Patent ID: 6329531
Filing Date: 2001-12-11
Classification: A61K,C07H,C08B,C09B,G01N

Abstract:
A compound of formula IFm(--A.sub.1)(--B.sub.n)(--W.sub.o) (I)in whichA is a biomolecule that binds to .beta.-amyloid-plaques,B is a dye that binds to .beta.-amyloid-plaques,W is a hydrophilic, low-molecular structural element that binds to .beta.-amyloid-plaques,m stands for number 1 or 2, or provided that n and o mean 0, m stands for an integer 3-20,l and n, independently of one another, stand for number 0, 1 or 2,o stands for an integer 0, 1, 2, 3 or 4, provided that the sum of l, n and o.gtoreq.1, andF is a dye-signal molecule, which has at least one absorption maximum in the range of 600 to 1200 nm, which is(a) a cyanine dye of formula V ##STR16##in whichp means an integer 2 or 3,X and Y, independently of one another, stand for O, S, --CH.dbd.CH-- or C(CH.sub.3).sub.2,R.sup.19 and R.sup.20, independently of one another, represent a radical --COOE.sup.1, --CONE.sup.1 E.sup.2, --NHCOE.sup.1, --NHCONHE.sup.1, --NE.sup.1 E.sup.2, --OE.sup.1, --OSO.sub.3 H, --SO.sub.3 H, --E.sup.1, wherein E.sup.1 and E.sup.2, independently of one another, stand for a hydrogen atom, a saturated or unsaturated, branched or straight-chain C.sub.1 -C.sub.50 alkyl chain, wherein the chain or portions of this chain optionally forms one or more aromatic or saturated cyclic C.sub.5 -C.sub.6 units or bicyclic C.sub.10 units, and wherein the C.sub.1 -C.sub.50 alkyl chain is interrupted by 0 to 15 oxygen atoms and/or by 0 to 3 carbonyl groups and/or is substituted with 0 to 5 hydroxy groups, provided that E.sup.1 and E.sup.2 are not hydrogen atoms at the same time, and R.sup.20 is not a hydrogen atom,and R.sup.21 and R.sup.22, independently of one another, stand for a radical --E.sup.1 with the above-indicated meaning, for a C.sub.1 -C.sub.4 sulfoalkyl chainor R.sup.19, R.sup.20, R.sup.21, R.sup.22, E.sup.1 or E.sup.2 binds to A, B or W,(b) a cyanine dye of formula VI ##STR17##in whichp, X, Y, R.sup.21 and R.sup.22 have the above-indicated meaning and,R.sup.23 stands for --OE.sup.3, --COOE.sup.3, --CONHE.sup.3, --CONH(CH.sub.2).sub.1-6 --NHE.sup.3, --CONH(CH.sub.2).sub.1-6 --OE.sup.3, --CONH(CH.sub.2).sub.1-6 --COOE.sup.3 or --CONH(CH.sub.2).sub.1-6 --CONHE.sup.3, in whichE.sup.3 stands for a mono-, oligo- or polysaccharide with at least one radical --OSO.sub.3 Hx, or(c) an oxonol dye of formula VII ##STR18##in whichp, R.sup.19 and R.sup.20 have the above-indicated meaning, andR.sup.24 and R.sup.25, independently of one another, stand for a phenyl ring that is substituted in one to three places with a hydroxy, carboxy, sulfate, sulfonate, alkyl or alkoxy or carboxylic acid ester radical, or a physiologically compatible salt thereof.