Thiolactones
AssigneeGuilford Pharmaceuticals Inc.
InventorsBarbara S. Slusher, Takashi Tsukamoto
Life of this patent
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Abstract
This invention provides new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, inhibiting angiogenesis, effecting a TGF-β activity or a neuronal activity, and treating a glutamate abnormality, a compulsive disorder, neuropathy, pain, a prostate disease, cancer, Huntington's disease, diabetes, a retinal disorder or glaucoma.
Claims8
A compound of formula I,
- or a pharmaceutically acceptable equivalent, an optical isomer or a mixture of isomers of the compound, wherein:
- X is C1–C4 alkylene, C2–C4 alkenylene, C2–C4 alkynylene, C3–C8 cycloalkylene, C5–C7 cycloalkenylene or Ar, wherein the alkylene, alkenylene, alkynylene, cycloalkylene or cycloalkenylene is unsubstituted or substituted with one or more substituent(s);
- L is a bond, —CR1R2—, —O—, —S—, —SO2— or —NR1—;
- Y is —CR3R4—;
- Z is —(CR5R6)n—;
- n is 2;
- Ar is a bivalent aryl or heteroaryl radical that is unsubstituted or substituted with one or more substituent(s);
- R1, R2, R3, R4, R5 and R6 are independently hydrogen, C1–C4 alkyl or C2–C4 alkenyl, wherein the alkyl or alkenyl is unsubstituted or substituted with one or more substituent(s);
- R7 is hydrogen, phenyl, phenylethyl or benzyl wherein the phenyl, phenylethyl or benzyl is unsubstituted or substituted with one or more substituent(s);
- and
- R8, R9, R10 and R11 are independently hydrogen, carboxy, hydroxy, halo, nitro, cyano, C1–C4 alkyl or C1–C4 alkoxy;
- provided that when the compound is of formula I, L is a bond and X is ethyl, then Y is not —CR3R4—.
A pharmaceutical composition comprising:
- (i) an effective amount of a compound of formula I,
- or a pharmaceutically acceptable equivalent, an optical isomer or a mixture of isomers of the compound, wherein:
- X is C1–C4 alkylene, C2–C4 alkenylene, C2–C4 alkynylene, C3–C8 cycloalkylene, C5–C7 cycloalkenylene or Ar, wherein the alkylene, alkenylene, alkynylene, cycloalkylene or cycloalkenylene is unsubstituted or substituted with one or more substituent(s);
- L is a bond, —CR1R2—, —O—, —S—, —SO2— or —NR1—;
- Y is —CR3R4;
- Z is —(CR5R6)n—;
- n is 2;
- Ar is a bivalent aryl or heteroaryl radical that is unsubstituted or substituted with one or more substituent(s);
- R1, R2, R3, R4, R5 and R6 are independently hydrogen, C1–C4 alkyl or C2–C4 alkenyl, wherein the alkyl or alkenyl is unsubstituted or substituted with one or more substituent(s);
- R7 is hydrogen, phenyl, phenylethyl or benzyl wherein the phenyl, phenylethyl or benzyl is unsubstituted or substituted with one or more substituent(s);
- and
- R8, R9, R10 and R11 are independently hydrogen, carboxy, hydroxy, halo, nitro, cyano, C1–C4 alkyl or C1–C4 alkoxy;
- and
- (ii) a pharmaceutically acceptable carrier.
A compound which is 3-(2-oxo-tetrahydrothiopyran-3-yl)-propionic acid or a pharmaceutically acceptable equivalent, an optical isomer or a mixture of isomers thereof.
Dependencies are inferred from the claim text.