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 formulawherein: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; andn 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 2-position 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 US6194386(B1) 申请公布日期 2001.02.27
申请号 US19990334254 申请日期 1999.06.16
申请人 MALLINCKRODT 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):A61K38/00 主分类号 A61K51/00
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