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US 2021/0253535 A1Published application
Inhibition of olig2 activity
AssigneeCurtana Pharmaceuticals, Inc.
InventorsGraham BEATON, Stanton F. McHARDY, Ambrosio LOPEZ, Jr., Bismarck CAMPOS, Hua-Yu Leo 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.
Claims82
A compound having the structure of Formula (I):
- wherein:
- naphthalene or a bicyclic C5-C9heteroaryl, wherein
- is unsubstituted or substituted by 1, 2, or 3 R1 groups;
- each R1 is independently halogen, —CN, —NO2, —OH, —OCF, —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-C9heteroaryl;
- R2 and R3 are each independently H, —CN, C1-C4alkyl, C3-C6cycloalkyl, or C2-C7heterocycloalkyl;
- or R2 and R3 are taken together to form a 5- or 6-membered heterocyclic ring;
- R4 and R5 are 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-C9heteroaryl;
- R6 is H, unsubstituted C1-C6alkyl, C1-C6haloalkyl, —(C(R14)(R15))mR17, —(C(R14)(R15))mN(R11)(R12), —(C(R14)(R15))mOR13, —(C(R14)(R15))nR16, or —OR22;
- each R8 is independently H or substituted or unsubstituted C1-C6alkyl;
- each R9 is independently substituted or unsubstituted C1-C6alkyl;
- R10 is H or unsubstituted C1-C4alkyl;
- R11 is H, substituted or unsubstituted C1-C6alkyl, —C(═O)R19, or —S(═O)2R19;
- R12 is H or substituted or unsubstituted C1-C6alkyl;
- R13 is H or substituted or unsubstituted C1-C6alkyl;
- each R14 and R15 is each independently H, halogen, or substituted or unsubstituted C1-C6alkyl;
- R16 is substituted or unsubstituted C2-C7heterocycloalkyl or —C(═O)N(R18)2;
- R17 is —C(═O)R20, —CO2R21, —C(═O)N(R21)2, or substituted or unsubstituted C2-C9heteroaryl;
- each R18 is independently H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C2-C7heterocycloalkyl, or substituted or unsubstituted C3-C8cycloalkyl;
- or
- two R18 are taken together to form a heterocycloalkyl ring;
- R19 is substituted or unsubstituted C1-C6alkyl;
- R20 is substituted or unsubstituted C1-C6alkyl;
- each R21 is independently H, or substituted or unsubstituted C1-C6alkyl;
- or two R21 are taken together to form a heterocycloalkyl ring;
- R22 is H, or substituted or unsubstituted C1-C6alkyl;
- m is 2-6;
- and
- n is 1-5;
- or
- a pharmaceutically acceptable salt, solvate, or prodrug thereof.
27 more elements
A compound having the structure of Formula (II):
- wherein:
- each R1 is independently halogen, —CN, —NO2, —OH, —OCF, —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 phenoxy, 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 and R3 are each independently H, —CN, C1-C4alkyl, C3-C6cycloalkyl, or C2-C7heterocycloalkyl;
- or R2 and R3 are taken together to form a 5- or 6-membered heterocyclic ring;
- R4 is 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;
- R6 is —OR7;
- R7 is H, or substituted or unsubstituted C1-C6alkyl;
- each R8 is independently H, or substituted or unsubstituted C1-C6alkyl;
- each R9 is independently substituted or unsubstituted C1-C6alkyl, or substituted or unsubstituted C6-C10aryl;
- and
- n is 0-5;
- or
- a pharmaceutically acceptable salt, solvate, or prodrug thereof.
11 more elements
A compound selected from:
- a pharmaceutically acceptable salt, solvate, or prodrug thereof.
A compound selected from:
- or a pharmaceutically acceptable salt solvate, or prodrug thereof.
A compound selected from:
- or a pharmaceutically acceptable salt, solvate, or prodrug thereof.
A compound having the structure:
- or a pharmaceutically acceptable salt, solvate or prodrug thereof.
A compound selected from:
- or a pharmaceutically acceptable salt, solvate, or prodrug thereof.
A compound selected from:
- or a pharmaceutically acceptable salt, solvate, or prodrug thereof.
Dependencies are inferred from the claim text.