Back to results
US 11,453,667 B2Granted
Pyridone-pyrimidine derivative acting as KRASG12C mutein inhibitor
AssigneeMedshine Discovery Inc.
InventorsYaxian Cai, Zhaobing Xu, Hailong Yang, Shiqi Han, Guoping Hu, Lihong Hu, Charles Z. Ding, Jian Li, Shuhui Chen
Life of this patent
Estimating the term…
Abstract
Provided are a class of KRAS G12C mutein inhibitors, which relate in particular to a compound represented by formula (I), an isomer thereof, and a pharmaceutically acceptable salt thereof.
Claims19
A compound of formula (I) or a pharmaceutically acceptable salt thereof,
- wherein
- ring A is selected from 3-8 membered heterocycloalkyl, and the 3-8 membered heterocycloalkyl is optionally substituted with 1, 2 or 3 R;
- R1, R2, R3, R4 and R5 are each independently selected from H, halogen, OH, NH2, CN, C1-6 alkyl and C1-6 heteroalkyl, and the C1-6 alkyl and C1-6 heteroalkyl are optionally substituted with 1, 2 or 3 R;
- or R1 and R2 are connected together to form ring B;
- or R2 and R3 are connected together to form ring B;
- or R3 and R4 are connected together to form ring B;
- or R4 and R5 are connected together to form ring B;
- ring B is selected from phenyl, C5-6 cycloalkenyl, 5-6 membered heterocycloalkenyl and 5-6 membered heteroaryl, and the phenyl, C5-6 cycloalkenyl, 5-6 membered heterocycloalkenyl and 5-6 membered heteroaryl are optionally substituted with 1, 2 or 3 Ra;
- Ra is selected from halogen, OH, NH2, CN, C1-6 alkyl and C1-6 heteroalkyl, and the C1-6 alkyl and C1-6 heteroalkyl are optionally substituted with 1, 2 or 3 R;
- R6 is selected from H, halogen and C1-6 alkyl, and the C1-6 alkyl is optionally substituted with 1, 2 or 3 R;
- R7 is selected from 4-6 membered heterocycloalkyl, 5-6 membered heteroaryl and C5-6 cycloalkyl, and 4-6 membered heterocycloalkyl, 5-6 membered heteroaryl and C5-6 cycloalkyl are optionally substituted with 1, 2 or 3 R;
- L is selected from a single bond, —NH—, —S—, —O—, —C(═O)—, —C(═S)—, —CH2—, —CH(Rb)— and —C(Rb)2—;
- L′ is selected from a single bond and —NH—;
- Rb is selected from C1-3 alkyl and C1-3 heteroalkyl, and the C1-3 alkyl and C1-3 heteroalkyl are optionally substituted with 1, 2 or 3 R;
- R8 is selected from H, C1-6 alkyl and C1-6 heteroalkyl, and the C1-6 alkyl and C1-6 heteroalkyl are optionally substituted with 1, 2 or 3 R;
- R is selected from halogen, OH, NH2, CN, C1-6 alkyl, C1-6 heteroalkyl and C3-6 membered cycloalkyl, and the C1-6 alkyl, C1-6 heteroalkyl and C3-6 membered cycloalkyl are optionally substituted with 1, 2 or 3 R′;
- R′ is selected from F, Cl, Br, I, OH, NH2, CN, CH3, CH3CH2, CH3O, CF3, CHF2, CH2F, cyclopropyl, propyl, isopropyl, N(CH3)2 and NH(CH3);
- “hetero” means a heteroatom or a heteroatomic group, the “hetero” in the 3-8 membered heterocycloalkyl, C1-6 heteroalkyl, 5-6 membered heterocycloalkenyl, 5-6 membered heteroaryl, 4-6 membered heterocycloalkyl and C1-3 heteroalkyl is each independently selected from —C(═O)N(R)—, —N(R)—, —NH—, N, —O—, —S—, —C(═O)O—, —C(═O)—, —C(═S)—, —S(═O)—, —S(═O)2— and —N(R)C(═O)N(R)—;
- in any of the cases above, the number of heteroatoms or heteroatomic groups is each independently selected from 1, 2 and 3.
16 more elements
A compound of the following formula or a pharmaceutically acceptable salt thereof, selected from
Dependencies are inferred from the claim text.