FUSED RING PYRIMIDINE AMINO COMPOUND AND PREPARATION METHOD, PHARMACEUTICAL COMPOSITION, AND USE THEREOF - SHANGHAI INSTITUTE OF MAT MEDICA CHINESE ACADEMY OF SCIENCES

Title:

FUSED RING PYRIMIDINE AMINO COMPOUND AND PREPARATION METHOD, PHARMACEUTICAL COMPOSITION, AND USE THEREOF

Document Type and Number:

WIPO Patent Application WO/2021/013084

Kind Code:

A1

Abstract:

The present invention relates to a fused ring pyrimidine amino compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically disclosed in the present invention are the compound shown in formula I, a pharmaceutically acceptable salt thereof, a tautomer thereof, a stereoisomer thereof, a metabolite thereof, a metabolic precursor thereof, or a prodrug thereof. The fused ring pyrimidine amino compound of the present application has good inhibitory activity against DDRs, particularly DDR2, and has a good therapeutic effect on tumours and fibrotic diseases, especially pulmonary inflammation and pulmonary fibrosis. Also disclosed in the present invention are a preparation method for the compound shown in formula I, and a use thereof.

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Inventors:

XIONG BING (CN)
LI JIA (CN)
GENG MEIYU (CN)
SHEN JINGKANG (CN)
ZANG YI (CN)
AI JING (CN)
CHEN DANQI (CN)
WANG QI (CN)
DONG YING (CN)
PENG XIA (CN)
JI YINCHUN (CN)
TAN QIAN (CN)

Application Number:

PCT/CN2020/102653

Publication Date:

January 28, 2021

Filing Date:

July 17, 2020

Export Citation:

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Assignee:

SHANGHAI INSTITUTE OF MAT MEDICA CHINESE ACADEMY OF SCIENCES (CN)

International Classes:

C07D239/84; A61K31/517; A61P35/00

Domestic Patent References:

WO2016051186A1	2016-04-07
WO2016051186A1	2016-04-07

Foreign References:

CN109305944A	2019-02-05
EP1836174B1	2013-02-27
EP1878727A1	2008-01-16
CN201910654591A	2019-07-19
CN202010667271A	2020-07-13

Other References:

BRAD HERBERICH ET AL.: "Discovery of Highly Selective and Potent p38 Inhibitors Based on a Phthalazine Scaffold", JOURNAL OF MEDICINAL CHEMISTRY, vol. 51, no. 20, 26 September 2008 (2008-09-26), pages 6271 - 6279, XP055776119
MARTIN GOLKOWSKI ET AL.: "Rapid proﬁling of protein kinase inhibitors by quantitative proteomics", MED. CHEM. COMMUN., vol. 5, no. 3, 11 December 2013 (2013-12-11), pages 363 - 369, XP055776121
BERGE ET AL.: "Pharmaceutical Salts", JOURNAL OF PHARMACEUTICAL SCIENCE, vol. 66, 1977, pages 1 - 19, XP002675560, DOI: 10.1002/jps.2600660104
SAULNIER,M.G., BIOORG.MED.CHEM.LETT., vol. 4, 1994, pages 1985 - 1990
GREENWALD,R.B., J.MED.CHEM., vol. 43, 2000, pages 475
See also references of EP 4001267A4

Attorney, Agent or Firm:

SHANGHAI BESHINING LAW OFFICE (CN)

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