Aryl substituted thiazolidinones and the use thereof
AssigneeEuro-Celtique S.A.
InventorsQun Sun, Donald J. Kyle, Parviz Gharagozloo, Ji Yang
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Abstract
This invention relates aryl substituted thiazolidinones of Formula I: or a pharmaceutically acceptable salt, or solvate thereof, wherein R1 and R2, are defined in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
Claims39
A compound having the Formula I:
- or a pharmaceutically acceptable salt, or solvate thereof, wherein:
- n is 1;
- R1 is selected from the group consisting of:
- where Y is alkylene, and
- R3 and R4 are the same or different and are selected from hydrogen, alkyl, aryl, or arylalkyl, or R3 and R4 together form an alkylene chain having 4 to 5 carbon atoms optionally interrupted by a nitrogen or oxygen;
- (ii) pyridylalkyl;
- and
- (iii) piperidin-4-yl, optionally substituted by alkyl, aryl or aralkyl;
- and
- R2 is selected from the group consisting of:
- (i) optionally substituted phenoxyphenyl;
- (ii) optionally substituted phenylthiophenyl;
- (iii) optionally substituted benzyloxyphenyl;
- (iv) optionally substituted benzylthiophenyl;
- wherein R6 and R7 are independently hydrogen or alkyl;
- and p and q are integers from 0 to 4;
- wherein R8 is hydrogen, halogen or alkyl;
- wherein R9 is hydrogen or alkyl;
- and
- (viii) naphthalenyl.
A compound selected from the group consisting of:
- 3-(2-piperidinylethyl)-2-phenylthiazolidin-4-one;
- 3-(2-piperidinylethyl)-2-(2-phenylethynyl)thiazolidin-4-one;
- 3-(2-piperidinylethyl)-2-(2-phenylethenyl)thiazolidin-4-one;
- 3-(2-piperidinylethyl)-2-ethylthiazolidin-4-one;
- 3-(2-piperidinylethyl)-2-propylthiazolidin-4-one;
- and
- 3-(2-piperidinylethyl)-2-methylthiazolidin-4-one.
Dependencies are inferred from the claim text.