Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1985-12-10
1987-12-01
Jiles, Henry R.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514212, 514227, 514228, 514232, 514233, 514234, 514235, 514236, 514237, 514239, 514278, 514316, 514322, 540543, 540597, 540598, 540603, 544 70, 544 80, 544130, 544139, 546 15, 546187, 546199, 548326, A61K 31415, A61K 3155, C07D48704
Patent
active
047105100
ABSTRACT:
The present invention provides new pyrrolobenzimidazoles of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical; R.sub.2 is a hydrogen atom, cyano group or alkyl or alkenyl radical or a carbonyl group substituted by hydroxyl, alkyl, alkoxy, amino, alkylamino, dialkylamino or hydrazino or together with R.sub.1 forms a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical; R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, each represent a hydrogen atom or an alkanesulphonyloxy, trifluoromethanesulphonyloxy, alkanesulphonylamino, trifluoromethanesulphonylamino, N-alkyl-alkanesulphonylamino, N-alkyl-trifluoromethanesulphonylamino, alkylsulphenylmethyl, alkylsulphinylmethyl or alkylsulphonylmethyl radical, a carbonyl group substituted by hydroxyl, alkoxy, amino, alkylamino or dialkylamino, a sulphonyl group substituted by amino, alkylamino, dialkylamino or cyclic imino, whereby a methylene group in the 4-position can be replaced by a sulphur or oxygen atom, an alkylcarbonylamino, aminocarbonylamino or alkylaminocarbonylamino radical, an alkylthio, alkylsulphinyl or alkylsulphonyl radical, a nitro, halogen, amino, hydroxyl, alkyl, trifluoromethyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, carboxyalkoxy, alkoxycarbonylalkoxy, dialkylamino, 1-imidazolyl or cyano group; X is a valency bond, a C.sub.1 -C.sub.4 alkylene radical or a vinyl radical; and T is an oxygen or sulphur atom; the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids.
The present invention also provides processes for the preparation of these compounds and pharmaceuticals containing them for the prophylaxis and treatment of heart and circulatory diseases.
REFERENCES:
patent: 4327099 (1982-04-01), Evans et al.
patent: 4333930 (1982-06-01), Creuzet et al.
patent: 4548943 (1985-10-01), Finizio
patent: 4579865 (1986-04-01), Musser et al.
Remington's Pharmaceutical Sciences, 14th Ed., 1970, pp. 528-529.
Holck Jens-Peter
Kampe Wolfgang
Mertens Alfred
Muller-Beckmann Bernd
Schaumann Wolfgang
Boehringer Mannheim GmbH
Briscoe Kurt G.
Jiles Henry R.
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