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Claims for Patent: 4,997,841

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Claims for Patent: 4,997,841

Title: Indole derivatives
Abstract:Compounds are disclosed of formula (I) ##STR1## wherein R.sub.1 represents H or C.sub.1-6 alkyl; R.sub.2 represents H or C.sub.1-6 alkyl; R.sub.3 represents H; R.sub.4 represents H or C.sub.1-3 alkyl; and pharmaceutically acceptable salts and solvates (for example hydrates thereof. The compounds are indicated as useful for the treatment of migraine, cluster headache, chronic paroxysmal hemicrania and headache associated with vascular disorders. Processes and intermediates for their preparation and pharmaceutical compositions containing them are also disclosed.
Inventor(s): Oxford; Alexander W. (Royston, GB), Sutina; Darko (Arlesey, GB), Owen; Martin R. (Puckeridge, GB)
Assignee: Glaxo Group Limited (GB2)
Application Number:07/231,274
Patent Claims: 1. A compound of formula (I) ##STR13## wherein R.sub.1 represents a hydrogen atom or a C.sub.1-6 alkyl group;

R.sub.2 represents a hydrogen atom or a C.sub.1-6 alkyl group;

R.sub.3 represents a hydrogen atom;

R.sub.4 represents a hydrogen atom or a C.sub.1-3 alkyl group;

or a pharmaceutically acceptable salt s solvate thereof.

2. A compound according to claim 1 wherein in the formula (I) R.sub.1 represents a hydrogen atom or a C.sub.1-3 alkyl group.

3. A compound according to claim 1 wherein in the formula (I) R.sub.2 represents a hydrogen atom or a C.sub.1-3 alkyl group.

4. A compound according to claim 1 wherein in the formula (I) R.sub.2 represents a C.sub.1-3 alkyl group.

5. A compound according to claim 1 wherein in the formula (I) R.sub.4 represents a C.sub.1-3 alkyl group.

6. A compound according to claim 1 which is N-Methyl-3-(1-methyl-4-piperidinyl)-1H-indole-5-ethanesulphonamide or a pharmaceutically acceptable salt or solvate thereof.

7. A compound according to claim 1 which is N,N-Dimethyl-3-(1-methyl-4-piperidinyl)-1H-indole-5-ethanesulphonamide or a pharmaceutically acceptable salt or solvate thereof.

8. A compound according to claim 1 which is N-Ethyl-3-(4-piperidinyl)-1H-indole-5-ethanesulphonamide or a pharmaceutically acceptable salt or solvate thereof.

9. A compound according to claim 1 which is N-Methyl-3-(4-piperidinyl)-1H-indole-5-ethanesulphonamide or a pharmaceutically acceptable salt or solvate thereof.

10. A compound according to claim 1 which is 3-(1-Methyl-4-piperidinyl)-1H-indole-5-ethanesulphonamide or a pharmaceutically acceptable salt or solvate thereof.

11. A pharmaceutical composition for use in the treatment of conditions associated with cephalic pain which comprises an effective amount to treat conditions associated with cephalic pain of at least one compound of formula (1) as defined in claim 1 or a pharmaceutically acceptable salt or solvate thereof together with one or more pharmaceutically acceptable carriers or excipients.

12. A pharmaceutical composition as claimed in claim 11 wherein the conditions associated with cephalic pain are migraine, cluster headache, chronic paroxysmal hemicrania or headache associated with vascular disorders.

13. A pharmaceutical composition according to claim 11 adapted for oral, parenteral or intranasal administration.

14. A pharmaceutical composition according to claim 11 which is formulated in unit dosage form comprising 0.1 mg to 100 mg of active ingredient.

15. A pharmaceutical composition according to claim 13 which is formulated in unit dosage form comprising 0.1 mg to 100 mg of active ingredient.

16. A method of treating a human susceptible to or suffering from migraine cluster headache, chronic paroxysmal hemicrania or headache associated with vascular disorders which comprises administering an effective amount of a compound of formula (I) as defined in claim 1 or a pharmaceutically acceptable salt or solvate thereof.

17. A method of treating a human susceptible to or suffering from migraine, cluster headache, chronic paroxysmal hemicrania or headache associated with vascular disorders which comprises administering a pharmaceutical composition according to claim 11.

18. A method of treating a human susceptible to or suffering from migraine, cluster headache, chronic paroxysmal hemicrania or headache associated with vascular disorders which comprises administering a pharmaceutical composition according to claim 13.
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