1,2-disubstituted ergolines useful for producing central
antidopanminergic or .alpha.2-receptor-blocking activity
    61.
    发明授权
    1,2-disubstituted ergolines useful for producing central antidopanminergic or .alpha.2-receptor-blocking activity 失效
    可用于产生中枢抗过敏能或α2受体阻断活性的1,2-二取代的麦角醇

    公开(公告)号:US4874768A

    公开(公告)日:1989-10-17

    申请号:US915358

    申请日:1986-10-06

    CPC分类号: C07D457/12

    摘要: The disclosure relates to 1,2-substituted ergoline derivatives of general Formula I ##STR1## wherein X is an oxygen or sulfur atom,R.sup.1 is a lower alkyl group,R.sup.2 is halogen, acyl, a saturated or unsaturated lower alkyl group which can optionally be substituted by OR.sup.4 wherein R.sup.4 is hydrogen, lower alkyl, tetrahydropyranyl or cycloalkyl, or by an optionally substituted aryl residue, an S-R.sup.5 -group wherein R.sup.5 means a lower alkyl group which can optionally be substituted by aryl or an optionally substituted aryl residue, a ##STR2## wherein n=2 o4 3, or a --CHO-group, R.sup.3 is lower alkyl or acyl, andC.sub.9 -C.sub.10 is a CC-single or a CC-double bond, and the hydrogen atom in the 10-position is in the .alpha.-location if C.sub.9 -C.sub.10 is a CC-single bond, as well as the acid addition salts thereof. The compounds exhibit valuable pharmacological properties.

    摘要翻译: 本公开涉及通式I的I取代麦角灵衍生物(I)其中X是氧或硫原子,R 1是低级烷基,R 2是卤素,酰基,饱和或不饱和的低级烷基 其可以任选地被OR 4取代,其中R 4是氢,低级烷基,四氢吡喃基或环烷基,或被任选取代的芳基残基取代,其中R 5表示可任选地被芳基或任选地取代的芳基残基取代的低级烷基 取代的芳基残基,其中n = 2 o4 3,或-CHO-基团,R 3为低级烷基或酰基,C 9 -C 10为CC-单或CC-双键, 如果C9-C10是CC-单键,则10位是α位置,以及其酸加成盐。 该化合物显示出有价值的药理学性质。

    2-substituted ergoline urea and thio-urea derivatives having
neurolyptic/dopaminergic activity
    62.
    发明授权
    2-substituted ergoline urea and thio-urea derivatives having neurolyptic/dopaminergic activity 失效
    2-取代麦角蛋白尿素和具有神经选择性/多巴胺能活性的硫脲衍生物

    公开(公告)号:US4826851A

    公开(公告)日:1989-05-02

    申请号:US915356

    申请日:1986-10-06

    CPC分类号: C07D457/12

    摘要: Novel 2-substituted ergolinyl urea and thioruea derivatives are disclosed, as well as their use as pharmaceuticals, specifically as neuroleptics. The compounds, which possess central dopaminergic activity, have the formula ##STR1## wherein X is an oxygen or sulfur atom,R.sup.1 is a lower alkyl group,Y is a sulfur atom, S--CH.sub.2 --, C.sub.2 H.sub.4 --, --CH.dbd.CH--, or --C.tbd.C--,R.sup.2 is an aromatic ring of 5-6 atoms, 0-3 of which are O, S or N; or an aromatic ring of 5-6 atoms, 0-3 of which are O, S or N, and which is substituted by C.sub.1-2 -alkyl, C.sub.1-2 -alkoxy, nitrile, nitro, amino, C.sub.1-2 -alkylamino, carbonylamino or halo group, and C.sub.9 C.sub.10 is a CC-single or a CC-double bond and, if C.sub.9 C.sub.10 means a CC-single bond, the hydrogen atom in the 10-position is in the .alpha.-location,or a pharmaceutically acceptable acid addition salt thereof, wherein, if X is an oxygen atom, R.sup.1 is methyl and C.sub.9 C.sub.10 is a single bond, Y--R.sup.2 does not mean --C.sub.2 H.sub.4 -phenyl or --C.tbd.C--phenyl.

    摘要翻译: 公开了新型2-取代的麦角酰羟基尿素和硫醇衍生物,以及它们作为药物的用途,特别是作为精神安定药。 具有中枢多巴胺能活性的化合物具有式(I)其中X为氧或硫原子,R 1为低级烷基,Y为硫原子,S-CH 2 - ,C 2 H 4 - , - CH = CH-或-C 3位C-,R 2为5-6个原子的芳环,其中0-3为O,S或N; 或5-6个原子的芳环,其中0-3是O,S或N,并被C1-2烷基,C1-2 - 烷氧基,腈,硝基,氨基,C1-2 - 烷基氨基 ,羰基氨基或卤代基,C9C10为CC-单或CC-双键,如果C9C10表示CC-单键,则10-位的氢原子位于α位,或其药学上可接受的酸 其中,如果X是氧原子,则R1是甲基,C9C10是单键,Y-R2不是指-C2H4-苯基或-C3ONC-苯基。

    Process for the production of .beta.-carbolines by dehydrogenation
    63.
    发明授权
    Process for the production of .beta.-carbolines by dehydrogenation 失效
    通过脱氢生产β-咔啉的方法

    公开(公告)号:US4644062A

    公开(公告)日:1987-02-17

    申请号:US825718

    申请日:1986-02-03

    IPC分类号: C07D471/04

    CPC分类号: C07D471/04

    摘要: .beta.-carbolines of formula I ##STR1## wherein R=C.sub.1-5 alkylR.sup.4 =H, C.sub.1-5 alkyl or --(CH.sub.2).sub.n --OR with n=1 or 2 andR.sup.A =H, R, (CHR).sub.n --OR, OCH.sub.2 Ph, OPh, OPh(Cl,Br),OR,OCH.sub.2 Ph(Cl,Br) NRR, Cl or Br,wherein n and R have the above meanings and there are one or two R.sup.A 's are prepared, by dehydrogenation at reaction temperatures below ambient temperature in an inert solvent with tert-butyl hypochlorite and a tertiary amine.

    摘要翻译: 式I的β-咔啉其中R = C 1 -C 5烷基R 4 = H,C 1-5烷基或 - (CH 2)n -OR,其中n = 1或2,RA = H,R )n-OR,OCH 2 Ph,OPh,OPh(Cl,Br),OR,OCH 2 Ph(Cl,Br)NRR,Cl或Br,其中n和R具有上述含义,并且通过脱氢制备一个或两个RA 在低于环境温度的反应温度下在惰性溶剂中与次氯酸叔丁酯和叔胺反应。

    Intermittent coating of moving surfaces
    64.
    发明授权
    Intermittent coating of moving surfaces 有权
    运动表面的间歇涂层

    公开(公告)号:US09391312B2

    公开(公告)日:2016-07-12

    申请号:US14342471

    申请日:2012-09-13

    摘要: A method of intermittently coating a moving surface with paste containing electrochemically active particles by a nozzle having a slot-shaped delivery opening includes supplying paste to the delivery opening from a paste reservoir via a transport channel and regulating paste supply to the delivery opening with a rotatably mounted control axle which enables the paste supply to the delivery opening in a first switching position and, in a second switching position, blocks the transport channel and disconnects a section of the transport channel extending as far as the delivery opening from the paste supply, wherein the rotatably mounted control axle comprises a passage via which the paste reservoir is in communicating connection with the delivery opening in the first switching position and the disconnected section of the transport channel is in communicating connection with the reduced pressure source in the second switching position.

    摘要翻译: 通过具有槽形输送口的喷嘴间歇地涂覆含有电化学活性粒子的糊剂的移动表面的方法包括通过输送通道从浆料储存器向输送口供给糊料,并且通过可转动的方式将浆料供给到输送口 其在第一切换位置中能够将浆料供应到输送口,并且在第二切换位置中阻塞输送通道并将从输送口延伸的输送通道的一部分从糊料供给部分断开,其中 可旋转地安装的控制轴包括通道,通过该通道,膏容器在第一切换位置与输送开口连通,输送通道的断开部分与第二切换位置中的减压源连通。

    Device and process for recognizing a correct use of an alcohol measuring device
    65.
    发明授权
    Device and process for recognizing a correct use of an alcohol measuring device 有权
    用于识别正确使用酒精测量装置的装置和过程

    公开(公告)号:US08795187B2

    公开(公告)日:2014-08-05

    申请号:US12546144

    申请日:2009-08-24

    摘要: A device and a process are provided for recognizing a correct use of an alcohol measuring device by a test subject. At least one alcohol measuring device is provided with a signal transmitter, an analysis and control unit and a camera unit. An image field of the camera unit is divided into an inner image field area and an outer image field area. The inner image field area detects at least the face area of the test subject. The camera unit records changes at a boundary between the inner image field area and the outer image field area. A signal sent by the signal transmitter in the inner image field area can be detected by the camera unit.

    摘要翻译: 提供了一种装置和方法,用于识别测试对象正确使用酒精测量装置。 至少一个酒精测量装置具有信号发射器,分析和控制单元以及相机单元。 相机单元的图像场被分成内部图像场区域和外部图像场域区域。 内部图像区域至少检测测试对象的面部区域。 相机单元记录内部图像场区域和外部图像场区域之间的边界处的变化。 信号发送器在内部图像区域中发送的信号可由相机单元检测。

    Membrane electrode assembly with hydrogenatable material for a fuel cell
    66.
    发明授权
    Membrane electrode assembly with hydrogenatable material for a fuel cell 有权
    具有用于燃料电池的可氢化材料的膜电极组件

    公开(公告)号:US08283081B2

    公开(公告)日:2012-10-09

    申请号:US12208411

    申请日:2008-09-11

    IPC分类号: H01M8/02 H01M8/04 H01M8/10

    摘要: The invention relates to a membrane-electrode assembly for a fuel cell with a proton-conducting membrane two catalyst layers adjoining both sides of the membrane, wherein the catalyst layers have an electrically conductive base material and at least one catalytic material deposited on the base material, and two gas diffusion layers adjoining the catalyst layers. The membrane and/or at least one of the catalyst layers and/or at least one of the gas diffusion layers includes at least one hydrogenatable material capable of binding hydrogen in a reversible exothermic hydrogenation operation by forming a hydride, depending on the temperature and/or pressure. The hydrogenatable material can be distributed in the gas diffusion layer and/or in the catalyst layer or can be present as a separate layer on at least one side of the gas diffusion electrode or the membrane.

    摘要翻译: 本发明涉及一种用于燃料电池的膜 - 电极组件,其具有质子传导膜,两个邻近膜两侧的催化剂层,其中催化剂层具有导电基材和沉积在基材上的至少一种催化材料 和与催化剂层相邻的两个气体扩散层。 膜和/或至少一个催化剂层和/或至少一个气体扩散层包括至少一种能够通过形成氢化物在可逆放热加氢操作中结合氢的至少一种可氢化材料,这取决于温度和/ 或压力。 可氢化材料可以分布在气体扩散层和/或催化剂层中,或者可以在气体扩散电极或膜的至少一侧作为单独的层存在。

    Radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy
    70.
    发明授权
    Radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy 有权
    放射性卤代苯甲酰胺衍生物及其在肿瘤诊断和肿瘤治疗中的应用

    公开(公告)号:US07850948B2

    公开(公告)日:2010-12-14

    申请号:US12207774

    申请日:2008-09-10

    IPC分类号: A61K51/00 A61M36/14

    摘要: This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.

    摘要翻译: 本发明涉及新的放射性卤代苯甲酰胺衍生物及其在肿瘤诊断和肿瘤治疗中的应用。 根据本发明的放射性卤代苯甲酰胺衍生物显示出新的和特别有利的特性,特别是关于肿瘤浓度和延迟,肝脏浓度和血液积聚。 与健康的身体组织相比,在肿瘤中实现的放射治疗剂量对于本发明的化合物是有利的。