Title:
PYRIMIDINE DERIVATIVE HAVING PROTEIN KINASE INHIBITORY ACTIVITY, AND THERAPEUTIC PHARMACEUTICAL COMPOSITION COMPRISING SAME
Document Type and Number:
WIPO Patent Application WO/2024/072075
Kind Code:
A1
Abstract:
The present invention relates to a pharmaceutical composition for preventing and treating cancers, including lung cancer, caused by abnormal cell growth, the composition containing, as active ingredients, a novel trisubstituted pyrimidine derivative having an inhibitory activity against protein kinases including EGFR, and a pharmaceutically acceptable salt thereof. The novel compound of the present invention has an excellent inhibitory activity against protein kinases. Particularly, the novel compound of the present invention has an excellent inhibitory effect on various drug-resistant EGFR mutants (EGFR mutants including exon 19 deletion-T790M-C797S-EGFR, L858R-T790M-C797S-EGFR, exon 19 deletion-C797S-EGFR, L858R-C797S-EGFR, exon 19 deletion-T790M-EGFR, L858R-T790M-EGFR, 19 deletion-EGFR and L858R-EGFR), and is useful as an agent for preventing and treating cancers caused by the EGFR mutants.
Inventors:
LEE KOO (KR)
CHUN KWANGWOO (KR)
LIM SUMIN (KR)
SIM TAE BO (KR)
SANDIP SENGUPTA (IN)
KIM YOUNGHOON (KR)
KIM NAMKYOUNG (KR)
JEON EUNHYE (KR)
CHUN KWANGWOO (KR)
LIM SUMIN (KR)
SIM TAE BO (KR)
SANDIP SENGUPTA (IN)
KIM YOUNGHOON (KR)
KIM NAMKYOUNG (KR)
JEON EUNHYE (KR)
Application Number:
PCT/KR2023/014982
Publication Date:
April 04, 2024
Filing Date:
September 27, 2023
Export Citation:
Assignee:
THERAPEX CO LTD (KR)
INDUSTRAY ACADEMIC COOPERATION FOUNDATION YONSEI UNIV (KR)
INDUSTRAY ACADEMIC COOPERATION FOUNDATION YONSEI UNIV (KR)
International Classes:
C07D401/12; A61K31/506; A61K31/5377; A61K31/541; A61K31/55; A61K31/551; A61P35/00; C07D401/14; C07D405/14
Domestic Patent References:
| WO2021098883A1 | 2021-05-27 | |||
| WO2020253862A1 | 2020-12-24 |
Foreign References:
| CN112538072A | 2021-03-23 |
Other References:
FANG HAOTIAN, WU YINGMING, XIAO QITAO, HE DONGBO, ZHOU TONGRUI, LIU WENZHONG, YANG CHUN-HAO, XIE YULI: "Design, synthesis and evaluation of the Brigatinib analogues as potent inhibitors against tertiary EGFR mutants (EGFRdel19/T790M/C797S and EGFRL858R/T790M/C797S)", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, ELSEVIER, AMSTERDAM NL, vol. 72, 1 September 2022 (2022-09-01), Amsterdam NL , pages 128729, XP093151842, ISSN: 0960-894X, DOI: 10.1016/j.bmcl.2022.128729
GUO YANLIANG; GAO BIAO; GAO PENG; FANG LEI; GOU SHAOHUA: "Novel anilinopyrimidine derivatives as potential EGFRT790M/C797S Inhibitors: Design, Synthesis, biological activity study", BIOORGANIC & MEDICINAL CHEMISTRY, ELSEVIER, AMSTERDAM, NL, vol. 70, 5 July 2022 (2022-07-05), AMSTERDAM, NL, XP087145581, ISSN: 0968-0896, DOI: 10.1016/j.bmc.2022.116907
GUO YANLIANG; GAO BIAO; GAO PENG; FANG LEI; GOU SHAOHUA: "Novel anilinopyrimidine derivatives as potential EGFRT790M/C797S Inhibitors: Design, Synthesis, biological activity study", BIOORGANIC & MEDICINAL CHEMISTRY, ELSEVIER, AMSTERDAM, NL, vol. 70, 5 July 2022 (2022-07-05), AMSTERDAM, NL, XP087145581, ISSN: 0968-0896, DOI: 10.1016/j.bmc.2022.116907
Attorney, Agent or Firm:
KWAK, Hyun Kyu (KR)
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