbocyclic ring containing 5-6 carbon atoms attached in spiro fashion to said imidazolidine ring; R.sup.5 is lower alkyl or cycloalkyl containing from 5-6 carbon atoms; and X is an oxygen or a sulfur atom. The compounds of this invention possess positive inotropic activity and are useful as cardiac stimulants.

    摘要翻译: 本文公开了式I的咪唑烷-2-酮和2-硫杂的衍生物及其与药理学上可接受的酸的酸加成盐,其中R 1是氢或低级烷基; R2是低级烷基,硝基噻唑基或硝基呋喃基; 或R 1和R 2与它们所连接的氮一起是含有4-6个碳原子或4个碳原子的杂环基,以及另外的氮原子,其可任选被低级烷基或4个碳原子和 氧原子,R3是氢或低级烷基; R 4是低级烷基或芳烷基,或者R 3和R 4与它们所连接的咪唑烷环的碳原子5一起是含5-6个碳原子的碳环,所述碳环与所述咪唑烷环螺旋连接; R5是含有5-6个碳原子的低级烷基或环烷基; X是氧或硫原子。 本发明的化合物具有正性肌力活性,可用作心脏兴奋剂。