Process for Preparing 6,7-Dihydro-5H-Imidazo[1,5-A]Pyridin-8-One
    18.
    发明申请
    Process for Preparing 6,7-Dihydro-5H-Imidazo[1,5-A]Pyridin-8-One 审中-公开
    6,7-二氢-5H-咪唑并[1,5-a]吡啶-8-酮的制备方法

    公开(公告)号:US20090118512A1

    公开(公告)日:2009-05-07

    申请号:US12225813

    申请日:2007-03-30

    摘要: 6,7-Dihydro-5H-imidazo[1,5-a]pyridin-8-one (I), is obtainable in high yields by: 1) a process which proceeds from a suitably protected C-(3-hydroxypyridin-2-yl)methylamine whose amine is converted to the formamide which is then cyclized to the imidazo[1,5-a]pyridine and hydrogenated to the 6,7-dihydro-5H-imidazo[1,5-a]pyridin-8-one, and suitably protected C-(3-hydroxypyridin-2-yl)methylamines can be prepared either in 2 steps proceeding from commercially available 3-hydroxy-2-cyanopyridine [932-35-4] or in 3 steps proceeding from commercially available 2-hydroxymethylpyridin-3-ol [14173-30-9]; 2) a process for preparing 4-hydroxy-1-(1H-imidazol-4-yl)butan-1-one, an intermediate from the synthesis of 6,7-dihydro-5H-imidazo[1,5-a]pyridin-8-one (formula I), as described in WO 2002/040484, proceeding from N,N-dimethyl-2-(trialkylsilanyl)imidazole-1-sulphonamide by lithiation and subsequent reaction with a suitably protected 4-hydroxybutyraldehyde, followed by oxidation of the secondary alcohol, acid-induced deprotection of the imidazole and deprotection of the alcohol functionality; 3) a process which proceeds from 5,6,7,8-tetrahydroimidazo[1,5-a]pyridine [38666-30-7], which is oxidized.

    摘要翻译: 6,7-二氢-5H-咪唑并[1,5-a]吡啶-8-酮(I)可以通过以下方式获得:1)从适当保护的C-(3-羟基吡啶-2 - 基)甲胺,其胺转化成甲酰胺,然后将其环化为咪唑并[1,5-a]吡啶,并氢化成6,7-二氢-5H-咪唑并[1,5-a] 一个和适当保护的C-(3-羟基吡啶-2-基)甲胺可以从市售的3-羟基-2-氰基吡啶[932-35-4]或以商业上可获得的3个步骤 2-羟甲基吡啶-3-醇[14173-30-9]; 2)制备4-羟基-1-(1H-咪唑-4-基)丁-1-酮,合成6,7-二氢-5H-咪唑并[1,5-a]吡啶的中间体 -8-(异构体I),如WO 2002/040484中所述,通过锂化从N,N-二甲基-2-(三烷基硅烷基)咪唑-1-磺酰胺进行,随后与适当保护的4-羟基丁醛反应,然后 仲醇的氧化,酸诱导的咪唑脱保护和醇官能团的脱保护; 3)从被氧化的5,6,7,8-四氢咪唑并[1,5-a]吡啶[38666-30-7]进行的方法。

    Sugar-modified gapped oligonucleotides
    19.
    发明授权
    Sugar-modified gapped oligonucleotides 失效
    糖修饰的间隙寡核苷酸

    公开(公告)号:US06451991B1

    公开(公告)日:2002-09-17

    申请号:US08802331

    申请日:1997-02-11

    IPC分类号: C12Q168

    CPC分类号: C07H21/00

    摘要: Oligonucleotides are provided which have increased nuclease resistance, substituent groups for increasing binding affinity to complementary nucleic acid strand, and subsequences of 2′-deoxy-erythro-pentofuranosyl nucleosides that activate RNase H. Such oligonucleotides are useful for diagnostics and other research purposes, for modulating the expression of a protein in organisms, and for the diagnosis, detection and treatment of other conditions susceptible to ooligonucleotide therapeutics.

    摘要翻译: 提供具有增加的核酸酶抗性的寡核苷酸,用于增加对互补核酸链的结合亲和力的取代基,以及激活RNase H的2'-脱氧 - 赤 - 戊呋喃糖基核苷的亚序列。这样的寡核苷酸可用于诊断和其它研究目的 调节生物体中蛋白质的表达,以及用于诊断,检测和治疗其他对寡核苷酸治疗剂敏感的病症。

    Cable raceways for modular system furniture
    20.
    发明授权
    Cable raceways for modular system furniture 失效
    用于模块化系统家具的电缆滚道

    公开(公告)号:US06244002B1

    公开(公告)日:2001-06-12

    申请号:US09193363

    申请日:1998-11-17

    申请人: Pierre Martin

    发明人: Pierre Martin

    IPC分类号: E04B276

    摘要: A modular panel system having a plurality of panels connected together, each of the panels would normally be of a rectangular configuration, the panels being connected together by means of a vertically extending member which is secured to side walls of the panels and an elongated flexible interconnecting member having first and second longitudinally extending side marginal edges and an enlarged edge portion designed to be retained by the vertically extending member. A U-shaped raceway member which may be placed on either the top or bottom of a panel or between panels to provide for horizontal cables.

    摘要翻译: 一种具有连接在一起的多个面板的模块化面板系统,每个面板通常为矩形构造,所述面板通过垂直延伸的构件连接在一起,所述垂直延伸构件固定在面板的侧壁上,以及细长的柔性互连 构件具有第一和第二纵向延伸的侧边缘和设计成由垂直延伸构件保持的扩大边缘部分。 U型滚道构件,其可以放置在面板的顶部或底部或面板之间以提供水平电缆。