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公开(公告)号：US20140066609A1
公开(公告)日：2014-03-06
申请号：US13604353
申请日：2012-09-05
申请人： Kuei-Lin LU , Yu CHANG , Cheng-Fang HSU , Mei-Hui WANG , Wuu-Jyh LIN
发明人： Kuei-Lin LU , Yu CHANG , Cheng-Fang HSU , Mei-Hui WANG , Wuu-Jyh LIN
IPC分类号： C07H15/04
摘要： A novel synthesis method of Glyco-drug radiotracer precursor is revealed. After completing synthesis of Z-Gly-ah (main structure), galactosamine GalNAc(OAc)4 is added to have coupling reaction. Then a product is separated directly from dichloromethane. Thus loss of galactosamine during extraction with liquid chromatography is reduced. Moreover, instead of trifluoroacetyl group, carbobenzoxy (abbreviated as Cbz or Z) is used as a protecting group to ensure uniformity of the phase. The cost and synthesis time are also dramatically reduced.
摘要翻译： 揭示了一种新型的糖 - 放射性示踪剂前体的合成方法。 完成Z-Gly-ah（主要结构）合成后，加入半乳糖胺GalNAc（OAc）4进行偶联反应。 然后将产物直接从二氯甲烷中分离出来。 因此，用液相色谱法提取过程中半乳糖胺的损失降低。 此外，代替三氟乙酰基，使用苄氧羰基（缩写为Cbz或Z）作为保护基，以确保相的均匀性。 成本和合成时间也大大降低。
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2.发明授权Precursor used for labeling hepatorcyte receptor and containing trisaccharide and diamide demercaptide ligand, method for preparing the same, radiotracer and pharmaceutical composition of the same 有权用于标记肝细胞受体并含有三糖和二酰胺十氯过硫酸配体的前体，其制备方法，放射性示踪剂及其药物组合物公开(公告)号：US09150602B2
公开(公告)日：2015-10-06
申请号：US13556486
申请日：2012-07-24
申请人： Show-Wen Liu , Yu Chang , Cheng-Fang Hsu , Ming-Che Tsai , Tsung-Hsien Chiang , Yueh-Feng Deng , Kuei-Lin Lu , Chih-Yuan Lin , Da-Ming Wang , Ching-Yun Li
发明人： Show-Wen Liu , Yu Chang , Cheng-Fang Hsu , Ming-Che Tsai , Tsung-Hsien Chiang , Yueh-Feng Deng , Kuei-Lin Lu , Chih-Yuan Lin , Da-Ming Wang , Ching-Yun Li
摘要： A precursor used for labeling hepatocyte receptors and applied to radiotracers for imaging or pharmaceutical compositions for liver cancers is revealed. The precursor is a bifunctional compound. The bifunctional group includes a trisaccharide structure and a diamide dimercaptide (N2S2) ligand. The trisaccharide has high affinity to asialoglycoprotein receptors (ASGPR) on surfaces of hepatocytes while N2S2 ligand reacts with radioisotopes to form neutral complexes. Thus the precursor stays on surfaces of hepatocytes to provide radioisotope labeling or treatment effect of liver cancers.
摘要翻译： 用于标记肝细胞受体并应用于放射性示踪剂以用于肝癌成像的前体或用于肝癌的药物组合物。 前体是双官能化合物。 双官能团包括三糖结构和二酰胺二硫醇（N 2 S 2）配体。 三糖对肝细胞表面的脱唾液酸糖蛋白受体（ASGPR）具有高亲和力，而N2S2配体与放射性同位素反应形成中性复合物。 因此，前体停留在肝细胞的表面，以提供肝癌的放射性同位素标记或治疗效果。
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3.发明申请PRECURSOR USED FOR LABELING HEPATORCYTE RECEPTOR AND CONTAINING TRISACCHARIDE AND DIAMIDE DEMERCAPTIDE LIGAND, METHOD FOR PREPARING THE SAME, RADIOTRACER AND PHARMACEUTICAL COMPOSITION OF THE SAME 有权用于标记HEPATORCYTE受体并含有TRISACCHARIDE和DIAMIDE DEMERCAPTIDE LIGAND的前体，其制备方法，RADIOTRACER及其相应的药物组合物公开(公告)号：US20140031533A1
公开(公告)日：2014-01-30
申请号：US13556486
申请日：2012-07-24
申请人： SHOW-WEN LIU , YU CHANG , CHENG-FANG HSU , MING-CHE TSAI , TSUNG-HSIEN CHIANG , YUEH-FENG DENG , KUEI-LIN LU , CHIH-YUAN LIN , DA-MING WANG , CHING-YUN LI
发明人： SHOW-WEN LIU , YU CHANG , CHENG-FANG HSU , MING-CHE TSAI , TSUNG-HSIEN CHIANG , YUEH-FENG DENG , KUEI-LIN LU , CHIH-YUAN LIN , DA-MING WANG , CHING-YUN LI
摘要： A precursor used for labeling hepatocyte receptors and applied to radiotracers for imaging or pharmaceutical compositions for liver cancers is revealed. The precursor is a bifunctional compound. The bifunctional group includes a trisaccharide structure and a diamide dimercaptide (N2S2) ligand. The trisaccharide has high affinity to asialoglycoprotein receptors (ASGPR) on surfaces of hepatocytes while N2S2 ligand reacts with radioisotopes to form neutral complexes. Thus the precursor stays on surfaces of hepatocytes to provide radioisotope labeling or treatment effect of liver cancers.
摘要翻译： 用于标记肝细胞受体并应用于放射性示踪剂以用于肝癌成像的前体或用于肝癌的药物组合物。 前体是双官能化合物。 双官能团包括三糖结构和二酰胺二硫醇（N 2 S 2）配体。 三糖对肝细胞表面的脱唾液酸糖蛋白受体（ASGPR）具有高亲和力，而N2S2配体与放射性同位素反应形成中性复合物。 因此，前体停留在肝细胞的表面，以提供肝癌的放射性同位素标记或治疗效果。
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公开(公告)号：US20140073803A1
公开(公告)日：2014-03-13
申请号：US13609938
申请日：2012-09-11
申请人： SHOW-WEN LIU , YU CHANG , CHENG-FANG HSU , MING-CHE TSAI , TSUNG-HSIEN CHIANG , YUEH-FENG DENG , KUEI-LIN LU , CHIH-YUAN LIN , DA-MING WANG , CHING-YUN LI
发明人： SHOW-WEN LIU , YU CHANG , CHENG-FANG HSU , MING-CHE TSAI , TSUNG-HSIEN CHIANG , YUEH-FENG DENG , KUEI-LIN LU , CHIH-YUAN LIN , DA-MING WANG , CHING-YUN LI
IPC分类号： C07D207/09
CPC分类号： C07D207/09 , C07F7/2208
摘要： A precursor SnBZM for a dopamine receptor radiotracer and a method for preparing the same are revealed. The precursor includes a tributyltin group (Bu3Sn) that is easy to be replaced. Thus a dopamine receptor radiotracer 123I-IBZM can be produced at high yield rate by a substitution reaction of the precursor. At the same time, both the method for preparing the precursor SnBZM and a method for preparing a reference standard IBZM are simplified. Moreover, stability of each product is improved.
摘要翻译： 显示了用于多巴胺受体放射性示踪剂的前体SnBZM及其制备方法。 前体包括易于置换的三丁基锡基（Bu 3 Sn）。 因此，可以通过前体的取代反应以高产率产生多巴胺受体放射性示踪剂123I-IBZM。 同时，制备前体SnBZM的方法和制备参考标准IBZM的方法都是简化的。 此外，提高了每种产品的稳定性。
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公开(公告)号：US08877943B2
公开(公告)日：2014-11-04
申请号：US13609938
申请日：2012-09-11
申请人： Show-Wen Liu , Yu Chang , Cheng-Fang Hsu , Ming-Che Tsai , Tsung-Hsien Chiang , Yueh-Feng Deng , Kuei-Lin Lu , Chih-Yuan Lin , Da-Ming Wang , Ching-Yun Li
发明人： Show-Wen Liu , Yu Chang , Cheng-Fang Hsu , Ming-Che Tsai , Tsung-Hsien Chiang , Yueh-Feng Deng , Kuei-Lin Lu , Chih-Yuan Lin , Da-Ming Wang , Ching-Yun Li
IPC分类号： C07D207/09
CPC分类号： C07D207/09 , C07F7/2208
摘要： A precursor SnBZM for a dopamine receptor radiotracer and a method for preparing the same are revealed. The precursor includes a tributyltin group (Bu3Sn) that is easy to be replaced. Thus a dopamine receptor radiotracer 123I-IBZM can be produced at high yield rate by a substitution reaction of the precursor. At the same time, both the method for preparing the precursor SnBZM and a method for preparing a reference standard IBZM are simplified. Moreover, stability of each product is improved.
摘要翻译： 显示了用于多巴胺受体放射性示踪剂的前体SnBZM及其制备方法。 前体包括易于置换的三丁基锡基（Bu 3 Sn）。 因此，可以通过前体的取代反应以高产率产生多巴胺受体放射性示踪剂123I-IBZM。 同时，制备前体SnBZM的方法和制备参考标准IBZM的方法都是简化的。 此外，提高了每种产品的稳定性。
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