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Details for Patent: 5,736,122

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Details for Patent: 5,736,122

Title: Technetium-99m labeled peptides for thrombus imaging
Abstract:This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to specific binding peptides, methods and kits for making such peptides, and methods for using such peptides labeled with technetium-99m via a radiolabel-binding moiety covalently linked to the peptide to image thrombus sites in a mammalian body.
Inventor(s): Dean; Richard T. (Bedford, NH), Lister-James; John (Bedford, NH)
Assignee: Diatide, Inc. (Londonberry, NH)
Filing Date:Jun 07, 1995
Application Number:08/482,880
Claims:1. A reagent for preparing a thrombus imaging agent for imaging a thrombus within a mammalian body comprising a specific binding peptide having an amino acid sequence of 4 to 100 amino acids and a technetium-99m binding moiety covalently linked to the specific binding peptide, wherein the peptide binds to a component of a thrombus, the technetium-99m binding moiety being selected from the group consisting of moieties having formula:

wherein C(pgp).sup.S is a cysteine having a protected thiol group and (aa) is any primary .alpha.- or .beta.-amino acid;

a moiety comprising a single thiol moiety of formula

wherein

A is H, HOOC, H.sub.2 NOC, or --NHOC;

B is SH or NHR";

X is H, methyl, SH or NHR";

Z is H or methyl;

R and R' are independently H or lower alkyl;

R" is H, lower alkyl or --C.dbd.O;

n is 0, 1 or 2;

and

where B is NHR", X is SH, Z is H and n is 1 or 2;

where X is NHR", B is SH, Z is H and n is 1 or 2;

where B is H, A is HOOC, H.sub.2 NOC, or --NHOC, X is SH, Z is H and n is 0 or 1;

where Z is methyl, X is methyl, A is HOOC, H.sub.2 NOC, or --NHOC, B is SH and n is 0;

and wherein the thiol moiety is in the reduced form; ##STR17## wherein X.dbd.H or a protecting group;

(amino acid)=any amino acid; ##STR18## wherein each R is independently H, CH.sub.3 or C.sub.2 H.sub.5 ;

each (pgp).sup.S is independently a thiol protecting group or H;

m, n and p are independently 2 or 3;

A=linear or cyclic lower alkyl, aryl, heterocyclyl, combinations or substituted derivatives thereof;

and ##STR19## wherein each R is independently H, CH.sub.3 or C.sub.2 H.sub.5 ;

m, n and p are independently 2 or 3;

A=linear or cyclic lower alkyl, aryl, heterocyclyl, combinations or substituted derivatives thereof;

V.dbd.H or --CO--peptide;

R'.dbd.H or peptide;

and wherein when V.dbd.H, R'.dbd.peptide and when R'.dbd.H, V.dbd.--CO--peptide;

wherein each R is independently H, lower alkyl having 1 to 6 carbon atoms, phenyl, or phenyl substituted with lower alkyl or lower alkoxy, and wherein each n is independently 1 or 2; and

wherein the technetium-99m binding moiety forms a complex with technetium-99m and the complex of the radiolabel-binding moiety and technetium-99m is electrically neutral;

wherein the reagent is radiolabeled with technetium-99m.

2. A complex formed by reacting the reagent of claim 1 with technetium-99m in the presence of a reducing agent.

3. The complex of claim 2, wherein the reducing agent is selected from the group consisting of a dithionite ion, a stannous ion and a ferrous ion.

4. A complex formed by labeling the reagent of claim 1 with technetium-99m by ligand exchange of a prereduced technetium-99m complex.

5. A method for labeling a reagent according to claim 1 comprising reacting the reagent with technetium-99m in the presence of a reducing agent.

6. The method of claim 5, wherein the reducing agent is selected from the group consisting of a dithionite ion, a stannous ion and a ferrous ion.
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