Labelled peptide compounds
AssigneeMallinckrodt Inc.
InventorsJohn Mertens, Dirk Tourwe, Marc Ceusters
Life of this patent
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AssigneeMallinckrodt Inc.
InventorsJohn Mertens, Dirk Tourwe, Marc Ceusters
Estimating the term…
The invention relates to a labelled peptide compound, wherein the peptide has a selective neurotensin receptor affinity and is represented by the general formula R.sub.1 -(.sup.1 Pro).sub.n -.sup.2 Xaa-.sup.3 Xbb-.sup.4 Xcc-.sup.5 Xdd-.sup.6 Xee-.sup.7 Leu-OH (SEQ ID NO:2) (I) wherein: R.sub.1 is a (C.sub.1 -C.sub.3)alkanoyl group, an arylcarbonyl group, an aryl-(C.sub.1 -C.sub.3)alkanoyl group, or a chelating group attached by an amide bond or through a spacing group to the peptide molecule; Xaa and Xbb are each individually Arg or Lys; Xcc is an unsubstituted or substituted cyclic amino acid, preferably selected from Pro and Hyp; Xdd is Tyr, Trp or Phe; Xee is Leu, Ile or t.-butylalanine; and n is 0 or 1; and wherein said peptide is labelled with (a) a metal isotope, or (b) with a radioactive halogen isotope; on the understanding that: (i) if the label is a metal isotope, R.sub.1 represents a chelating group for chelating said isotope; and (ii) if the label is a radioactive halogen isotope, said halogen isotope is attached to .sup.4 Tyr in the 2-position of the phenyl ring, to .sup.4 Trp, or to the aryl group of substituent R.sub.1.
A labelled peptide compound, wherein the peptide selectively binds to neurotensin receptors and is represented by the general formula
A kit for preparing a radiopharmaceutical composition, comprising
A kit for preparing a radiopharmaceutical composition, comprising (i) a peptide compound which selectively binds to neurotensin receptors and having the general formula II, to which compound, if desired, an inert pharmaceutically acceptable carrier and/or formulating agents and/or adjuvants is/are added, (ii) a reducing agent, and, if desired, a chelator, said ingredients (i) and (ii) optionally being combined, and (iii) instructions for use with a prescription for reacting the ingredients of the kit with .sup.99m Tc in the form of a pertechnetate solution or with .sup.186 Re or .sup.188 Re in the form of a perrhenate solution.
Dependencies are inferred from the claim text.