Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1993-09-16
1995-05-02
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
5142225, 5142228, 540578, 544 8, 544 10, A61K 3154, C07D51304
Patent
active
054119553
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION
The invention relates to compounds of the general formula I ##STR2## in which R.sup.1 denotes a lower alkyl radical, an aryl radical, a heteroaryl radical or an aryl-lower-alkyl radical, heteroaryl radical, an aryl-lower-alkyl radical or a saturated, unbranched C.sub.1 -C.sub.4 -alkyl radical which is monosubstituted by a radical selected from the group consisting of --OR.sup.7, --NR.sup.8 R.sup.9, --CO--OR.sup.10, --SR.sup.11, --CO--NR.sup.12 R.sup.13 or --NH--C(NH.sub.2) (.dbd.NH), alkylene radical having two, three, four or five carbon atoms and thus, together with the adjacent nitrogen atom and carbon atom of the thiadiazine ring system, form a ring having four, five, six or seven ring members, aryl-lower-alkyl radical, heteroaryl radical or an aryl-lower-alkyl radical, independently of one another denoting a hydrogen atom, a lower alkyl radical, an aryl radical or an aryl-lower-alkyl radical, radical or a 2-naphthyl radical, each of which is optionally substituted by one, two or three identical or different substituents selected from the group of the halogen atoms, hydroxyl radicals, lower alkyl radicals, lower alkyloxy radicals, carboxyl radicals, lower alkyloxycarbonyl radicals, nitro groups, sulfo radicals, trifluoromethyl radicals or hydrogen-atom- or lower-alkyl-radical-substituted amino groups, following radicals: furanyl radicals, thienyl radicals, pyrrolyl radicals, pyrazolyl radicals, imidazolyl radicals, triazolyl radicals, thiazolyl radicals, oxazolyl radicals, isothiazolyl radicals, isoxazolyl radicals, thiadiazolyl radicals, pyridyl radicals, pyrimidyl radicals, pyrazinyl radicals, triazinyl radicals, benzofuranyl radicals, benzothienyl radicals, indolyl radicals, benzoxazolyl radicals, benzothiazolyl radicals, benzimidazolyl radicals, quinolinyl radicals or isoquinolinyl radicals, it being possible for the abovementioned radicals to be linked to the basic structure of the compounds of the general formula I via each ring carbon atom and it being possible for the abovementioned rings to be optionally substituted by one or two identical or different substituents selected from the group of the halogen atoms, hydroxyl radicals, lower alkyl radicals, lower alkyloxy radicals, carboxyl radicals, lower alkyloxycarbonyl radicals, nitro groups, sulfo radicals, trifluoromethyl radicals or hydrogen-atom or lower-alkyl-radical-substituted amino groups, radical or an ethyl radical each of which is substituted by an aryl radical as defined above, in connection with lower alkyloxy radical or lower alkyloxycarbonyl radical denoting an unbranched or branched saturated hydrocarbon radical having up to six carbon atoms.
In general, the compounds of the general formula I according to the invention exist individually in the sense of keto-enol tautomerism or in the form of mixture.
The following explanations apply to the various substituents or radicals in formula I which have been mentioned in connection with the present application:
Examples of lower alkyl radicals are methyl radicals, ethyl radicals, n-propyl radicals, iso-propyl radicals, n-butyl radicals, iso-butyl radicals, 1-methylpropyl radicals, tert.-butyl radicals, n-pentyl radicals, 1-methylbutyl radicals, 2-methylbutyl radicals, 3-methylbutyl radicals, 1,1-dimethylpropyl radicals, 2,2-dimethylpropyl radicals, 1,2-dimethylpropyl radicals, 1-ethylpropyl radicals, n-hexyl radicals, 1-methylpentyl radicals, 2-methylpentyl radicals, 3-methylpentyl radicals, 4-methylpentyl radicals, 1,1-dimethylbutyl radicals, 2,2-dimethylbutyl radicals, 3,3-dimethylbutyl radicals, 1,2-dimethylbutyl radicals, 2,3-dimethylbutyl radicals, 1,3-dimethylbutyl radicals, 1-ethylbutyl radicals, 2-ethylbutyl radicals, 1,1,2-trimethylpropyl radicals, 1,2,2-trimethylpropyl radicals, 1-ethyl-2-methylpropyl radicals or 1-ethyl-1-methylpropyl radicals. Preferred in this context are methyl radicals, ethyl radicals, n-propyl radicals, iso-propyl radicals, n-butyl radicals, iso-butyl radicals, tert.-butyl radicals, 2,2-dimethylpropyl radicals or 1-methylpropyl radicals. Part
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Klauser Rainer J.
Strasser Rupert
Zeiller Peter
Grumbling Matthew V.
Luitpold Pharma GmbH
Shah Mukund J.
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