Detectable molecules, method of preparation and use

G - Physics – 21 – H

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260/170, 167/47,

G21H 5/02 (2006.01) A61K 51/04 (2006.01) A61K 51/10 (2006.01) C07H 21/00 (2006.01) G01N 33/533 (2006.01) G01N 33/553 (2006.01)

Patent

CA 1314503

ABSTRACT OF THE INVENTION A detectable molecule of the formula A3-(-X-R1-E-Detb)m where A3 is A2 or a polymer, where A3 has at least one modifiable reactive group selected from the group con- sisting of amino, hydroxy, cis OH, halides, aryl, imidazoyl, carbonyl, carboxy, thiol or a residue com- prising an activated carbon; -X- is selected from the group consisting of -NH-?-, -NH-?-, -N=N-, -NHSO2-, -OSO2-, -NH-N=N-, -NH-?-CH2-NH-, -CH2-NH-, -O-?-, -NH-?-CH2-S- -NH-CH2-, O-?-CH2, -S-CH2-, -O-CO-NH- -R1- is Image , Image or a C1-C10 branched or unbranched alkyl or aralkyl, which may be substituted by -OH; -Y- is a direct bond to -E-, or -Y- is -E-R2- where R2 is a C1-C10 branched or unbranched alkyl; Za is chlorine, bromine or io- dine E is O, NH or an acyclic divalent sulfur atom; Detb is a chemical moiety capable of being de- tected, preferably comprising biotin or a metal chela- tor of the formula: Image or the 4-hydroxy or acyloxy derivative thereof, where R3 is C1-C4 alkyl or CH2COOM, M it the same or dif- ferent and selected from the group consisting of hy- drogen, a metal or non-metal cation or is C1-C10 alkyl, aryl or aralkyl; and m is an integer from 1 to the total number of modified reactive groups on A3. She detectable molecoles are useful in in vitro or in vivo assays or therapy.

472862

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