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1. WO2008002596 - ANTAGONISTES DU RÉCEPTEUR A2A DE L'ADÉNOSINE

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

[ EN ]

We claim:

1. A compound represented by the structural formula



or a pharmaceutically acceptable salt thereof, wherein:
X1 is 1-3 substituents independently selected from the group consisting of H, alkyl, halo, -CF3, -OCF3, alkoxy, -OH and -CN;
X2 is 1-3 substituents independently selected from the group consisting of H, alkyl, halo, -CF3, -OCF3, alkoxy, -OH and -CN;
n is 0, 1 or 2; and
R and R1 are independently selected from the group consisting of H and alkyl.

2. A compound of claim 1 wherein n is 1.

3. A compound of claim 1 wherein R and R1 are each H.

4. A compound of claim 1 wherein X1 is 1 or 2 substituents independently selected from H, halo, alkyl, alkoxy and -CF3.

5. A compound of claim 4 wherein X1 is 1 or 2 substituents independently selected from H, fluoro, chloro, methyl, methoxy and -CF3.

6. A compound of claim 1 wherein X2 is 1, 2 or 3 substituents independently selected from H, halo, alkyl, alkoxy, -CF3, -OCF3 and -CN.

7. A compound of claim 6 wherein X2 is 1 , 2 or 3 substituents independently selected from H, fluoro, chloro, methyl, methoxy, -CF3, -OCF3 and -CN.

8. A compound of claim 1 wherein n is 1 ; R and R1 are each H; X1 is 1 or 2 substituents independently selected from H, halo, alkyl, alkoxy and -CF3; and X2 is 1, 2 or 3 substituents independently selected from H, halo, alkyl, alkoxy, -CF3, -OCF3 and -CN.

9. A compound of claim 8 wherein X1 is 1 or 2 substituents independently selected from H, fluoro, chloro, methyl, methoxy and -CF3, and X2 is 1 , 2 or 3 substituents independently selected from H, fluoro, chloro, methyl, methoxy, -CF3, -OCF3 and -CN.

10. A compound of claim 1 selected from the group consisting of



and

11. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 in a pharmaceutically acceptable carrier.

12. A method of treating a central nervous system disease or stroke, comprising administering an effective amount of a compound of claim 1 to a mammal in need of such treatment.

13. A method of claim 12 for treating depression, cognitive diseases or
neurodegenerative diseases.

14. A method of claim 13 for treating Parkinson's disease, senile dementia, psychoses, attention deficit disorder, Extra Pyramidal Syndrome, dystonia, restless leg syndrome or periodic limb movement in sleep.

15. A pharmaceutical composition comprising a therapeutically effective amount of a combination of a compound of claim 1 and one to three other agents useful in treating Parkinson's disease in a pharmaceutically acceptable carrier

16. A method of treating Parkinson's disease comprising administering to a mammal in need of such treatment an effective amount of a combination of a compound of claim 1 and one to three other agents useful in treating Parkinson's disease.

17. The method of claim 16 wherein the other agents are selected from the group consisting of L-DOPA, dopaminergic agonists, MAO-B inhibitors, DOPA
decarboxylase inhibitors; COMT inhibitors and NMDA receptor antagonists.

18. A kit comprising in separate containers in a single package pharmaceutical compositions for use in combination to treat Parkinson's disease wherein one container comprises a pharmaceutical composition comprising an effective amount of a compound of claim 1 in a pharmaceutically acceptable carrier, and wherein, in separate containers, one or more pharmaceutical compositions each comprise an effective amount of an agent useful in the treatment of Parkinson's disease in a pharmaceutically acceptable carrier.