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Last Updated: April 16, 2024

Claims for Patent: 4,385,047


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Summary for Patent: 4,385,047
Title: Antiallergic imidodisulfamides
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 non-nucleophilic organic base. Pharmaceutical compositions and methods of alleviating the symptoms of an allergic response are also disclosed.
Inventor(s): Ali; Fadia E. (Cherry Hill, NJ)
Assignee: SmithKline Beckman Corporation (Philadelphia, PA)
Application Number:06/222,478
Patent Claims:1. A compound of the formula (I): ##STR4## wherein R.sub.1 is hydrogen, bromo, chloro, nitro, methyl, trifluoromethyl or methoxy and R.sub.2 is hydrogen, chloro or methyl with the proviso that when R.sub.2 is chloro, R.sub.1 is chloro, methyl or trifluoromethyl; or an alkali metal salt of said compound.

2. A compound according to claim 1 wherein R.sub.1 is hydrogen; 3- or 4-bromo; 2-, 3- or 4-chloro; 3-nitro; 3- or 4-trifluoromethyl; or 4-methoxy and R.sub.2 is hydrogen or an alkali metal salt of said compound.

3. A compound according to claim 1 wherein R.sub.1 is 4-chloro or 4-methyl and R.sub.2 is 3-chloro or an alkali metal salt of said compound.

4. A compound according to claim 1 wherein R.sub.1 is 3-trifluoromethyl and R.sub.2 is 4-chloro or an alkali metal salt of said compound.

5. A compound according to claim 1 wherein R.sub.1 is 4-methyl and R.sub.2 is 3-methyl or an alkali metal salt of said compound.

6. A compound according to claim 1 which is N,N'-bis[7-(4-chlorobenzoylmethylsulfonyl)-1,2,3,4-tetrahydroisoquinoyl]di sulfonylimide or an alkali metal salt of said compound.

7. A pharmaceutical composition of 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.

8. A pharmaceutical composition according to claim 7 in a form suitable for administration by inhalation.

9. A pharmaceutical composition according to claim 7 comprising a solution or suspension of the active ingredient in sterile water.

10. A pharmaceutical composition according to claim 7 in the form of an aerosol formulation.

11. A pharmaceutical composition according to claim 7 in which the pharmaceutical carrier or diluent is a solid.

12. A method of alleviating the symptoms of asthma which comprises administering to a subject in need of said alleviating a therapeutically effective amount for producing said alleviation of a compound of claim 1.

13. The method according to claim 12 in which the active ingredient is administered in a daily dosage regimen of from about 0.5 mg. to about 2000 mg.

14. 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 produce said antagonism of a compound of claim 1.

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