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    Labelled peptide compounds
    3.
    发明授权
    Labelled peptide compounds 失效
    标记肽化合物

    公开(公告)号：US06194386B1

    公开(公告)日：2001-02-27

    申请号：US09334254

    申请日：1999-06-16

    申请人： John Mertens ,  Dirk Tourwe ,  Marc Ceusters

    发明人： John Mertens ,  Dirk Tourwe ,  Marc Ceusters

    IPC分类号： A61K3800

    CPC分类号： A61K51/08 ,  A61K38/00 ,  A61K51/085 ,  A61K51/088 ,  A61K2121/00 ,  A61K2123/00 ,  C07K7/083

    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 R1—(1Pro)n—2Xaa—3Xbb—4Xcc—5Xdd—6Xee—7Leu—OH(SEQ ID NO.2)  (I) 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 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.

    摘要翻译： 本发明涉及一种标记肽化合物，其中该肽具有选择性神经降压素受体亲和性，并由通式化合物代表：R1是（C1-C3）烷酰基，芳基羰基，芳基 - （C1-C3）烷酰基 基团或螯合基团，其通过酰胺键或间隔基团与肽分子连接; Xaa和Xbb各自为Arg或Lys; Xcc为未取代或取代的环状氨基酸，优选选自Pro和Hyp; Xdd为 Tyr，Trp或Phe; Xee是Leu，Ile或t.-丁基丙氨酸; andn为0或1;并且其中所述肽用（a）金属同位素或（b）与放射性卤素同位素标记; 理解为：（i）如果标记是金属同位素，则R1表示螯合所述同位素的螯合基团; 和（ii）如果标记是放射性卤素同位素，则所述卤素同位素与苯环的2位，4Trp或取代基R 1的芳基连接至4Tyr。本发明进一步涉及药物组合物 包括所述标记的肽化合物，用于所述用于诊断和治疗的组合物，以及用于制备放射性药物组合物的试剂盒。

    Labelled peptide compounds
    5.
    发明授权
    Labelled peptide compounds 失效
    标记肽化合物

    公开(公告)号：US5952464A

    公开(公告)日：1999-09-14

    申请号：US737299

    申请日：1997-07-21

    申请人： John Mertens ,  Dirk Tourwe ,  Marc Ceusters

    发明人： John Mertens ,  Dirk Tourwe ,  Marc Ceusters

    IPC分类号： A61K38/00 ,  A61K51/08 ,  C07K7/08 ,  A61K38/04 ,  A61K51/00

    CPC分类号： C07K7/083 ,  A61K51/085 ,  A61K51/088 ,  A61K2121/00 ,  A61K2123/00 ,  A61K38/00

    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 formulaR.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; 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, 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.

    摘要翻译： PCT No.PCT / US95 / 02131 Sec。 371日期1997年7月21日 102（e）日期1997年7月21日PCT提交1995年2月21日PCT公布。 WO95 / 22341 PCT出版物 日期：1995年8月24日本发明涉及一种标记肽化合物，其中该肽具有选择性神经降压素受体亲和性，并由通式R1-（1Pro）n-2Xaa-3Xbb-4Xcc-5Xdd-6Xee-7Leu-OH SEQ ID NO：2）（I）其中：R1是（C1-C3）烷酰基，芳基羰基，芳基 - （C1-C3）烷酰基或通过酰胺键连接的螯合基团或间隔 组分子肽分子; Xaa和Xbb各自为Arg或Lys; Xcc是未取代或取代的环状氨基酸，优选选自Pro和Hyp; Xdd是Tyr，Trp或Phe; Xee是Leu，Ile或叔丁基丙氨酸; 并且n为0或1; 并且其中所述肽用（a）金属同位素或（b）与放射性卤素同位素标记; 理解为：（i）如果标记是金属同位素，则R1表示螯合所述同位素的螯合基团; 和（ii）如果标记是放射性卤素同位素，则所述卤素同位素与苯环的2位，4Trp或取代基R 1的芳基连接至4Tyr。