Conversion of amine- to carboxyl groups on solid surfaces
    92.
    发明授权
    Conversion of amine- to carboxyl groups on solid surfaces 有权
    在固体表面上胺转化为羧基

    公开(公告)号:US07704543B2

    公开(公告)日:2010-04-27

    申请号:US10573377

    申请日:2004-09-27

    Abstract: This invention provides a new method of obtaining a high density, reproducible and uniform coverage of a solid surface, compounds suitable for such a method and methods of preparing such compounds. This invention further relates to methods of the chemical modification (carboxylation) of solid surfaces and their subsequent use for the attachment of amine-containing molecules including DNA, proteins and other polymers.

    Abstract translation: 本发明提供了一种获得固体表面高密度,可再现和均匀覆盖的新方法,适用于制备此类化合物的方法和方法的化合物。 本发明还涉及固体表面的化学修饰(羧化)的方法及其随后用于连接包含DNA,蛋白质和其它聚合物的含胺分子的用途。

    PROTEIN INTERACTION REPORTER AGENTS AND METHODS FOR USING SAME
    94.
    发明申请
    PROTEIN INTERACTION REPORTER AGENTS AND METHODS FOR USING SAME 审中-公开
    蛋白质相互作用记录剂及其使用方法

    公开(公告)号:US20100047814A1

    公开(公告)日:2010-02-25

    申请号:US12423459

    申请日:2009-04-14

    Abstract: Particular aspects provide novel protein interaction reporter (PIR) compounds (e.g., formulas I and II), comprising at least two protein reactive moieties (e.g., N-hydroxysuccinamide), each linked to a reporter moiety (e.g., mass reporter) by a covalent labile bond that is differentially cleavable with respect to peptide bonds (e.g., by a method such as collisional activation in a mass spectrometer, activation by electron capture dissociation (ECD), photoactivation, etc.), wherein the reporter moiety is operatively releasable from the PIR agent upon cleavage of the labile bonds, the released reporter moiety having a characteristic identifying property or label (e.g., m/z value). Particular PIRs comprise a mass reporter moiety, and further comprise an affinity group, (e.g., biotin), linked to the PIR (e.g., to the mass reporter moiety) by a selectively cleavable bone (e.g. photo-labile bond)). Additional aspects provide methods for characterizing intermolecular or intramolecular protein interactions using one or more inventive PIR compounds.

    Abstract translation: 特别的方面提供新的蛋白质相互作用报告物(PIR)化合物(例如式I和II),其包含至少两个蛋白质反应性部分(例如,N-羟基琥珀酰胺),其各自通过共价键连接到报道部分(例如质量报告基团) 相对于肽键可以差异地切割的不稳定键(例如,通过诸如质谱仪中的碰撞激活的方法,通过电子捕获解离的激活(ECD),光活化等),其中报道部分可操作地从 裂解不稳定键时的PIR试剂,具有特征识别性质或标记的释放的报导部分(例如,m / z值)。 具体的PIR包括质量报告基因部分,并且还包含通过可选择性切割的骨(例如光不稳定键)与PIR连接的亲和基团(例如,生物素)(例如与质量报告基团部分))。 另外的方面提供了使用一种或多种本发明的PIR化合物表征分子间或分子内蛋白质相互作用的方法。

    Cosmetic Process for Preventing or Treating the Signs of Skin Ageing or the Orange-Peel Appearance
    95.
    发明申请
    Cosmetic Process for Preventing or Treating the Signs of Skin Ageing or the Orange-Peel Appearance 审中-公开
    用于预防或治疗皮肤老化或橙皮外观的迹象的化妆过程

    公开(公告)号:US20090047224A1

    公开(公告)日:2009-02-19

    申请号:US10580230

    申请日:2004-11-08

    Abstract: The present invention relates to the use of at least one compound capable of cleaving the diketone crosslinking bonds between two proteins, in a composition applied topically to the skin, as an agent for preventing or treating the signs of ageing of the skin or the orange-peel appearance. The above compound is preferably a N-hydroxy imide of formula (I). These N-hydroxy imides have inhibitory properties on the glycation of proteins and also antioxidant properties. The invention also relates to novel N-hydroxy imides included in formula (I) above.

    Abstract translation: 本发明涉及至少一种能够在两种蛋白质之间切割二酮交联键的化合物在局部施用于皮肤的组合物中的用途,作为用于预防或治疗皮肤老化迹象或橙 - 剥皮外观。 上述化合物优选为式(I)的N-羟基酰亚胺。 这些N-羟基酰亚胺对蛋白质的糖基化以及抗氧化性质具有抑制性。 本发明还涉及上述式(I)中所含的新型N-羟基酰亚胺。

    Reconfigurable molecules and molecular switches, sensors, and dyes employing the same
    97.
    发明申请
    Reconfigurable molecules and molecular switches, sensors, and dyes employing the same 失效
    可重构分子和分子开关,传感器和使用它们的染料

    公开(公告)号:US20080269486A1

    公开(公告)日:2008-10-30

    申请号:US11799147

    申请日:2007-04-30

    Abstract: Various embodiment of the present invention are directed to organic molecules that are reconfigurable under application of an external electric field. One organic molecule embodiment of the present invention has the structure: where L1X1 and L2X2 are optional connector groups, A represents an electron acceptor group, D represents an electron donor group, R and R′ represent spacer molecules, and R1, R2, R3, R4, R5, R6, R7, and R8 represent atoms and hydrocarbons.

    Abstract translation: 本发明的各种实施方案涉及在外部电场的应用下可重新配置的有机分子。 本发明的一个有机分子实施方案具有以下结构:其中L 1 X 1和X 2 X 2 X 2 是可选的连接基团,A表示电子受体基团,D表示电子给体基团,R和R'表示间隔基分子,R 1,R 2, R 3,R 4,R 5,R 6,R 7和R 7, 8 表示原子和烃。

    Novel Green and Orange Fluorescent Labels and Their Uses
    98.
    发明申请
    Novel Green and Orange Fluorescent Labels and Their Uses 失效
    新型绿色和橙色荧光标签及其用途

    公开(公告)号:US20080261235A1

    公开(公告)日:2008-10-23

    申请号:US11967134

    申请日:2007-12-29

    Abstract: The present invention provides novel fluorescent compounds and covalent attachment chemistries which facilitate the use of these compounds as labels for ultrasensitive and quantitative fluorescent detection of low levels of biomolecules. In a preferred embodiment, the fluorescent labels of this invention are novel derivatives of the hydroxy-pyrene trisulpbonic and disulphonic acids which may be used in any assay in which radioisotopes, colored dyes or other fluorescent molecules are currently used. Thus, for example, any assay using labeled antibodies, proteins, oligonucleotides or lipids, including fluorescent cell sorting, fluorescence microscopy (including dark-field microscopy), fluorescence polarization assays, ligand, receptor binding assays, receptor activation assays and diagnostic assays can benefit from use of the compounds disclosed herein.

    Abstract translation: 本发明提供了新颖的荧光化合物和共价附着化学物质,其有助于这些化合物用作低水平生物分子的超敏感和定量荧光检测的标签。 在一个优选的实施方案中,本发明的荧光标记是羟基芘三羰基和二磺酸的新衍生物,其可用于目前使用放射​​性同位素,着色染料或其它荧光分子的任何测定中。 因此,例如,使用标记的抗体,蛋白质,寡核苷酸或脂质,包括荧光细胞分选,荧光显微术(包括暗视野显微镜),荧光偏振测定,配体,受体结合测定,受体激活测定和诊断测定法的任何测定都可以受益 使用本文公开的化合物。

    Antharquinone Compounds as Anti Cancer Compounds
    99.
    发明申请
    Antharquinone Compounds as Anti Cancer Compounds 失效
    蒽醌化合物作为抗癌化合物

    公开(公告)号:US20080027107A1

    公开(公告)日:2008-01-31

    申请号:US10596783

    申请日:2004-12-22

    Abstract: Anthraquinone compounds of the general formula (I) or a salt thereof (Formula I) in which R1 to R4 are each selected from the group consisting of H, C1-4 alkyl, X1, —NHR0N (Rs)2 in which R° is a C1l12 alkanediyl and each R5 is H or optionally substituted C14 alkyl, and a group of formula (11) in which at least one of R6,R7 and R8 is selected from X2 , and X2 substituted C1-4 alkyl and any others are H or C14 alkyl; R9 is selected from H, C14 alkyl, X2 and X2 substituted C1-4 alkyl; m is 0 or 1; n is 1 or 2; X1 is a halogen atom, a hydroxyl group, a C1.6 alkoxyl group, an aryloxy group or an acyloxy group; and X2 is a halogen atom, a hydroxyl group, a C16 alkoxyl group, an aryloxy group or an acyloxy group; provided that at least one of R1 to R4 is a group of formula (II). The N-oxides are useful prodrugs which are selectively bioreduced in hypoxic tumours to the corresponding cyclic amine derivatives. The amine compounds are cytotoxic and may be used as alkylating agents having topoisomerase II inhibiting activities in cancer therapy.

    Abstract translation: 通式(I)的蒽醌化合物或其盐(式I)其中R 1至R 4各自分别选自H,C < 其中R 1是C 1 ,其中R 1是C 1 H 2, 烷二基和每个R 5是H或任选取代的C 14-14烷基,和式(11)的基团,其中至少 R 6,R 7和R 8中的一个选自X 2,X 2, 取代的C 1-4烷基,任何其它的是H或C 14烷基; R 9选自H,C 1-4烷基,X 2和X 2取代的C 1 -C 4烷基, 1-4烷基; m为0或1; n为1或2; X 1是卤素原子,羟基,C 1 -C 6烷氧基,芳氧基或酰氧基; X 2是卤素原子,羟基,C 1〜6烷氧基,芳氧基或酰氧基; 条件是R 1至R 4中的至少一个为式(II)的基团。 N-氧化物是有用的前药,其在缺氧肿瘤中选择性地生物还原成相应的环胺衍生物。 胺化合物是细胞毒性的,并且可以用作在癌症治疗中具有拓扑异构酶II抑制活性的烷化剂。

    Green and orange fluorescent labels and their uses
    100.
    发明授权
    Green and orange fluorescent labels and their uses 失效
    绿色和橙色荧光标签及其用途

    公开(公告)号:US07317111B2

    公开(公告)日:2008-01-08

    申请号:US10669584

    申请日:2003-09-23

    Abstract: The present invention provides novel fluorescent compounds and covalent attachment chemistries which facilitate the use of these compounds as labels for ultrasensitive and quantitative fluorescent detection of low levels of biomolecules. In a preferred embodiment, the fluorescent labels of this invention are novel derivatives of the hydroxy-pyrene trisulphonic and disulphonic acids which may be used in any assay in which radioisotopes, colored dyes or other fluorescent molecules are currently used. Thus, for example, any assay using labeled antibodies, proteins, oligonucleotides or lipids, including fluorescent cell sorting, fluorescence microscopy (including dark-field microscopy), fluorescence polarization assays, ligand, receptor binding assays, receptor activation assays and diagnostic assays can benefit from use of the compounds disclosed herein.

    Abstract translation: 本发明提供了新颖的荧光化合物和共价附着化学物质,其有助于这些化合物用作低水平生物分子的超敏感和定量荧光检测的标签。 在优选的实施方案中,本发明的荧光标记是羟基芘三磺酸和二磺酸的新衍生物,其可用于目前使用放射​​性同位素,着色染料或其它荧光分子的任何测定中。 因此,例如,使用标记的抗体,蛋白质,寡核苷酸或脂质,包括荧光细胞分选,荧光显微术(包括暗视野显微镜),荧光偏振测定,配体,受体结合测定,受体激活测定和诊断测定法的任何测定都可以受益 使用本文公开的化合物。

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