METHOD FOR OBTAINING NOVEL DERIVATIVES OF NAPHTHALENE FOR THE IN VIVO DIAGNOSIS OF ALZHEIMER'S DISEASE

摘要

This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belong to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wherein R represents mutually independent groups. In I: R1: -alkylenyl-C(O)NH-alkylenyl-R3, -alkylenyl-C(O)O—R4, R3: —COOH, —OH, —SH, —NH2, -alkyl-NH-alkyl-N-dithiocarbamate alkaline earth metal salts, R4: H, succinimidyl group, R2: —H, -alkyl. In II: R1: -alkyl, -alkylenyl-halide-alkylenyl-hydroxyl-alkylenyl-O-aryl, —O-alkylsulfonate alkylenyl, R2: -halide-alkylenyl-O-aryl, -alkylenyl-O-alkylsulfonate, -alkylenyl-halide-, —CH(O), —HC═C(CN)2, —HC═CHNO2, -alkylenyl-NH2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate alkaline salts. The terms “alkyl” and “alkylenyl” refer to linear or branched aliphatic chains, preferably from 1 to 4 carbon atoms and the term halide to fluorine, bromine or iodine. These compounds are neutral, lipophilic and have low molecular weight and therefore they cross the blood brain barrier and attach to the amyloid sheets. The present invention provides procedures for obtaining naphthalene derivatives with good yields, which can be practical, economical and adapted to a larger-scale manufacturing.

主权项

1. A method for displaying the density of amyloid sheets in a mammalian brain comprising (a) administering an amyloid binding compound composition comprising a radioisotopic form of a compound of structure II, wherein; R1 is alkyl-, and R2 is -alkylenyl-O-arylsulfonate, -alkylenyl-halide, —CH(O), -alkylenyl-NH2, -alkylenyl-NH-alkyl, or an -alkylenyl-alkyl-N-dithiocarbamate salt, or alternately; wherein; R1 is -alkylenyl-halide, or -alkylenyl-O-arylsulfonate and R2 is -halide, -alkylenyl-O-arylsulfonate, -alkylenyl-O-alkylsulfonate, -alkylenylhalide, —CH(O), —HC═C(CN)2, —HC═CHNO2, -alkylenyl-NH2, -alkylenyl-NH-alkyl or an alkylenyl-alkyl-N-dithiocarbamate salt; and wherein at least one or more of the oxygen, halogen or carbon atoms are substituted by a corresponding radioactive isotope; and determining whether the structures have been displayed.