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Details for Patent: 6,380,226

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Details for Patent: 6,380,226

Title: Salts of an anti-migraine indole derivatives
Abstract:A crystalline, .beta.-polymorphic form of a compound of formula (I): ##STR1##
Inventor(s): Harding; Valerie Denise (Sandwich, GB), Macrae; Ross James (Sandwich, GB), Ogilvie; Ronald James (Sandwich, GB)
Assignee: Pfizer Inc (New York, NY)
Filing Date:Jun 15, 2000
Application Number:09/596,017
Claims:1. A crystalline, .beta.-polymorphic form of a compound of formula (I): ##STR3##

2. A crystalline, .beta.-polymorphic form of a compound according to claim 1 characterised by an infra-red spectrum as a mull in nujol which shows significant absorption bands at .nu.=3239, 2672, 2656, 2632, 1409, 1366, 1351, 1334, 1303, 1293, 1152, 1138, 1122, 1098, 1086, 791, 771, 746, 688, 634, 557, 528, 484, 476, 469, 463, 455, 432, 424, 413 and 401 cm.sup.-1.

3. A compound according to claim 2 which is further characterised by a powder X-ray diffraction pattern obtained using copper radiation filtered with a graphite monochromator (.lambda.=0.15405 nm) which shows main peaks at 11.0, 17.2, 19.2, 20.1, 21.6. 22.6. 23.6 and 24.8 degrees 2.theta..

4. A pharmaceutical composition for the treatment of a medical condition for which a selective agonist of 5-HT.sub.1 receptors is indicated, comprising an amount of the compound of claim 1 effective in treating such condition and a pharmaceutically acceptable carrier.

5. A pharmaceutical composition for the treatment of a medical condition selected from the group consisting of migraine, cluster headache, chronic paroxysmal hemicrania or headache associated with a vascular disorder, depression, anxiety, an eating disorder, obesity, drug abuse, hypertension and emesis, comprising an amount of the compound of claim 1 effective in treating such condition and a pharmaceutically acceptable carrier.

6. A method of treatment of a human being for a medical condition for which a selective agonist of 5-HT.sub.1 receptors is indicated, comprising administering to said human being an amount of a compound according to claim 1 effective in treating such condition.

7. A method for the treatment of a medical condition selected from the group consisting of migraine, cluster headache, chronic paroxysmal hemicrania or headache associated with a vascular disorder, depression, anxiety, an eating disorder, obesity, drug abuse, hypertension, and emesis, comprising administering to said human being an amount of a compound according to claim 1 effective in treating such condition.

8. A process for the preparation of a crystalline, .beta.-polymorphic form of a compound of formula (I): ##STR4##

characterized by an infra-red spectrum as mull in nujol which shows significant absorption bands at v=3239, 2672, 2656, 2632, 1409, 1366, 1351, 1334, 1303, 1293, 1152, 1138, 1122, 1098, 1086, 791, 771, 746, 688, 634, 557, 528, 484, 476, 469, 463, 455, 432, 424, 413, and 401 cm.sup.-1 which comprises (a) treatment of a solution of a compound of formula (II): ##STR5##

in a suitable solvent with an aqueous solution of hydrogen bromide and (b) crystallisation from said suitable solvent.

9. A process according to claim 8 wherein the suitable solvent is acetone or an ether solvent such as tetrahydrofuran or 1,2-dimethoxyethane, the aqueous solution of hydrogen bromide is 49% w/w and the treatment therewith is conducted at from 0 to 10.degree. C.

10. A process according to claim 8 wherein the suitable solvent is 1,2-dimethoxyethane.
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