Novel small molecule brd4 modulators for hiv epigenetic regulation
AssigneeBoard of Regents, The University of Texas System
InventorsHaitao Hu, Jia Zhou, Zhiqing Liu
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Abstract
The invention relates generally to novel small molecule BRD4 modulators for HIV, the preparation thereof as well as the use thereof.
Claims18
A compound, or a pharmaceutically acceptable salt thereof, having the formula:
- wherein
- R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently H, —OH, alkyl, alkoxy, halogen, —NH2, —OCF3 or —CF3;
- R10, R11 and R12 are independently H, —OH, halogen, alkoxy, —NH2, —CF3, —(CO)R13 where R13 is alkyl, alkoxy, amino, or alkylamino;
- —NR22R23 where R22 and R23 are independently H, alkyl;
- or R22 and R23 are optionally joined to form a 3-6 membered substituted or unsubstituted heterocycle having 1-3 heteroatoms;
- Linker is —(CO)NR25-, NR26 or —R27(CO)—, wherein R25, R26 and R27 are independently H or C1-C6 alkyl;
- and
- n is 0-3.
- Ring A is chosen from 5-6 membered aromatic rings containing 0-3 nitrogen atoms.
A compound, or a pharmaceutically acceptable salt thereof, having the formula:
- wherein
- R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently H, —OH, alkyl, alkoxy, halogen, —NH2, —OCF3 or —CF3;
- Ring B is chosen from substituted or unsubstituted C4-C7 aliphatic rings;
- Linker is —NHCONR24-, —CONR25-, NR26 or —R27CO—, where R24, R25, R26 and R27 are independently H or C1-C6 alkyl;
- and
- n is 0-3.
A compound, or a pharmaceutically acceptable salt thereof, having the formula:
- wherein
- R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently H, —OH, alkyl, alkoxy, halogen, —NH2, —OCF3 or —CF3;
- R10, R11 and R12 are independently H, —OH, halogen, alkoxy, —NH2, —CF3, —(CO)R13 where R13 is alkyl, alkoxy, amino, or alkylamino;
- —NR22R23 where R22 and R23 are independently H, alkyl;
- or R22 and R23 are optionally joined to form a 3-6 membered substituted or unsubstituted heterocycle having 1-3 heteroatoms.
A compound of any of the preceding claims, where the compound is:
A compound, or a pharmaceutically acceptable salt thereof, having the formula:
- wherein
- R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently H, —OH, alkyl, alkoxy, halogen, —NH2, —OCF3 or —CF3;
- R10, R11 and R12 are independently H, —OH, halogen, alkoxy, —NH2, —CF3, —(CO)R13 where R13 is alkyl, alkoxy, amino, or alkylamino;
- —NR22R23 where R22 and R23 are independently H, alkyl;
- or R22 and R23 are optionally joined to form a 3-6 membered substituted or unsubstituted heterocycle having 1-3 heteroatoms;
- Linker is —NH(CO)NR24-, wherein R24 is C1-C6 alkyl;
- n is 0-3;
- and
- Ring A is chosen from 5-6 membered aromatic rings containing 0-3 nitrogen atoms.
A compound, or a pharmaceutically acceptable salt thereof, having the formula:
- wherein
- R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently H, —OH, alkyl, alkoxy, halogen, —NH2, —OCF3 or —CF3;
- R10, R11 and R12 are independently H, —OH, halogen, alkoxy, —NH2, —CF3, —(CO)R13 where R13 is alkyl, alkoxy, amino, or alkylamino;
- —NR22R23, where R22 and R23 are independently H, alkyl;
- or R22 and R23 are optionally joined to form a 3-6 membered substituted or unsubstituted heterocycle having 1-3 heteroatoms;
- Linker is —NH(CO)NH—,
- n is 0-3;
- and
- Ring A is chosen from 5-6 membered aromatic rings containing 0-3 nitrogen atoms.
A method comprising contacting one or more cells with one or more compounds of Formulas I, II, III, IV, Ia, or Ib, or a pharmaceutically acceptable salt thereof.
A method of treating HIV comprising administering one or more compounds of Formulas I, II, III, IV, V, Va′, Va″, Vb, Vb′, Vb″, Ia, and Ib, or a pharmaceutically acceptable salt thereof, to a subject.
A compound, or a pharmaceutically acceptable salt thereof, having the formula:
- wherein R28 is substituted or unsubstituted aryl.
Dependencies are inferred from the claim text.