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1. 发明授权

US09382202B2 Precursor for labeling therapeutic agent for liver cancer and method for manufacturing the same 有权
标题翻译：用于标记肝癌治疗剂的前体及其制造方法
公开(公告)号：US09382202B2
公开(公告)日：2016-07-05
申请号：US14272682
申请日：2014-05-08
申请人： ATOMIC ENERGY COUNCIL—INSTITUTE OF NUCLEAR ENERGY RESEARCH
发明人： Show-Wen Liu , Yu Chang , Cheng-Fang Hsu
IPC分类号： C07F13/00 , C07C323/25 , C07C319/20 , A61K51/04
CPC分类号： C07C323/25 , A61K51/0474 , A61K51/0478 , C07C319/20 , C07C323/60 , C07F13/00
摘要： A precursor for labeling therapeutic agents for liver cancer and a method for manufacturing the same are revealed. The chemical structure of the precursor has a ligand linked to complex compounds of radioisotopes. Moreover, the chemical structure of the precursor further includes a specific functional group soluble in Lipiodol or having properties of Lipiodol. Thus the radioisotopes attached to the precursor are allowed to retain in hepatic tissues of patients with liver cancer for internal radiation therapy of liver cancer.
摘要翻译：揭示了用于标记肝癌治疗剂的前体及其制造方法。前体的化学结构具有与放射性同位素的复合化合物连接的配体。此外，前体的化学结构还包括可溶于Lipiodol或具有Lipiodol性质的特定官能团。因此，将与前体连接的放射性同位素保留在肝癌患者的肝组织中，用于肝癌的内部放射治疗。

2. 发明授权

US09096623B1 Method for preparing radiotracer precursor SnADAM 有权
标题翻译：制备放射性示踪剂前体SnADAM的方法
公开(公告)号：US09096623B1
公开(公告)日：2015-08-04
申请号：US14272676
申请日：2014-05-08
申请人： ATOMIC ENERGY COUNCIL—INSTITUTE OF NUCLEAR ENERGY RESEARCH
发明人： Ching-Yun Lee , Yu Chang , Cheng-Fang Hsu , Yueh-Feng Deng
IPC分类号： C07F7/22
CPC分类号： C07F7/2208 , C07F15/0066
摘要： A method for preparing a radiotracer precursor SnADAM is revealed. The method overcomes shortcomings of conventional synthesis methods including lower yield rate and time-consuming. Moreover, Pd/C catalyst and hydrogen gas are used to catalyze reduction reaction for avoiding the generation of a large amount of intermediate products with similar structures. Thus there is no need to perform isolation and purification processes. The yield rate of the intermediate products is also increased so that its impact on the low yield rate of the final product SnADAM is minimized. A part of the reaction is significantly accelerated by using tris(dibenzylideneacetone)-dipalladium(0) (Pd2(dba)3) as a catalyst. Thus the production time of SnADAM is shortened.
摘要翻译：揭示了制备放射性示踪剂前体SnADAM的方法。该方法克服了常规合成方法的缺点，包括较低的产率和耗时。此外，Pd / C催化剂和氢气用于催化还原反应，以避免产生大量具有类似结构的中间产物。因此，不需要进行分离和纯化过程。中间产物的产率也增加，使其对最终产品SnADAM的低产率的影响最小化。通过使用三（二亚苄基丙酮） - 二钯（0）（Pd 2（dba）3）作为催化剂，反应的一部分显着加速。因此，SnADAM的生产时间缩短。

3. 发明授权

US09044519B2 Radiotracer precursor for imaging of hypoxic tissue, radiotracer, and method for preparing the same 有权
标题翻译：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
公开(公告)号：US09044519B2
公开(公告)日：2015-06-02
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： C07F13/00 , 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。

4. 发明授权

US09024035B2 Radiotracer precursor BANI for imaging of hypoxic tissue, radiotracer, and method for preparing the same 有权
标题翻译：用于低氧组织成像的放射性示踪剂前体BANI，放射性示踪剂及其制备方法
公开(公告)号：US09024035B2
公开(公告)日：2015-05-05
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。

5. 发明授权

US09580394B2 Benzodiazepine derivative and method of producing the same 有权
标题翻译：苯并二氮杂衍生物及其制备方法
公开(公告)号：US09580394B2
公开(公告)日：2017-02-28
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： C07D243/14 , 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。

6. 发明授权

US09227931B1 Bifunctional compound and method for manufacturing the same 有权
标题翻译：双功能化合物及其制造方法
公开(公告)号：US09227931B1
公开(公告)日：2016-01-05
申请号：US14445183
申请日：2014-07-29
申请人： ATOMIC ENERGY COUNCIL-INSTITUTE OF NUCLEAR ENERGY RESEARCH
发明人： Show-Wen Liu , Yu Chang , Cheng-Fang Hsu
IPC分类号： C07C323/41 , C07C319/18 , C07C319/20
CPC分类号： C07C323/41 , C07C227/18 , C07C319/14 , C07C319/18 , C07C319/20 , C07C323/25 , C07C229/26
摘要： A bifunctional compound and a method for manufacturing the same are revealed. The structural formula of the compound includes two main functional groups. One functional group is a diamide dithiolate (N2S2) ligand able to bind with radioisotopes. The other functional group is polybasic carboxylic acid that binds to biochemical substances. Based on properties of the above two functional groups, the compound of the present invention can be used for preparation of radiopharmaceuticals such as radiotracter for disease diagnosis or radioactive therapeutic agent for disease treatment.
摘要翻译：揭示双功能化合物及其制造方法。该化合物的结构式包括两个主要官能团。一个官能团是能够与放射性同位素结合的二酰胺二硫醇盐（N2S2）配体。另一个官能团是与生化物质结合的多元羧酸。基于上述两种官能团的性质，本发明的化合物可用于制备放射性药物，例如用于疾病诊断的放射性杆菌或用于疾病治疗的放射性治疗剂。

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