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Title:
INDAZOLE COMPOUND FOR USE IN INHIBITING KINASE ACTIVITY, COMPOSITION AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2019/001379
Kind Code:
A1
Abstract:
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.

Inventors:
WANG YIHAN (CN)
LI HUANYIN (CN)
Application Number:
PCT/CN2018/092570
Publication Date:
January 03, 2019
Filing Date:
June 25, 2018
Export Citation:
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Assignee:
SHENZHEN TARGETRX INC (CN)
International Classes:
A61K31/33; C07D231/56; A61P35/00
Foreign References:
CN101754956A2010-06-23
CN102603734A2012-07-25
US5376645A1994-12-27
Other References:
MARIA MENICHINCHERI, ELENA ARDINI, PAOLA MAGNAGHI, NILLA AVANZI, PATRIZIA BANFI, ROBERTO BOSSI, LAURA BUFFA, GIULIA CANEVARI, LUCI: "Discovery of Entrectinib: A New 3-Aminoindazole As a Potent Anaplastic Lymphoma Kinase (ALK), c-ros Oncogene 1 Kinase (ROS1), and Pan-Tropomyosin Receptor Kinases (Pan-TRKs) inhibitor", JOURNAL OF MEDICINAL CHEMISTRY, vol. 59, no. 7, 22 March 2016 (2016-03-22), pages 3392 - 3408, XP055663585, DOI: 10.1021/acs.jmedchem.6b00064
CURRENT OPINIONIN CHEMICAL BIOLOGY, vol. 3, 1999, pages 459 - 465
T. HIGUCHIV. STELLA: "Bioreversible Carriers in Drug Design", vol. 14, 1987, AMERICAN PHARMACEUTICAL ASSOCIATION AND PERGAMON PRESS
D. FLEISHERS. RAMONH. BARBRA: "Improved oral drug delivery: solubility limitations overcome by the use of prodrugs", ADVANCED DRUG DELIVERY REVIEWS, vol. 19, no. 2, 1996, pages 115 - 130
WUTSGREENE: "Protective Groups in Organic Synthesis", 2006, JOHN WILEY & SONS
"Remington's Pharmaceutical Sciences", 1985, MACK PUBLISHING COMPANY
See also references of EP 3626709A4
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