EFGR inhibitor, preparation method therefor and application thereof
AssigneeAbbisko Therapeutics Co., Ltd.
InventorsFei Yang, Shuqun Yang, Hongping Yu, Zhui Chen, Yaochang Xu
Life of this patent
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Abstract
An EGFR inhibitor having the structure of formula (I), a preparation method therefor, a pharmaceutical composition containing same, a use of same as an EGFR inhibitor, and a use of same in preparing a drug for treating and/or preventing a cancer, a tumor, or a metastatic disease at least partially related to an EGFR exon 20 insertion, deletion, or other mutation, and in particular a use in preparing a drug for treating and/or preventing a hyperproliferative disease and an induced cell death disorder. Each substituent of formula (I) has the same definition as in the description.
Claims3
A compound of formula (IIb) or formula (IIc), a stereoisomer or pharmaceutically acceptable salt thereof:
- wherein ring A, together with —(R4)n, forms the following structure:
- wherein each R is independently hydrogen;
- each R1 s independently vinyl optionally further substituted with one or more R1 substituents selected from the group consisting of deuterium, fluoro, cyano, methyl, and dimethylaminomethyl;
- each R2 is independently selected from the group consisting of hydrogen, deuterium, fluoro, chloro, bromo, C1-4 alkyl, C2-4 alkynyl, 3-6 membered heterocyclyl, —O—R9, and —NR12R13, the above R2 groups independently optionally further substituted with one or more R2 substituents selected from the group consisting of deuterium, fluoro, chloro, bromo, cyano, C1-4 alkyl, C3-6 cycloalkyl, 3-6 membered heterocyclyl, ═O, —O—R9, and —NR12R13, the above one or more R2 substituent groups independently optionally further substituted with one or more R2 further substituents selected from the group consisting of deuterium, fluoro, chloro, bromo, cyano, C1-4 alkyl, C1-4 haloalkyl, C1-4 deuterioalkyl, C3-6 cycloalkyl, 3-6 membered heterocyclyl, ═O, —O—R9, and —NR12R13;
- each R3 is independently selected from the group consisting of hydrogen;
- each R4 is independently selected from the group consisting of hydrogen, fluoro, chloro and bromo;
- each R9 is independently selected from the group consisting of hydrogen, deuterium, C1-4 alkyl, C2-4 alkenyl, C3-6 cycloalkyl, 3-6 membered heterocyclyl, C6-8 aryl, and 5-8 membered heteroaryl, the above R9 groups independently optionally further substituted with one or more R9 substituents selected from the group consisting of deuterium, halogen, hydroxy, oxo, cyano, C1-4 alkyl, C1-4 alkoxy, C3-6 cycloalkyl, C3-6 cycloalkyloxy, 3-6 membered heterocyclyl, 3-6 membered heterocyclyloxy, C6-8 aryl, C6-8 aryloxy, 5-8 membered heteroaryl, 5-8 membered heteroaryloxy, and —NR12R13;
- each of R12 and R13 is independently selected from the group consisting of hydrogen, deuterium, hydroxy, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C3-6 cycloalkyl, 3-6 membered heterocyclyl, C6-8 aryl, 5-8 membered heteroaryl, sulfinyl, sulfonyl, methylsulfonyl, isopropylsulfonyl, cyclopropylsulfonyl, p-toluenesulfonyl, aminosulfonyl, dimethylaminosulfonyl, amino, monoC1-4 alkylamino, diC1-4 alkylamino, and C1-4 alkanoyl, each of the above R12/R13 groups independently optionally further substituted with one or more R12/R13 substituents selected from the group consisting of deuterium, halogen, hydroxy, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C1-4 haloalkyl, C1-4 deuterioalkyl, C1-4 alkoxy, C3-6 cycloalkyl, C3-6 cycloalkyloxy, 3-6 membered heterocyclyl, 3-6 membered heterocyclyloxy, C6-8 aryl, C6-8 aryloxy, 5-8 membered heteroaryl, 5-8 membered heteroaryloxy, amino, monoC1-4 alkylamino, diC1-4 alkylamino, and C1-4 alkanoyl,
- or, R12 and R13, together with the nitrogen atom to which they are directly attached, form a 4-8 membered heterocyclyl, or 5-8 membered heteroaryl, the 4-8 membered heterocyclyl or 5-8 membered heteroaryl optionally further substituted with one or more R12/R13 substituents selected from the group consisting of deuterium, halogen, hydroxy, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C1-4 haloalkyl, C1-4 deuterioalkyl, C1-4 alkoxy, C3-6 cycloalkyl, C3-6 cycloalkyloxy, 3-6 membered heterocyclyl, 3-6 membered heterocyclyloxy, C6-8 aryl, C6-8 aryloxy, 5-8 membered heteroaryl, 5-8 membered heteroaryloxy, amino, monoC1-4 alkylamino, diC1-4 alkylamino, and C1-4 alkanoyl.
Dependencies are inferred from the claim text.