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1. WO2000032589 - MONOHYDRATE DE BROMHYDRATE D'ELETRIPTAN

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

[ EN ]

CLAIMS
1. Eletriptan hydrobromide monohydrate of the formula (I):


2. A pharmaceutical composition including eletriptan hydrobromide
monohydrate as claimed in claim 1 together with a pharmaceutically acceptable excipient, diluent or carrier.

3. Eletriptan hydrobromide monohydrate as claimed in claim 1 for use as a medicament.

4. The use of eletriptan hydrobromide monohydrate as claimed in claim 1 for the manufacture of a medicament for the treatment of a disease or condition for which a selective agonist of a 5-HT, receptor is indicated.

5. Use as claimed in claim 4 for the treatment of a disease or condition for which a selective agonist of a 5-HT1B/1D receptor is indicated.

6. The use of eletriptan hydrobromide monohydrate as claimed in claim 1 for the manufacture of a medicament for the treatment of a disease or condition selected from migraine, recurrent migraine, hypertension, depression, emesis, anxiety, an eating disorder, obesity, drug abuse, cluster headache, pain, chronic paroxysmal hemicrania and headache associated with a vascular disorder.

7. Use as claimed in claim 6 for the treatment of migraine or recurrent migraine.

8. A method of treatment of a mammal to treat a disease or condition for which a selective agonist of a 5-HT, receptor is indicated which includes treating said mammal with an effective amount of eletriptan hydrobromide
monohydrate as claimed in claim 1.

9. A method as claimed in claim 8 to treat a disease or condition for which a selective agonist of a 5-HT1B/1D receptor is indicated.

10. A method of treatment of a mammal to treat a disease or condition selected from migraine, recurrent migraine, hypertension, depression, emesis, anxiety, an eating disorder, obesity, drug abuse, cluster headache, pain, chronic paroxysmal hemicrania and headache associated with a vascular disorder which includes treating said mammal with an effective amount of eletriptan hydrobromide monohydrate as claimed in claim 1.

11. A method as claimed in claim 10 to treat migraine or recurrent migraine.

12. A process for the preparation of eletriptan hydrobromide monohydrate as claimed in claim 1 which comprises treatment of a solution of eletriptan in water, or in an organic solvent containing a sufficient amount of water to facilitate formation of the required monohydrate, with hydrogen bromide or a source thereof.

13. A process as claimed in claim 12 wherein the organic solvent is
tetrahydrofu ran or acetone.

14. A process as claimed in claim 12 or 13 wherein hydrogen bromide is used in the form of an aqueous solution.

15. A process for the preparation of eletriptan hydrobromide monohydrate as claimed in claim 1 which comprises crystallisation of any other form of eletriptan hydrobromide, or a mixture thereof, from water, or from an organic solvent containing a sufficient amount of water to facilitate formation of the required monohydrate.

16. A process as claimed in claim 15 wherein the organic solvent is acetone.

17. A process for the preparation of anhydrous eletriptan hydrobromide which comprises dehydration of any hydrated form of eletriptan hydrobromide, preferably eletriptan hydrobromide monohydrate as claimed in claim 1 , or a mixture thereof.