发明名称 LABELLED PEPTIDE COMPOUNDS
摘要 The invention relates to a labelled peptide compound, wherein the peptide has a selective neurotensin receptor affinity and is represented by the general formula (I): R1 - (1Pro)n - 2Xaa - 3Xbb -4Xcc - 5Xdd - 6Xee - 7Leu - OH, wherein R1 is a (C1-C3)alkanoyl group, an arylcarbonyl group, an aryl-(C1-C3)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, R1 represents a chelating group for chelating said isotope; and (ii) if the label is a radioactive halogen isotope, said halogen isotope is attached to 4Tyr in the 2position of the phenyl ring, to 4Trp, or to the aryl group of substituent R1. The invention further relates to a pharmaceutical composition comprising said labelled peptide compound, to the use of said composition for diagnosis and therapy, and to a kit for preparing a radiopharmaceutical composition.
申请公布号 CA2183421(A1) 申请公布日期 1995.08.24
申请号 CA19952183421 申请日期 1995.02.21
申请人 MALLINCKRODT MEDICAL, INC. 发明人 MERTENS, JOHN;TOURWE, DIRK;CEUSTERS, MARC
分类号 A61K51/00;A61K31/00;A61K38/00;A61K49/00;A61K51/08;A61P35/00;C07K1/13;C07K5/00;C07K5/06;C07K7/00;C07K7/06;C07K7/08;C07K17/00;(IPC1-7):C07K7/06 主分类号 A61K51/00
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