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Claims for Patent: 6,110,940

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Claims for Patent: 6,110,940

Title: Salts of an anti-migraine indole derivative
Abstract:The present invention relates to hydrobromide salts of 3-(N-methyl-2(R)-pyrrolidinylmethyl)-5-(2-phenylsulphonylethyl)-1H-indole having the 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)
Application Number:08/776,680
Patent Claims: 1. .alpha.-polymorphic form of a compound of formula (I): ##STR3##

2. A crystalline, .alpha.-polymorphic form of a compound according to claim 1 further characterised by an infra-red spectrum as a mull in nujol which shows significant absorption bands at .nu.=3371, 3293, 2713, 2524, 1419, 1343, 1307, 1264, 1151, 1086, 1020, 1008, 999, 922, 900, 805, 7581 740, 728, 689, 672, 652, 640, 598, 581, 573, 531, 498, 465, 457, 443, 428, 422, 414 and 399 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 9.7, 10.7, 15.9, 16.5, 17.8, 18.3, 19.3, 19.8, 20.1, 21.2, 24.4, 25.5, 25.8, 26.7, 27.6 and 29.4 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, .alpha.-polymorphic form of a compound of formula (I): characterised by an infra-red spectrum as a mull in nujol which shows significant absorption bands at .nu.=3371, 3293, 2713, 2524, 1419, 1343, 1307, 1264, 1151, 1086, 1020, 1008, 999, 922, 900, 805, 758, 740, 728, 689, 672, 652, 640, 598, 581, 573, 531, 498, 465, 457, 443, 428, 422, 414 and 399 cm.sup.-1,

which comprises

a) treatment of a solution of a compound of formula (II): ##STR4## in a first suitable solvent with an aqueous solution of hydrogen bromide, followed by crystallisation of the isolated crude oil from a second suitable solvent;

b) crystallisation of a .beta.-polymorphic form of a compound of formula (I), 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, from a suitable solvent, followed by slurrying of the resulting mixture; or

c) treatment of a solution of a compound of formula (II) in a suitable solvent with an aqueous solution of hydrogen bromide and then slurrying of the reaction mixture, optionally followed by heating under reflux, cooling and further slurrying.

9. A process according to claim 8 wherein in

a) the first suitable solvent is acetone, the second suitable solvent is 2-propanol, the aqueous solution of hydrogen bromide is 49% w/w and the treatment therewith is conducted at from 20-25.degree. C.;

b) the suitable solvent is aqueous acetone; and

c) the suitable solvent is acetone, the aqueous solution of hydrogen bromide is 62% w/w and the treatment therewith is conducted at from 0 to 5.degree. C.

10. A process according to claim 8 wherein the .alpha.-polymorphic form of a compound of formula (I) 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 9.7, 10.7, 15.9, 16.5, 17.8, 18.3, 19.3, 19.8, 20.1, 21.2, 24.4, 25.5, 25.8, 26.7, 27.6 and 29.4 degrees 2.theta. and the .beta.-polymorphic form of a compound of formula (I) 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..

11. 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 2 effective in treating such condition and a pharmaceutically acceptable carrier.

12. 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 2 effective in treating such condition and a pharmaceutically acceptable carrier.

13. 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 2 effective in treating such condition.

14. A method for the treatment of 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 2 effective in treating such condition.
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