发明名称 |
TRICARBONYL TECHNETIUM-99M OR RHENIUM-188 LABEL RING RGD DERIVATIVE, A PREPARATION METHOD THEREOF, AND A PHARMACEUTICAL COMPOSITION CONTAINING THE DERIVATIVE AS AN ACTIVE INGREDIENT FOR USE IN THE DIAGNOSIS OR TREATMENT OF ANGIOGENESIS-RELATED DISEASES |
摘要 |
The present invention relates to a tricarbonyl technetium-99m or rhenium-188 label ring RGD derivative, a preparation method thereof, and a pharmaceutical composition containing the derivative as an active ingredient for use in the diagnosis or treatment of angiogenesis-related diseases. The tricarbonyl technetium-99m or rhenium-188 label ring RGD derivative of the present invention has a high subnanomolar affinity to avss3 integrin (also called as a vitronectin receptor that is activated in an angiogenic action induced by a tumor, reflects a high tumor image after an animal in which cancer cells are transplanted received an initial intake of the tricarbonyl technetium-99m label ring RGD derivative, and acts exclusively upon cancer cells having selectively activated avss3 integrin because of a substantially low intake into the liver and intestines,; compared to existing known radioactive isotope label ring RGD derivatives. These results show that the rhenium-188 label derivative, a therapeutic nuclide using the same precursor as used in the technetium-99m label, effectively inhibits the growth of a tumor and demonstrates therapeutic efficacy when administered via tail vein injection to an animal model of a tumor, compared to a case where only saline has been injected, thereby making it useful as a medicine for the diagnosis or treatment of angiogenesis-related diseases. |
申请公布号 |
EP2583966(B1) |
申请公布日期 |
2016.08.10 |
申请号 |
EP20110786882 |
申请日期 |
2011.05.24 |
申请人 |
BIO IMAGING KOREA CO., LTD. |
发明人 |
LEE, BYUNG CHUL;KIM, SANG EUN;KIM, JI SUN;MOON, BYUNG SEOK;JUNG, JAE HO |
分类号 |
C07D273/06;A61K31/5395;A61K51/04;A61K51/08;A61P35/00;C07D498/06;C07D498/16;C07K7/64;G01N33/574;G01N33/60 |
主分类号 |
C07D273/06 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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