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1. (WO2019001379) INDAZOLE COMPOUND FOR USE IN INHIBITING KINASE ACTIVITY, COMPOSITION AND APPLICATION THEREOF
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Pub. No.: WO/2019/001379 International Application No.: PCT/CN2018/092570
Publication Date: 03.01.2019 International Filing Date: 25.06.2018
IPC:
C07D 231/56 (2006.01) ,A61K 31/33 (2006.01) ,A61P 35/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
231
Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
54
condensed with carbocyclic rings or ring systems
56
Benzopyrazoles; Hydrogenated benzopyrazoles
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
P
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35
Antineoplastic agents
Applicants:
深圳市塔吉瑞生物医药有限公司 SHENZHEN TARGETRX, INC. [CN/CN]; 中国广东省深圳市 南山区科苑路15号科兴科学园A1栋301 Room 301, Building A1, Kexing Science Park No.15 of Keyuan Road, Nanshan District Shenzhen, Guangdong 518057, CN
Inventors:
王义汉 WANG, Yihan; CN
李焕银 LI, Huanyin; CN
Priority Data:
201710493792.426.06.2017CN
Title (EN) INDAZOLE COMPOUND FOR USE IN INHIBITING KINASE ACTIVITY, COMPOSITION AND APPLICATION THEREOF
(FR) COMPOSÉ D'INDAZOLE DESTINÉ À ÊTRE UTILISÉ DANS L'INHIBITION DE L'ACTIVITÉ KINASE, COMPOSITION ET APPLICATION DE CELUI-CI
(ZH) 用于抑制激酶活性的吲唑类化合物及其组合物及应用
Abstract:
(EN) The present invention relates to an indazole compound for use in inhibiting kinase activity, and relates to a preparation and use thereof. Specifically disclosed in the present invention is an indazole compound represented by formula (I), or a pharmaceutical composition of a crystal form, a prodrug, a pharmaceutically acceptable salt, a stereoisomer, a tautomer, a solvate or a hydrate thereof. The compound of the present invention and the composition comprising the compound have an excellent inhibitory effect on kinase proteins, and have better pharmacokinetic parameter characteristics, may increase the drug concentration of the compound in an animal, and improve the efficacy and safety of the drug.
(FR) La présente invention concerne un composé d'indazole destiné à être utilisé dans l'inhibition de l'activité kinase, une préparation et une utilisation de celui-ci. La présente invention concerne particulièrement un composé d'indazole représenté par la formule (I), ou une composition pharmaceutique d'une forme cristalline, un promédicament, un sel pharmaceutiquement acceptable, un stéréoisomère, un tautomère, un solvate ou un hydrate de celui-ci. Le composé et la composition comprenant le composé selon la présente invention ont un excellent effet inhibiteur sur les protéines kinases, et présentent de meilleures caractéristiques des paramètres pharmacocinétiques, peuvent également augmenter la concentration en médicament du composé chez un animal, et améliorent l'efficacité et la sécurité du médicament.
(ZH) 本发明涉及抑制激酶活性的吲唑类化合物,以及涉及它们的制备和用途。具体地,该发明公开了式(I)所示的吲唑类化合物,或其晶型、前药、药学上可接受的盐、立体异构体、互变异构体、溶剂合物或水合物的药物组合物。本发明化合物及包含该化合物的组合物对激酶蛋白具有优异的抑制性,同时具有更好的药代动力学参数特性,能够提高化合物在动物体内的药物浓度,以及提高药物疗效和安全性。
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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, 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)