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1. (WO2018102974) CONJUGATE FOR NATURAL ACTIVE INGREDIENT CARDIOTONIC STEROID AND OCTREOTIDE, AND PREPARATION METHOD THEREFOR AND USES THEREOF
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Pub. No.: WO/2018/102974 International Application No.: PCT/CN2016/108630
Publication Date: 14.06.2018 International Filing Date: 06.12.2016
IPC:
A61K 47/28 (2006.01) ,A61K 47/42 (2017.01) ,A61P 35/00 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
06
Organic compounds
28
Steroids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47
Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives
30
Macromolecular compounds
42
Proteins; Polypeptides; Degradation products thereof; Derivatives thereof
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
江苏大学 JIANGSU UNIVERSITY [CN/CN]; 中国江苏省镇江市 京口区学府路301号 No.301 Xuefu Road, Jingkou District Zhenjiang, Jiangsu 212013, CN
Inventors:
徐希明 XU, Ximing; CN
张辉云 ZHANG, Huiyun; CN
余江南 YU, Jiangnan; CN
徐文倩 XU, Wenqian; CN
Agent:
南京知识律师事务所 NANJING ZHISHI LAW FIRM OF INTELLECTUAL PROPERTY; 中国江苏省南京市 新模范马路5号南京科技广场B座9楼 9F, Block B Nanjing Sci-Tech Center, 5# Xinmofan Road Nanjing, Jiangsu 210009, CN
Priority Data:
Title (EN) CONJUGATE FOR NATURAL ACTIVE INGREDIENT CARDIOTONIC STEROID AND OCTREOTIDE, AND PREPARATION METHOD THEREFOR AND USES THEREOF
(FR) CONJUGUÉ DESTINÉ À UN STÉROÏDE ET À UN OCTRÉOTIDE CARDIOTONIQUES DE PRINCIPE ACTIF NATUREL, ET PROCÉDÉ DE PRÉPARATION ET UTILISATIONS S'Y RAPPORTANT
(ZH) 一种天然活性成分强心甾类固醇与奥曲肽的偶联物及其制法和用途
Abstract:
(EN) A conjugate for a natural active ingredient cardiotonic steroid and octreotide, and a preparation method therefor and uses thereof. The conjugate is synthesized by using succinic anhydride as a linker, so as to synthesize a cardiotonic steroid octreotide conjugate. The conjugate significantly improves the toxicity of cardiotonic steroids to tumor cells (comprising human hepatocellular carcinoma cells HepG2 and human breast cancer cells MCf-7) in in-vitro cytotoxicity experiments, and at the same time, decreases the toxicity to normal cells, improves tumor targeting, decreases heart and liver toxicity, and improves the effect of tumor treatment.
(FR) La présente invention concerne un conjugué destiné à un stéroïde et à un octréotide cardiotoniques de principe actif naturel, et un procédé de préparation et des utilisations s'y rapportant. Le conjugué est synthétisé à l'aide d'un anhydride succinique en tant que lieur, de manière à synthétiser un conjugué de stéroïde et d'octréotide cardiotoniques. Le conjugué améliore considérablement la toxicité de stéroïdes cardiotoniques vis-à-vis de cellules de tumeurs (y compris des cellules de carcinome hépatocellulaire humain HepG2 et des cellules du cancer du sein humain MCf-7) dans des expériences de cytotoxicité in vitro, tout en diminuant la toxicité vis-à-vis de cellules normales, en améliorant le ciblage des tumeurs, en diminuant la toxicité vis-à-vis du cœur et du foie, et en améliorant l'effet du traitement des tumeurs.
(ZH) 一种天然活性成分强心甾类固醇与奥曲肽的偶联物及其制备方法,它是以丁二酸酐为连接剂,合成得到强心甾类固醇-奥曲肽偶联物。该偶联物在体外细胞毒实验中,明显提高了强心甾类固醇对肿瘤细胞的毒性(包括人肝癌细胞HepG2、人乳腺癌细胞MCf-7),同时降低了对正常细胞的毒性,同时肿瘤靶向性提高、心脏和肝脏毒性降低、肿瘤治疗效果增强。
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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, 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)