Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1992-10-09
1994-10-04
Cintins, Marianne M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514314, 514318, 514343, 546168, 546183, 546194, 546281, A61K 3144, A61K 31445, C07D40106, C07D40112
Patent
active
053526848
DESCRIPTION:
BRIEF SUMMARY
FIELD OF USE OF THE INVENTION
The invention relates to new pyridines, processes for their preparation, their use and medicaments containing them. The compounds according to the invention are employed in the pharmaceutical industry for the preparation of medicaments.
Known Technical Background
It is known that certain pyridines substituted in various ways have pharmacologically beneficial properties. European Patent Application EP-A-285 267 thus describes certain pyridines and dihydropyridines which are to be employed for the treatment and prevention of liver damage. Chemical Abstracts (Volume 112, 1990, page 5, Abstract 89s) references an article from the Journal of Chromatography (1989, 494, 209-17), in which the isolation of pyridine metabolites corresponding to manidipine is described. Surprisingly, it has now been found that the new compounds described below in more detail have particularly interesting pharmacological properties, by which they differ in an advantageous manner from the compounds of the prior art.
DESCRIPTION OF THE INVENTION
The invention relates to new pyridines of the formula I ##STR1## wherein one of the radicals R1 and R5 denotes 1-6C-alkyl and the other denotes the grouping -E1-E2-N(R6a)R6b together with R2, 2-3C-alkylene, 1-4C-alkyl, 1-4C-alkoxy, 1-4C-alkoxy which is completely or partly substituted by fluorine, 1-4C-alkonycarbonyl, 2-5C-acyl, amino or mono-or di-1-4C-alkylamino, 1-4--C-alkyl, 1-4C-alkoxy, 1-4C-alkoxy which is completely or partly substituted by fluorine, 1-4C-alkoxycarbonyl, 2-5C-acyl, amino or mono- or di-1-4C-alkylamino, -E-(CH.sub.2).sub.n - or the grouping -A1-O-A2, both bonded, represent a radical of the formula ##STR2## wherein A denotes --CH.sub.2 --CH.sub.2 --C(R7)R8--CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --CHR9--CH.sub.2 --CH.sub.2 --or --CH.sub.2 --CH.sub.2 --CH.sub.2 --CHR10-, ##STR3## wherein R11 and R12 are identical or different and denote hydrogen (H), 1-4--C-alkyl, 1-4C-alkoxy, halogen, hydroxyl, trifluoromethyl or, together, methylenedioxy,
1-6C-Alkyl is straight-chain or branched and denotes, for example, a hexyl, neopentyl, isopentryl, butyl, i-butyl, sec-butyl, t-butyl, propyl, isopropyl or, in particular, ethyl or methyl radical.
2-3C-Alkylene is ethylene or propylene, so that R2 and R3, if they have this meaning together, form, together with the carbonyl group, a 5- or 6-membered ring fused onto the dihydropyridine ring. i-butyl, sec-butyl, t-butyl, propyl, isopropyl, ethyl or, in particular, methyl radical,
1-4C-Alkoxy contains, in addition to the oxygen atom, one of the above-mentioned 1-4C-alkyl radicals. Preferred 1-4C-alkoxy radicals R41, R42, R11 and R12 are the methoxy and the ethoxy radical. Preferred 1-4C-alkoxy radicals R3 are the isopropoxy and the t-butyoxy radical.
3-5C-Alkoxyalkyl represents, for example, a methoxyethyl, ethoxyethyl, propxyethyl or ethoxymethyl radical.
3-5C-Alkoxyalkyl represents, for example, a methoxyethoyl, ethoxyethoxy or propoxyethoxy radical.
Halogen is the context of the invention denotes bromine, fluorine and, in particular, chlorine.
1-4C-Alkoxy which is completely or partly substituted by fluorine is, for example, 1,1,2,2--tetrafluoroethoxy, trifluoromethoxy, 2,2,2--trifluoroethoxy or, in particular, difluoromethoxy.
2-5C-Acyl contains, in addition to the carbonyl group, one of the above-mentioned 1-4C-alkyl radicals. The acetyl radical is preferred. Mono- or di-1-4C-alkylamino contains, in addition to the nitrogen atom, one or two of the abovementioned 1-4C-alkyl radicals. Di-1-4C-alkylamino is preferred, and here in particular dimethyl-, diethyl- or diisopropylamino.
Straight-chain or branched 1-7C-alkylene is, for example, methylene (--CH.sub.2 --), ethylene (--CH.sub.2 --CH.sub.2 --), trimethylene (--CH.sub.2 --CH.sub.2 --CH.sub.2 --), tetramethylene (--CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --), 1,2--dimethylethylene [--CH(CH.sub.3)--CH(CH.sub.3)-], 1,1-dimethylethylene [--C(CH.sub.3).sub.2 --CH.sub.2 --], 1,1-dimethylpropylene [--C(CH.sub.3).sub.2 --CH.sub.2 --CH.sub.2 --9 , 2
REFERENCES:
patent: 4707486 (1987-11-01), Flockerzi et al.
patent: 4975440 (1990-12-01), Flockerzi et al.
Chemical Abstracts, Band 112, 1990 112:895.
Ulrich Wolf-Rudiger
Zimmermann Peter
ByK Gulden Lomberg Chemische Fabrik GmbH
Cintins Marianne M.
Spivack Phyllis G.
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