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US 10,093,656 B2Granted
Fused-ring or tricyclic aryl pyrimidine compound used as kinase inhibitor
AssigneeNanjing Sanhome Pharmaceutical Co., Ltd.
InventorsCharles Z. Ding, Shuhui Chen, Baoping Zhao, Xile Liu, Linxia Xiao, Chao Ding, Fei Wang, Jian Li
Life of this patent
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Abstract
Disclosed is a fused-ring or tricyclic aryl pyrimidine compound used as a mutation selectivity EGFR inhibitor. Specifically, disclosed is a compound represented by formula (I) and used as an EGFR inhibitor or a pharmaceutically acceptable salt thereof.
Claims14
A compound having a structural of formula (I) or a pharmaceutically acceptable salt, an isomer or a solvate thereof,
- wherein,
- w is
- n=1;
- Y1, Y2 and Y3 are —C(R)2—;
- X1 is selected from CRX1, and N;
- X2 is selected from CRX2, and N;
- X3 is selected from CRX3, and N;
- each of RX1, RX2, RX3 is independently selected from H, F, Cl, Br, I, CN, OH, SH, and NH2, or each of RX1, RX2, RX3 is independently selected from a C1-6 alkyl and a C1-6 heteroalkyl which is optionally substituted by one, two, three or four R(s),
- R1 is selected from H, F, Cl, Me, CN, and CF3;
- R2 is selected from R02, OR02, and SR02;
- R02 is independently selected from a C1-4 alkyl, a C1-4 heteroalkyl, and a C3-5 cycloalkyl-(CH2)0-3—, each of which is optionally substituted by one, two, three or four R(s);
- R3 is selected from a C1-6 alkyl, a C1-6 heteroalkyl, a C2-4 alkynyl, a 3- to 7-membered cycloalkyl, a 3- to 7-membered cycloalkyl-L-, a 3- to 7-membered heterocycloalkyl, and a 3- to 7-membered heterocycloalkyl-L-, each of which is optionally substituted by one, two, three or four R(s);
- L is selected from —O—, —S—, —C(═O)—, —S(═O)2—, and —S(═O)—, or L is selected from NH, a C1-4 alkyl, and a C1-4 heteroalkyl, each of which is optionally substituted by one, two, three or four R(s);
- the “hetero” represents a heteroatom or a hetero-atomic group, which is selected from —C(═O)NH—, —NH—, —O—, —S—, N, ═O, ═S, —C(═O)O—, —C(═O)—, —C(═S)—, —S(═O)—, and —S(═O)2—;
- the number of the heteroatom or the hetero-atomic group is independently selected from 0, 1, 2, and 3;
- R is selected from H, F, Cl, Br, I, OH, and CN, or R is selected from NH2, a C1-4 alkyl, a C1-4 heteroalkyl, a 3- to 7-membered cycloalkyl, and a 3- to 7-membered heterocycloalkyl which is optionally substituted by one, two, three or four R′(s);
- R′ is selected from F, Cl, Br, I, CN, OH, NH2, CF3, NHCH3, CH2OCH3, and N(CH3).
14 more elements
Dependencies are inferred from the claim text.