Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-05-08
1997-01-21
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
055959881
DESCRIPTION:
BRIEF SUMMARY
CROSS-REFERENCE TO RELATED APPLICATIONS
This application is based upon PCT Application Ser. No. PCT/EP 93/03322, filed Nov. 25, 1993, which claims priority from European Application Ser. No. 92.203.777.5, filed on Dec. 4, 1992.
The present invention is concerned with novel triazolo(pyrrolo, thieno or furano)azepine derivatives having antiallergic activity.
In EP-A-0,339,978 there are described (benzo- or pyrido)cyclohepta heterocyclics which are useful as PAF antagonists, antihistaminics and/or anti-inflammatory agents.
In the J. Med. 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.
In WO 92/06981 there are described substituted imidazobenzazepines and imidazopyridoazepines having antiallergic and anti-inflammatory activity.
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 triazole ring, and by their favorable antiallergic activity.
The present invention is concerned with novel triazolo(pyrrolo, thieno or furano)azepines of formula ##STR2## the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, wherein halo, ethenyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxyC.sub.1-4 alkyl, formyl, hydroxycarbonyl or hydroxycarbonylC.sub.1-4 alkyl; hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxyC.sub.1-4 alkyl, formyl or hydroxycarbonyl; hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkyl substituted with hydroxycarbonyl or C.sub.1-4 alkyloxycarbonyl, hydroxyC.sub.1-4 alkyl, formyl, hydroxycarbonyl, phenyl or pyridinyl; one substituent selected from the group consisting of hydroxy, C.sub.1-4 alkyloxy, hydroxycarbonyl, C.sub.1-4 alkyloxycarbonyl, C.sub.1-4 alkloxycarbonylC.sub.1-4 alkyloxy, hydroxycarbonylC.sub.1-4 alkyloxy, C.sub.1-4 alkylaminocarbonylamino, C.sub.1-4 alkylaminothiocarbonylamino, aryl and aryloxy; C.sub.1-6 alkyl substituted with both hydroxy and aryloxy; C.sub.3-6 alkenyl; C.sub.3-6 alkenyl substituted with aryl; wherein each aryl is phenyl or phenyl substituted with halo, cyano, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkyloxy or aminocarbonyl; or, oxazolyl, thiazolyl or imidazolyl each optionally substituted with one or two C.sub.1-4 alkyl substituents; pyrrolyl or pyrazolyl optionally substituted with formyl, hydroxyC.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; and 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## wherein --CH.sub.2, CH.dbd.CH--CH.dbd.CH, or CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2.
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, 3-pentenyl, 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
Janssens Frans E.
Lacrampe Jean F. A.
Pilatte Isabelle N. C.
Datlow Philip I.
Janssen Pharmaceutica N.V.
Metz Charles J.
LandOfFree
Triazolo(pyrrolo, thieno or furano)azepine derivatives does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Triazolo(pyrrolo, thieno or furano)azepine derivatives, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Triazolo(pyrrolo, thieno or furano)azepine derivatives will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-2324310