Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-09-25
2000-09-05
Bernhardt, Emily
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
51425301, 51425401, 51425501, 544365, 544372, 544374, 544379, 544393, A61K 31496, C07D40310, C07D40510, C07D40910
Patent
active
061143359
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to novel benzoylguanidine derivatives, processes for preparing them and their use in the preparation of pharmaceutical compositions.
The novel benzoylguanidine derivatives correspond to the general formula (I) ##STR2## wherein R.sub.1 denotes R.sub.3 --SO.sub.2 -- or R.sub.3 --NH--SO.sub.2 --, F, Cl or CF.sub.3 ; benzoylguanidine system via a nitrogen atom: ##STR3## and m represents 0, 1, 2, 3, 4, 5 or 6 (--CH.sub.2).sub.a, (--CHOH--).sub.b, (--CO--).sub.c, (--CS--).sub.d and/or (--NR.sub.11 --) and unsubstituted or substituted aryl, --NR.sub.5 R.sub.6 or a preferably 5- or 6-membered heterocyclic group ##STR4## which may optionally be ring-condensed with one or two phenyl systems and wherein U, V, W, X, Y and optionally Z, which may be the same or different, denote: R.sub.7 when this represents hydrogen, being optionally substituted by B; -alkyl, wherein the phenyl group may contain up to three substituents selected from the group comprising halogen, C.sub.1-4 -alkyl or C.sub.1-4 -alkoxy, hydrogen, C.sub.1-4 -alkyl R.sub.4 and R.sub.4 ' may also denote phenyl, benzyl and C.sub.3-7 -cycloalkyl;
Preferred compounds of general formula I are those wherein benzoylguanidine system via a nitrogen atom ##STR5## m is an integer 0, 1, 2, 3, 4, 5 or 6 n is an integer 0 or 1 --).sub.a, (--CHOH--).sub.b, (--CO--).sub.c, (--CS--).sub.d and/or (--NR.sub.11 --) and or unsubstituted aryl, --NR.sub.5 R.sub.6 or a 5- or 6-membered heterocyclic group ##STR6## which may optionally be ring-condensed by one or two phenyl systems and wherein U, V, W, X, Y and optionally Z, which may be the same or different, denote: R.sub.7 when this represents hydrogen, being optionally substituted by B; hydrogen, C.sub.1-4 -alkyl R.sub.4 and R.sub.4 ' may also denote phenyl, benzyl and C.sub.3-7 -cycloalkyl;
Particularly preferred compounds of formula I are those wherein ##STR7## B denotes one or more of the following groups in any desired sequence (--CH.sub.2 --).sub.a, (--CHOH--).sub.b, (--CO--).sub.c, (--CS--).sub.d and/or (--NR.sub.11 --) and ##STR8## which may optionally be ring-condensed by one or two phenyl systems and wherein U, V, W, X, Y and optionally Z, which may be the same or different, denote: R.sub.7 when this represents hydrogen, being optionally substituted by B and only one heteroatom is present in the ring system; hydrogen, C.sub.1-4 -alkyl;
Unless specifically stated otherwise, the general definitions are used in the following way: unbranched hydrocarbon group having 1 to 4 or 8 carbon atom(s) which may optionally be substituted by one or more halogen atoms, preferably fluorine, and these substituents may be identical to one another or different from one another. The following hydrocarbon groups are mentioned by way of example: 2-methylpropyl, 1,1-dimethyl-ethyl, pentyl, 1-methylbutyl, 2-methylbutyl, 3-methyl-butyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, 2,2-dimethylpropyl, 1-ethylpropyl, hexyl, 1-methylpentyl, 2-methylpentyl, 3-methylpentyl, 4-methylpentyl, 1,1-dimethylbutyl, 1,2-dimethylbutyl, 1,3-dimethylbutyl, 2,2-dimethylbutyl, 2,3-dimethylbutyl, 3,3-dimethylbutyl, 1-ethylbutyl, 2-ethylbutyl, 1,1,2-trimethylpropyl, 1,2,2-trimethylpropyl, 1-ethyl-1-methylpropyl and 1-ethyl-2-methylpropyl. Unless otherwise specified, lower alkyl groups having 1 to 4 carbon atoms such as methyl, ethyl, propyl, isopropyl, n-butyl, 1-methylpropyl, 2-methylpropyl or 1,1-dimethylethyl are preferred.
Alkoxy generally represents a straight-chained or branched hydrocarbon group having 1 to 8 carbon atoms which is bound via an oxygen atom. A lower alkoxy group having 1 to 4 carbon atoms is preferred. The methoxy group is particularly preferred.
Aryl generally represents an aromatic group having 6 to 10 carbon atoms, including those in compositions in which the aromatic group may be substituted by one or more lower alkyl groups, trifluoromethyl groups, cyano groups, alkoxy groups, nitro groups, amino groups and/or one or more halogen atoms, either identical or different; the preferred aryl group is an optionally sub
REFERENCES:
patent: 5753680 (1998-05-01), Gericke et al.
patent: 5783576 (1998-07-01), Roos et al.
Medicinal Chemistry (3rd Ed.) by Alfred Burger, p. 72-77, 1970.
Buerger Erich
Eickmeier Christian
Roos Otto
Bernhardt Emily
Boehringer Ingelheim KG
Devlin, Esq. M-E M.
Raymond R. P.
Stempel, Esq. A. R.
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