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    REACTIVE MULTI-FUNCTIONAL ADDITIVES FOR COATINGS COMPOSITIONS
    8.
    发明申请
    REACTIVE MULTI-FUNCTIONAL ADDITIVES FOR COATINGS COMPOSITIONS 审中-公开
    用于涂料组合物的反应性多官能添加剂

    公开(公告)号：US20150087817A1

    公开(公告)日：2015-03-26

    申请号：US14486059

    申请日：2014-09-15

    Applicant: Dow Global Technologies LLC ,  Rohm and Haas Company

    Inventor： Sudhakar Balijepalli ,  Paul Doll ,  Alvin M. Maurice ,  Jenny B. Werness

    IPC: C07H15/08

    CPC classification number: C07H15/08 ,  C08G65/3311 ,  C08G65/332 ,  C08G65/3322 ,  C08G2650/26 ,  C08L71/00 ,  C08L2205/00 ,  C08L2205/02

    Abstract: A composition comprising:(a) from 20 to 60 wt % of a saccharide component comprising from two to five sugar ring units having polymerized units of at least one alkylene oxide selected from the group consisting of ethylene oxide, propylene oxide and butylene oxide bonded to oxygen atoms on said sugar rings and at least three acetoacetyl groups bonded to terminal oxygen atoms of said polymerized units of at least one alkylene oxide; and(b) from 40 to 80 wt % of a non-saccharide component comprising a polyol unit not containing a sugar ring and having a hydroxyl functionality from two to five; said polyol unit having polymerized units of at least one alkylene oxide selected from the group consisting of ethylene oxide, propylene oxide and butylene oxide bonded to hydroxyl oxygen atoms of the polyol and at least two acetoacetyl groups bonded to terminal oxygen atoms of said polymerized units of at least one alkylene oxide;wherein total polymerized units of at least one alkylene oxide comprise from 20 to 80 wt % of said multi-functional additive.

    Abstract translation: 一种组合物，其包含：（a）20至60重量％的糖组分，其包含2至5个糖环单元，所述糖环单元具有至少一种选自环氧乙烷，环氧丙烷和环氧丁烷的环氧烷的聚合单元， 所述糖环上的氧原子和至少一个与至少一个烯化氧的所述聚合单元的末端氧原子键合的乙酰乙酰基; 和（b）40至80重量％的非糖组分，其包含不含糖环且羟基官能度为2至5的多元醇单元; 所述多元醇单元具有至少一种选自环氧乙烷，环氧丙烷和与该多元醇的羟基氧原子键合的环氧丁烷的环氧烷烃的聚合单元，和至少两个与所述聚合单元的末端氧原子键合的乙酰乙酰基 至少一种环氧烷; 其中至少一种烯化氧的总聚合单元包含所述多功能添加剂的20至80重量％。

    Anticoagulant antithrombotic dual inhibitors comprising a biotin label
    10.
    发明授权
    Anticoagulant antithrombotic dual inhibitors comprising a biotin label 有权
    包含生物素标记的抗凝血剂抗血栓双重抑制剂

    公开(公告)号：US08183228B2

    公开(公告)日：2012-05-22

    申请号：US12083212

    申请日：2006-10-06

    Applicant: Martin De Kort ,  Constant Adriaan Anton Van Boeckel ,  Charles David Nicholson

    Inventor： Martin De Kort ,  Constant Adriaan Anton Van Boeckel ,  Charles David Nicholson

    IPC: A61K31/715 ,  C07H3/06

    CPC classification number: C07H15/04 ,  A61K47/54 ,  A61K47/557 ,  A61K47/60 ,  C07H3/06 ,  C07H15/08 ,  C07H15/18

    Abstract: The present invention relates compounds of the formula: oligosaccharide-spacer-(GpIIb/IIIa antagonist), wherein the oligosaccharide is a negatively charged oligosaccharide residue comprising four to twenty five monosaccharide units, the charge being compensated by positively charged counterions, and wherein the oligosaccharide residue is derived from an oligosaccharide which has (AT-III mediated) anti-Xa activity per se; the spacer is a bond or an essentially pharmacologically inactive linking residue; the GpIIb/IIIa antagonist is a residue mimicking the RGD and/or K(QA)GD fragment of fibrinogen, comprising a carboxylate moiety and a basic moiety located within the residue at a distance of 10-20 Å from each other; or a pharmaceutically acceptable salt thereof or a prodrug or a solvate thereof; wherein the compound of formula I further comprises at least one covalent bond with a biotin label or an analogue thereof. The compounds of the invention have antithrombotic activity and can be used in treating or preventing thrombotic diseases. The antithrombotic activity of the compound of this invention can be neutralized in case of emergency upon administration of avidin, streptavidin and analogues thereof having high biotin affinity.

    Abstract translation: 本发明涉及下式的化合物：寡糖 - 间隔基（GpIIb / IIIa拮抗剂），其中寡糖是包含四至二十五个单糖单元的带负电荷的寡糖残基，电荷通过带正电荷的抗衡离子补偿，其中寡糖 残基衍生自具有（AT-III介导的）抗Xa活性本身的寡糖; 间隔基是键或基本上药理学上无活性的连接残基; GpIIb / IIIa拮抗剂是模拟纤维蛋白原的RGD和/或K（QA）GD片段的残基，其包含位于残基内的羧基部分和位于彼此间隔10-20处的碱性部分; 或其药学上可接受的盐或其前药或溶剂合物; 其中式I化合物还包含与生物素标记或其类似物的至少一个共价键。 本发明化合物具有抗血栓形成活性，可用于治疗或预防血栓形成疾病。 在施用具有高生物素亲和力的抗生物素蛋白，链霉亲和素及其类似物时，本发明化合物的抗血栓形成活性可以在紧急情况下被中和。

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