Fourth-generation egfr tyrosine kinase inhibitor

Patent metadata

Field	Value
Publication number	US-2021122759-A1
Application number	US-201816497917-A
Country	US
Kind code	A1
Filing date	Mar 29, 2018
Priority date	Mar 29, 2017
Publication date	Apr 29, 2021
Grant date	—

Abstract

or a salt thereof.

First claim

1 . A compound represented by the formula (I):

wherein
X is O or NH,
R 1 and R 2 are each independently a hydrogen atom or an optionally substituted hydrocarbon group;
R 3 and R 4 are each independently a hydrogen atom, a halogen atom or an optionally substituted hydrocarbon group, and
R 5 and R 6 are each independently an optionally substituted hydrocarbon group, excluding the following compounds:

or a salt thereof.

2 . A method for inhibiting C797S resistant mutant EGFR tyrosine kinase activity, the method comprising contacting a cell expressing C797S resistant mutant EGFR with a compound represented by the formula (I):

wherein
X is O/or N
R 1 and R 2 are each independently a hydrogen atom or an optionally substituted hydrocarbon group;
R 3 and R 4 are each independently a hydrogen atom, a halogen atom or an optionally substituted hydrocarbon group, and
R 5 and R 6 are each independently an optionally substituted hydrocarbon group,

or a salt thereof.

3 . A method for treating non-small cell lung cancer in a subject in need thereof, the method comprising administering to the subject a compound represented by the formula (I):

wherein
X is O or NH,
R 1 and R 2 are each independently a hydrogen atom or an optionally substituted hydrocarbon group;
R 3 and R 4 are each independently a hydrogen atom, a halogen atom or an optionally substituted hydrocarbon group, and
R 5 and R 6 are each independently an optionally substituted hydrocarbon group,

or a salt thereof.

4 . The method of claim 3 , wherein the non-small cell lung cancer is associated with C797S resistant mutant EGFR.

Assignees

• Univ Nagasaki
• Univ Iwate Medical
• Japanese Found For Cancer Res

Inventors

• Iwao Masatomo
• Fukuda Tsutomu
• Ishibashi Fumito
• Uehara Yoshimasa
• NISHIYA Naoyuki
• Oku Yusukef
• DAN Shingo
• Yamori Takao

Classifications

• C07D491/147 Primary

  the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom · CPC title

• C07D487/14

  Ortho-condensed systems · CPC title

• A61P11/00

  Drugs for disorders of the respiratory system · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title