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NEW VITAMIN D DERIVATIVE, USE THEREOF IN TREATMENT, AND USE THEREOF IN TEST OF VITAMIN D METABOLITE

机译:新的维他命D衍生物,用于治疗,并在维他命D代谢物的试验中使用

摘要

Vitamin D derivatives corresponding to the following formula I IMAGE I in which R1 denotes a substituted alkyl group having 1 to 15 carbon atoms, in particular the side chains of vitamin D2 (C20 to C28) or D3 (C20 to C27), or these same chains partially modified, Y denotes H or OH or groups derived from the latter such as ester and ether; X denotes an alkyl chain, in particlar of 1 to 6 carbon atoms, optionally substituted at different points by one or more functional group (s) an unsaturated alkyl chain having one or more carbon-carbon double or triple bond(s), it being possible for these chains, in addition, to bear functional groups, or an aromatic or heteroaromatic ring, optionally substituted with halogens, one (or more) hydroxyl, amine, formyl carboxyl, thiol, cyano or nitro group(s), or alternatively groups derived from these latter, such as ether, ester, acetal or amide, or a halogen, a cyano, sulfoxide, sulfone, hydroxyl, thiol or amine group, or alternatively derivatives of these latter, such as ether, ester, amine and hydrazine; R2 denotes a methyl group and R3 an H, or R2 is H and R3 is methyl, or R2 and R3 are H, or alternatively R2 and R3 together denote a methylene group=CH2. The present invention relates to the therapeutic application of these derivatives. The present invention also relates to a method for preparing these derivatives; and to an antigen prepared by the covalent binding of these derivatives with an immunogenic carrier protein and antibodies prepared using this antigen. Finally, the present invention also relates to tracers consisting of the conjugation of a derivative according to the invention with a labeling component such as an enzyme or an iodinated molecule, as well as to an assay method for metabolites of vitamin D comprising the use of these tracers as a reagent.
机译:对应于下式I I的维生素D衍生物,其中R1表示具有1至15个碳原子的取代的烷基,特别是维生素D2(C20至C28)或D3(C20至C27)的侧链,或这些相同的链被部分修饰,Y表示H或OH或由后者衍生的基团,例如酯和醚; X表示特别是1-6个碳原子的烷基链,其在不同的位置任选地被一个或多个官能团取代的具有一个或多个碳-碳双键或三键的不饱和烷基链,这些链还可能带有官能团,或可能被卤素,一个(或多个)羟基,胺基,甲酰基羧基,硫醇基,氰基或硝基取代的芳族或杂芳族环,或其他基团衍生自这些化合物,例如醚,酯,缩醛或酰胺,或卤素,氰基,亚砜,砜,羟基,硫醇或胺基,或这些衍生物的衍生物,例如醚,酯,胺和肼; R 2表示甲基,R 3表示H,或者R 2是H,R 3是甲基,或者R 2和R 3是H,或者R 2和R 3一起表示亚甲基= CH 2。本发明涉及这些衍生物的治疗应用。本发明还涉及制备这些衍生物的方法。通过将这些衍生物与免疫原性载体蛋白共价结合而制备的抗原,以及使用该抗原制备的抗体。最后,本发明还涉及由根据本发明的衍生物与标记组分如酶或碘化分子缀合组成的示踪剂,以及涉及维生素D代谢物的测定方法,包括使用这些示踪剂。示踪剂作为试剂。

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