АЙВИСОН Питер Брайан (GB),БХАЛЛА Раджив (AU),АЙНДРЕВОЛЛ Бард (NO),ГЕТВОЛЬДСЕН Гарет (GB)
申请号：
RU2013105491/04
公开号：
RU2013105491A
申请日:
2011.08.11
申请国别(地区):
RU
年份:
2014
代理人:
摘要：
1. The imaging agent comprising radioaktivnymF labeled cMet-binding cyclic peptide, wherein said cMet-binding cyclic peptide is a 18-30-mer cyclic peptide of formula I:, wherein cMBP (cMet-binding cyclic peptide) has the formula II:, wherein Q is the amino acid sequence (SEQ-1): -Cys-X-Cys-X-Gly-Pro-Pro-X-Phe-Glu-Cys-Trp-Cys-Tyr-XXX-, wherein X b is Asn, His or Tyr X b is Gly, Ser, Thr or Asn X b is Thr or Arg X g is Ala, Asp, Glu, Gly or Ser X b is Thr or Ser X b is Asp yl Glu and all Cyspredstavlyayut are cysteine residues so that residues a and b, and c and d are cyclized to form two separate disulfide bonds A and A independently represent any amino acid other than Cys, with the proviso that at least one of A and A is present and represents Lys x and y are independently an integer value from 0 to 13 and are selected so that the sum of x and y is from 1 to 13 Zprisoedinen to the N-end sMVR and represents H or M Zprisoedinen the C-terminus and sMVR represents OH, OBili M, where a BIOS Bpredstavlyaet Compatibility of the cation, and each represents a group Mnezavisimo inhibiting metabolism, which is a biocompatible group, an inhibitory or suppressing the metabolism sMVR peptide in vivo wherein sMVR posredstvomF labeled by the residue Lys or Groups A A.2. Imaging agent according to claim 1, wherein sMVR has the formula IIA: wherein z is an integer of value from 0 to 12 and the sum of x and z is from 0 to 12, and cMBP comprises only one Lys.3 residue. Imaging agent according to claim 1 or claim 2, wherein Q comprises the amino acid sequence of SEQ-2 or SEQ-3: Ser-Cys-X-Cys-X-Gly-Pro-Pro-X-Phe-Glu-Cys-Trp- cys-Tyr-X-1. Визуализирующий агент, содержащий меченый радиоактивным 18F cMet-связывающий циклический пептид,где указанный cMet-связывающий циклический пептид представляет собой 18-30-мерный циклический пептид формулы I:Z1−[cMBP]−Z2 (I) ,где cMBP (cMet-связывающий циклический пептид) имеет формулу II:−(A)x−Q−(A)y− (II) ,где
