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Claims for Patent: 4,804,666

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Claims for Patent: 4,804,666

Title: Antiallergic 6,11-dihydro-11-(4-piperidylidene)-5H-benzo(5,6)cyclohepta(1,2-B)pyridin es
Abstract:Derivatives of 6,11-dihydro-11-(4-piperidylidene)-5H-benzo[5,6]cyclohepta[1,2-b]pyridine, and pharmaceutically acceptable salts and solvates thereof are disclosed, which possess anti-allergic activity, making them effective as anti-allergic compounds. Methods for preparing and using the compounds are also described.
Inventor(s): Piwinski; John J. (Parsippany, NJ), Green; Michael J. (Skillman, NJ), Ganguly; Ashit K. (Upper Montclair, NJ), Wong; Jesse K. (Union, NJ), Katchen; Bernard (Livingston, NJ), Cramer; Jeffrey (Westfield, NJ)
Assignee: Schering Corporation (Kenilworth, NJ)
Application Number:07/043,409
Patent Claims: 1. A compound represented by structural formula I: ##STR22## or a pharmaceutically acceptable salt or solvate thereof, wherein: R represents H or alkyl having 1 to 20 carbon atoms;

one of A and B represents H and OC(O)R.sup.1, .dbd.NOR.sup.1 or O--(CH.sub.2).sub.n --O--, and the other represents H.sub.2 or one of the above listed groups;

W, X, Y and Z may be the same or different and each independently represents H, halo, alkyl having 1 to 20 carbon atoms, --CF.sub.3, --NO.sub.2, --OC(O)R.sup.1, --SR.sup.1, --OR.sup.1, --CO.sub.2 --R.sup.1 or --N(R.sup.1).sub.2 ;

R.sup.1 is H, alkyl having 1 to 20 carbon atoms, or aryl having 6 to 15 carbon atoms, and in --N(R.sup.1).sub.2, R.sup.1 can be alkanediyl having 1 to 20 carbon atoms; and n is 2, 3 or 4 with the proviso that when A is .dbd.NOR.sup.1, R.sup.1 is other than H.

2. A compound as defined in claim 1 wherein R represents alkyl having 1 to 20 carbon atoms.

3. A compound as defined in claim 1 where R represents H.

4. A compound as defined in claim 2 where R represents lower alkyl having 1 to 6 carbon atoms.

5. A compound represented by the structural formula I: ##STR23## or a pharmaceutically acceptable salt or solvate thereof, wherein: R represents H or alkyl having from 1 to 20 carbon atoms, such that

(1) when R represents alkyl having 1 to 20 carbon atoms, at least one of A and B represents a substituent group selected from H and OR.sup.1, H and OC(O)R.sup.1, .dbd.NOR.sup.1 or --O--(CH.sub.2).sub.n --O--, and the other may represent H.sub.2 or one of the above listed substituent groups;

W represents halo, alkyl having 1 to 20 carbon atoms, --CF.sub.3, --NO.sub.2, --OC(O)R.sup.1, --SR.sup.1, --OR.sup.1, --CO.sub.2 R.sup.1 or --N(R.sup.1).sub.2 ;

X, Y and Z may be the same or different, and each independently represents H or one of the above defined W groups;

R.sup.1 is H, alkyl having 1 to 20 carbon atoms or aryl having 6 to 15 carbon atoms, and in --N(R.sup.1).sub.2, R.sup.1 can be alkanediyl having from 1 to 20 carbon atoms;

n is 2, 3 or 4, and

(2) when R represents H,

A and B may be the same or different and each independently represents H.sub.2, H and OR.sup.1, H and OC(O)R.sup.1, .dbd.O, .dbd.NOR.sup.1 or --O--(CH.sub.2).sub.n --O--;

X, Y and Z may be the same or different and each independently represents H, halo, alkyl having 1 to 20 carbon atoms, --CF.sub.3, --NO.sub.2, --OC(O)R.sup.1, --SR.sup.1, --OR.sup.1, --CO.sub.2 R.sup.1 or --N(R.sup.1).sub.2 ;

W represents halo, alkyl having 1 to 20 carbon atoms, --CF.sup.3, --NO.sub.2, --OC(O)R.sup.1, --SR.sup.1, --OR.sup.1, --CO.sub.2 R.sup.1 or --N(R.sup.1).sub.2, with the provisos that when A and B both represent H.sub.2, W is OR.sup.1 and R.sup.1 is H, and

R.sup.1 and n are as defined above.

6. A compound as defined in claim 5 where R represents alkyl having 1 to 20 carbon atoms.

7. A compound as defined in claim 6 wherein R represents lower alkyl having 1 to 6 carbon atoms and A, B, W, X, Y and Z are as defined therein.

8. A compound as defined in claim 7 wherein R represents lower alkyl of from 1 to 3 carbon atoms and A, B, W, X, Y and Z are as defined therein.

9. A compound as defined in claim 5 wherein one of A and B is H.sub.2 and the other of A and B represents H and OR.sup.1, H and OC(O)R.sup.1, .dbd.O, .dbd.NOR.sup.1 or --O--(CH.sub.2).sub.n O--, and W, X, Y, Z, R and R.sup.1 are as defined therein.

10. A compound as defined in claim 5 wherein at least one of A and B represent H and OR.sup.1 and W, X, Y, Z, R and R.sup.1 are as previously defined.

11. A compound as defined in claim 5 wherein A and B represent H.sub.2, W represents OR.sup.1 and X, Y, Z, R and R.sup.1 are as previously defined.

12. A compound as defined in claim 11 wherein R.sup.1 represents H.

13. A compound as defined in claim 1 or 5 wherein at least one of Y and Z represents halo.

14. A compound as defined in claim 1 or 5 wherein one of Y and Z represents halo.

15. A compound of claim 14 wherein Y represents halo at position 8.

16. A compound as defined in claim 15 wherein Y represents chloro at position 8.

17. A compond as defined in claim 1 or 5 wherein W represents OR.sup.1 at position 3.

18. A compound as defined in claim 17 wherein R.sup.1 represents H.

19. A compound as defined in claim 5 where R represents H.

20. A compound having the name 3-hydroxy-8-chloro-11-[4-piperidylidene]-6,11-dihydro-5H-benzo[5,6]cyclohe pta[1,2-b]pyridine, 8-chloro-11-(1-methyl-4-piperidylidene)-6,11-dihydro-5H-benzo[5,6]cyclophe pta[1,2-b]pyridin-6-ol acetate or 8-chloro-6-hydroxyimino-11-[1-methyl-4-piperidylidene]-6H-benzo[5,6]cycloh epta[1,2-b]pyridine.

21. A pharmaceutical antiallergic composition comprising a compound as defined in claim 1 in an amount effective to treat allergy in combination with a pharmaceutically acceptable carrier.

22. A pharmaceutical antiallergic composition comprising a compound as defined in claim 5 in an amount effective to treat allergy in combination with a pharmaceutically acceptable carrier.

23. A method of treating allergy in a mammal comprising administering to said mammal an anti-allergic effective amount of a compound as defined in claim 1.

24. A method of treating allergy in a mammal comprising administering to said mammal an anti allergic effective amount of a compound as defined in claim 5.
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