IDO inhibitors and methods of use
AssigneeLankenau Institute for Medical Research
InventorsGeorge C. Prendergast, Alexander J. Muller, James B. Duhadaway, William Malachowski
Life of this patent
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Abstract
Compounds, compositions and methods for the treatment of malignancy are disclosed.
Claims8
A pharmaceutical composition comprising an effective amount of a compound having indoleamine 2,3 dioxygenase (IDO) inhibitory activity and a pharmaceutically acceptable carrier medium, said compound being of formula (I):
- wherein R1 is H or lower alkyl;
- R2 is H;
- R3 is
- wherein RA is selected from the group consisting of (C3-C6)alkenyl, substituted or unsubstituted aralkyl and substituted or unsubstituted cycloalkyl, and RB is selected from the group consisting of H, (C1-C6) alkyl, (C3-C6) alkenyl, substituted or unsubstituted aralkyl and substituted or unsubstituted cycloalkyl, said substituted aralkyl and substituted cycloalyl having one or two substituents selected from the group of halo, (C1-C4)haloalkyl, (C1-C4)alkoxy, (C1-C4)alkythio, hydroxyl, carbonyl, epoxy, —C(═O)—OR, —OC(═O)—R, amino, —NHC(═O)—R, —NHCONH2, —NHCONHR or thiol wherein R represents hydrogen or (C1-C4)alkyl;
- X, Y, and Z may be the same or different and are selected from the group consisting of H, halogen, NO2, and hydrocarbyl;
- with the proviso that formula (I) does not include 3-(N-allyl-thiohydantoin)-indole.
A pharmaceutical composition comprising an effective amount of at least one indoleamine 2,3-dioxygenase (IDO) inhibitor and at least one signal transduction inhibitor (STI) in a pharmaceutically acceptable carrier medium, wherein said at least one IDO inhibitor is selected from the group of compounds of the structure of formula (I):
- wherein R1 is H or lower alkyl;
- R2 is H;
- R3 is
- wherein RA is selected from the group consisting of (C3-C6)alkenyl, substituted or unsubstituted aralkyl and substituted or unsubstituted cycloalkyl, and RB is selected from the group consisting of H, (C1-C6) alkyl, (C3-C6) alkenyl, substituted or unsubstituted aralkyl and substituted or unsubstituted cycloalkyl, said substituted aralkyl and substituted cycloalyl having one or two substituents selected from the group of halo, (C1-C4)haloalkyl, (C1-C4)alkoxy, (C1-C4)alkythio, hydroxyl, carbonyl, epoxy, —C(═O)—OR, —OC(═O)—R, amino, —NHC(═O)—R, —NHCONH2, —NHCONHR or thiol wherein R represents hydrogen or (C1-C4)alkyl;
- X, Y, and Z may be the same or different and are selected from the group consisting of H, halogen, NO2, and hydrocarbyl;
- with the proviso that formula (I) does not include 3-(N-allyl-thiohydantoin)-indole.
A pharmaceutical composition comprising an effective amount of at least one indoleamine 2,3-dioxygenase (IDO) inhibitor and at least one chemotherapeutic agent in a pharmaceutically acceptable carrier medium, wherein said at least one IDO inhibitor is selected from the group of compounds of formula (I):
- wherein R1 is H or lower alkyl;
- R2 is H;
- R3 is
- wherein RA is selected from the group consisting of (C3-C6)alkenyl, substituted or unsubstituted aralkyl and substituted or unsubstituted cycloalkyl, and RB is selected from the group consisting of H, (C1-C6) alkyl, (C3-C6) alkenyl, substituted or unsubstituted aralkyl and substituted or unsubstituted cycloalkyl, said substituted aralkyl and substituted cycloalyl having one or two substituents selected from the group of halo, (C1-C4)haloalkyl, (C1-C4)alkoxy, (C1-C4)alkythio, hydroxyl, carbonyl, epoxy, —C(═O)—OR, —OC(═O)—R, amino, —NHC(═O)—R, —NHCONH2, —NHCONHR or thiol wherein R represents hydrogen or (C1-C4)alkyl;
- X, Y, and Z may be the same or different and are selected from the group consisting of H, halogen, NO2, and hydrocarbyl;
- with the proviso that formula (I) does not include 3-(N-allyl-thiohydantoin)-indole.
Dependencies are inferred from the claim text.