Substituted benzamidine compounds which have useful pharmaceutic

Details Substituted benzamidine compounds which have useful pharmaceutic Substituted benzamidine compounds which have useful pharmaceutic

1997-03-28

1998-03-24

Davis, Zinna Northington

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514637, 546328, 564244, 564246, C07D21381, C07C25718, A61K 31165, A61K 3144

Patent

active

057313326

DESCRIPTION:

BRIEF SUMMARY
CROSS-REFERENCES TO RELATED APPLICATIONS

This application was field pursuant to 35 U.S.C. .sctn.371 and corresponds to International Application Number PCT/EP95/02112, filed on Jun. 3, 1995.


FIELD OF THE INVENTION

The invention relates to new substituted benzamidines, the preparation thereof using conventional methods and their use, as pharmaceuticals with in particular, an LTB.sub.4 -receptor-antagonist activity.


DESCRIPTION OF THE INVENTION

The new substituted benzamidines correspond to the formula ##STR2## wherein the A denotes the group ##STR3## X.sub.1 denotes O, NH or NCH.sub.3 X.sub.2 denotes O, NH, NCH.sub.3 or ##STR4## X.sub.3 denotes --X--C.sub.n H.sub.2n --; X.sub.4 denotes --C.sub.n H.sub.2n --X-- (n=1 or 2, X=O, NH or NCH.sub.3); -C.sub.7 -cycloalkyl, aryl, O-aryl, CH.sub.2 -aryl, CR.sub.5 R.sub.6 -aryl, C(CH.sub.3).sub.2 -R.sub.7 ; and also H, when A is a group of Formula III or when X.sub.2 is a group of Formula IV; and also C.sub.1 -C.sub.6 -alkoxy, when A is the group II, X.sub.1 is as hereinbefore defined and X.sub.2 denotes NH, NCH.sub.3 or the group IV, or when A denotes the group III, X.sub.3 is as hereinbefore defined and in X.sub.4 X denotes NH or NCH.sub.3 ; -C.sub.6 alkoxy when R.sub.2 denotes aryl, O-aryl, CH.sub.2 -aryl, CR.sub.5 R.sub.6 -aryl or C(CH.sub.3).sub.2 -R.sub.7 or when X.sub.2 denotes the group IV; heteroaromatic ring; (C.sub.1 -C.sub.4 -alkyl); group; CONR.sub.10 R.sub.11 or CH.sub.2 NR.sub.10 R.sub.11 ; C.sub.1 -C.sub.6 -alkoxy; -C.sub.6 -alkyl), COR.sub.12, COOR.sub.12, CHO, CONH.sub.2, CONHR.sub.12, SO.sub.2 -(C.sub.1 -C.sub.6 -alkyl), SO.sub.2 -phenyl, wherein the phenyl group may be mono- or polysubstituted by Cl, F, CF.sub.3, C.sub.1 -C.sub.4 alkyl, OH, C.sub.1 -C.sub.4 -alkoxy; group; aryl, heteroaryl, aralkyl or heteroaryl-(C.sub.1 -C.sub.6 -alkyl), wherein the aryl or heteroaryl group may be mono or polysubstituted by Cl, F, CF.sub.3, C.sub.1 -C.sub.4 -alkyl, OH or C.sub.1 -C.sub.4 -alkoxy.
The new compounds may occur as free bases or as salts with acids, preferably physiological acceptable acids; if they contain one or more chiral centres, they may be in the form of racemates, in enantiomerically pure or concentrated form, optionally as pairs of diastereomers. Any tautomers (with --C(NH)--NHR.sub.1) are also included.
The preferred compounds of Formula I are those wherein CH.sub.2 -aryl or CR.sub.5 R.sub.6 -aryl, and, if X.sub.2 is the group IV, R.sub.2 may also represent C.sub.1 -C.sub.6 -alkoxy; R.sub.6 -aryl, R.sub.3 also denotes C.sub.1 -C.sub.6 -alkoxy;
Particular mention should be made of the compounds wherein, within the scope of the above definitions CR.sub.5 R.sub.6 -aryl; CR.sub.5 R.sub.6 -aryl, R.sub.3 may also denote C.sub.1 -C.sub.6 alkoxy; -cycloalkyl.
Where the symbols according to the above definitions may have the same or different meanings, both possibilities should be included. Aliphatic chains which have a sufficient number of carbon atoms may be straight chained or branched.
"Aryl" denotes an optionally (mono- or poly-) substituted aryl group, such as naphthyl, but preferably an optionally (mono- or poly-) substituted phenyl group. The preferred substituents are: Cl, F, Br, OH, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, and CF.sub.3 ; other possibilities are groups which are generally present only once, such as NH.sub.2, NH(C.sub.1 -C.sub.6 -alkyl), N(C.sub.1 -C.sub.6 -alkyl).sub.2, NH(SO.sub.2 -(C.sub.1 -C.sub.6 -alkyl, NH(SO.sub.2 -phenyl), wherein the phenyl group may in turn be substituted, in particular by F, Cl, CF.sub.3, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 alkoxy or OH. The term "aralkyl" denotes a C.sub.1 -C.sub.6 -alkyl group which is substituted by an aryl (as hereinbefore defined). The term "heteroaryl" here preferably refers to pyridyl, pyrimidyl, pyridazinyl and pyrazinyl, thienyl and furyl, which may be mono or polysubstituted, in particular, by Cl, F, Br, OH, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, CF.sub.3. The cycloalkyl groups may be substituted by C.sub.1 -C.sub.6 -alkyl groups, e.g. as

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