Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of Olig2. Also described herein are methods of using such Olig2 inhibitors, alone and in combination with other compounds, for treating cancer and other diseases. In particular the Ol
Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of Olig2. Also described herein are methods of using such Olig2 inhibitors, alone and in combination with other compounds, for treating cancer and other diseases. In particular the Olig2 inhibitors may be used to treat glioblastoma.
대표청구항▼
1. A compound having the structure of Formula (I): A is O or CH2;X, Y, and Z are each independently N, or C(R7);each R1 is independently halogen, —CN, —NO2, —OH, —OCF3, —OCH2F, —OCF2H, —CF3, —SR8, —N(R8)S(═O)2R9, —S(═O)2N(R8)2, —S(═O)R9, —S(═O)2R9, —C(═O)R9, —CO2R8, —N(R8)2, —C(═O)N(R8)2, —N(R8)C(═O
1. A compound having the structure of Formula (I): A is O or CH2;X, Y, and Z are each independently N, or C(R7);each R1 is independently halogen, —CN, —NO2, —OH, —OCF3, —OCH2F, —OCF2H, —CF3, —SR8, —N(R8)S(═O)2R9, —S(═O)2N(R8)2, —S(═O)R9, —S(═O)2R9, —C(═O)R9, —CO2R8, —N(R8)2, —C(═O)N(R8)2, —N(R8)C(═O)R9, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6alkoxy, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C2-C7heterocycloalkyl, substituted or unsubstituted C3-C8cycloalkyl, substituted or unsubstituted C6-C10aryl, or substituted or unsubstituted C2-C7heteroaryl; or two R1 are taken together to form a substituted or unsubstituted heterocyclic ring or a substituted or unsubstituted carbocyclic ring;R2, R3, and R4 are each independently H, —CN, C1-C4alkyl, C3-C6cycloalkyl, or C2-C7heterocycloalkyl; or two of R2, R3, and R4 are taken together to form a 5- or 6-membered heterocyclic ring;R5 is halogen, —CN, —OH, —CF3, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6alkoxy, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C2-C7heterocycloalkyl, substituted or unsubstituted C3-C8cycloalkyl, substituted or unsubstituted C6-C10aryl, or substituted or unsubstituted C2-C7heteroaryl;R6 is R11 and R12 are each independently H, or substituted or unsubstituted C1-C6alkyl; or R11 and R12 are taken together to form a 5-, 6-, 7-, or 8-membered heterocyclic ring;J is C(H), or N;R13 is H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C7heterocycloalkyl, substituted or unsubstituted C3-C8cycloalkyl, substituted or unsubstituted —C1-C4alkylC6-C10aryl, or substituted or unsubstituted —C1-C4alkylC2-C7heteroaryl;each R7 is independently H, halogen, —CN, —OH, —CF3, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6alkoxy, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C2-C7heterocycloalkyl, substituted or unsubstituted C3-C8cycloalkyl, substituted or unsubstituted C6-C10aryl, or substituted or unsubstituted C2-C7heteroaryl;each R14 and R15 are each independently H, or substituted or unsubstituted C1-C6alkyl; or R14 and R15 are taken together to form a 4-, 5-, 6-membered cycloalkyl ring;R21 is halogen, —CN, —NO2, —OH, —OCF3, —OCH2F, —OCF2H, —CF3, —SR22, —N(R22)S(═O)2R23, —S(═O)2N(R22)2, —S(═O)R23, —S(═O)2R23, —C(═O)R23, —CO2R22, —C(═O)N(R22)2, —N(R22)C(═O)R23, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6alkoxy, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C2-C7heterocycloalkyl, substituted or unsubstituted C3-C8cycloalkyl, substituted or unsubstituted C6-C10aryl, or substituted or unsubstituted C2-C7heteroaryl;each R22 is independently H, or substituted or unsubstituted C1-C6alkyl;R23 is substituted or unsubstituted C1-C6alkyl;each R8 is independently H, or substituted or unsubstituted C1-C6alkyl;R9 is substituted or unsubstituted C1-C6alkyl;R10 is H, or C1-C4alkyl;m is 2-6;n is 0-5;p is 1-3;q is 1-3; ora pharmaceutically acceptable salt or solvate thereof. 2. The compound of claim 1, wherein R2, R3, and R4 are each independently H, —CN, C1-C4alkyl, C3-C6cycloalkyl, or C2-C7heterocycloalkyl. 3. The compound of claim 1, wherein R2 is C1-C4alkyl, C3-C6cycloalkyl, or C2-C7heterocycloalkyl; R3 is H; and R4 is H. 4. The compound of claim 3, wherein R2 is CH3 or C3-C6cycloalkyl. 5. The compound of claim 1, wherein R2 is H; R3 is C1-C4alkyl, C3-C6cycloalkyl, or C2-C7heterocycloalkyl; and R4 is H. 6. The compound of claim 5, wherein R3 is CH3. 7. The compound of claim 1, wherein R13 is —CH3 or —CH2CH3. 8. The compound of claim 1, wherein J is N. 9. The compound of claim 1, wherein R5 is substituted or unsubstituted C1-C6alkyl. 10. The compound of claim 9, wherein R5 is CH3 or CH2CH3. 11. The compound of claim 1, wherein each R1 is independently halogen, —CN, —NO2, —OH, —CF3, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6alkoxy, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C2-C7heterocycloalkyl, substituted or unsubstituted C3-C8cycloalkyl, substituted or unsubstituted C6-C10aryl, or substituted or unsubstituted C2-C7heteroaryl. 12. The compound of claim 1, wherein X is C(R7); Y is N; Z is N; and R7 is H. 13. A compound having a structure selected from: or a pharmaceutically acceptable salt or solvate thereof. 14. A pharmaceutical composition comprising a compound of claim 1, or a pharmaceutically acceptable salt or solvate thereof, and at least one pharmaceutically acceptable excipient. 15. A method for treating a disease in a subject comprising administering to the subject in need thereof a composition comprising a compound of claim 1, or a pharmaceutically acceptable salt or solvate thereof; wherein the disease is Down's Syndrome or cancer selected from brain cancer, glioblastoma multiforme, medulloblastoma, astrocytomas, brain stem gliomas, meningiomas, oligodendrogliomas, melanoma, lung cancer, breast cancer, or leukemia.
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