Title:
SELECTIVE INHIBITOR OF EXON 20 INSERTION MUTANT EGFR
Document Type and Number:
WIPO Patent Application WO/2018/079310
Kind Code:
A1
Abstract:
An antitumor agent for treating a patient suffering from a malignant tumor expressing EGFR that has an exon 20 insertion mutation, said antitumor agent comprising a compound selected from the group consisting of compounds A to D described in the description or a salt thereof.
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Inventors:
MIYADERA KAZUTAKA (JP)
AOYAGI YOSHIMI (JP)
HASAKO SHINICHI (JP)
AOYAGI YOSHIMI (JP)
HASAKO SHINICHI (JP)
Application Number:
PCT/JP2017/037186
Publication Date:
May 03, 2018
Filing Date:
October 13, 2017
Export Citation:
Assignee:
TAIHO PHARMACEUTICAL CO LTD (JP)
International Classes:
A61K31/519; A61P35/00
Domestic Patent References:
| WO2015025936A1 | 2015-02-26 | |||
| WO2015175632A1 | 2015-11-19 | |||
| WO2015025936A1 | 2015-02-26 | |||
| WO2013125709A1 | 2013-08-29 |
Other References:
YASUDA, HIROYUKI: "Targeting EGFR exon 20 insertion mutations in non-small cell lung cancer", THE MEDICAL FRONTLINE, vol. 71, no. 8, August 2016 (2016-08-01), pages 1721 - 1725, XP055589103, ISSN: 0370-8241
HIRANO , TOSHIYUKI: "In vitro modeling to deternine mutation specificity of EGFR tyrosine kinase inhibitors against clinically relevant: EGFR mutant in non-small lung cancer", ONCOTARGET, vol. 6, no. 36, 15 October 2015 (2015-10-15), pages 38787 - 38803, XP055589110
JIA, YONG: "EGF816 Exerts Anticancer Effects in Non- Small Cell lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor", CANCER RESEARCH, vol. 76, no. 6, 15 March 2016 (2016-03-15), pages 1591 - 1602, XP009191015
YASUDA, HIROYUKI: "Structual, Biochemical, and Clinical Characterization of epidemal Growth Factor Receptor !EGFR) Exon 20 lnsertion mutations in Lung cancer", SCIENCE TRANSLATIONAL MEDICINE, vol. 5, no. 214-216, December 2013 (2013-12-01), pages 135 - 144, XP055589118
NAT. REV. CANCER, vol. 6, 2006, pages 803 - 812
NATURE MEDICINE, vol. 19, 2013, pages 1389 - 1400
NAT. REV. CANCER, vol. 7, 2007, pages 169 - 181
LANCET ONCOL., vol. 13, 2012, pages 23 - 31
LANCET ONCOL. VOL., vol. 16, 2015, pages 830 - 838
"GenBank", Database accession no. NP _005219.2
"Molecular Design", vol. 7, 1990, HIROKAWA SHOTEN CO., article "Iyakuhin no Kaihatsu [Development of Pharmaceuticals", pages: 163 - 198
"GenBank", Database accession no. NM_005228.4
See also references of EP 3533449A4
HIRANO , TOSHIYUKI: "In vitro modeling to deternine mutation specificity of EGFR tyrosine kinase inhibitors against clinically relevant: EGFR mutant in non-small lung cancer", ONCOTARGET, vol. 6, no. 36, 15 October 2015 (2015-10-15), pages 38787 - 38803, XP055589110
JIA, YONG: "EGF816 Exerts Anticancer Effects in Non- Small Cell lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor", CANCER RESEARCH, vol. 76, no. 6, 15 March 2016 (2016-03-15), pages 1591 - 1602, XP009191015
YASUDA, HIROYUKI: "Structual, Biochemical, and Clinical Characterization of epidemal Growth Factor Receptor !EGFR) Exon 20 lnsertion mutations in Lung cancer", SCIENCE TRANSLATIONAL MEDICINE, vol. 5, no. 214-216, December 2013 (2013-12-01), pages 135 - 144, XP055589118
NAT. REV. CANCER, vol. 6, 2006, pages 803 - 812
NATURE MEDICINE, vol. 19, 2013, pages 1389 - 1400
NAT. REV. CANCER, vol. 7, 2007, pages 169 - 181
LANCET ONCOL., vol. 13, 2012, pages 23 - 31
LANCET ONCOL. VOL., vol. 16, 2015, pages 830 - 838
"GenBank", Database accession no. NP _005219.2
"Molecular Design", vol. 7, 1990, HIROKAWA SHOTEN CO., article "Iyakuhin no Kaihatsu [Development of Pharmaceuticals", pages: 163 - 198
"GenBank", Database accession no. NM_005228.4
See also references of EP 3533449A4
Attorney, Agent or Firm:
SAEGUSA & PARTNERS (JP)
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