US 2019/0292182 A1Published application

Quinazoline compound

AssigneeAstellas Pharma Inc.

InventorsKazuyuki Kuramoto, Michinori Akaiwa, Tomoaki Abe, Takanobu Araki, Susumu Yamaki, Shigeki Kunikawa, Tomoyoshi Imaizumi, Takahiro Nigawara, Keisuke Arakawa, Itsuro Shimada, Masashi Shimazaki, Yoshiki Satake, Kazushi Watanabe, Takanori Koike

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Abstract

[Problem] Provided is a compound which is useful as an active ingredient of a pharmaceutical composition for treating lung cancer. [Means for Solution] The present inventors have studied a compound useful as an active ingredient of a pharmaceutical composition for treating lung cancer, and as a result, it was found that a quinazoline compound has an excellent G12C mutation KRAS inhibitory activity, and which can be used as a therapeutic agent for lung cancer, and thereby the present invention has been completed. The quinazoline compound of the present invention and a salt thereof may be used as the therapeutic agent for lung cancer.

Claims12

Dependent claims

A compound or the salt thereof,

wherein the compound is selected from the group consisting of (+)-1-(7-{8-ethoxy-7-(5-methyl-1H-indazol-4-yl)-2-[(1-methylpiperidin-4-yl)oxy]-6-vinylquinazolin-4-yl}-2,7-diazaspiro[3.5]non-2-yl)prop-2-en-1-one,
(+)-1-{7-[6-cyclopropyl-2-{[1-(2-methoxyethyl)piperidin-4-yl]oxy}-7-(5-methyl-1H-indazol-4-yl)-8-(2,2,2-trifluoroethoxy)quinazolin-4-yl]-2,7-diazaspiro[3.5]non-2-yl}prop-2-en-1-one,
(+)-1-{7-[2-{[1-(2-methoxyethyl)piperidin-4-yl]oxy}-7-(5-methyl-1H-indazol-4-yl)-8-(2,2,2-trifluoroethoxy)-6-vinylquinazolin-4-yl]-2,7-diazaspiro[3.5]non-2-yl}prop-2-en-1-one,
(+)-1-{7-[2-{[1-(2-ethoxyethyl)piperidin-4-yl]oxy}-7-(5-methyl-1H-indazol-4-yl)-8-(2,2,2-trifluoroethoxy)-6-vinylquinazolin-4-yl]-2,7-diazaspiro[3.5]non-2-yl}prop-2-en-1-one,
(+)-1-{7-[6-cyclopropyl-2-{[1-(3-methoxypropyl)piperidin-4-yl]oxy}-7-(5-methyl-1H-indazol-4-yl)-8-(2,2,2-trifluoroethoxy)quinazolin-4-yl]-2,7-diazaspiro[3.5]non-2-yl}prop-2-en-1-one,
(+)-1-{7-[7-(5-methyl-1H-indazol-4-yl)-2-{[1-(tetrahydro-2H-pyran-4-yl)piperidin-4-yl]oxy}-8-(2,2,2-trifluoroethoxy)-6-vinylquinazolin-4-yl]-2,7-diazaspiro[3.5]non-2-yl}prop-2-en-1-one, and
(+)-1-{7-[2-{[1-(2-hydroxy-2-methylpropyl)piperidin-4-yl]oxy}-7-(5-methyl-1H-indazol-4-yl)-8-(2,2,2-trifluoroethoxy)-6-vinylquinazolin-4-yl]-2,7-diazaspiro[3.5]non-2-yl}prop-2-en-1-one.

4 more elements

Dependencies are inferred from the claim text.

Facts

Application: 16/432,077Filed 5 Jun 2019
Priority: JP 2017-0172662 Feb 2017
Published: 26 Sep 2019
Term ends: Not estimatedThe source records don’t support an estimate.

Classification9 codes

C07D 471/10
In which the condensed system contains two hetero rings: spiro-condensed systems
A61K 31/517
Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim: ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/5377
1,4-Oxazines, e.g. morpholine: not condensed and containing further heterocyclic rings, e.g. timolol
A61K 31/55
Having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins: having seven-membered rings, e.g. azelastine, pentylenetetrazole

Family

Application16/432,077Continuation
US 10,556,906 B2Related patent
US 2019/0292182 A1This patent

From the US filing history. Foreign family members aren’t listed.

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