公开(公告)号：US20080241063A1

公开(公告)日：2008-10-02

申请号：US11727996

申请日：2007-03-29

申请人： Tsai-Yueh Luo ,  Te-Sheng Liang ,  Chang-Mau Shing ,  Shiou-Shiow Farn ,  Wuu-Jyh Lin ,  Haw-Jan Chen

发明人： Tsai-Yueh Luo ,  Te-Sheng Liang ,  Chang-Mau Shing ,  Shiou-Shiow Farn ,  Wuu-Jyh Lin ,  Haw-Jan Chen

IPC分类号： A61K51/00 ,  C07C279/02

CPC分类号： A61K51/0406 ,  A61K51/1282 ,  C07C279/06

摘要： The present invention relates to a combination set of meta-iodobenzyl guanidine (MIBG) freezing crystal and making method thereof and method of radioactive marker for making. The combination set of freezing crystal includes a first container having freezing crystal and a second container having sodium acetate buffer solution. The method for making a combination set of freezing crystal includes the steps of mixing (meta-iodobenzyl guanidine)2·sulfuric acid and ammonium sulfate into first non-pyrogenic injection water; getting a first container having freezing crystal after freezing and drying; and getting a second container having the sodium acetate buffer solution after sterilizing. The method of radioactive marker for making includes the steps of adding radioactive iodine ion into freezing crystal to react and adding sodium acetate buffer solution to get radioactive MIBG solution. The present invention adjusts agent easily and is instant to use so the radioactive iodine marker don't lose activity easily before using it.

摘要翻译： 本发明涉及一种间碘碘苄基胍（MIBG）冷冻结晶的组合及其制备方法和放射性标记物的制备方法。 冷冻结晶组合包括具有冷冻晶体的第一容器和具有乙酸钠缓冲溶液的第二容器。 制备冷冻结晶组合的方法包括将（间碘碘苄基胍）亚磺酸和硫酸铵混合到第一非致热性注射水中的步骤; 在冷冻和干燥后得到具有冷冻晶体的第一容器; 并在灭菌后得到具有乙酸钠缓冲溶液的第二容器。 放射性标记物的制备方法包括将放射性碘离子加入冷冻结晶反应并加入乙酸钠缓冲溶液，得到放射性MIBG溶液的步骤。 本发明容易调节剂并且即时使用，所以放射性碘标记物在使用前不容易失去活性。

公开(公告)号：US5889146A

公开(公告)日：1999-03-30

申请号：US978615

申请日：1997-11-26

申请人： Te-Wei Lee ,  Shui-Tein Chen ,  Shiang-Rong Chang ,  Shyh-Yi Chyi ,  Chang-Mau Shing ,  Tian-Fu Huang ,  Lie-Hang Shen ,  Zei-Tsan Tsai ,  Kung-Tsung Wang ,  Gann Ting

发明人： Te-Wei Lee ,  Shui-Tein Chen ,  Shiang-Rong Chang ,  Shyh-Yi Chyi ,  Chang-Mau Shing ,  Tian-Fu Huang ,  Lie-Hang Shen ,  Zei-Tsan Tsai ,  Kung-Tsung Wang ,  Gann Ting

IPC分类号： A61K51/08 ,  C07K7/06 ,  A61K38/12 ,  C07K5/00 ,  C07K7/00 ,  C07K17/00

CPC分类号： C07K7/06 ,  A61K51/083 ,  A61K51/088 ,  A61K2123/00

摘要： This invention is a novel synthesis of BCA-peptides (BCA: bifunctional chelating agents). In this method, the starting material--Fmoc-Thr(ol)-Terephthal-Acetal-Amide Resin is coupled with the various amino acids. The straight peptide-resin of D-Phe-Cys(Trt)-Phe-D-Trp(Boc)-Lys(Boc)-Thr(tBu)-Cys(Trt)-Thr(ol)-Terephthal-Acetal-Amide Resin was obtained. This compound reacted with iodine to give disulfide-containing peptide resin of ##STR1## Cleavage of the peptide from the resin was achieved by TFA. The cleavaged peptide was protected by the reaction of octreotide with di-t-butyldicarbonate. BCA was coupled to the selectively protected octreotide. This product was obtained by reaction of protected BCA-peptides with TFA. The final product was labeled by radioisotope .sup.111 InCl.sub.3 for tumor imaging radiopharmaceuticals.

摘要翻译： 本发明是BCA肽（BCA：双功能螯合剂）的新型合成。 在该方法中，起始物质-Fmoc-Thr（ol） - 对 - 对 - 乙酰胺树脂与各种氨基酸偶联。 D-Phe-Cys（Trt）-Phe-D-Trp（Boc）-Lys（Boc）-Thr（tBu）-Cys（Trt）-Thr（ol） - 对 - 缩醛酰胺树脂的直链肽 - 树脂 获得。 该化合物与碘反应，得到含二硫化物的肽树脂，通过TFA实现了树脂中肽的切割。 通过奥曲肽与二碳酸二叔丁酯的反应来保护切割的肽。 BCA与选择性保护的奥曲肽偶联。 该产物通过保护的BCA-肽与TFA的反应获得。 最终产品用放射性同位素111InCl3标记用于肿瘤成像放射性药物。