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Last Updated: April 25, 2024

Claims for Patent: 4,923,892


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Summary for Patent: 4,923,892
Title: Tricyclic aromatic compounds
Abstract:The present invention relates to compounds of formula I ##STR1## or a salt, ester or amide thereof; wherein R.sup.1 is --CH.sub.2 --CH.sub.2 --, CH.sub.2 --O-- or --O--CH.sub.2 --; R.sup.2 and R.sup.3 are the same or different and are each hydrogen, C.sub.1-4 alkyl or taken together with the nitrogen comprise a nitrogen-containing heterocyclic ring having four to six ring members; R.sup.4 is a single bond or a C.sub.1-7 bivalent aliphatic hydrocarbon group and may be joined to the aromatic ring system at the 2,3,8 or 9 positions; n is 0 to 3, and their use as antihistamine and antiasthma agents.
Inventor(s): Lever, Jr.; O. William (Skillman, NJ), Leighton; Harry J. (Chapel Hill, NC)
Assignee: Burroughs Wellcome Co. (Research Triangle Park, NC)
Application Number:07/356,884
Patent Claims: 1. A method of treating allergy in a mammal which comprises administering to a mammal in need thereof an effective allergy treatment amount of a compound of formula (I) ##STR10## or a pharmacologically and pharmaceutically acceptable salt thereof; wherein R.sup.1 is --CH.sub.2 --O--, R.sup.2 and R.sup.3 are the same or different and are each hydrogen or C.sub.1-4 alkyl, R.sup.4 is a C.sub.1-2 bivalent hydrocarbon group and is joined to the aromatic ring system at the 2 position and n is 2.

2. The method of claim 1 in which R.sup.2 and R.sup.3 are methyl.

3. A method of claim 1 in which the compound of formula (I) is:

(Z)-11-(3-(Dimethylamino)propylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acryl ic acid.

4. A method of treating asthma in a mammal which comprises administering to a mammal in need thereof an effective asthma treatment amount of a compound of formula (I) ##STR11## or a pharmacologically and pharmaceutically acceptable salt thereof; wherein R.sup.1 is --CH.sub.2 --O--, R.sup.2 and R.sup.3 are the same or different and are each hydrogen or C.sub.1-4 alkyl, R.sup.4 is a C.sub.1-2 bivalent hydrocarbon group and is joined to the aromatic ring system at the 2 position and n is 2.

5. The method of claim 4 in which R.sup.2 and R.sup.3 are methyl.

6. The method of claim 4 in which the compound of formula (I) is:

(Z)-11-(3-(Dimethylamino)propylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acryl ic acid.

7. A pharmaceutical formulation for use in treating allergy or asthma comprising an effective allergy or asthma treatment amount of: ##STR12## or a pharmacologically and pharmaceutically acceptable salt thereof; wherein R.sup.1 is --CH.sub.2 --O--, R.sup.2 and R.sup.3 are the same or different and are each hydrogen or C.sub.1-4 alkyl, R.sup.4 is a C.sub.1-2 bivalent hydrocarbon group and is joined to the aromatic ring system at the 2 position and n is 2 and a pharmaceutically acceptable carrier therefore.

8. The formulation of claim 7 in which R.sup.1 and R.sup.2 are methyl.

9. The formulation of claim 8 in which the compound is:

(Z)-11-(3-(Dimethylamino)propylidene)-6,11-dihydrodibenz[b,e]oxepin-2-acryl ic acid.

10. The formulation of claim 7 in the form of a tablet or capsule.

11. The formulation of claim 8 in the form of a tablet or capsule.

12. The formulation of claim 9 in the form of a tablet or capsule.

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