US4849208A
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Detectable molecules, method of preparation and use
Assignee: Enzo Therapeutics Inc
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Filing: 1987-04-28
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Granted: 1989-07-18
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Expires: 2007-04-28
Abstract
Abstract A detectable molecule of the formula A3-(-X-R1-E-Detb)m wherein A3 is A2 or a polymer, where A3 has at least one modifiable reactive group selected from the group consisting of amino, hydroxy, cis .OH, halides, aryl, imidazoly, carbonyl, carboxy, thiol or a residue comprising an activated carbon; -X- is selected from the group consisting of <IMAGE> <IMAGE> <IMAGE> <IMAGE> OCONH +TR <IMAGE> 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 iodine; E is O, NH or an acyclic divalent sulfur atom; Detb is a chemical moiety capable of being detected, preferably comprising biotin or a metal chelator of the formula: <IMAGE> or the 4-hydroxy or acyloxy derivative thereof, where R3 is C1-C4 alkyl or CH2COOM, M is the same or different and selected from the group consisting of hydrogen, a metal or non-metal cation or is C1-C10 alkyl, aryl or aralkyl; and mm is an integer from 1 to the total number of modified reactive groups on A3. The detectable molecules are useful in in vitro or in vivo assays or therapy.
Inventors
- 👤 Jannis G. Stavrianopoulos
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-04 15:01
CPC Classifications
A; A61; A61K; A61K51/00; A61K51/02; A61K51/04; A61K51/0497; A61K51/08; A61K51/10; A61K51/1093; G; G01; G01N; G01N33/00; G01N33/48; G01N33/50; G01N33/53; G01N33/531; G01N33/532; G01N33/533; G01N33/543; G01N33/551; G01N33/553
Claims Analysis
Total Claims: 6
Claim 1
Independent Claim
215 words
An imaging procedure which comprises: administering to an individual a detectable molecule of the formula A 3 --(X--R 1 --E--Det b ) m where A 3 is A 2 or a polymer, both A 2 and the polymer having at least one modifiable reactive group consisting of amino, hydroxy, cis OH, halide, aryl, imidazoyl, carbonyl, carboxyl, thiol or a residue comprising an activated carbon; A 2 is a specific binding ligand having a molecular weight of less than about 2,000; --X-- is selected from the group consisting of ##STR52## or 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 O, NH or an acyclic divalent sulfur atom; Det b is a metal chelator which has the formula: ##STR53## or the 4-hydroxy or acyloxy derivative thereof, where R3 is Cl-C4 alkyl or is --CH2--COOM, and each M is a metal or non-metal cation; and m is an integer from 1 to the total number of modified reactive groups on A 3 ; and, thereafter, observing the distribution of said compound in said individual.
Claim 2
Dependent Claim
215 words
An imaging procedure which comprises: administering to an individual a detectable molecule of the formula A 3 --(X--R 1 --E--Det b ) m where A 3 is A 2 or a polymer, both A 2 and the polymer having at least one modifiable reactive group consisting of amino, hydroxy, cis OH, halide, aryl, imidazoyl, carbonyl, carboxyl, thiol or a residue comprising an activated carbon; A 2 is a specific binding ligand having a molecular weight of less than about 2,000; --X-- is selected from the group consisting of ##STR52## or 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 O, NH or an acyclic divalent sulfur atom; Det b is a metal chelator which has the formula: ##STR53## or the 4-hydroxy or acyloxy derivative thereof, where R3 is Cl-C4 alkyl or is --CH2--COOM, and each M is a metal or non-metal cation; and m is an integer from 1 to the total number of modified reactive groups on A 3 ; and, thereafter, observing the distribution of said compound in said individual.
Claim 3
Dependent Claim
27 words
The imaging procedure of claim 1 which comprises administering said detectable molecule wherein Det b is a metal chelator having the formula and M is a radiometal.
Claim 4
Independent Claim
175 words
A method of radiation therapy which comprises administering to a human or animal situs a therapeutically effective amount of a radiometal chelated with a detectable molecule of the formula A 3 --(X--R 1 --E--Det b ) m where A 3 is an antibody specific for said human or animal situs --X-- is selected from the group consisting of ##STR54## or 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 unbranced alkyl; Z a is chlorine, bromine or iodine; --E-- is O, NH or an acyclic divalent sulfur atom; Det b is a metal chelator which has the formula: ##STR55## or the 4-hydroxy or acyloxy derivative thereof, where R3 is Cl-C4 alkyl or is --CH2--COOM, and each M is a metal or non-metal cation; and m is an integer from 1 to the total number of modified reactive groups on A 3 .
Claim 5
Independent Claim
175 words
A method of radiation therapy which comprises administering to a human or animal situs a therapeutically effective amount of a radiometal chelated with a detectable molecule of the formula A 3 --(X--R 1 --E--Det b ) m where A 3 is an antibody specific for said human or animal situs --X-- is selected from the group consisting of ##STR54## or 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 unbranced alkyl; Z a is chlorine, bromine or iodine; --E-- is O, NH or an acyclic divalent sulfur atom; Det b is a metal chelator which has the formula: ##STR55## or the 4-hydroxy or acyloxy derivative thereof, where R3 is Cl-C4 alkyl or is --CH2--COOM, and each M is a metal or non-metal cation; and m is an integer from 1 to the total number of modified reactive groups on A 3 .
Claim 6
Dependent Claim
13 words
The method of claim 3 wherein said antibody is a human monoclonal antibody.
References Cited (Backward Citations)
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