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US 2016/0237069 A1Published application
Inhibition of olig2 activity
AssigneeCurtana Pharmaceuticals, Inc.
InventorsGraham BEATON, Fabio TUCCI, Satheesh B. RAVULA, Hua-Yu WANG
Life of this patent
Estimating the term…
Abstract
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.
Claims23
A compound having the structure of Formula (I):
- wherein:
- A is a bond, O, CH2, or N(R10);
- 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, —NR8)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 substituted or unsubstituted C2-C7heterocycloalkyl, substituted or unsubstituted C3-C8cycloalkyl, substituted or unsubstituted C2-C7heteroaryl, —(C(R14)(R15))mR21, —(C(R14)(R15))mN(R11)(R12), or
- 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;
- or
- a pharmaceutically acceptable salt, solvate, or prodrug thereof.
25 more elements
A compound having a structure selected from:
- or a pharmaceutically acceptable salt, solvate, or prodrug thereof.
A compound having a structure selected from:
- or a pharmaceutically acceptable salt, solvate, or prodrug thereof.
A compound having a structure selected from:
- or a pharmaceutically acceptable salt, solvate, or prodrug thereof.
Dependencies are inferred from the claim text.