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1. (WO2014194848) MULTI-TARGETED UBENIMEX PRODRUG DERIVATIVE AND PREPARATION METHOD AND USE THEREOF
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2014/194848    International Application No.:    PCT/CN2014/079312
Publication Date: 11.12.2014 International Filing Date: 06.06.2014
IPC:
C07D 239/553 (2006.01), A61K 31/553 (2006.01), A61P 35/00 (2006.01)
Applicants: WEIFANG BOCHUANG INTERNATIONAL ACADEMY OF BIOTECHNOLOGY AND MEDICINE [CN/CN]; 36 Gaoxin'er Road, New and Hi-tech Industrial Development Zone Weifang, Shandong 261061 (CN)
Inventors: XU, Wenfang; (CN).
JIANG, Yuqi; (CN).
ZHANG, Yingjie; (CN).
ZOU, Mingming; (CN).
HOU, Jinning; (CN).
LI, Jin; (CN).
WANG, Xuejian; (CN).
LI, Xiaoyang; (CN)
Agent: RUNPING&PARTNERS; Suite 515, Yingu Mansion, No.9 Beisihuanxilu, Haidian District Beijing 100190 (CN)
Priority Data:
201310225754.2 07.06.2013 CN
201310393152.8 03.09.2013 CN
Title (EN) MULTI-TARGETED UBENIMEX PRODRUG DERIVATIVE AND PREPARATION METHOD AND USE THEREOF
(FR) DÉRIVÉ DE PROMÉDICAMENT D'UBÉNIMEX À CIBLES MULTIPLES ET PROCÉDÉ DE PRÉPARATION ET UTILISATION CORRESPONDANTS
(ZH) 多靶点型乌苯美司前药衍生物及其制备方法和用途
Abstract: front page image
(EN)Disclosed in the invention are the design, synthesis and activity study of a multi-targeted ubenimex prodrug derivative. More particularly, provided in the present invention is a compound as shown by general structural formula (I) (wherein the definition of R is shown in the description). The derivative is a multi-targeted compound obtained by binding an aminopeptidase (APN/CD13) inhibitor, ubenimex, with some anti-tumour drugs already on the market through an ester bond or amide bond, and is suitable for use as an anti-tumour drug for treating various malignant tumours, and is especially suitable for treating various solid tumours.
(FR)L'invention concerne la conception, la synthèse et l'étude d'activité d'un dérivé de promédicament d'ubénimex à cibles multiples. Plus particulièrement, la présente invention concerne un composé tel que représenté par la formule développée générale (I) (dans laquelle la définition de R est indiquée dans la description). Le dérivé est un composé à cibles multiples obtenu par la liaison d'un inhibiteur d'aminopeptidase (APN/CD13), l'ubénimex, à certains médicaments antitumoraux déjà sur le marché via une liaison ester ou une liaison amide et convient pour une utilisation comme médicament antitumoral en vue du traitement de diverses tumeurs malignes et convient en particulier pour le traitement de diverses tumeurs solides.
(ZH)本发明公开了一类多靶点型乌苯美司前药衍生物的设计、合成及活性研究。更具体的说,本发明提供了结构通式(I)所示的化合物(其中R的定义见说明书),该类衍生物是由氨肽酶(APN/CD13) 抑制剂乌苯美司与某些已上市的抗肿瘤药物通过酯键或酰胺键连接而得到的一类多靶点化合物,适合作为抗肿瘤药物用于治疗各种恶性肿瘤,尤其适用于治疗各种实体瘤。
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, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, 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 (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (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)