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Details for Patent: 6,667,389

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Details for Patent: 6,667,389

Title: Technetium-99m labeled peptides for imaging
Abstract:This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to peptides, methods and kits for making such peptides, and methods for using such peptides to image sites in a mammalian body labeled with technetium-99m (Tc-99m) via (Tc-99m) binding moieties. In particular, the peptide reagents of the invention are covalently linked to a polyvalent linker moiety, so that the polyvalent linker moiety is covalently linked to a multiplicity of the specific-binding peptides, and the Tc-99m binding moieties are covalently linked to a plurality of the specific-binding peptides, the polyvalent linker moiety, or to both the specific-binding peptides and the polyvalent linker moiety.
Inventor(s): Dean; Richard T. (Bedford, NH), Lister-James; John (Bedford, NH)
Assignee: Diatide, Inc. (Londonderry, NH)
Filing Date:Jul 08, 1997
Application Number:08/889,212
Claims:1. A reagent comprising: (a) a polyvalent linker; (b) at least two specific-binding peptides, each peptide having an amino acid sequence of 3 to 100 amino acids and being covalently linked to said linker; and (c) a technetium-99m binding moiety covalently linked to said linker.

2. The reagent of claim 1 further comprising technetium-99m.

3. The reagent of claim 1 wherein said technetium-99m binding moiety is selected from the group consisting of: I.

A.sup.1 --CZ.sup.1 (B.sup.1)--[C(R.sup.1 R.sup.2)].sub.n --X.sup.1 wherein A.sup.1 is H, HOOC, H.sub.2 NOC or --NHOC; B.sup.1 is SH or NHR.sup.3 ; X.sup.1 is H, methyl, SH or NHR.sup.3 ; Z.sup.1 is H or methyl; R.sup.1 and R.sup.2 are independently H or lower alkyl; R.sup.3 is H, lower alkyl or --C.dbd.O; and n is 0, 1 or 2; and when B.sup.1 is NHR.sup.3 : X.sup.1 is SH; Z.sup.1 is H; and n is 1 or 2; when X.sup.1 is NHR.sup.3 : B.sup.1 is SH; Z.sup.1 is H; and n is 1 or 2; when B.sup.1 is H: A.sup.1 is HOOC, H.sub.2 NOC or --NHOC; X.sup.1 is SH; Z.sup.1 is H; and n is 0 or 1; and when Z.sup.1 is methyl: X.sup.1 is methyl; A.sup.1 is HOOC, H.sub.2 NOC or --NHOC; B.sup.1 is SH; and n is 0;

and wherein said thiol moiety is in the reduced form; ##STR8## wherein X.sup.2 is H or a protecting group; and (amino acid)=any amino acid; ##STR9## wherein X.sup.2 is H or a protecting group; and (amino acid)=any amino acid; ##STR10## 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; and A.sup.2 is linear lower alkyl, cyclic lower alkyl, aryl, heterocyclyl, a combination thereof or a substituted derivative thereof;

and ##STR11## 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.sup.3 is linear lower alkyl, cyclic lower alkyl, aryl, heterocyclyl, a combination thereof or a substituted derivative thereof; V is H or --CO-peptide; and R.sup.4 is H or peptide; and when V is H: R.sup.4 is peptide; and when R.sup.4 is H: V is --CO-peptide.

4. The reagent of claim 3 wherein said technetium-99m binding moiety is

and (pgp).sup.s has a formula

wherein R is a lower alkyl having 1 to 6 carbon atoms, 2-pyridyl, 3-pyridyl, 4-pyridyl, phenyl, or phenyl substituted with lower alkyl, hydroxy, lower alkoxy, carboxy, or lower alkoxycarbonyl.

5. The reagent of claim 3 wherein said technetium-99m binding moiety has the formula: ##STR12##

6. The reagent of claim 1 wherein said linker comprises at least two identical functional groups capable of covalently bonding to the peptides or to the technetium-99m binding moiety.

7. The reagent of claim 6 wherein said functional groups are selected from the group consisting of primary amines, secondary amines, hydroxyl groups, carboxylic acid groups and thiol-reactive groups.

8. The reagent of claim 1 wherein said linker is a branched polyvalent linker.

9. The reagent of claim 1 wherein said peptide is chemically synthesized in vitro.

10. The reagent of claim 9 wherein said peptide is synthesized by solid phase peptide synthesis.

11. The reagent of claim 9 wherein said technetium-99m binding moiety is covalently linked to said peptide during in vitro chemical synthesis.

12. The reagent of claim 11 wherein said technetium-99m binding moiety is covalently linked to said peptide during solid phase peptide synthesis.

13. The reagent of claim 1 wherein said peptide comprises a linear peptide or a cyclic peptide.
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