Linkers For Radiopharmaceutical Compounds
    34.
    发明申请
    Linkers For Radiopharmaceutical Compounds 审中-公开
    放射性药物化合物的接头

    公开(公告)号:US20110280802A1

    公开(公告)日:2011-11-17

    申请号:US13179035

    申请日:2011-07-08

    摘要: A new and improved method for extending the half life of pharmaceutical compounds for use in diagnostic imaging or therapy uses a novel linker to attach a diagnostic or therapeutic moiety to a targeting peptide or another diagnostic or therapeutic moiety. The resulting compound may have the general formula M-N—O—P-Q, wherein M is the diagnostic or therapeutic moiety, N—O—P is the linker of the present invention, and Q is the targeting peptide. In another embodiment the compounds may have the formula M-N—O—P-M, wherein M is independently a diagnostic or therapeutic moiety and N—O—P is the linker of the invention. Methods for imaging or treating a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound are further provided. Methods for radiotherapy of a patient using the compounds are further provided, as are methods for preparing a radiotherapeutic agent from the compounds.

    摘要翻译: 用于延长用于诊断成像或治疗的药物化合物的半衰期的新的和改进的方法使用新的接头将诊断或治疗部分附着于靶向肽或另一诊断或治疗部分。 所得化合物可具有通式M-N-O-P-Q,其中M为诊断或治疗部分,N-O-P为本发明的接头,Q为靶向肽。 在另一个实施方案中,化合物可以具有式M-N-O-P-M,其中M独立地是诊断或治疗性部分,N-O-P是本发明的接头。 还提供了使用本发明化合物对患者进行成像或治疗的方法。 还提供了用于从化合物制备诊断显像剂的方法和试剂盒。 还提供了使用该化合物的患者放射治疗的方法,以及从化合物制备放射治疗剂的方法。

    GASTRIN RELEASING PEPTIDE COMPOUNDS
    35.
    发明申请
    GASTRIN RELEASING PEPTIDE COMPOUNDS 审中-公开
    GASTRIN释放肽化合物

    公开(公告)号:US20110250133A1

    公开(公告)日:2011-10-13

    申请号:US12950720

    申请日:2010-11-19

    IPC分类号: A61K51/08 A61P43/00 C07K7/02

    CPC分类号: A61K51/088 C07K14/57572

    摘要: Methods and compositions for diagnosing, staging disease, monitoring therapeutic effect of drugs and imaging a patient are provided, including radiopharmaceutical formulations. Compositions comprising Ga-AMBA complexed with a radioactive isotope are provided; as are methods of imaging Gastrin Releasing Peptide receptor (GRP-R) bearing tissue and methods of diagnosing or staging disease in patients suspected of having disease associated with aberrant GRP-R function. Further, methods of monitoring therapeutic effect of a drug targeted to a receptor that crosstalks with GRP-R are provided; as are methods of pre-dosing/co-dosing non-target tissues containing GRP-R. Particularly, methods of monitoring activity of receptors and receptor pathways in vivo/in vitro by using a ligand that binds to the GRP-R are provided; as are methods of measuring the activity of a receptor or group of receptors and their associated pathways that exhibit crosstalk with the GRP-R by using such a ligand which is also detectable by external means.

    摘要翻译: 提供用于诊断,分期疾病,监测药物的治疗效果和成像患者的方法和组合物,包括放射性药物制剂。 提供了包含与放射性同位素复合的Ga-AMBA的组合物; 成像胃泌素释放肽受体(GRP-R)携带组织的成像方法以及疑似与异常GRP-R功能相关疾病的患者诊断或分期疾病的方法。 此外,提供监测靶向与GRP-R串扰的受体的药物的治疗效果的方法; 预先给药/共同给予含有GRP-R的非靶组织的方法也是如此。 特别地,提供了通过使用与GRP-R结合的配体来体内/体外监测受体和受体途径的活性的方法; 以及通过使用也可以通过外部手段检测的这种配体来测量与GRP-R显示串扰的受体或受体组及其相关途径的活性的方法。

    Linkers for radiopharmaceutical compounds
    36.
    发明授权
    Linkers for radiopharmaceutical compounds 失效
    放射性药物化合物的接头

    公开(公告)号:US07989417B2

    公开(公告)日:2011-08-02

    申请号:US10542396

    申请日:2003-12-24

    IPC分类号: A61K38/28

    摘要: A new and improved method for extending the half life of pharmaceutical compounds for use in diagnostic imaging or therapy uses a novel linker to attach a diagnostic or therapeutic moiety to a targeting peptide or another diagnostic or therapeutic moiety. The resulting compound may have the general formula M-N-O-P-Q, wherein M is the diagnostic or therapeutic moiety, N-O-P is the linker of the present invention, and Q is the targeting peptide. In another embodiment the compounds may have the formula M-N-O-P-M, wherein M is independently a diagnostic or therapeutic moiety and N-O-P is the linker of the invention. Methods for imaging or treating a patient using the compounds of the invention are also provided. Methods and kits for preparing a diagnostic imaging agent from the compound are further provided. Methods for radiotherapy of a patient using the compounds are further provided, as are methods for preparing a radiotherapeutic agent from the compounds.

    摘要翻译: 用于延长用于诊断成像或治疗的药物化合物的半衰期的新的和改进的方法使用新的接头将诊断或治疗部分附着于靶向肽或另一诊断或治疗部分。 所得化合物可具有通式M-N-O-P-Q,其中M为诊断或治疗部分,N-O-P为本发明的接头,Q为靶向肽。 在另一个实施方案中,化合物可以具有式M-N-O-P-M,其中M独立地是诊断或治疗性部分,N-O-P是本发明的接头。 还提供了使用本发明化合物对患者进行成像或治疗的方法。 还提供了用于从化合物制备诊断显像剂的方法和试剂盒。 还提供了使用该化合物的患者放射治疗的方法,以及从化合物制备放射治疗剂的方法。

    GASTRIN RELEASING PEPTIDE COMPOUNDS
    40.
    发明申请
    GASTRIN RELEASING PEPTIDE COMPOUNDS 审中-公开
    GASTRIN释放肽化合物

    公开(公告)号:US20130136691A1

    公开(公告)日:2013-05-30

    申请号:US12993620

    申请日:2009-05-19

    IPC分类号: A61K51/08

    摘要: Methods and compositions for diagnosing, staging disease, monitoring therapeutic effect of drugs and imaging a patient are provided, including radiopharmaceutical formulations. Compositions comprising Ga-AMBA complexed with a radioactive isotope are provided; as are methods of imaging Gastrin Releasing Peptide receptor (GRP-R) bearing tissue and methods of diagnosing or staging disease in patients suspected of having disease associated with aberrant GRP-R function. Further, methods of monitoring therapeutic effect of a drug targeted to a receptor that crosstalks with GRP-R are provided; as are methods of pre-dosing/co-dosing non-target tissues containing GRP-R. Particularly, methods of monitoring activity of receptors and receptor pathways in vivo/in vitro by using a ligand that binds to the GRP-R are provided; as are methods of measuring the activity of a receptor or group of receptors and their associated pathways that exhibit crosstalk with the GRP-R by using such a ligand which is also detectable by external means.

    摘要翻译: 提供用于诊断,分期疾病,监测药物的治疗效果和成像患者的方法和组合物,包括放射性药物制剂。 提供了包含与放射性同位素复合的Ga-AMBA的组合物; 成像胃泌素释放肽受体(GRP-R)携带组织的成像方法以及疑似与异常GRP-R功能相关疾病的患者诊断或分期疾病的方法。 此外,提供监测靶向与GRP-R串扰的受体的药物的治疗效果的方法; 预先给药/共同给予含有GRP-R的非靶组织的方法也是如此。 特别地,提供了通过使用与GRP-R结合的配体来体内/体外监测受体和受体途径的活性的方法; 以及通过使用也可以通过外部手段检测的这种配体来测量与GRP-R显示串扰的受体或受体组及其相关途径的活性的方法。