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16 条记录 (耗时 0.034 秒)

    5′-primary aminoalkyl psoralen compositions with platelets
    11.
    发明授权
    5′-primary aminoalkyl psoralen compositions with platelets 失效
    具有血小板的5'-氨基烷基补骨脂素组合物

    公开(公告)号：US06218100B1

    公开(公告)日：2001-04-17

    申请号：US08900032

    申请日：1997-07-24

    申请人： Susan Wollowitz ,  Stephen T. Isaacs ,  Henry Rapoport ,  Hans Peter Spielmann

    发明人： Susan Wollowitz ,  Stephen T. Isaacs ,  Henry Rapoport ,  Hans Peter Spielmann

    IPC分类号： A01N102

    CPC分类号： C07D493/04 ,  A01N1/0215 ,  A61K31/365 ,  A61K31/37 ,  A61K41/0019 ,  A61K41/0066 ,  A61L2/0011

    摘要： Psoralen compounds are synthesized which have substitutions on the 4, 4′, 5′, and 8 positions of the psoralen, which permit enhanced binding to nucleic acid of pathogens. Higher psoralen binding levels and lower mutagenicity are described, resulting in safer, more efficient, and reliable inactivation of pathogens in blood products. The invention contemplates inactivation methods using the new psoralens which do not compromise the function of blood products for transfusion. In particular, use of 5′-primary aminoalkyl psoralens to inactivate pathogens in platelets is disclosed.

    摘要翻译： 合成补骨脂素化合物，其在补骨脂素的4,4'，5'和8位上具有取代，其允许增强与病原体核酸的结合。 描述了更高的补骨脂素结合水平和较低的致突变性，导致血液制品中病原体的更安全，更有效和可靠的失活。 本发明考虑使用新的补骨脂素的灭活方法，其不损害用于输血的血液制品的功能。 特别地，公开了使用5'-氨基烷基补骨脂素灭活血小板中的病原体。

    Farnesyl pyrophosphate analogs
    14.
    发明授权
    Farnesyl pyrophosphate analogs 失效
    法呢基焦磷酸酯类似物

    公开(公告)号：US06284910B1

    公开(公告)日：2001-09-04

    申请号：US09461002

    申请日：1999-12-15

    申请人： Hans Peter Spielmann ,  Douglas A. Andres ,  Kareem A. H. Chehade

    发明人： Hans Peter Spielmann ,  Douglas A. Andres ,  Kareem A. H. Chehade

    IPC分类号： C07F908

    CPC分类号： C07F9/098

    摘要： The post-translational addition of a farnesyl moiety to the Ras oncoprotein is essential for its membrane localization and is required for both its biological activity and ability to induce malignant transformation. The present invention describes design and synthesis of a farnesylpyrophosphate (FPP) analog, 8-anilinogeranyl pyrophosphate (AGPP) that is transferred to Ras by farnesyltransferase (FTase), in which the &ohgr;-terminal isoprene unit of the farnesyl group has been replaced with an aniline functionality. AGPP potently inhibited FTase activity in vitro (IC50=0.6 &mgr;M) and is highly selective showing little inhibitory activity against either geranylgeranyl-protein transferase type I (GGTase I) (IC50=31 &mgr;M) or the utilization of FPP by the enzyme squalene synthase (IC50=1000 &mgr;M). Kinetic analyses suggest that AGPP acts as a competitive inhibitor of FTase with respect to FPP. In vitro studies using [3H]AGPP show that the analog was appropriately transferred by FTase to Ras. Derivitization of AGPP with a bulky iodo group on the aniline ring does not significantly alter its biochemical properties. These data indicate that the modified molecules are the first truly transferable analogs of FPP and open the door to additional analogs to probe the biological function of protein farnesylation.

    摘要翻译： 法尼基部分向Ras癌蛋白的翻译后添加对于其膜定位是必需的，并且对于其生物学活性和诱导恶性转化的能力都是必需的。 本发明描述了通过法呢基转移酶（FTase）转移到Ras的法尼基焦磷酸（FPP）类似物8-苯氨基甘氨基焦磷酸（AGPP）的设计和合成，其中法呢基的ω-末端异戊二烯单元已被 苯胺功能。 AGPP有效地抑制了体外的FTase活性（IC50 =0.6μM），并且具有很高的选择性，显示出对香叶基香叶素 - 蛋白转移酶I（GGTase I）的抑制活性（IC50 =31μM）或通过酶角鲨烯合酶 IC50 =1000μM）。 动力学分析表明，AGPP作为FPP竞争性抑制剂。 使用[3H] AGPP的体外研究表明，通过FTase将类似物适当转移至Ras。 在苯胺环上衍生具有大体积碘基团的AGPP不会显着改变其生物化学性质。 这些数据表明，修饰的分子是FPP的第一个真正可转移的类似物，并为额外的类似物打开门来探测蛋白质法呢基的生物学功能。

    Tetrafluoroazidoaniline and method of making and using the same
    15.
    发明授权
    Tetrafluoroazidoaniline and method of making and using the same 失效
    四氟代叠氮苯胺及其制备及使用方法

    公开(公告)号：US06252096B1

    公开(公告)日：2001-06-26

    申请号：US09525753

    申请日：2000-03-14

    申请人： Hans Peter Spielmann ,  Kareem Abdel Hassan Chehade

    发明人： Hans Peter Spielmann ,  Kareem Abdel Hassan Chehade

    IPC分类号： C07C24710

    CPC分类号： C07C247/16 ,  C07C311/44

    摘要： The invention is directed to a novel compounds comprising 4-azidotetrafluoroaniline and the alkyl, acyl and sulfonamide derivatives thereof and to methods of making and using the same. The novel compounds are useful as a photoaffinity probe to study protein structure and function. Two methods for preparing 4-azidotetrafluoroaniline are disclosed, each employing a stable carbamate intermediate from which the 4-azidotetrafluoroaniline is derived.

    摘要翻译： 本发明涉及包含4-叠氮四氟四苯胺及其烷基，酰基和磺酰胺衍生物的新化合物及其制备和使用方法。 新型化合物可用作光亲和性探针来研究蛋白质结构和功能。 公开了制备4-叠氮四氟苯胺的两种方法，每种方法使用得自4-叠氮四氟乙苯的稳定的氨基甲酸酯中间体。