Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1993-11-29
1995-10-24
Datlow, Philip I.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
540578, A61K 3155, C07D48714, C07D491147, C07D49514
Patent
active
054610508
DESCRIPTION:
BRIEF SUMMARY
CROSS-REFERENCE TO RELATED APPLICATIONS
This application is based upon PCT Application No. PCT/EP 92/01331, filed Jun. 9, 1992, which claims priority from U.S. application Ser. No. 714,487, filed Jun. 13, 1991, now abandoned.
BACKGROUND OF THE INVENTION
In EP-A-0,339,978 there are described (benzo- or pyfido)cyclohepta heterocyclics which are useful as PAF antagonists, antihistaminics and/or anti-inflammatory agents.
In the J. Meal. Chem., 26 (1983), 974-980 there are described some 1-methyl-4-piperidinylidene-9-substituted pyrrolo[2,1-b][3]benzazepine derivatives having neuroleptic properties.
The compounds of the present invention differ structurally from the cited art-known compounds by the fact that the central 7-membered ring invariably contains a nitrogen atom of a fused imidazole ring, and by their favorable antiallergic activity.
DESCRIPTION OF THE INVENTION
The present invention is concerned with novel imidazo[1,2-a](pyrrolo, thieno or furano)[3,2-d]azepines of formula ##STR2## the pharmaceutically acceptable addition salts and stereochemically isomefic forms thereof, wherein each of the dotted lines independently represents an optional bond; with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxy C.sub.1-4 alkyl, formyl, hydroxycarbonyl or hydroxycarbonyl C.sub.1-4 alkyl; hydroxycarbonyl or hydroxycarbonyl or hydroxycarbonyl; phenyl or halo; one substiuent selected from the group consisting of hydroxy, halo, C.sub.1-4 alkyloxy, hydroxycarbonyl, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyloxycarbonyl C.sub.1-4 alkyloxy, hydroxycarbonyl C.sub.1-4 alkyloxy, C.sub.1-4 alkyloxycarbonylamino, C.sub.1-4 alkylaminocarbonyl, C.sub.1-4 alkylaminocarbonylamino, C.sub.1-4 alkylaminothiocarbonylamino, aryl, aryloxy and arylcarbonyl; C.sub.1-6 alkyl substituted with both hydroxy and aryloxy; C.sub.3-6 alkenyl; C.sub.3-6 alkenyl substituted with aryl; hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, aminocarbonyl or phenyl substituted with C.sub.1-4 alkyloxycarbonyl or hydroxycarbonyl; or, Het.sup.1, Het.sup.2 and Het.sup.3 each represent furanyl, thienyl, oxazolyl, thiazolyl or imidazolyl each optionally substituted with one or two C.sub.1-4 alkyl substituents; pyrrolyl or pyrazolyl optionally substituted with formyl, hydroxy C.sub.1-4 alkyl, hydroxycarbonyl, C.sub.1-4 alkyloxycarbonyl or with one or two C.sub.1-4 alkyl substituents; thiadiazolyl or oxadiazolyl optionally substituted with amino or C.sub.1-4 alkyl; pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl each optionally substituted with C.sub.1-4 alkyl, C.sub.1-4 alkyloxy, amino, hydroxy or halo; imidazo[4,5-c]pyridin-2-yl; and Het.sup.3 may also represent 4,5-dihydro-5-oxo-1H-tetrazolyl substituted with C.sub.1-4 alkyl, 2-oxo-3-oxazolidinyl, 2,3-dihydro-2-oxo-1H-benzimidazol-1-yl or a radical of formula ##STR3## R.sup.4 represents hydrogen or C.sub.1-4 alkyl; and A-Z represents S--CH.dbd.CH, S--CH.sub.2 --CH.sub.2, S--CH.sub.2 --CH.sub.2 CH.sub.2, CH.dbd.CH--CH.dbd.CH, CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2, --N(CH.sub.3)--C(CH.sub.3)--CH-- or --CH--C(CH.sub.3)--O--;
As used in the foregoing definitions halo defines fluoro, chloro, bromo and iodo; C.sub.1-4 alkyl defines straight and branched chain saturated hydrocarbon radicals having from 1 to 4 carbon atoms such as, for example, methyl, ethyl, propyl, 1-methylethyl, butyl, 1-methylpropyl, 2-methylpropyl and 1,1-dimethylethyl; C.sub.1-6 alkyl defines C.sub.1-4 alkyl radicals as defined hereinbefore and the higher homologs thereof having from 5 to 6 carbon atoms such as, for example, pentyl and hexyl; C.sub.3-6 alkenyl defines straight and branched chain hydrocarbon radicals containing one double bond and having from 3 to 6 carbon atoms such as, for example, 2-propenyl, 2-butenyl, 3-butenyl, 2-methyl-2-propenyl, 2-pentenyl, 3opentenyl, 3,3-dimethyl-2-propenyl, hexenyl and the like; C.sub.1-4 alkanediyl defines bivalent straight or branched chain hydrocarbon radicals containing from 1 to 4 carbon atoms such as, for example, methylene, 1,1-ethanediyl, 1,2-ethanediyl, 1,3-propanediyl, 1,4-buta
REFERENCES:
patent: 5008268 (1991-04-01), Janssens et al.
Cooymans Ludwig P.
Diels Gaston S. M.
Janssens Frans E.
Leenaerts Joseph E.
Datlow Philip I.
Janssen Pharmaceutica N.V.
Metz Charles J.
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