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    Novel Diverse Lead Compound Autotaxin Inhibitors
    1.
    发明申请
    Novel Diverse Lead Compound Autotaxin Inhibitors 有权
    新型多样化铅复合自体贴剂抑制剂

    公开(公告)号：US20110160148A1

    公开(公告)日：2011-06-30

    申请号：US12828053

    申请日：2010-06-30

    申请人： Abby Louise Parrill-Baker ,  Daniel Lee Baker ,  Elton Jeffrey North

    发明人： Abby Louise Parrill-Baker ,  Daniel Lee Baker ,  Elton Jeffrey North

    IPC分类号： A61K38/07 ,  A61K31/185 ,  A61K31/655 ,  C12N9/99 ,  C07C309/52 ,  C07C245/10 ,  C07C309/49 ,  A61P43/00

    CPC分类号： A61K31/167 ,  A61K31/10 ,  A61K31/136

    摘要： Classes of compounds that exhibit effective inhibition of autotaxin enzymes are provided. Such classes include naphthalenesulfones, phenylsulfones, and certain peptides with unnatural amino acids and exhibit reactivity with autotaxin to ultimately reduce the size of the reactive sites thereon to prevent conversion of lysophosphatidyl choline to lysophophatidic acid. Furthermore, such compounds can be incorporated within delivery forms for human ingestion. As such, these compounds accord an excellent manner of potentially reducing generation of certain cancers attributable to the presence of naturally occurring autotaxin within the human body. Methods of inactivating autotaxin to certain degrees therewith such compounds are encompassed within invention as well.

    摘要翻译： 提供表现出有效抑制自体素蛋白酶的化合物类别。 这些类别包括萘磺酸盐，苯基砜和具有非天然氨基酸的某些肽，并显示出与自分泌素的反应性，以最终减小其上的反应位点的大小，以防止溶血磷脂酰胆碱转化为溶血磷脂酸。 此外，这些化合物可以并入用于人体摄取的递送形式中。 因此，这些化合物具有潜在地减少由于天然存在的自体贴剂在人体内的存在而导致某些癌症的产生的优异方式。 用自动吸入素灭活一定程度的方法也包括在本发明范围内。

    Fluorescent indicator dyes for calcium ions
    3.
    发明授权
    Fluorescent indicator dyes for calcium ions 失效
    用于钙离子的荧光指示剂染料

    公开(公告)号：US4603209A

    公开(公告)日：1986-07-29

    申请号：US648649

    申请日：1984-09-07

    申请人： Roger Y. Tsien ,  Grzegorz Grynkiewicz

    发明人： Roger Y. Tsien ,  Grzegorz Grynkiewicz

    IPC分类号： A61K38/00 ,  A61K38/22 ,  A61P5/00 ,  C07C229/18 ,  C07C229/52 ,  C07C237/30 ,  C07C255/59 ,  C07C309/49 ,  C07C311/39 ,  C07C317/32 ,  C07D209/08 ,  C07D209/14 ,  C07D215/40 ,  C07D307/79 ,  C07D307/82 ,  C07D413/04 ,  C07K7/23 ,  G01N21/78 ,  G01N33/84 ,  C07C101/447 ,  C07D307/87

    CPC分类号： C07D307/79 ,  C07D209/08 ,  C07D215/40 ,  C07D413/04 ,  Y10S436/80

    摘要： The present invention discloses a new class of highly fluorescent indicator dyes that are specific for calcium ions. The new fluorescent indicator dyes combine a stilbene-type fluorophore with a tetracarboxylate parent Ca.sup.2+ chelating compound having the octacoordinate pattern of liganding groups characteristic of EGTA and BAPTA. Preferred forms contain extra heterocyclic bridges to reinforce the ethylenic bond of the stilbene and to reduce hydrophobicity. Compared to their widely used predecessor, "quin2", the new dyes offer up to thirty-fold brighter fluorescence, major changes in wavelength (not just intensity) upon Ca.sup.2+ binding, slightly lower affinities for Ca.sup.2+, slightly longer wavelengths of excitation, and considerably improved selectivity for Ca.sup.2+ over other divalent cations. These properties, particularly the wavelength sensitivity to Ca.sup.2+, make the dyes useful indicators for many intracellular applications, especially in single cells, adherent cell layers, or bulk tissues.The present invention also discloses an improved method for synthesizing alpha-acyloxyalkyl bromides wherein the bromides so synthesized are free of contaminating bis(1-bromoalkyl)ether. The improved method is exemplified herein in the synthesis of acetoxymethyl bromide, a compound useful in preparing the acetoxymethyl esters disclosed herein as novel Ca.sup.2+ specific fluorescent indicators.

    摘要翻译： 本发明公开了一类对钙离子具有特异性的高荧光指示剂染料。 新的荧光指示剂染料将二苯乙烯型荧光团与具有EGTA和BAPTA特征的连接组的八配位图案的四羧酸母体Ca 2+螯合化合物结合。 优选的形式包含额外的杂环桥，以加强1,2-二苯乙烯的烯键并降低疏水性。 与其广泛使用的前身“quin2”相比，新型染料提供高达三十倍的荧光，Ca2 +结合时的波长（不仅仅是强度）的主要变化，Ca2 +的亲和力略低，激发波长稍长， 提高Ca2 +对其他二价阳离子的选择性。 这些性质，特别是对Ca2 +的波长敏感性，使得染料对于许多细胞内应用尤其是在单细胞，贴壁细胞层或体组织中是有用的指标。 本发明还公开了一种合成α-酰氧基烷基溴化物的改进方法，其中如此合成的溴化物没有污染的双（1-溴烷基）醚。 改进的方法在本文中示例性地合成乙酰氧甲基溴，其是可用于制备本文公开的乙酰氧基甲酯作为新型Ca 2+特异性荧光指示剂的化合物。

    N,N,N',N'-TETRADODECYL-SUBSTITUTED DIPHENYL ETHER SULFONATE ANIONIC GEMINI SURFACTANT AND SYNTHESIS METHOD THEREOF
    6.
    发明申请
    N,N,N',N'-TETRADODECYL-SUBSTITUTED DIPHENYL ETHER SULFONATE ANIONIC GEMINI SURFACTANT AND SYNTHESIS METHOD THEREOF 审中-公开

    公开(公告)号：US20200208045A1

    公开(公告)日：2020-07-02

    申请号：US16691969

    申请日：2019-11-22

    申请人： PetroChina Company Limited

    发明人： Xiangfei GENG ,  Bin DING ,  Jianhui LUO ,  Bo HUANG ,  Jianyong XIE ,  Pingmei WANG ,  Yang GAO ,  Baoliang PENG

    IPC分类号： C09K8/60 ,  C07C309/49 ,  C07C303/06

    摘要： The present invention discloses a N,N,N′,N′-tetradodecyl-substituted diphenyl ether sulfonate anionic Gemini surfactant and the synthesis method thereof. It has a structural formula of: and is prepared in a two-step reaction comprising: S1. subjecting 4,4′-diaminodiphenyl ether and bromododecane to an amine alkylation reaction to obtain N,N,N′,N′-tetradodecyl-substituted diphenyl ether; and S2. sulfonating the N,N,N′,N′-tetradodecyl-substituted diphenyl ether with concentrated sulfuric acid to produce the target product, N,N,N′,N′-tetradodecyl-substituted diphenyl ether sulfonate. The surfactant of the present invention has a high surface activity and can be synthesized with a simple procedure under mild reaction conditions, and can be easily separated and purified. The surfactant of the present invention is promising in applications for alkaline/surfactant in tertiary oil recovery, for polymer/surfactant binary compound flooding, alkaline/surfactant/polymer tertiary compound flooding, microemulsion emulsifier, and the like, and may also be compounded with common surfactants to lower the cost, thereby enabling its application in a large scale.