Claims for Patent: 4,317,826

Summary for Patent: 4,317,826

Title:	N,N\'-Bis[substituted-1,2,3,4 tetrahydroisoquinolyl]disulfonylimides and antiallergic compositions and method of use
Abstract:	Imidodisulfamide derivatives useful in the treatment of allergic conditions are prepared by reaction of an appropriately substituted tetrahydroisoquinoline and bis (chlorosulfonyl)imide in the presence of a tertiary amine. Pharmaceutical compositions and methods of inhibiting the symptoms of an allergic response are also disclosed.
Inventor(s):	Gleason; John G. (Delran, NJ)
Assignee:	SmithKline Corporation (Philadelphia, PA)
Application Number:	06/153,653
Patent Claims:	1. A compound of the formula (I): ##STR6## in which R.sub.1 is hydrogen, bromo, chloro, methyl or trifluoromethyl; R.sub.2 is bromo, chloro, trifluoromethyl or tetrafluoroethylthio; and X and Y independently are hydrogen or alkyl of 1 to 4 carbon atoms; or an alkali metal salt of said compound. 2. A compound according to claim 1 in which R.sub.1 is hydrogen, 8-bromo, 7-chloro, 7-methyl or 7-trifluoromethyl; R.sub.2 is 5-bromo, 6-chloro, 8-chloro, 8-trifluoromethyl or 8-tetrafluoroethylthio; X is hydrogen, isopropyl or cyclopropyl; and Y is hydrogen or methyl. 3. A compound according to claim 1, in which R.sub.1, X and Y are hydrogen; and R.sub.2 is 5-bromo or 6-chloro. 4. A compound according to claim 1, in which R.sub.1 is 7-chloro; R.sub.2 is 6-chloro, 8-chloro or 8-tetrafluoroethylthio; and X and Y are hydrogen. 5. A compound according to claim 1, in which R.sub.1 is 7-chloro; R.sub.2 is 8-chloro; X is hydrogen, isopropyl or cyclopropyl; and Y is hydrogen or methyl, provided that when X is isopropyl or cyclopropyl, Y is hydrogen. 6. A compound according to claim 1 which is N,N'-bis(5-bromo-1,2,3,4-tetrahydroisoquinolyl)disulfonylimide or an alkali metal salt thereof. 7. A compound according to claim 1 which is N,N'-bis(7,8-dichloro-1,2,3,4-tetrahydroisoquinolyl)disulfonylimide or an alkali metal salt thereof. 8. A compound according to claim 1 which is N,N'-bis(8-chloro-7-methyl-1,2,3,4-tetrahydroisoquinolyl)disulfonylimide or an alkali metal salt thereof. 9. A compound according to claim 1 which is N,N'-bis(6,7-dichloro-1,2,3,4-tetrahydroisoquinolyl)disulfonylimide or an alkali metal salt thereof. 10. A compound according to claim 1 which is N,N'-bis(7,8-dichloro-3-methyl-1,2,3,4-tetrahydroisoquinolyl)-disulfonylim ide or an alkali metal salt thereof. 11. A compound according to claim 1 which is N,N'-bis(7,8-dichloro-1-isopropyl-1,2,3,4-tetrahydroisoquinolyl)disulfonyl imide or an alkali metal salt thereof. 12. A compound according to claim 1 which is N,N'bis(7,8-dichloro-1-cyclopropyl-1,2,3,4-tetrahydroisoquinolyl)disulfony limide or an alkali metal salt thereof. 13. A pharmaceutical composition for inhibiting the symptoms of asthma comprising a pharmaceutical carrier or diluent and an amount sufficient to produce said inhibition of a compound of claim 1. 14. A pharmaceutical composition according to claim 13 in a form suitable for administration by inhalation. 15. A pharmaceutical composition according to claim 13 comprising a solution or suspension of the active ingredient in sterile water. 16. A pharmaceutical composition according to claim 13 in the form of an aerosol formulation. 17. A pharmaceutical composition according to claim 13 in which the pharmaceutical carrier or diluent is a solid. 18. A method of inhibiting the symptoms of asthma which comprises administering to a subject in need of said inhibition a therapeutically effective amount for producing said inhibition of a compound of claim 1. 19. The method according to claim 18 in which the active ingredient is administered in a daily dosage regimen of from about 0.5 mg. to about 2000 mg. 20. A method of antagonizing the effects of SRS-A on bronchial smooth muscle which comprises administering to a subject in need of said antagonism an amount sufficient to product said antagonism of a compound of claim 1.

Details for Patent 4,317,826

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Merck Sharp & Dohme Corp.	ZOSTAVAX	zoster vaccine live	For Injection	125123	05/25/2006		2039-09-23