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1. (WO2017152756) CRGD-ERLOTINIB CONJUGATE AND PREPARATION METHOD THEREOF
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Pub. No.: WO/2017/152756 International Application No.: PCT/CN2017/074384
Publication Date: 14.09.2017 International Filing Date: 22.02.2017
IPC:
C07K 7/64 (2006.01) ,C07K 1/13 (2006.01) ,C07K 1/04 (2006.01) ,A61K 38/12 (2006.01) ,A61P 35/00 (2006.01)
[IPC code unknown for C07K 7/64][IPC code unknown for C07K 1/13][IPC code unknown for C07K 1/04][IPC code unknown for A61K 38/12][IPC code unknown for A61P 35]
Applicants:
徐州瑞康生物科技有限公司 XUZHOU RUIKANG BIOTECH COMPANY [CN/CN]; 中国江苏省徐州市 新城区绿地商务城唐盛路悦庭小区B02#903室/李书文 B02#903, Yueting/LI Shuwen Shentang Road,Ludi Business Town Xuzhou, Jiangsu 221000, CN
Inventors:
李书鹏 LI, Shupeng; CN
张海龙 ZHANG, Hailong; CN
Agent:
南京苏科专利代理有限责任公司 NANJING SUKE PATENT AGENT CO.,LTD.; 中国江苏省南京市 广州路37号江苏科技大厦2502室/徐振兴 XU, Zhenxing 25th Floor, Jiangsu Science And Technology Mansion No.37 Guangzhou Road Nanjing, Jiangsu 210008, CN
Priority Data:
201610141976.X11.03.2016CN
Title (EN) CRGD-ERLOTINIB CONJUGATE AND PREPARATION METHOD THEREOF
(FR) CONJUGUÉ CRGD-ERLOTINIB ET SON PROCÉDÉ DE PRÉPARATION
(ZH) cRGD-厄洛替尼缀合物及其制备方法
Abstract:
(EN) Provided are a cRGD-erlotinib/icotinib conjugate and a preparation method thereof, wherein the cRGD is a cyclic polypeptide. Erlotinib and icotinib are small molecule inhibitors of a epidermal growth factor receptor (EGFR) that interfere with the growth of cancer cells and are thus used to treat metastatic non-small cell lung cancer (NSCLC). The cRGD-erlotinib/icotinib conjugate synthesized by the present invention selectively delivers the erlotinib/icotinib to non-small cell lung cancer cells and improves the site delivery efficiency, while also reducing the side effects for cancer patients.
(FR) L'invention concerne un conjugué cRGD-erlotinib/icotinib et son procédé de préparation, le cRGD étant un polypeptide cyclique. L'erlotinib et l'icotinib sont des petites molécules inhibitrices d'un récepteur du facteur de croissance épidermique (EGFR) qui interfèrent avec la croissance de cellules cancéreuses et sont donc utilisées pour traiter le cancer du poumon non à petites cellules (NSCLC) métastatique. Le conjugué cRGD-erlotinib/icotinib synthétisé par la présente invention administre sélectivement l'erlotinib/icotinib aux cellules du cancer du poumon non à petites cellules, et améliore l'efficacité d'administration tout en réduisant les effets secondaires chez le patient.
(ZH) 提供了cRGD-厄洛替尼/埃克替尼缀合物及其制备方法,其中,cRGD为环状多肽。厄洛替尼及埃克替尼是表皮生长因子受体(EGFR)的小分子抑制剂,其干扰癌细胞的生长,从而用于治疗转移性非小细胞肺癌(NSCLC)。本发明合成的cRGD-厄洛替尼/埃克替尼缀合物有选择性地将厄洛替尼/埃克替尼递送至非小细胞肺癌细胞,提高了位点递送效率的同时,也减少了癌症患者的副作用。
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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, 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)