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1. (WO2018049861) TYROSINE KINASE INHIBITOR AND APPLICATION THEREOF
Latest bibliographic data on file with the International Bureau    Submit observation

Pub. No.: WO/2018/049861 International Application No.: PCT/CN2017/089501
Publication Date: 22.03.2018 International Filing Date: 22.06.2017
IPC:
C07D 413/12 (2006.01) ,C07D 215/22 (2006.01) ,C07D 413/14 (2006.01) ,C07D 401/04 (2006.01) ,A61K 31/5377 (2006.01) ,A61P 29/00 (2006.01) ,A61P 35/00 (2006.01)
Applicants: SHANGHAI XIANGJIN BIOTECHNOLOGY CO., LTD[CN/CN]; Room 543, Building A, No.2528 Panyuan Road Changxing Town, Chongming County Shanghai 201913, CN
Inventors: SUN, Fang; CN
ZHAN, Youni; CN
Agent: SHULUN & PARTNERS (SHANGHAI); Suite 1104A, No.333 Zhaojiabang Road Xuhui District Shanghai 200032, CN
Priority Data:
201610822529.013.09.2016CN
Title (EN) TYROSINE KINASE INHIBITOR AND APPLICATION THEREOF
(FR) INHIBITEUR DE TYROSINE KINASE ET APPLICATION ASSOCIÉE
(ZH) 酪氨酸激酶抑制剂及其应用
Abstract: front page image
(EN) The present invention discloses a compound having the following general formula (I), K being selected from a cycloalkyl group aa or bb, a halogenated alkyl group cc, or N-R6. The invention also discloses a tyrosine kinase inhibitor containing the compound and applications of the compound in the preparation of medicaments for treating cancer. The tyrosine kinase inhibitor of the present invention can inhibit the biological activity of various signaling kinases such as C-MET, VEGF, and KDR and can effectively inhibit cell proliferation, and has good therapeutic effects on various diseases such as cancer and especially has significant therapeutic effects on lung cancer, gastric cancer, ovarian cancer, glioblastoma, and others, and has a broad application prospect.
(FR) La présente invention concerne un composé ayant la formule générale suivante (I), K étant choisi parmi un groupe cycloalkyle aa ou bb, un groupe alkyle halogéné cc, ou N-R6. L'invention concerne également un inhibiteur de tyrosine kinase contenant le composé et des applications du composé dans la préparation de médicaments pour le traitement du cancer. L'inhibiteur de tyrosine kinase de la présente invention peut inhiber l'activité biologique de diverses kinases de signalisation telles que C-MET, VEGF et KDR et peut inhiber efficacement la prolifération cellulaire, et a de bons effets thérapeutiques sur diverses maladies telles que le cancer et présente en particulier des effets thérapeutiques significatifs sur le cancer du poumon, le cancer gastrique, le cancer de l'ovaire, le glioblastome et autres, et a une large perspective d'application.
(ZH) 本发明公开了一种具有下述通式(I)的化合物,其中,K选自:环烷烃基aa、bb、卤代烷烃基cc、或N-R6。本发明还公开了包含上述化合物的酪氨酸激酶抑制剂及该化合物在制备治疗癌症的药物中的应用。本发明的酪氨酸激酶抑制剂,能够抑制C-MET、VEGF、KDR等多种信号传导激酶的生物活性,能有效抑制细胞增殖,对多种疾病如癌症具有良好的治疗效果,尤其是对肺癌、胃癌、卵巢癌、恶性胶质瘤等具有显著的治疗效果,应用前景非常广阔。
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)