Compound binding to leukocytes and medicinal composition containing the compound in labeled state as the active ingredient
    1.
    发明申请
    Compound binding to leukocytes and medicinal composition containing the compound in labeled state as the active ingredient 失效
    化合物与白细胞结合,含有标记状态的化合物作为活性成分的药物组合物

    公开(公告)号:US20060057064A1

    公开(公告)日:2006-03-16

    申请号:US10528771

    申请日:2003-09-26

    IPC分类号: A61K51/00 A61K38/12

    摘要: A compound binding to leukocytes, which comprises Met-Leu-Phe or Nle-Leu-Phe serving as the leukocyte-binding site of a formyl peptide receptor (FPR), a binding part comprising Ser or Thr elevating the binding ratios to monocytes and lymphocytes in all leukocytes, a group which can be labeled with a radioactive metal or a paramagnetic metal, and a spacer binding them shows binding properties specific to all leukocytes, i.e., neutrophils, monocytes and lymphocytes both in vivo and in vitro and can be labeled with a radioactive metal or a paramagnetic metal. Owing to these characteristics, this compound is highly useful in SPECT image diagnosis, PET image diagnosis, MRI image diagnosis and so on wherein imaging is performed in a site with vigorous leukocyte infiltration accompanied by an immune reaction in an individual.

    摘要翻译: 与白细胞结合的化合物,其包含作为甲酰基肽受体(FPR)的白细胞结合位点的Met-Leu-Phe或Nle-Leu-Phe,包含Ser或Thr的结合部分提高与单核细胞和淋巴细胞的结合比 在所有的白细胞中,可以用放射性金属或顺磁性金属标记的基团和结合它们的间隔基团显示出对体内和体外所有白细胞,即嗜中性粒细胞,单核细胞和淋巴细胞特异性的结合特性,并且可以用 放射性金属或顺磁性金属。 由于这些特征,该化合物在SPECT图像诊断,PET图像诊断,MRI图像诊断等中非常有用,其中在具有伴随着个体的免疫反应的剧烈白细胞浸润的部位进行成像。

    Compound binding to leukocytes and medicinal composition containing the compound in labeled state as the active ingredient
    2.
    发明授权
    Compound binding to leukocytes and medicinal composition containing the compound in labeled state as the active ingredient 失效
    化合物与白细胞结合,含有标记状态的化合物作为活性成分的药物组合物

    公开(公告)号:US07220827B2

    公开(公告)日:2007-05-22

    申请号:US10528771

    申请日:2003-09-26

    IPC分类号: A61K38/04

    摘要: A compound that comprises Met-Leu-Phe or Nle-Leu-Phe serving as the leukocyte-binding site of a formyl peptide receptor (FPR), a binding part comprising Ser or Thr that increases the binding ratio to monocytes and lymphocytes in all leukocytes, a group that can be labeled with a radioactive metal or a paramagnetic metal, and spacers binding the three moieties together shows binding properties specific to all leukocytes, i.e., neutrophils, monocytes and lymphocytes both in vivo and in vitro. Owing to this characteristic, this compound is highly useful in SPECT image diagnosis, PET image diagnosis, MRI image diagnosis and the like, for imaging sites of inflammation.

    摘要翻译: 包含作为甲酰肽受体(FPR)的白细胞结合位点的Met-Leu-Phe或Nle-Leu-Phe的化合物,包含Ser或Thr的结合部分,其增加与所有白细胞中的单核细胞和淋巴细胞的结合比 ,可以用放射性金属或顺磁金属标记的基团,以及将三个部分结合在一起的间隔物在体内和体外都显示出对所有白细胞,即嗜中性粒细胞,单核细胞和淋巴细胞特异性的结合特性。 由于该特征,该化合物在SPECT图像诊断,PET图像诊断,MRI图像诊断等中对于炎症成像部位是非常有用的。

    Metal chelate forming peptides and use thereof
    3.
    发明授权
    Metal chelate forming peptides and use thereof 失效
    金属螯合物形成肽及其用途

    公开(公告)号:US5770178A

    公开(公告)日:1998-06-23

    申请号:US575863

    申请日:1995-12-20

    摘要: The invention provides a metal chelate forming peptide having an amino acid sequence of three amino acid residues represented by: X1-X2-Cys, wherein X1 represents an amino acid residue other than Cys residue; X2 represents an amino acid residue other than Cys residue and Pro residue; functional groups at the N-terminus, C-terminus and side chain may be substituted with protecting groups; and each of the amino acid residues may be any of D-form and L-form. Further, the invention provides a complex of the peptide with a physiologically active peptide, protein or other substance; a labeled reagent obtained by labeling the peptide or the complex with a metal radionuclide; and a radiodiagnostic and radiotherapeutic composition comprising the metal radionuclide-labeled reagent.

    摘要翻译: 本发明提供一种形成金属螯合物的肽,其具有由以下基团表示的三个氨基酸残基的氨基酸序列:X1-X2-Cys,其中X1表示除Cys残基以外的氨基酸残基; X2表示除Cys残基和Pro残基之外的氨基酸残基; N-末端,C-末端和侧链的官能团可以被保护基团取代; 并且每个氨基酸残基可以是D型和L-型中的任何一种。 此外,本发明提供了肽与生理活性肽,蛋白质或其他物质的复合物; 通过用金属放射性核素标记肽或配合物获得的标记试剂; 以及包含金属放射性核素标记试剂的放射诊断和放射治疗组合物。

    Tumor affinity peptide, and radioactive diagnostic agent and radioactive
therapeutic agent containing the peptide
    4.
    发明授权
    Tumor affinity peptide, and radioactive diagnostic agent and radioactive therapeutic agent containing the peptide 失效
    肿瘤亲和肽,放射性诊断剂和含有该肽的放射性治疗剂

    公开(公告)号:US5827498A

    公开(公告)日:1998-10-27

    申请号:US463230

    申请日:1995-06-05

    摘要: A peptide having affinity with tumor or a salt thereof, which comprises an amino acid sequence containing 20 or less amino acid residues, said amino acid sequence being described as X.sub.1 -YCAREPPT-X.sub.2 wherein A, C, E, P, R, T and Y represent amino acid residues expressed by standard one-letter symbols, each of amino acid residues A, C, R and Y in the amino acid sequence YCAR may be in either L-form or D-form, X.sub.1 represents a basic organic compound having 1-3 amino groups, and X.sub.2 represents any given amino acid sequence, is provided together with a radioactive diagnostic agent and a radioactive therapeutic agent containing the above peptide or a salt thereof. The present tumor affinity peptide is high in radioactive metal labeling yield, useful for imaging and treating pathological tissues such as of breast cancer, ovarian cancer and colon cancer of mammals including human, and difficult to be readily metabolized in organisms and to accumulate in normal tissues especially at kidney and liver.

    摘要翻译: 一种与肿瘤或其盐具有亲和力的肽,其包含含有20个或更少氨基酸残基的氨基酸序列,所述氨基酸序列描述为X1-YCAREPPT-X2,其中A,C,E,P,R,T和 Y代表由标准单字母符号表示的氨基酸残基,氨基酸序列YCAR中的氨基酸残基A,C,R和Y中的每一个可以是L-型或D-型,X1表示具有 1-3个氨基,X2代表任何给定的氨基酸序列,与放射性诊断剂和含有上述肽或其盐的放射性治疗剂一起提供。 本发明的肿瘤亲和肽具有放射性金属标记产率高,可用于成像和治疗诸如乳腺癌,卵巢癌和包括人在内的哺乳动物的结肠癌的病理组织,并且难以在生物体中代谢并积累在正常组织中 特别是在肾脏和肝脏。

    Compound accumulating in inflammatory site, diagnostic agent containing the compound in labeled state and its precursor compound for labeling
    9.
    发明授权
    Compound accumulating in inflammatory site, diagnostic agent containing the compound in labeled state and its precursor compound for labeling 有权
    化合物累积在炎症部位,含有标记状态的化合物的诊断剂及其前体化合物进行标记

    公开(公告)号:US09044520B2

    公开(公告)日:2015-06-02

    申请号:US13434722

    申请日:2012-03-29

    IPC分类号: A61K51/00 A61M36/14 A61K51/08

    CPC分类号: A61K51/088 G01N2800/042

    摘要: Embodiments of the invention provide a compound accumulating in an inflammatory site, a diagnostic agent containing the compound in labeled state and its precursor compound for labeling. Such a compound accumulating in inflammatory site may be represented by the following formula (1): Z—Y-Leu-Phe-(X)n-DLys(-(DLys)m-HalB)-(DLys)k-NH2  (1) wherein in the formula (1), Z represents a protective group for an amino group; Y represents Met or Nle; X represents a spacer consisting of one or more of amino acid and/or synthetic organic compounds; n represents 1 or 0; m represents 1 or 0; k represents 1 or 0; and HalB represents a substituted benzoic acid having a radioactive halogen in an aromatic ring.

    摘要翻译: 本发明的实施方案提供了一种在炎症部位中积聚的化合物,含有标记状态的化合物的诊断剂及其用于标记的前体化合物。 Z-Y-Leu-Phe-(X)n-DLys( - (DLys)m-HalB) - (DLys)k-NH 2(1)的化合物可以由下述式(1)表示: )其中在式(1)中,Z表示氨基的保护基; Y表示Met或Nle; X表示由一种或多种氨基酸和/或合成有机化合物组成的间隔物; n表示1或0; m表示1或0; k表示1或0; HalB表示在芳香环中具有放射性卤素的取代苯甲酸。