NOVEL SESQUITERPENOID STAT3 INHIBITORS

摘要

The present disclosure provides a method of purifying pharmaceutical compositions consisting essentially of STAT3 inhibitors from a mixture of compounds, pharmaceutical compositions comprising STAT3 inhibitors used to inhibit STAT3 in tumor cells, and certain pharmaceutically acceptable salts thereof, and methods of use.

主权项

1. A compound represented by Formula I: wherein R1 is selected from the group consisting of H or methyl (CH3), 4-hydroxytigloyl, tigoyl, 2-methylacryloyl, acryloyl, acetyl, proponyl, butanyl, pentanyl, hexanyl, isodecenyl, isopentenyl, amide, substituted amide, cinnamyl, triazoles, substituted triazoles, (3-(4-(trifluoromethyl)phenyl)acryl, 3-(4-fluorophenyl)acryl, 3,7-dimethylocta-2,6-dienyl, 3-methylbut-2-enyl, 3,7-dimethyloct-6-enyl, 2-methylbut-2-enyl, 2-methylbut-2-enyl, substituted or unsubstituted C1-C4alkyl, substituted or unsubstituted C1-C9heteroalkyl, C1-C9alkoxyalkyl, C1-C9alkylaminoalkyl, substituted or unsubstituted C3-C8cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted C2-C8heterocycloalkyl, substituted or unsubstituted heteroaryl, C1-C9alkyl(aryl), C1-C4alkyl(heteroaryl), C1-C4alkyl(C3-C8cycloalkyl), or C1-C4alkyl(C2-C9heterocycloalkyl); R2 is selected from the group consisting of H, 4-hydroxytigloyl, tigoyl, 2-methylacryloyl, acryloyl, amide, substituted amide, cinnamyl, triazoles, substituted triazoles, (3-(4-(trifluoromethyl)phenyl)acryl, 3-(4-fluorophenyl)acryl, 3,7-dimethylocta-2,6-dienyl, 3-methylbut-2-enyl, 3,7-dimethyloct-6-enyl, 2-methylbut-2-enyl, 2-methylbut-2-enyl, acetyl, proponyl, butanyl, pentanyl, hexanyl, isodecenyl, isopentenyl methyl (CH3), substituted or unsubstituted C1-C9alkyl, substituted or unsubstituted C1-C9alkenyl substituted or unsubstituted C1-C4heteroalkyl, C1-C9alkoxyalkyl, C1-C9alkylaminoalkyl, substituted or unsubstituted C3-C9cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted C2-C9heterocycloalkyl, substituted or unsubstituted heteroaryl, C1-C4alkyl(aryl), C1-C4alkyl(heteroaryl), C1-C4alkyl(C3-C8cycloalkyl), or C1-C4alkyl(C2-C9heterocycloalkyl); R3 is selected from the group consisting of H or methyl (CH3) or acetyl; pharmaceutically active metabolites, or pharmaceutically acceptable solvates, pharmaceutically acceptable salts, or pharmaceutically acceptable prodrugs thereof, with the proviso that the compound is not previously known.