BINDING amyloid BENZOTIAZOLOVYE COMPOUND (OPTIONS), pharmaceutical compositions thereof, a method for detecting amyloid deposits (VARIANTS) METHOD distinguishing diseased ALZHEIMER BRAIN FROM NORMAL AND A METHOD OF MEASURING QUANTITY amyloid METHOD FOR SELECTIVE BINDING WITH amyloid plaques (VARIANTS) AND A METHOD FOR IDENTIFYING prodromal stage DISEASES ASSOCIATED WITH AMYLOID DEPOSITS WITH THEIR HELP

摘要

1. Amyloid-binding benzothiazole compounds encompassed by the general structural formula (I)! ! where Y is selected from the group consisting of H, F, Cl, BR, I, -NR'3 + and - (CR'2) n-X,! in which X represents F, Cl, BR or I, and! n means 1 -5,! R 'represents H or a lower alkyl group; ! R3-R10 are independently selected from the group consisting of H, F, Cl, BR, I, C1-C5 alkyl, (CH2) 1-3-OR11, CF3, - (CH2) 1-3-X, -O - (CH2) 1-3-X, CN, -CO-R11, -N (R11) 2, -N (R ') 3 +, -NO2, -CO-N (R11) 2, -O- (СО ) -R11, OR11, SR11, COOR11, Rph, -CR11 = CR11-Rph and -C (R11) 2-C (R11) 2-Rph,! in which X represents F, Cl, BR or I, and! Rph is phenyl optionally substituted with one or more substituents selected from the group consisting of F, Cl, BR, I, C1-C5 alkyl, (CH2) 1-3-OR11, CF3, - (CH2) 1-3-X , -O- (CH2) 1-3-X, CN, -CO-R11, -N (R11) 2, -N (R ') 3 +, -NO2, -CO-N (R11) 2, -O - (СО) -R11, OR11, SR11, COOR11,! each R11 independently of one another is H or C1-C5 alkyl; ! in which Y or R3-R10 includes at least one detectable label selected from the group consisting of 131I, 123I, 124I, 125I, 76BR, 75BR, 18F, 19F, 11C, 13C, 14C and 3H,! and their pharmaceutically acceptable salts. ! 2. The compounds according to claim 1, in which each of R3, R4, R5, R6, R7 and R10 represents H and R8 and R9 independently from each other represent OR11. ! 3. The compounds according to claim 1, in which Y contains a detectable label. ! 4. The compounds according to claim 1, covered by structural formulas selected from the group consisting of! ! or ! or ! or ! 5. Amyloid-binding benzothiazole compounds encompassed by structural formulas selected from the group consisting of! ! 6. A pharmaceutical composition comprising an effective amount of an amyloid-binding compound according to any one of claims 1 to 5 and a pharmaceutically acceptable carrier. ! 7. A method for detecting in vivo amyloid deposits in a mammal, characterized