1,2-DIOXETANES
    2.
    发明授权
    1,2-DIOXETANES 失效
    1,2-二氧环乙烷。

    公开(公告)号:EP0368946B1

    公开(公告)日:1994-09-14

    申请号:EP89901890.7

    申请日:1989-01-03

    申请人: TROPIX, INC.

    摘要: Compounds having formula (I), wherein T is a polycycloalkylidene group (e.g., adamant-2-ylidene); R is a C1-20 alkyl, aralkyl or cycloalkyl group; and Y is a fluorescent chromophore (e.g., m-phenylene), produced by reacting a compound having formula (II) with an R-ylating agent (e.g., R2SO4) in the presence of an alkali metal alkoxide in a polar aprotic solvent. Also, compounds having formula (III) are produced by reacting a compound having formula (IV) with formula (V), wherein X is an electronegative leaving group (e.g., a halogen anion such as chloride ion) in the presence of a Lewis base (e.g., a trialkyl-amine) dissolved in an aprotic organic solvent (e.g., benzene or toluene). Also, compounds having formula (VI) are produced by reacting a compound of formula (VII) with a tetra-O-acylated-O-hexopyranoside halide, then hydrolyzing off the protective acyl groups. The aforementioned compounds and procedures are useful in the synthesis of enzyme-cleavable 1,2-dioxetane ring systems that can serve as members of a binding pair employed, for example, in chemiluminescent immunoassays, DNA probe assays, and direct assays for an enzyme.

    摘要翻译: 具有式(I)的化合物,其中T是聚亚烷基(例如,金刚烷-2-亚基); R是C 1-20烷基,芳烷基或环烷基; Y是通过在极性非质子溶剂中在碱金属醇盐存在下使具有式(II)的化合物与R-取代剂(例如R 2 SO 4)反应制备的荧光发色团(例如,间亚苯基)。 另外,具有式(III)的化合物是通过式(Ⅳ)化合物与式(Ⅴ)反应制得的,其中X是一个电负离子基团(如卤素阴离子如氯离子),在路易斯碱 (例如三烷基胺)溶于非质子有机溶剂(如苯或甲苯)中。 此外,具有式(VI)的化合物通过使式(VII)的化合物与四-O-酰化的O-六吡喃糖苷卤化物反应,然后水解保护性酰基而制备。 上述化合物和方法可用于合成可切割的1,2-二氧杂环丁烷环系统,其可以用作结合对的成员,例如在化学发光免疫测定,DNA探针测定和酶的直接测定中使用。

    AZULENYL NITRONE SPIN TRAPPING AGENTS, METHODS OF MAKING AND USING SAME
    10.
    发明授权
    AZULENYL NITRONE SPIN TRAPPING AGENTS, METHODS OF MAKING AND USING SAME 失效
    AZULENYLNITRONE ALS RADIKAL FANGER(旋转代理),VERFAHREN ZU IHRER HERSTELLUNG UND IHRE ANWENDUNG

    公开(公告)号:EP0888290B1

    公开(公告)日:2006-12-27

    申请号:EP96940538.0

    申请日:1996-11-15

    摘要: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be colorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g., structural and the like) about the original reactive free radical species.

    摘要翻译: 本发明涉及发色性硝酮自旋捕获剂,制备这些试剂的方法,包含它们的组合物及其使用方法。 特别地,本发明的薁基硝酸盐是捕获自由基物质的有效试剂,可用作物理化学和生物体系中的有效抗氧化剂。 因此,本发明还涉及由薁基硝酮与自由基的组合形成的旋转加合物。 本发明的化合物可以容易地从可用的原料制备,并进一步用于测定和许多诊断,预防和治疗应用,包括但不限于缓解,调节和抑制碳中心的负面影响 或氧中心的自由基物质和其他氧化产物。 此外,组合加合物可以被热量检测,并且任选地分离和表征,以获得关于原始反应性自由基物质的有价值的信息(例如结构等)。