Phenylene derivatives and anti-allergic use thereof

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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Details

514570, 548251, 548252, 562450, C07D25704, C07D25706, C07C10102, A61K 3171, A61K 3119

Patent

active

049944797

DESCRIPTION:

BRIEF SUMMARY
DESCRIPTION

1. FIELD OF THE INVENTION
The present invention relates to novel phenylene derivatives useful as drugs, particularly SRS-A (slow reacting substance of anaphylaxis) antagonists. (Means for solving the problems)
2. DESCRIPTION OF THE INVENTION
The compounds of the present invention are phenylene derivatives represented by general formula (I) described below.
Compounds represented by general formula (I) or pharmaceutically acceptable salts thereof: ##STR5## wherein symbols represent: A: a hydrogen atom, a phenyl group or a phenoxy group, --Y.sub.1 -- (wherein Y.sub.1 : --O--, --S-- or --NH--), --Y.sub.1 --CH.sub.2 --, --CO--Y.sub.2 -- (wherein Y.sub.2 : --NH--, --CH.sub.2 --Y.sub.1 -- or --Y.sub.1 --CH.sub.2 --) or --Y.sub.2 --CO--.
.circle. : a group represented by: ##STR6## wherein: R.sub.2 : a hydrogen atom, a halogen atom, a nitro group, a hydroxy group, a lower alkoxy group, a carboxy group, a cyano group, an oxaloamido group (--NHCOCOOH), a lower alkoxycarbonyl group, a lower alkyl group, a hydroxy-lower alkyl group, a lower alkoxy-lower alkyl group, a carboxy-lower alkyl group, a lower alkoxycarbonyl-lower alkyl group, a carboxy-lower alkylthio-lower alkyl group, a lower alkoxycarbonyl-lower alkylthio-lower alkyl group, a halo-lower alkyl group, a carboxyl-lower alkoxy group, a lower alkoxycarbonyl-lower alkoxy group, a lower alkanoyl-lower alkoxy group, a lower alkoxycarbonyl-lower alkoxycarbonyl-lower alkoxy group, a lower alkanoyl group or a group represented by the formula: ##STR7## (wherein R.sub.4 and R.sub.5, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, a carboxy-lower alkyl group, a lower alkoxycarbonyl-lower alkyl group, a lower alkanoyl group, a carboxy-lower alkanoyl group, a lower alkoxycarbonyl-lower alkanoyl group, a substituted or unsubstituted phenyl-lower alkoxycarbonyl-lower alkanoyl group, a carbamoyl group, a lower alkoxy oxalyl group or a mono- or di-lower alkylaminocarbonyl group),
X.sub.2 : a group represented by --CH.dbd.CH-- or --Y.sub.3 --Y.sub.4 -- (wherein Y.sub.3 : a single bond, --O--, --S-- or --NH--; Y.sub.4 : an alkylene group having 1 to 6 carbon atoms which may be interrupted by a sulfur atom),
D: a carboxy group, a lower alkoxycarbonyl group or a group represented by: ##STR8## provided that .circle. is: or D is: ##STR9## when A is a hydrogen atom.
Definitions of the aforesaid general formula (I) and general formulae later described, and preferred specific examples thereof, are described in detail below.
The term "lower" as used throughout the present specification refers to a straight or branched carbon chain having 1 to 6 carbon atoms, unless otherwise indicated.
Accordingly, the "lower alkyl group" includes a methyl group, an ethyl group, a propyl group, an isopropyl group, a butyl group, an isobutyl group, a sec-butyl group, a tert-butyl group, a pentyl group, an isopentyl group, a hexyl group, an isohexyl group, etc. Also the "lower alkoxy" and "lower alkoxy group" include a methoxy group, an ethoxy group, a propoxy group, an isopropoxy group, a butoxy group, an isobutoxy group, a sec-butoxy group, a tert-butoxy group, a pentyloxy group, an isopentyloxy group, a hexyloxy group, an isohexyloxy group, etc.
The "alkylene group having 1 to 6 carbon atoms which may be interrupted with a sulfur atom" for Y.sub.4 includes a methylene group, an ethylene group and the aforesaid alkylene group having 3 to 6 carbon atoms; in addition thereto, includes these alkylene groups interrupted by one sulfur atom at an optional position thereof, specifically --CH.sub.2 --S--CH.sub.2 --, --(CH.sub.2).sub.2 --S--CH.sub.2 --, --(CH.sub.2).sub.3 --S--CH.sub.2 --, --(CH.sub.2).sub.4 --S--CH.sub.2 --, --(CH.sub.2).sub.2 --S--(CH.sub.2).sub.3 --, --CH.sub.2 --S--(CH.sub.2).sub.4 --, --CH.sub.2 --CH(CH.sub.3)--CH.sub.2 --S--CH.sub.2 --, etc.
Specific examples of the "group shown by formula: --CH.sub.2 --Y.sub.1 -- or --Y.sub.1 --CH.sub.2 --" for X.sub.1 include a methyleneoxy group (--CH.sub.2 --O--), a methylenethio group (--CH.sub.2

REFERENCES:
patent: 4250192 (1981-02-01), Sallmann et al.
patent: 4254035 (1981-03-01), Kleemann et al.

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