公开(公告)号：US08124054B2

公开(公告)日：2012-02-28

申请号：US12409288

申请日：2009-03-23

申请人： Young-Don Hong ,  Sun-Ju Choi ,  So-Young Lee ,  Kang-Hyuk Choi

发明人： Young-Don Hong ,  Sun-Ju Choi ,  So-Young Lee ,  Kang-Hyuk Choi

IPC分类号： A61K51/00 ,  A61M36/14

CPC分类号： C07K14/685 ,  A61K51/086 ,  A61K51/088

摘要： Disclosed are chelating agent-conjugated α-MSH peptide derivatives, preparation methods thereof, and compositions for use in a diagnosis or treatment of a melanoma tumor containing the same as an active ingredient. The novel α-MSH peptide derivatives conjugated with chelating agent according to the present invention are highly selective to the melanocortin-1 receptor which is α-MSH receptor expressing in melanoma tumor and their labeling rate of a radioactive isotope is high. Also, they remain in kidney shortly and have high taking rate of the melanoma tumor. Therefore, with the aforesaid reasons, they may be effectively used for early diagnosis or treatment of melanoma tumor.

摘要翻译： 公开了螯合剂缀合的α-MSH肽衍生物，其制备方法和用于诊断或治疗含有其作为活性成分的黑素瘤肿瘤的组合物。 与根据本发明的螯合剂缀合的新型α-MSH肽衍生物对黑素细胞-1受体具有高选择性，黑素皮质素-1受体是黑素瘤肿瘤中表达的α-MSH受体，并且其放射性同位素的标记率高。 此外，他们很快就保持在肾脏，并且具有高的黑色素瘤肿瘤的摄入率。 因此，由于上述原因，它们可以有效地用于黑色素瘤肿瘤的早期诊断或治疗。

公开(公告)号：US20090304586A1

公开(公告)日：2009-12-10

申请号：US12409288

申请日：2009-03-23

申请人： Young-Don Hong ,  Sun-Ju Choi ,  So-Young Lee ,  Kang-Hyuk Choi

发明人： Young-Don Hong ,  Sun-Ju Choi ,  So-Young Lee ,  Kang-Hyuk Choi

IPC分类号： A61K51/08 ,  C07K7/00 ,  A61K103/32 ,  A61K103/10 ,  A61K103/20 ,  A61K103/00

CPC分类号： C07K14/685 ,  A61K51/086 ,  A61K51/088

摘要： Disclosed are chelating agent-conjugated α-MSH peptide derivatives, preparation methods thereof, and compositions for use in a diagnosis or treatment of a melanoma tumor containing the same as an active ingredient. The novel α-MSH peptide derivatives conjugated with chelating agent according to the present invention are highly selective to the melanocortin-1 receptor which is α-MSH receptor expressing in melanoma tumor and their labeling rate of a radioactive isotope is high. Also, they remain in kidney shortly and have high taking rate of the melanoma tumor. Therefore, with the aforesaid reasons, they may be effectively used for early diagnosis or treatment of melanoma tumor.

摘要翻译： 公开了螯合剂缀合的α-MSH肽衍生物，其制备方法和用于诊断或治疗含有其作为活性成分的黑素瘤肿瘤的组合物。 与根据本发明的螯合剂缀合的新型α-MSH肽衍生物对黑皮质素-1受体具有高度选择性，黑素皮质素-1受体是黑素瘤肿瘤中表达的α-MSH受体，并且其放射性同位素的标记率高。 此外，他们很快就保持在肾脏，并且具有高的黑色素瘤肿瘤的摄入率。 因此，由于上述原因，它们可以有效地用于黑色素瘤肿瘤的早期诊断或治疗。

公开(公告)号：US20090246128A1

公开(公告)日：2009-10-01

申请号：US12270932

申请日：2008-11-14

申请人： Sun-Ju Choi ,  Young-Don Hong ,  So-Young Lee ,  Sun-Ha Yoon ,  Hong Kwon Kim

发明人： Sun-Ju Choi ,  Young-Don Hong ,  So-Young Lee ,  Sun-Ha Yoon ,  Hong Kwon Kim

IPC分类号： A61K51/10 ,  A61P35/04

CPC分类号： G01N33/505 ,  A61K51/103 ,  G01N33/5052 ,  G01N33/538 ,  G01N33/54313

摘要： A radio-immunoconjugate for diagnosis and treatment of cancer or metastasis and development of metastasis inhibitory formulations using the same is provided. Also, a radio-immunoconjugate is used as a material indicating a metastatic cancer that has antibody marked with any lanthanum radionuclide and/or gamma, beta or alpha ray emitting radioisotopes targeting a vascular endothelial growth factor receptor (VEGFR) is provided. Such a radio-immunoconjugate is advantageous in that it maintains structural stability of a protein and immune activity thereof and is effectively adsorbed to the surface of vascular endothelial cells. This makes it useful as a pre-metastatic site detection factor. When the radio-immunoconjugate is administered to an animal model with cancer, the radio-immunoconjugate is accumulated in cancerous tissues. Therefore, it is useful for development of radioactive metastasis inhibitory formulations.

摘要翻译： 提供了用于诊断和治疗癌症或转移的放射性免疫缀合物以及使用其的转移抑制性制剂的开发。 此外，使用放射免疫缀合物作为指示具有用任何放射性核素和/或靶向血管内皮生长因子受体（VEGFR）的γ，β或α射线放射性同位素标记的抗体的转移性癌症的材料。 这样的放射性免疫偶联物的优点在于它保持蛋白质的结构稳定性和其免疫活性，并且有效地吸附到血管内皮细胞的表面。 这使得它作为转移前位点检测因子是有用的。 当将放射性免疫缀合物施用于具有癌症的动物模型时，放射性免疫缀合物积累在癌组织中。 因此，对放射性转移抑制剂的开发是有用的。

公开(公告)号：US07666390B2

公开(公告)日：2010-02-23

申请号：US11411643

申请日：2006-04-25

申请人： Young-Don Hong ,  Sun-Ju Choi ,  Ok Ja Choi

发明人： Young-Don Hong ,  Sun-Ju Choi ,  Ok Ja Choi

IPC分类号： A61K51/00 ,  A61K49/04 ,  A61M36/14 ,  A61B5/055 ,  C07F5/00

CPC分类号： A61K49/0002 ,  A61K49/0438 ,  A61K49/103 ,  A61K51/0478 ,  C07C237/46

摘要： The present invention relates to diethylenetriamine pentaacetic acid (DTPA) derivates and metal complexes thereof, and radiation sources and contrast agents including the metal complexes. More particularly, the present invention relates to DTPA derivatives, which contain iodine and are useful as contrast agents for diagnosing renal function, metal complexes of the DTPA derivatives with 99mTc, 166Ho, 111In, 90Y, 153Sm, 186Re, 188Re, 68Ga, or 177Lu, which are useful as liquid radiation sources for treating vascular stenosis and contrast agents for diagnosing renal function, and radiation sources and contrast agents including the metal complexes. The DTPA derivatives and metal complexes thereof are safe because the metal complexes are excreted via the kidneys and bladder within several minutes from the time of use as liquid radiation sources for treating vascular stenosis, and are cost-effective because they are potentially useful as contrast agents and as agents for diagnosing renal function.

摘要翻译： 本发明涉及二亚乙基三胺五乙酸（DTPA）衍生物及其金属络合物，以及包括金属络合物的辐射源和造影剂。 更具体地，本发明涉及含有碘的DTPA衍生物，其可用作诊断肾功能的造影剂，DTPA衍生物与99mTc，166Ho，111In，90Y，153Sm，186Re，188Re，68Ga或177Lu的金属络合物 ，其可用作用于治疗血管狭窄的液体辐射源和用于诊断肾功能的造影剂，以及包括金属络合物的辐射源和造影剂。 DTPA衍生物及其金属络合物是安全的，因为金属络合物在用作治疗血管狭窄的液体辐射源之后的几分钟内通过肾和膀胱排出，并且是成本有效的，因为它们潜在地用作造影剂 并作为诊断肾功能的药剂。

公开(公告)号：US20060251583A1

公开(公告)日：2006-11-09

申请号：US11411643

申请日：2006-04-25

申请人： Young-Don Hong ,  Sun-Ju Choi ,  Ok Choi

发明人： Young-Don Hong ,  Sun-Ju Choi ,  Ok Choi

IPC分类号： A61K49/10 ,  C07F5/00

CPC分类号： A61K49/0002 ,  A61K49/0438 ,  A61K49/103 ,  A61K51/0478 ,  C07C237/46

摘要： The present invention relates to diethylenetriamine pentaacetic acid (DTPA) derivates and metal complexes thereof, and radiation sources and contrast agents including the metal complexes. More particularly, the present invention relates to DTPA derivatives, which contain iodine and are useful as contrast agents for diagnosing renal function, metal complexes of the DTPA derivatives with 99mTc, 166Ho, 111In, 90Y, 153Sm, 186Re, 188Re, 68Ga, or 177Lu, which are useful as liquid radiation sources for treating vascular stenosis and contrast agents for diagnosing renal function, and radiation sources and contrast agents including the metal complexes. The DTPA derivatives and metal complexes thereof are safe because the metal complexes are excreted via the kidneys and bladder within several minutes from the time of use as liquid radiation sources for treating vascular stenosis, and are cost-effective because they are potentially useful as contrast agents and as agents for diagnosing renal function.

摘要翻译： 本发明涉及二亚乙基三胺五乙酸（DTPA）衍生物及其金属络合物，以及包括金属络合物的辐射源和造影剂。 更具体地，本发明涉及含有碘的DTPA衍生物，其可用作诊断肾功能的造影剂，DTPA衍生物与99m Tc的金属配合物， Ho，111 In，90 Y，153 Sm，186 Re，188和/ Re，68 Ga或177 Lu，其可用作用于治疗血管狭窄的液体辐射源和用于诊断肾功能的造影剂，以及辐射源和造影剂，包括 金属配合物。 DTPA衍生物及其金属络合物是安全的，因为金属络合物在用作治疗血管狭窄的液体辐射源之后的几分钟内通过肾和膀胱排出，并且是成本有效的，因为它们潜在地用作造影剂 并作为诊断肾功能的药剂。