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1. (WO2018227977) 99MTC-LABELLED ISONITRILE-CONTAINING GLUCOSE DERIVATIVE AND PREPARATION METHOD AND USE
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Pub. No.: WO/2018/227977 International Application No.: PCT/CN2018/073950
Publication Date: 20.12.2018 International Filing Date: 24.01.2018
IPC:
C07F 13/00 (2006.01) ,A61K 51/04 (2006.01) ,A61K 103/10 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
F
ACYCLIC, CARBOCYCLIC, OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
13
Compounds containing elements of the 7th Group of the Periodic System
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
51
Preparations containing radioactive substances for use in therapy or testing in vivo
02
characterised by the carrier
04
Organic compounds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
103
Radioactive metals
10
Technetium; Rhenium
Applicants:
北京师宏药物研制中心 BEIJING SHIHONG PHARMACEUTICAL RESEARCH CENTER [CN/CN]; 中国北京市 海淀区新街口外大街19号北京师范大学化学学院 College of Chemistry, Beijing Normal University, No.19 XinjiekouWai Street, Haidian District Beijing 100875, CN
Inventors:
张俊波 ZHANG, Junbo; CN
张旭冉 ZHANG, Xuran; CN
甘倩倩 GAN, Qianqian; CN
邵欣 SHAO, Xin; CN
王学斌 WANG, Xuebin; CN
唐志刚 TANG, Zhigang; CN
陆洁 LU, Jie; CN
张站斌 ZHANG, Zhanbin; CN
Agent:
北京路浩知识产权代理有限公司 CN-KNOWHOW INTELLECTUAL PROPERTY AGENT LIMITED; 中国北京市 海淀区丹棱街3号中国电子大厦B座18层 18th Floor Tower B, CEC Plaza, No. 3 Dan Ling Street, Haidian District Beijing 100080, CN
Priority Data:
201710451094.815.06.2017CN
Title (EN) 99MTC-LABELLED ISONITRILE-CONTAINING GLUCOSE DERIVATIVE AND PREPARATION METHOD AND USE
(FR) DÉRIVÉ DE GLUCOSE CONTENANT UN ISONITRILE MARQUÉ AU 99MTC, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
(ZH) 99mTc标记含异腈的葡萄糖衍生物及制备方法和应用
Abstract:
(EN) Disclosed are a 99mTc-labelled isonitrile-containing glucose derivative of the structural general formula [99mTc-(CNDG)6]+ and a preparation method and the use. The derivative takes 99mTc+ as a central core, and the isonitrile carbon atom in the CNDG and 99mTc(I) coordinate to form a six-coordinated complex [99mTc-(CNDG)6]+. The [99mTc-(CNDG)6]+ derivative is obtained through the synthesis of the ligand CNDG and the preparation of a CNDG freeze-dried medicine box. The derivative of the present invention has good stability and is easy to prepare, has a high uptake and good retention on a tumour site, has a high tumour/non-target ratio, and is a high-performance new type 99mTc-labelled isonitrile-containing glucose derivative useful for tumour imaging, which is easy to popularize and apply.
(FR) L'invention concerne un dérivé de glucose contenant un isonitrile marqué au 99mTc de formule générale structurale [99mTc-(CNDG)6]+, un procédé de préparation et une utilisation. Le dérivé prend 99mTc+ comme noyau central, et l'atome de carbone d'isonitrile dans CNDG et 99mTc(I) se cordonnent pour former un complexe [99mTc-(CNDG)6]+ à six coordonnées. Le dérivé [99mTc-(CNDG)6]+ est obtenu par la synthèse du ligand CNDG et de la préparation d'une boîte de médicament lyophilisée de CNDG. Le dérivé de la présente invention a une bonne stabilité et est facile à préparer, présente une absorption élevée et une bonne rétention sur un site tumoral, a un rapport tumeur/non-cible élevé, et est considéré comme un nouveau type de dérivé de glucose contenant un isonitrile marqué au 99mTc hautement performant, qui est utile pour l'imagerie tumorale, facile à populariser et à appliquer.
(ZH) 一种结构通式为[ 99mTc-(CNDG) 6] +99mTc标记的含异腈的葡萄糖衍生物及制备方法和应用。该类衍生物以 99mTc +为中心核,CNDG中的异腈碳原子与 99mTc(I)配位形成六配位的[ 99mTc-(CNDG) 6] +配合物。通过配体CNDG的合成及CNDG冻干药盒的制备,得到[ 99mTc-(CNDG) 6] +衍生物。本发明的衍生物稳定性良好,制备简便,在肿瘤部位有较高的摄取与良好的滞留,肿瘤/非靶比值高,是性能优良的可用于肿瘤显像的新型 99mTc标记的含异腈的葡萄糖衍生物,便于推广应用。
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: Chinese (ZH)
Filing Language: Chinese (ZH)