公开(公告)号：US20150025248A1

公开(公告)日：2015-01-22

申请号：US13947222

申请日：2013-07-22

申请人： ATOMIC ENERGY COUNCIL - INSTITUTE OF NUCLEAR ENERGY RESEARCH

发明人： SHOW-WEN LIU ,  YU CHANG ,  CHENG-FANG HSU ,  SHENG-LUN LIN ,  TSUNG-HSIEN CHIANG ,  CHIH-YUAN LIN

IPC分类号： C07F13/00 ,  C07D233/91

CPC分类号： C07F13/005 ,  C07D233/91

摘要： The present invention relates to a radiotracer precursor for imaging of hypoxic tissues, a radiotracer and a method for preparing the same. The radiotracer precursor, BANI, includes a nitroimidazole functional group with a feature of retention in hypoxic tissues and a bifunctional ligand able to complex with radioisotopes. Thus BANI can be used to produce radiotracers retained in hypoxic tissues and the radiotracers are applied to medical imaging of malignant tumor with hypoxic layer.

摘要翻译： 本发明涉及一种用于对缺氧组织进行成像的放射性示踪剂前体，一种放射性示踪剂及其制备方法。 放射性示踪剂前体BANI包括具有保留在缺氧组织中的特征的硝基咪唑官能团和能够与放射性同位素复合的双官能配体。 因此，BANI可用于产生保留在缺氧组织中的放射性示踪剂，放射性示踪剂用于具有缺氧层的恶性肿瘤的医学成像。

公开(公告)号：US20150252009A1

公开(公告)日：2015-09-10

申请号：US14200393

申请日：2014-03-07

申请人： ATOMIC ENERGY COUNCIL-INSTITUTE OF NUCLEAR ENERGY RESEARCH

发明人： YU CHANG ,  CHING-YUN LEE ,  TSUNG-HSIEN CHIANG ,  CHENG-FANG HSU

IPC分类号： C07D243/12

CPC分类号： C07D243/12

摘要： In a benzodiazepine derivative and a method of producing the derivative, isatoic anhydride or 5-chloroisatoic anhydride is reacted with amino acid ester hydrochloride for conducting a simple cyclization to obtain a produce with a low percentage of by-product directly without requiring the complicated separation and purification processes of column chromatography, and a chlorine-containing structure of the structure can improve the lipo-solubility and chlorine ion permeability and allow a functional group of a radioisotope to be modified to maximize the effects of the pharmacological properties such as the sedative, anticonvulsant and anti-spasmodic effects on the central nervous system or the benzodiazepine derivative can be used as a contrast agent of the system with excellent effects on applications.

摘要翻译： 在苯并二氮杂衍生物和衍生物的制造方法中，将丙酸酐或5-氯代酸酐与氨基酸酯盐酸盐反应，进行简单的环化，直接得到副产物的百分比低的产物，无需复杂的分离， 柱层析的纯化方法和结构的含氯结构可以改善脂溶性和氯离子渗透性，并允许改性放射性同位素的官能团以最大化药理学性质的影响，例如镇静剂，抗惊厥药 对中枢神经系统或苯并二氮杂衍生物的抗痉挛作用可用作系统的造影剂，对应用效果优异。

公开(公告)号：US20140371434A1

公开(公告)日：2014-12-18

申请号：US13920364

申请日：2013-06-18

申请人： ATOMIC ENERGY COUNCIL-INSTITUTE OF NUCLEAR ENERGY RESEARCH

发明人： SHOW-WEN LIU ,  YU CHANG ,  CHENG-FANG HSU ,  TSUNG-HSIEN CHIANG ,  SHENG-LUN LIN ,  CHIH-YUAN LIN

IPC分类号： A61K51/04

CPC分类号： A61K51/0478 ,  A61K51/0474

摘要： A radiotracer precursor for imaging of hypoxic tissues, a radiotracer and a method for preparing the same are revealed. The radiotracer precursor, DANI, includes a nitroimidazole functional group with a feature of retention in hypoxic tissues and a bifunctional ligand able to complex with radioisotopes. Thus DANI can be used to produce radiotracers stayed in hypoxic tissues and the radiotracers are applied to medical imaging of malignant tumor with hypoxic layer.

摘要翻译： 揭示了用于低氧组织成像的放射性示踪剂前体，放射性示踪剂及其制备方法。 放射性示踪剂前体DANI包括具有保留在缺氧组织中的特征的硝基咪唑官能团和能够与放射性同位素复合的双官能配体。 因此，DANI可用于产生放置在缺氧组织中的放射性示踪剂，放射性示踪剂用于具有缺氧层的恶性肿瘤的医学成像。