Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-08-30
2000-11-07
Huang, Evelyn Mei
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546 81, A61K 314375, A61P 1100, C07D47104
Patent
active
06143759&
DESCRIPTION:
BRIEF SUMMARY
FIELD OF APPLICATION OF THE INVENTION
The invention relates to novel 6-[(tetrazol-5-yl)phenyl]benzonaphthyridines, which are used in the pharmaceutical industry for the production of medicaments.
KNOWN TECHNICAL BACKGROUND
DE-A 21 23 328 and U.S. Pat. No. 3,899,494 describe substituted benzonaphthyridines which are distinguished by marked inhibition of blood platelet aggregation. EP 247 971 and WO91/17991 disclose 6-phenylbenzonaphthyridines for the treatment of inflammatory airway disorders.
DESCRIPTION OF THE INVENTION
It has now been found that the following compounds of the formula I described in greater detail below, which differ from the compounds of EP 247 971 and WO91/17991, in particular, by the substitution on the 6-phenyl ring, have surprising and particularly advantageous properties.
The invention thus relates to compounds of the formula I ##STR1## in which R1 is 1-4C-alkyl, 1-4C-alkoxy which is completely or predominantly substituted by fluorine, 1-4C-alkoxy which is completely or predominantly substituted by fluorine, or in which Ar-1-4C-alkyl, where R8, and the salts of these compounds.
One embodiment of the invention are compounds of the formula I, in which 1-4C-alkoxy which is completely or predominantly substituted by fluorine, 1-4C-alkoxy which is completely or predominantly substituted by fluorine, or in which Ar-1-4C-alkyl, where R8, and the salts of these compounds.
1-4C-Alkyl represents a straight-chain or branched alkyl radical having 1 to 4 carbon atoms. Examples which may be mentioned are the butyl, isobutyl, sec-butyl, tert-butyl, propyl, isopropyl and, preferably, the ethyl and methyl radicals.
1-4C-Alkoxy represents radicals which in addition to the oxygen atom contain a straight-chain or branched alkyl radical having 1 to 4 carbon atoms. Examples which may be mentioned are the butoxy, isobutoxy, sec-butoxy, tert-butoxy, propoxy, isopropoxy and, preferably, the ethoxy and methoxy radicals.
3-7C-Cycloalkoxy represents cyclopropyloxy, cyclobutyloxy, cyclopentyloxy, cyclohexyloxy and cycloheptyloxy, of which cyclopropyloxy, cyclobutyloxy and cyclopentyloxy are preferred.
3-7C-Cycloalkylmethoxy represents cyclopropylmethoxy, cyclobutylmethoxy, cyclopentylmethoxy, cyclohexylmethoxy and cycloheptylmethoxy, of which cyclopropylmethoxy, cyclobutylmethoxy and cyclopentylmethoxy are preferred.
Examples of 1-4C-alkoxy which is completely or predominantly substituted by fluorine are the 2,2,3,3,3-pentafluoropropoxy, the perfluoroethoxy and the 1,2,2-trifluoroethoxy radicals, in particular the 1,1,2,2-tetrafluoroethoxy, the trifluoromethoxy, the 2,2,2-trifluoroethoxy and, preferably, the difluoromethoxy radicals.
1-2C-Alkylenedioxy represents, for example, the methylenedioxy radical (--O--CH.sub.2 --O--) and the ethylenedioxy radical (--O--CH.sub.2 --CH.sub.2 --O--).
1-10C-Alkyl represents straight-chain or branched alkyl radicals having 1 to 10 carbon atoms. Examples which may be mentioned are the decyl, nonyl, octyl, heptyl, isoheptyl (5-methylhexyl), hexyl, isohexyl (4-methylpentyl), neohexyl (3,3-dimethylbutyl), pentyl, isopentyl (3-methylbutyl), neopentyl (2,2-dimethylpropyl), butyl, isobutyl, sec-butyl, tert-butyl, propyl, isopropyl, ethyl and methyl radicals.
3-7C-Cycloalkyl represents the cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl radicals. The 5-7C-cycloalkyl radicals cyclopentyl, cyclohexyl and cycloheptyl may be preferably mentioned.
3-7C-Cycloalkylmethyl represents a methyl radical which is substituted by one of the abovementioned 3-7C-cycloalkyl radicals. Examples which may be mentioned are the cyclopentylmethyl and the cyclohexylmethyl radicals.
Ar-1-4C-alkyl represents one of the abovementioned 1-4C-alkyl radicals which is substituted by one of the aryl radicals defined above. Examples which may be mentioned are the p-methoxybenzyl, the phenethyl and the benzyl radicals.
Suitable salts for compounds of the formula I--depending on substitution--are all acid addition salts or all salts with bases. Particular mention may be made of the pharmacologica
REFERENCES:
patent: 3899494 (1975-08-01), Ott et al.
patent: 5346904 (1994-09-01), Flockerzi et al.
ByK Gulden Lomberg Chemische Fabrik GmbH
Huang Evelyn Mei
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