Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-12-17
1999-09-28
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514252, 514256, 514318, 514326, 514328, 514331, 544238, 544335, 544336, 546194, 546209, 546210, 546220, 546221, 546231, A61K 31155, A61K 31445, C07D21106, C07D21174
Patent
active
059589523
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP96/01615, filed Apr. 18, 1996.
The invention relates to phenylamidines of general formula ##STR2## the tautomers thereof, the stereoisomers including the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting properties, pharmaceutical compositions containing these compounds, the use thereof and processes for preparing them.
In the above general formula I straight-chained alkylene group, which may optionally be substituted by one or two alkyl groups, by an alkenyl group having 2 to 4 carbon atoms, by an alkynyl group having 2 to 4 carbon atoms, by an aryl, arylmethyl, heteroaryl or heteroarylmethyl group, one or two alkyl groups, substituted by one or two alkyl groups, whilst in the abovementioned rings one or two methylene groups adjacent to a nitrogen atom may be replaced by a carbonyl group, one or two alkyl groups, whilst in the abovementioned rings one or two methylene groups adjacent to a nitrogen atom may be replaced by a carbonyl group, alkyloxycarbonyl group, an arylalkyloxycarbonyl group having 1 to 3 carbon atoms in the alkyl moiety or a group of formula ##STR3## wherein R.sup.a denotes a hydrogen atom or an alkyl group and hydrogen, fluorine, chlorine, bromine or iodine atom, an alkyl, trifluoromethyl or alkoxy group, group and a 4- to 7-membered cycloalkyl group optionally substituted by one or two alkyl groups, an aryl or arylalkyl group or a group of formula ##STR4## wherein R.sup.c denotes a hydrogen atom or an alkyl group, group or a 5- to 7-membered cycloalkoxy group, a phenyl group, which may be monosubstituted by R.sup.6, mono, di- or trisubstituted by R.sup.7 or monosubstituted by R.sup.6 and additionally mono- or disubstituted by R.sup.7, wherein the substituents may be identical or different and dialkylaminocarbonyl, alkoxycarbonyl, alkylcarbonyl, alkylsulphenyl, alkylsulphinyl, alkylsulphonyl, alkylsulphonyloxy, perfluoralkyl, trifluoromethoxy, nitro, amino, alkylamino, dialkylamino, alkylcarbonylamino, phenylalkylcarbonylamino, phenylcarbonylamino, alkylsulphonylamino, phenylalkylsulphonylamino, phenylsulphonylamino, N-alkyl-alkylcarbonylamino, N-alkyl-phenylalkylcarbonylamino, N-alkyl-phenylcarbonylamino, N-alkyl-alkylsulphonylamino, N-alkyl-phenylalkylsulphonylamino, N-alkyl-phenylsulphonylamino, aminosulphonyl, alkylaminosulphonyl- or dialkylaminosulphonyl group and bromine or iodine atom, wherein two groups R.sup.6, if they are attached to adjacent carbon atoms, may also denote an alkylene group having 3 to 6 carbon atoms, a 1,3-butadiene-1,4-diylene group or a methylenedioxy group, refer to a 5-membered heteroaromatic ring, which contains an oxygen, sulphur or nitrogen atom, a nitrogen atom and an oxygen, sulphur or nitrogen atom or two nitrogen atoms and an oxygen, sulphur or nitrogen atom, or a 6-membered heteroaromatic ring, which contains 1, 2 or 3 nitrogen atoms and wherein additionally one or two --CH.dbd.N-groups may each be replaced by an --CO--NR.sup.8 -group, wherein R.sup.8 denotes a hydrogen atom or an alkyl group, and additionally the abovementioned heteroaromatic rings may be substituted by one or two alkyl groups or may also be substituted at the carbon skeleton by a fluorine, chlorine, bromine or iodine atom or by a trifluoromethyl, hydroxy or alkyloxy group, moieties may each contain 1 to 4 carbon atoms.
However, the preferred compounds of the above general formula I are those wherein which may be substituted by one or two alkyl groups, by an alkenyl group having 2 or 3 carbon atoms, by an alkynyl group having 2 or 3 carbon atoms, by a phenyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, oxazolyl, thiazolyl, 2-imidazolyl, 4-imidazolyl or 5-imidazolyl group, wherein the abovementioned imidazolyl groups may additionally be substituted by an alkyl group at one of the nitrogen atoms, by one or two alkyl groups, by an alkenyl group having 2 or 3 carbon atoms, by an
REFERENCES:
patent: 5378727 (1995-01-01), Bovy et al.
patent: 5399585 (1995-03-01), Alig et al.
patent: 5455348 (1995-10-01), Austel et al.
patent: 5591769 (1997-01-01), Himmelsbach et al.
Takada et al., Chemical Abstracts, vol. 126, abstract 317393, 1997.
Ohshika et al., Chemical Abstracts, vol. 126, abstract 157821, 1997.
Fukushi et al., Chemical Abstracts, vol. 126, abstract 31374, 1997.
Ono et al., Chemical Abstracts, vol. 125, abstract 114709, 1996.
Austel Volkhard
Guth Brian
Himmelsbach Frank
Linz Gunther
Pieper Helmut
Devlin M-E. M.
Dr. Karl Thomae GmbH
Raymond R. P.
Raymond Richard L.
Stempel A. R.
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