Thiazole derivatives for treating dyskinesias caused by a chemical treatment
View Patent ↗The invention relates to the use of derivatives of thiazoles having general formula (I) for the preparation of a medicament for the treatment or prevention of dyskinesias caused by a chemical treatment. The invention also relates to a combination of thiazole derivatives having general formula (I) and at least one compound selected from among neuroleptics or products that act on the dopaminergic system for the treatment or prevention of dyskinesias caused by a chemical treatment.
1. A method for treating a dyskinesia caused by a chemical treatment comprising administering to a patient in need thereof a compound of general formula (I)
wherein:
A represents (A1)
wherein R 5 represents hydrogen or alkyl, R 6 , R 7 , and R 8 represent independently hydrogen, alkyl, cycloalkyl, hydroxy, or alkoxy;
B represents hydrogen or alkyl;
n represents an integer from 0 to 5;
R 1 and R 2 represent independently hydrogen, alkyl, or cycloalkyl;
R 3 and R 4 represent independently hydrogen, alkyl or R 3 and R 4 form together with the nitrogen atom to which they are attached a heterocycle comprising 1 to 2 heteroatoms and 5 to 7 members, wherein the members of the heterocycle include —CH 2 —, —NR 14 —, —O— or —S—, R 14 representing a hydrogen, alkyl, —COR 15 , —COOR 15 , or —CONR 16 R 17 , R 15 representing alkyl and R 16 and R 17 represent independently hydrogen or alkyl;
or of a salt of general formula (I) defined above, wherein the compound of general formula (I) is the only active ingredient for treating the dyskinesia.
2. The method of claim 1 , wherein R 5 is hydrogen.
3. The method of claim 1 , wherein R 6 , R 7 , and R 8 represent independently hydrogen or alkyl.
4. The method of claim 1 , wherein n is between 0 and 3.
5. The method of claim 1 , wherein n is equal to 0.
6. The method of claim 1 , wherein R 1 represents hydrogen.
7. The method of claim 1 , wherein R 2 represents hydrogen or alkyl.
8. The method of claim 1 , wherein R 3 or R 4 represents hydrogen or alkyl.
9. The method of claim 1 , wherein the method treats induced dyskinesia or tardive dyskinesia.
10. The method of claim 1 , wherein the method treats a dyskinesia caused by levodopa (L-Dopa), levodopa-benzerazide combination, levodopa-carbodopa combination, pergolide, quinpirole, carbergoline, benzotropine, trihexylphenidyl, ropinirole, or pramipexole.
11. The method of claim 1 , wherein the compound is:
4-[2-(aminomethyl)-1,3-thizol-4-yl]-2,6-di(tert-butyl)phenyl;
4-{2-[(1R)-1-aminoethyl]-1,3-thiazol-4-yl}-2,6-di-tert-butylphenol; or
4-{2-[(1S)-1-aminoethyl]-1,3-thiazol-4-yl}-2,6-di-tert-butylphenol.