Back to results
US 12,583,870 B2Granted
Azaheteroaryl compound and application thereof
AssigneeShanghai Blueray Biopharma Co., Ltd.
InventorsShichao Ma, Zhongguo Zhang, Song Zhang, Wenjia Yuan
Life of this patent
Estimating the term…
Abstract
Disclosed in the present disclosure are an azaheteroaryl compound, a pharmaceutically acceptable salt thereof, and a solvate thereof. The present disclosure also provides a method for preparing said compound, a composition containing said compound, and a use of said compound in the preparation of a drug for treating a disease or disorder related to the mechanism of action of an EED protein and/or a PRC2 protein complex. (Formula 1)
Claims18
A compound as shown in formula (I), a pharmaceutically acceptable salt, hydrate, stereoisomer, or solvate thereof:
- wherein
- A is
- R01, R02 and R03 are each independently hydrogen or halogen;
- n is 0;
- m is 1 or 2;
- X is N;
- R1 is any one of the following structures:
- X1 is independently C or N;
- X2 is independently N or CR2;
- X3 is independently N or CR3;
- X4 is independently N or CR4;
- X8 is independently CR8 or N;
- X9 is independently N or CR9;
- R2 is H, halogen, —CN, —NRaRb, C1-4 alkyl, C1-4 alkyl substituted with 1, 2 or 3 R5 groups, C1-4 haloalkyl, C1-4 alkoxy, C3-6 heterocycloalkyl, C3-6 heterocycloalkyl substituted with 1, 2 or 3 R5 groups, C3-6 heterospirocycloalkyl, —CO2R16, —C(═O) NR16R17, or —NRaRb;
- each R16 and R17 are independently H or C1-4 alkyl;
- Ra and Rb are independently H or C1-4 alkyl;
- each R5 is independently —OH, C1-4 alkyl, C1-4 alkoxy, C1-4 alkoxy substituted with 1, 2 or 3 hydroxyl groups, —NRa1Rb1, C3-6 heterocycloalkyl, C3-6 heterocycloalkyl substituted with 1, 2 or 3 C1-4 alkyl groups, C36 heterocycloalkyl substituted with 1, 2 or 3 C3-6 heterocycloalkyl groups, or C1-15 heteroaryl;
- Ra1 and Rb1 are independently H, C1-4 alkyl, C1-4 alkyl substituted with 1, 2 or 3 —NRa2Rb2 groups, or C1-4 alkyl substituted with 1, 2 or 3 hydroxyl groups;
- Ra2 and Rb2 are independently H or C1-4 alkyl;
- the heteroatom in the C3-6 heterocycloalkyl is selected from N, O and S, and the number of the heteroatom is 1, 2, 3 or 4;
- the heteroatom in the C3-6 heterospirocycloalkyl is selected from N, O and S, and the number of the heteroatom is 1, 2, 3 or 4;
- the heteroatom in the C1-15 heteroaryl is selected from N, O and S, and the number of the heteroatom is 1, 2, 3, 4, 5 or 6;
- R3 is H, halogen, —CN, C1-4 alkyl, C1-4 alkoxy, C1-4 haloalkyl, or —C(═O) NR16R17;
- R4 is H, halogen, or C1-4 alkyl;
- R6 is H, halogen, —CN, C1-4 alkyl, C1-4 alkyl substituted with 1, 2 or 3 R5 groups, —CO2R16, —C(═O)NR16R17, —(C═O)R16, SO2R16, or —POR16R17;
- each R16 and each R17 are independently H, C1-4 alkyl, or C3-6 heterocycloalkyl;
- each R5 is independently —OH, —CN, —NRa1Rb1, C6-18 aryl, —C(═O)NR16aR17a, —CO2R16a, —O(C═O)R16a, —NH(C═O)R16a, or —(C═O)R16a;
- Ra1 and Rb1 are independently H or C1-4 alkyl;
- each R16a and R17a are independently H, C1-4 alkyl or C3-6 heterocycloalkyl;
- R7 is H, —OH, —NRaRb, C1-4 alkyl, C1-4 alkyl substituted with 1, 2 or 3 hydroxyl groups, C1-4 haloalkyl, —CO2R16, or —C(═O)NR16R17;
- Ra and Rb are independently H or C1-4 alkyl;
- R16 and R17 are independently H, C1-4 alkyl or C1-4 haloalkyl;
- R8 is H or C1-4 alkyl;
- R9 is H, halogen, or C1-4 alkyl;
- R10 is H, halogen, C1-4 alkyl, or C1-4 alkyl substituted with 1, 2 or 3 R5 groups;
- each R5 is independently —NRa1Rb1;
- Ra1 and Rb1 are independently H or C1-4 alkyl;
- R11 is H, halogen, or C1-4 alkyl;
- R12, R13, R14, and R15 are H.
36 more elements
Dependencies are inferred from the claim text.