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US 8,946,444 B2Granted
Tetrahydrocarbazoles as active agents for inhibiting VEGF production by translational control
AssigneePTC Therapeutics, Inc.
InventorsWilliam Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
Life of this patent
Estimating the term…
Abstract
The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.
Claims12
A compound of Formula (I),
- or an enantiomer, a diastereomer, a pharmaceutically acceptable salt, or a mixture thereof, wherein:
- (a) X is selected from the group consisting of:
- wherein NR9R10 is selected from the group consisting of:
- wherein NR9R10 is capable of being substituted with substituents selected from the group consisting of:
- or wherein X may be a substituted
- (b) R1, R2 and R3 are each —H;
- (c) n is 1 or 2;
- (d) R4, R6 and R7 are each independently —H, or halo;
- R5 is independently —OH, substituted or unsubstituted C1-6 alkyl, unsubstituted aminocarbonyl, unsubstituted alkoxy, halo, haloalkyl, haloalkoxy, nitro, cyano, substituted or unsubstituted heterocyclic ring, substituted or unsubstituted amino, substituted or unsubstituted phenyl, substituted or unsubstituted phenoxy, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, or substituted or unsubstituted alkoxycarbonyl, or hydroxycarbonyl;
- (e) W is N;
- (f) R8 is H;
- wherein the term “substituted” denotes that a moiety has one or more hydrogen atoms replaced by one or more substituents selected from the group consisting of:
- wherein R30 and R31 are each independently H or alkyl;
- or R30 and R31 together with the nitrogen to which they are bound form a 5-7 membered nitrogen containing heterocyclic ring;
- and
- (g) with the proviso that a compound of Formula I is not a compound having the structure:
13 more elements
A compound selected from the group consisting of:
- and an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof.
A compound of Formula (VII),
- wherein
- (a) R5 is halo or C1-C6 alkyl;
- (b) R20 is H or oxo;
- (c) R21 and R22 are H;
- or
- R21 and R22, taken together with the atoms to which they are attached, may optionally form a carbocyclic aromatic ring, or a five or six membered heterocyclic ring, the heterocyclic ring containing, including the atoms to which R21 and R22 are attached, one to three heteroatoms selected from the group consisting of N, O, and S;
- and
- (d) R23 is H or oxo.
5 more elements
A compound of Formula (VIII),
- wherein
- (a) R5 is halo or C1-C6 alkyl;
- (b) R23 and R24 are selected from the group consisting of H, substituted or unsubstituted alkoxycarbonyl, substituted or unsubstituted alkylcarbonyl, formyl, cyano, and substituted or unsubstituted phenylaminoalkyl;
- or
- R23 and R24, taken together with the atoms to which they are attached, may optionally form a carbocyclic aromatic ring, or a five or six membered heterocyclic ring, the heterocyclic ring containing, including the atoms to which R23 and R24 are attached, one to three heteroatoms selected from the group consisting of N, O, and S;
- and
- (c) R8 is substituted or unsubstituted carbonyl.
4 more elements
A pharmaceutical composition comprising a pharmaceutically acceptable excipient and one or more compounds selected from the group consisting of:
- and an enantiomer, a diastereomer, a pharmaceutically acceptable salt, or a mixture thereof.
Dependencies are inferred from the claim text.