EP0154788A2
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EP
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Detectable molecules, method of preparation and use
Assignee: Enzo Biochem Inc
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Filing: 1985-01-29
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Granted: —
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Expires: 2005-01-29
Abstract
Abstract A detectable molecule of the formula where A 3 is A 2 or a polymer, where A3 has at least one modifiable reactive group selected from the group consisting of amino, hydroxy, cis OH, halides, aryl, imidazoyi, carbonyl, carboxy, thiol or a residue comprising an activated carbon; -X- is selected from the group consisting of a C 1 -C 10 branched or unbranched alkyl or aralkyl, which may be substituted by -OH; -Y- is a direct bond to -E-, or -Y- is -E-R 2 - where R 2 is a C 1 -C 10 branched or unbranched alkyl; Z a is chlorine, bromine or iodine; E is 0, NH or an acyclic divalent sulfur atom; Det b is a chemical moiety capable of being detected, preferably comprising biotin or a metal chelator of the formula: or the 4-hydroxy or acyloxy derivative thereof, where R 3 is C 1 -C 4 alkyl or CH 2 COOM, M is the same or different and selected from the group consisting of hydrogen, a metal or non-metal cation or is C,-C, o alkyl, aryl or aralkyl; and m is an integer from 1 to the total number of modified reactive groups on A 3 . The detectable molecules are useful in in vitro or in vivo assays or therapy.
Inventors
- 👤 Yannis Stavrianopoulos
Bibliographic Details
Application Number
—
Jurisdiction
EP
Data Source
google_patents
Last Synchronized
2026-10-30 01:08
CPC Classifications
G; G01; G01N; G01N33/00; G01N33/48; G01N33/50; G01N33/53; G01N33/531; G01N33/532; G01N33/534; A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0497; A61K51/08; A61K51/10; A61K51/1093; G01N33/533; G01N33/543; G01N33/551; G01N33/553
Claims Analysis
Total Claims: 32
Claim 1
Independent Claim
198 words
A detectable molecule of the formula A 3 -(-X-R 1 -E-Det b ) m characterized in that A3 is A 2 or a polymer or a polypeptide or a polysaccharide; A 2 , the polymer, the polypeptide or polysaccharide, having at least one modifiable reactive group selected from the group consisting of amino, hydroxy, cis-OH, halide, aryl, imidazoyl, carbonyl, carboxyl, thiol or a residue comprising an activated carbon; A 2 is a chemical entity having a molecular weight of less than about 2,000; -X- is selected from the group consisting of or a C 1 -C 10 branched or unbranched alkyl or aralkyl, which may be substituted by -OH; -Y- is a directed bond to -E-, or -Y- is -E-R 2- where - R 2 - is a C 1 -C 10 branched or unbranched alkyl; Z a is chlorine, bromine or iodine; -E- is 0, NH or an acyclic divalent sulfur atom; Det b is a chemical moiety capable of being detected, comprising biotin or a substituted or unsubstituted metal chelator or a compound capable of yielding a metal chelator; and m is an integer from 1 to the total number of modified reactive groups on A3.
Claim 2
Dependent Claim
198 words
A detectable molecule of the formula A 3 -(-X-R 1 -E-Det b ) m characterized in that A3 is A 2 or a polymer or a polypeptide or a polysaccharide; A 2 , the polymer, the polypeptide or polysaccharide, having at least one modifiable reactive group selected from the group consisting of amino, hydroxy, cis-OH, halide, aryl, imidazoyl, carbonyl, carboxyl, thiol or a residue comprising an activated carbon; A 2 is a chemical entity having a molecular weight of less than about 2,000; -X- is selected from the group consisting of or a C 1 -C 10 branched or unbranched alkyl or aralkyl, which may be substituted by -OH; -Y- is a directed bond to -E-, or -Y- is -E-R 2- where - R 2 - is a C 1 -C 10 branched or unbranched alkyl; Z a is chlorine, bromine or iodine; -E- is 0, NH or an acyclic divalent sulfur atom; Det b is a chemical moiety capable of being detected, comprising biotin or a substituted or unsubstituted metal chelator or a compound capable of yielding a metal chelator; and m is an integer from 1 to the total number of modified reactive groups on A3.
Claim 3
Dependent Claim
45 words
The molecule according to Claim 1, characterized in that said metal chelator has the formula: or the 4-hydroxy or acyloxy derivative thereof, where R 3 is C 1 -C 4 alkyl or is -CH 2 -COOM, and each M is a metal or non-metal cation.
Claim 4
Dependent Claim
24 words
The molecule according to Claim 1, characterized in that said Det b is selected from the group of compounds consisting of the formulae: and
Claim 5
Dependent Claim
23 words
The molecule according to Claim 2, characterized in that Det b is selected from the group of compounds consisting of the formulae: and
Claim 6
Dependent Claim
69 words
A detectable molecule of the formula characterized in that A 1 is a compound of MW less than about 2,000 and is not a monosaccharide or a mononucleotide; and Det a is a biotin or a detectable chemical moiety comprising a substituted or unsubstituted metal chelator or a compound capable of yielding a metal chelator; where "..." indicates a covalent link between - 1 and De t a .
Claim 7
Dependent Claim
69 words
A detectable molecule of the formula characterized in that A 1 is a compound of MW less than about 2,000 and is not a monosaccharide or a mononucleotide; and Det a is a biotin or a detectable chemical moiety comprising a substituted or unsubstituted metal chelator or a compound capable of yielding a metal chelator; where "..." indicates a covalent link between - 1 and De t a .
Claim 8
Dependent Claim
67 words
A molecule of the formula: characterized in that A3 is A 2 or a polymer, both A 2 and the polymer having at least one modifiable reactive group selected from the group consisting of amino and a residue comprising an activated carbon; Z b is chlorine or bromine; and m is an integer from 1 to the total number of modified reactive groups on A 3 .
Claim 9
Dependent Claim
67 words
A molecule of the formula: characterized in that A3 is A 2 or a polymer, both A 2 and the polymer having at least one modifiable reactive group selected from the group consisting of amino and a residue comprising an activated carbon; Z b is chlorine or bromine; and m is an integer from 1 to the total number of modified reactive groups on A 3 .
Claim 10
Dependent Claim
117 words
A compound of the formula: or the 4-hydroxy or acyloxy derivative thereof, characterized in that R 3 is C 1 -C 4 alkyl or is -CH 2 COOM, each M is a metal or non-metal cation; -S- is divalent sulfur atom; and Q 2- is H ; branched or unbranched C 1 -C 10 alkyl or aralkyl which carries at least one group selected from the group consisting of -OH, -SH,-NH 2 , O -CONHNH2, or -C-L v , where L v is a displaceable leaving group; or Q 2 is where Zc is hydrogen, chlorine or bromine, and J is -NH 2 or - N 2 + CA - , where CA - is a counteranion.
Claim 11
Dependent Claim
117 words
A compound of the formula: or the 4-hydroxy or acyloxy derivative thereof, characterized in that R 3 is C 1 -C 4 alkyl or is -CH 2 COOM, each M is a metal or non-metal cation; -S- is divalent sulfur atom; and Q 2- is H ; branched or unbranched C 1 -C 10 alkyl or aralkyl which carries at least one group selected from the group consisting of -OH, -SH,-NH 2 , O -CONHNH2, or -C-L v , where L v is a displaceable leaving group; or Q 2 is where Zc is hydrogen, chlorine or bromine, and J is -NH 2 or - N 2 + CA - , where CA - is a counteranion.
Claim 12
Dependent Claim
19 words
The compound according to Claim 7, characterized in that it is selected from the group consisting of the formulae:
Claim 13
Dependent Claim
21 words
A compound of the formula: or its metal or non-metal cationic salts, or C 1 -C 10 alkyl esters or amides.
Claim 14
Dependent Claim
21 words
A compound of the formula: or its metal or non-metal cationic salts, or C 1 -C 10 alkyl esters or amides.
Claim 15
Dependent Claim
12 words
A compound of the formula or its metal or non-metal cationic salts.
Claim 16
Dependent Claim
12 words
A compound of the formula or its metal or non-metal cationic salts.
Claim 17
Dependent Claim
143 words
A compound of the formula: characterized in that P z is or metal or non-metal salt thereof; Q 1 is H or HO; BA is a modifiable purine or pyrimidine base; X is selected from the group consisting of or a C 1 -C 10 branched or unbranched alkyl or aralkyl which may be substituted by OH: -Y- is.a direct bond to -S-, or -Y- is -S-R 2- where -R 2- is a C 1 -C 10 branched or unbranched alkyl; Z a is chlorine, bromine or iodine; -S- is an acylic divalent sulfur atom; D et b is a chemical moiety capable of being detected, comprising biotin or a metal chelator of the formula: or the 4-hydroxy or acyloxy derivative thereof, where R 3 is C 1 -C 4 alkyl or -CH 2 COOM, each M is a metal or non-metal cation.
Claim 18
Dependent Claim
143 words
A compound of the formula: characterized in that P z is or metal or non-metal salt thereof; Q 1 is H or HO; BA is a modifiable purine or pyrimidine base; X is selected from the group consisting of or a C 1 -C 10 branched or unbranched alkyl or aralkyl which may be substituted by OH: -Y- is.a direct bond to -S-, or -Y- is -S-R 2- where -R 2- is a C 1 -C 10 branched or unbranched alkyl; Z a is chlorine, bromine or iodine; -S- is an acylic divalent sulfur atom; D et b is a chemical moiety capable of being detected, comprising biotin or a metal chelator of the formula: or the 4-hydroxy or acyloxy derivative thereof, where R 3 is C 1 -C 4 alkyl or -CH 2 COOM, each M is a metal or non-metal cation.
Claim 19
Dependent Claim
31 words
A compound of the formula: characterized in that P z is or metal or non-metal salts thereof; Q 1 is H or HO; and BA is modifiable purine or pyrimidine base.
Claim 20
Dependent Claim
31 words
A compound of the formula: characterized in that P z is or metal or non-metal salts thereof; Q 1 is H or HO; and BA is modifiable purine or pyrimidine base.
Claim 21
Dependent Claim
20 words
A compound of the formula: or metal or non-metal salts thereof, or C 1 -C 10 alkyl esters or amides.
Claim 22
Dependent Claim
20 words
A compound of the formula: or metal or non-metal salts thereof, or C 1 -C 10 alkyl esters or amides.
Claim 23
Independent Claim
63 words
A method of modifying a biopolymer and introducing a chlorine or bromine group thereinto, which biopolymer contains at least one residue comprising an activated carbon capable of coupling with a diazo compound, which method comprises: reacting under coupling conditions said biopolymer with a diazo compound of the formula: where CA - is an appropriate inert counteranion, and Z b is chlorine or bromine.
Claim 24
Independent Claim
63 words
A method of modifying a biopolymer and introducing a chlorine or bromine group thereinto, which biopolymer contains at least one residue comprising an activated carbon capable of coupling with a diazo compound, which method comprises: reacting under coupling conditions said biopolymer with a diazo compound of the formula: where CA - is an appropriate inert counteranion, and Z b is chlorine or bromine.
Claim 25
Dependent Claim
23 words
An assay or procedure utilizing a radiolabeled molecule comprising employing a molecule according to Claim 2, characterized in that M is a radiometal.
Claim 26
Dependent Claim
41 words
A radiometal which is chelated by a monoclonal antibody in position A3 in the molecule of Claim 1 for use in a method of radiation therapy comprising radiating an animal situs.with radiation emitted from said radiometal locally present at said situs.
Claim 27
Dependent Claim
31 words
A process for the preparation of a compound of the formula (I): or a metal or non-metal salt thereof, which comprises the step of hydroxybrominating a compound of the formula (II):
Claim 28
Dependent Claim
31 words
A process for the preparation of a compound of the formula (I): or a metal or non-metal salt thereof, which comprises the step of hydroxybrominating a compound of the formula (II):
Claim 29
Dependent Claim
100 words
A detectable molecule of the formula: wherein A4 is A 2 or a polymer, both A 2 and the polymer having at least one modifiable reactive group selected from the group consisting of amino, aryl, imidazoyl and a residue comprising an activated carbon; A 2 is a chemical entity having a molecular weight of less than about 2,000; j is an electron withdrawing group; K is a signal generating entity or a solid matrix; r is an integer from one to about two; and m is an integer from one to the total number of modified reactive groups on A4.
Claim 30
Dependent Claim
100 words
A detectable molecule of the formula: wherein A4 is A 2 or a polymer, both A 2 and the polymer having at least one modifiable reactive group selected from the group consisting of amino, aryl, imidazoyl and a residue comprising an activated carbon; A 2 is a chemical entity having a molecular weight of less than about 2,000; j is an electron withdrawing group; K is a signal generating entity or a solid matrix; r is an integer from one to about two; and m is an integer from one to the total number of modified reactive groups on A4.
Claim 31
Dependent Claim
38 words
A compound of the formula: wherein j is an electron withdrawing group; K is a signal generating entity or a solid matrix; CA - is a suitable counteranion; and n is an integer from one to about two.
Claim 32
Dependent Claim
38 words
A compound of the formula: wherein j is an electron withdrawing group; K is a signal generating entity or a solid matrix; CA - is a suitable counteranion; and n is an integer from one to about two.
References Cited (Backward Citations)
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