Pyrrole derivatives, their preparation and pharmaceutical compos

Details Pyrrole derivatives, their preparation and pharmaceutical compos Pyrrole derivatives, their preparation and pharmaceutical compos

1989-09-05

1992-04-07

Springer, David B.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546159, 546157, 546122, 546270, 546167, 544350, 544127, 544128, 544131, 544362, 544363, 544364, 548482, 5142345, 514314, 5142352, 514253, A61K 31535, C07D21538, C07D47102, C07D47100

Patent

active

051028905

ABSTRACT:
This invention relates to pyrrole derivatives of formula: ##STR1## in which A forms with the pyrrole ring an isoindoline, 6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, 2,3,6,7-tetrahydro-5H-[1,4]oxathiino[2,3-c]pyrrole or 2,3,6,7-tetrahydro-5H-[1,4]dithiino[2,3-c]pyrrole ring-system and Hetis naphthyridinyl, pyridyl or quinolyl which is unsubstituted or substituted with halogen, (1 to 4 C) alkyl, (1 to 4 C) alkyloxy, (1 to 4 C) alkylthio or CF.sub.3 and R=(3 to 10 C) straight- or branched-chain alkenyl or alkyl which is unsubstituted or substituted with alkyloxy, alkylthio, (3 to 6 C) cycloalkyl, NH.sub.2, alkylamino, dialkylamino, alkylcarbonylamino, (in which the amino portion is optionally substituted with alkyl), 1- or 2-piperazinyl, piperidyl, piperidino, morpholino, pyrrolidinyl, 1-azetidinyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, (1-piperazinyl)carbonyl, piperidinocarbonyl, (1-pyrrolidinyl)carbonyl, phenyl, pyridyl, 1-imidazolyl, or alternatively R=2- or 3-pyrrolidinyl, 2-, 3- or 4-piperidyl, on the understanding that the alkyl radicals are straight- or branched-chain radicals and contain, except where specifically stated, 1 to 10 C, and that the piperazinyl, piperidino, piperidyl, pyrrolidinyl and azetidinyl radicals can be unsubstituted or substituted at any position with alkyl, alkylcarbonyl, benzyl or hydroxyalkyl, or can alternatively form a lactam group with the nitrogen atom of the ring, and, where they exist, their pharmaceutically acceptable salts and optical isomers, are useful as anxiolytics.

REFERENCES:
patent: 3847921 (1974-11-01), Cotrel et al.
Copy of European Search Report dated Sep. 17, 1987.
Liebigs Annalen Der Chemie, 1985, pp. 1679-1691, DE; L. Somogyi: "Isoindoline derivatives of opianic acid".

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