Title:
PYRIMIDINE-4,6-DIAMINE DERIVATIVE, A PREPARATION METHOD THEREFOR, AND A PHARMACEUTICAL APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/011299
Kind Code:
A1
Abstract:
The present invention relates to a pyrimidine-4,6-diamine derivative, a preparation method therefor, and a pharmaceutical application thereof. Particularly, the present invention relates to a pyrimidine-4,6-diamine derivative having the structure of formula (I), a preparation method therefor, a pharmaceutical composition containing same, and a use of same as an EGFR inhibitor and a use of same in the preparation of drugs for the treatment and/or prevention of cancers, tumors, or metastatic diseases at least partially related to EGFR Del19 mutation, EGFR L858R mutation, EGFR L858R/C797S double mutation or EGFRDel19/C797S double mutation, in particular a use of same in the preparation of drugs for the treatment and/or prevention of hyperproliferative diseases and induced cell death disorders. The definition of each substituent in formula (I) is the same as that in the description.
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Inventors:
YANG FEI (CN)
YANG SHUQUN (CN)
YU HONGPING (CN)
CHEN ZHUI (CN)
XU YAOCHANG (CN)
YANG SHUQUN (CN)
YU HONGPING (CN)
CHEN ZHUI (CN)
XU YAOCHANG (CN)
Application Number:
PCT/CN2022/108432
Publication Date:
February 09, 2023
Filing Date:
July 28, 2022
Export Citation:
Assignee:
ABBISKO THERAPEUTICS CO LTD (CN)
International Classes:
C07D401/12; A61K31/505; A61K31/506; A61P35/00; C07D401/14; C07D403/12; C07D403/14
Foreign References:
| US20170369449A1 | 2017-12-28 | |||
| CN101902911A | 2010-12-01 | |||
| CN102448462A | 2012-05-09 |
Other References:
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HIRSCH, F. R. ET AL.: "Lung cancer: current therapies and new targeted treatments", LANCET, vol. 389, 2017, pages 299 - 311, XP029892196, DOI: 10.1016/S0140-6736(16)30958-8
PASSARO, A.JANNE, P.A.MOK, T. ET AL.: "Overcoming therapy resistance in EGFR-mutant lung cancer", NAT CANCER, vol. 2, 2021, pages 377 - 391
PASSARO, A. ET AL.: "Recent Advances on the Role of EGFR Tyrosine Kinase Inhibitors in the Management of NSCLC With Uncommon, Non Exon 20 Insertions, EGFR Mutations", JOURNAL OF THORACIC ONCOLOGY: OFFICIAL PUBLICATION OF THE INTERNATIONAL ASSOCIATION FOR THE STUDY OF LUNG CANCER, vol. 16, 2021, pages 764 - 773
ROSELL, R. ET AL.: "Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial", THE LANCET. ONCOLOGY, vol. 13, 2012, pages 239 - 246
SEQUIST, L. V ET AL.: "Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations", JOURNAL OF CLINICAL ONCOLOGY: OFFICIAL JOURNAL OF THE AMERICAN SOCIETY OF CLINICAL ONCOLOGY, vol. 31, 2013, pages 3327 - 3334
MITSUDOMI, T. ET AL.: "Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of the epidermal growth factor receptor (WJTOG3405): an open label, randomised phase 3 trial", THE LANCET. ONCOLOGY, vol. 11, 2010, pages 121 - 128, XP026884314, DOI: 10.1016/S1470-2045(09)70364-X
PARK, K. ET AL.: "Afatinib versus gefitinib as first-line treatment of patients with EGFR mutation-positive non-small-cell lung cancer (LUX-Lung 7): a phase 2B, open-label, randomised controlled trial", THE LANCET. ONCOLOGY, vol. 17, 2016, pages 577 - 589
SORIA, J. C. ET AL.: "Osimertinib in Untreated EGFR-Mutated Advanced Non-Small-Cell Lung Cancer", THE NEW ENGLAND JOURNAL OF MEDICINE, vol. 378, 2018, pages 113 - 125, XP002790155, DOI: 10.1056/NEJMoa1713137
RAMALINGAM, S. S. ET AL.: "LBA50 Mechanisms of acquired resistance to first-line osimertinib: preliminary data from the phase III FLAURA study", ANN. ONCOL., 2018
TUMBRINK, H. L.HEIMSOETH, A.SOS, M. L: "The next tier of EGFR resistance mutations in lung cancer", ONCOGENE, vol. 40, 2021, pages 1 - 11, XP037332472, DOI: 10.1038/s41388-020-01510-w
HIRSCH, F. R. ET AL.: "Lung cancer: current therapies and new targeted treatments", LANCET, vol. 389, 2017, pages 299 - 311, XP029892196, DOI: 10.1016/S0140-6736(16)30958-8
PASSARO, A.JANNE, P.A.MOK, T. ET AL.: "Overcoming therapy resistance in EGFR-mutant lung cancer", NAT CANCER, vol. 2, 2021, pages 377 - 391
PASSARO, A. ET AL.: "Recent Advances on the Role of EGFR Tyrosine Kinase Inhibitors in the Management of NSCLC With Uncommon, Non Exon 20 Insertions, EGFR Mutations", JOURNAL OF THORACIC ONCOLOGY: OFFICIAL PUBLICATION OF THE INTERNATIONAL ASSOCIATION FOR THE STUDY OF LUNG CANCER, vol. 16, 2021, pages 764 - 773
ROSELL, R. ET AL.: "Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial", THE LANCET. ONCOLOGY, vol. 13, 2012, pages 239 - 246
SEQUIST, L. V ET AL.: "Phase III study of afatinib or cisplatin plus pemetrexed in patients with metastatic lung adenocarcinoma with EGFR mutations", JOURNAL OF CLINICAL ONCOLOGY: OFFICIAL JOURNAL OF THE AMERICAN SOCIETY OF CLINICAL ONCOLOGY, vol. 31, 2013, pages 3327 - 3334
MITSUDOMI, T. ET AL.: "Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of the epidermal growth factor receptor (WJTOG3405): an open label, randomised phase 3 trial", THE LANCET. ONCOLOGY, vol. 11, 2010, pages 121 - 128, XP026884314, DOI: 10.1016/S1470-2045(09)70364-X
PARK, K. ET AL.: "Afatinib versus gefitinib as first-line treatment of patients with EGFR mutation-positive non-small-cell lung cancer (LUX-Lung 7): a phase 2B, open-label, randomised controlled trial", THE LANCET. ONCOLOGY, vol. 17, 2016, pages 577 - 589
SORIA, J. C. ET AL.: "Osimertinib in Untreated EGFR-Mutated Advanced Non-Small-Cell Lung Cancer", THE NEW ENGLAND JOURNAL OF MEDICINE, vol. 378, 2018, pages 113 - 125, XP002790155, DOI: 10.1056/NEJMoa1713137
RAMALINGAM, S. S. ET AL.: "LBA50 Mechanisms of acquired resistance to first-line osimertinib: preliminary data from the phase III FLAURA study", ANN. ONCOL., 2018
TUMBRINK, H. L.HEIMSOETH, A.SOS, M. L: "The next tier of EGFR resistance mutations in lung cancer", ONCOGENE, vol. 40, 2021, pages 1 - 11, XP037332472, DOI: 10.1038/s41388-020-01510-w
Attorney, Agent or Firm:
GE CHENG & CO., LTD. (CN)
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