Water-soluble derivatives of lipophilic drugs
    1.
    发明授权
    Water-soluble derivatives of lipophilic drugs 失效
    亲脂性药物的水溶性衍生物

    公开(公告)号:US07029918B2

    公开(公告)日:2006-04-18

    申请号:US10057762

    申请日:2002-01-25

    摘要: A water-soluble reference standard is useful for immunoassays of a lipophilic drugs. The reference standard is a compound of formula (I): G-(L)n—Y;  (I) where G is a lipophilic drug; L is a linker which is an alkyl group or heteroalkyl group containing from 1 to 20 carbon atoms; n is 0 or 1; and Y is a water-solubilizing group such as —SO3−, —NR—SO3−, —P(═O)(OH)(O−), or —O—P(═O)(OH)(O−); where R is H or an alkyl group of 1 to 10 carbon atoms.

    摘要翻译: 水溶性参考标准对亲脂性药物的免疫测定是有用的。 参考标准是式(I)的化合物:<?in-line-formula description =“In-line Formulas”end =“lead”?> G-(L) (I)<?in-line-formula description =“In-line Formulas”end =“tail”?>其中G是亲脂性药物; L是含有1至20个碳原子的烷基或杂烷基的连接体; n为0或1; Y是水溶性基团,例如-SO 3 - , - SO 2 SO 3 - , - SO 2 - -P(-O)(OH)(O-O)或-OP(-O)(OH)(O-O) 其中R是H或1-10个碳原子的烷基。

    Tricyclic antidepressant derivatives and immunoassay
    2.
    发明授权
    Tricyclic antidepressant derivatives and immunoassay 有权
    三环抗抑郁药衍生物和免疫测定

    公开(公告)号:US06368814B1

    公开(公告)日:2002-04-09

    申请号:US09747809

    申请日:2000-12-22

    IPC分类号: G01N33535

    摘要: The present invention is directed to novel tricyclic antidepressant drug derivatives synthesized for covalent attachment to proteins or polypeptide antigens for use in the preparation of antibodies or receptors to tricyclic antidepressant drugs and tricyclic antidepressant metabolites. The new derivatives are characterized by a saturated double bond on the amitriptyline portion of the molecule and are represented by the structure where R1 is a saturated or unsaturated, substituted or unsubstituted, straight or branched chain of 0-10 carbon or heteroatoms, X is a linker group consisting of 0-2 substituted or unsubstituted aromatic rings, and Y is an activated ester or NH—Z, where Z is a poly(amino acid). The novel tricyclic antidepressant activated hapten derivatives are useful for preparing tracers and conjugates for tricyclic antidepressant immunoassays, including an enzyme immunoassay and a microparticle capture inhibition assay using an antibody produced from the novel immunogen with a conjugate derivatized either at the N-1 position of imipramine or at the C-2 position of dihydroamitriptyline.

    摘要翻译: 本发明涉及用于共价连接蛋白质或多肽抗原的新型三环抗抑郁药物衍生物,用于制备三环抗抑郁药物和三环抗抑郁药代谢物的抗体或受体。 新衍生物的特征在于分子的阿米替林部分上具有饱和双键并且由其中R 1是饱和或不饱和的,取代或未取代的0-10个碳原子或杂原子的直链或支链的结构表示,X是连接基 由0-2个取代或未取代的芳环组成的基团,Y是活化酯或NH-Z,其中Z是聚(氨基酸)。 新型三环抗抑郁药活化的半抗原衍生物可用于制备用于三环抗抑郁药免疫测定的示踪剂和缀合物,包括酶免疫测定和使用由新型免疫原产生的抗体的微粒捕获抑制测定与在丙咪嗪的N-1位衍生的缀合物 或在二氢阿米替林的C-2位置。