Phenylamidine derivatives, a process for preparing the same and

Details Phenylamidine derivatives, a process for preparing the same and Phenylamidine derivatives, a process for preparing the same and

1998-07-31

2000-10-03

Nazario-Gonzalez, Porfirio

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

514825, 514826, 514863, 514903, 514908, 560105, 560138, 564 47, 564 52, 564 53, 564116, 564244, A61K 31155, C07C25718

Patent

active

061274232

DESCRIPTION:

BRIEF SUMMARY
The invention relates to new phenylamidine derivatives, processes for preparing them and their use as pharmaceutical compositions. The phenylamidines according to the invention correspond to the general formula I ##STR2## wherein A denotes X.sub.1 --C.sub.m H.sub.2m --X.sub.2 --, in which m is an integer 2, 3, 4, 5 or 6 or ##STR3## and X.sub.1 denotes O, NH or NCH.sub.3 ; ##STR4## X.sub.3 denotes X.sub.1 --C.sub.n H.sub.2n in which n is the integer 1 or 2; 2; --Ar.sub.2 ; CR.sub.4 R.sub.5 Ar.sub.3, C(CH.sub.3).sub.2 R.sub.6 ; COO(C.sub.1-4)-alkyl; R.sub.10, CH.sub.2 NR.sub.9 R.sub.10 ; COR.sub.11, COOR.sub.11, CHO, CONH.sub.2, CONHR.sub.11, SO.sub.2 -(C.sub.1-6 -alkyl) SO.sub.2 -phenyl, wherein the phenyl ring may be mono- or polysubstituted by halogen, CF.sub.3, C.sub.1-4 -alkyl, OH, C.sub.1-4 -alkoxy; aralkyl or heteroaryl-(C.sub.1-6 -alkyl), wherein the aryl or heteroaryl groups may be mono- or polysubstituted by Cl, F, CF.sub.3, C.sub.1-4 -alkyl, OH or C.sub.1-4 -alkoxy; the exception of the unsubstituted phenyl group and the phenyl group which is monosubstituted by halogen, C.sub.1-4 -alkyl or monosubstituted by C.sub.1-4 -alkoxy; the exception of the unsubstituted phenyl group; C.sub.1-4 -alkylene unit; individual enantiomers or racemates and in the form of the free bases or the corresponding acid addition salts with pharmacologically acceptable acids.
Preferred compounds according to general formula I are those wherein 2 ##STR5## and X.sub.1 is O; ##STR6## X.sub.3 denotes --X.sub.1 --C.sub.n H.sub.2n -- wherein n is the integer 1 or 2; or 2; --Ar.sub.2 ; CR.sub.4 R.sub.5 Ar.sub.3, C(CH.sub.3).sub.2 R.sub.6 ; R.sub.10, CH.sub.2 NR.sub.9 R.sub.10 ; group; the exception of the unsubstituted phenyl group and the phenyl group which is monosubstituted by halogen, C.sub.1-4 -alkyl and monosubstituted by C.sub.1-4 -alkoxy; the exception of the unsubstituted phenyl group; C.sub.1-4 -alkylene unit; individual enantiomers or racemates and in the form of the free bases or the corresponding acid addition salts with pharmacologically acceptable acids.
Particularly preferred compounds of general formula I are those wherein ##STR7## and X.sub.1 is O; --Ar.sub.2 ; CR.sub.4 R.sub.5 Ar.sub.3, C(CH.sub.3).sub.2 R.sub.6 ; R.sub.10, CH.sub.2 NR.sub.9 R.sub.10 ; hydroxy or by hydroxy and C.sub.1-6 -alkyl; hydroxy or by hydroxy and C.sub.1-6 -alkyl; hydroxy or by hydroxy and C.sub.1-6 -alkyl individual enantiomers or racemates and in the form of the free bases or the corresponding acid addition salts with pharmacologically acceptable acids.
Unless specifically stated otherwise, the general definitions are used as follows:
C.sub.1-4 -alkyl, C.sub.1-6 -alkyl and C.sub.1-8 -alkyl, respectively, generally denote a branched or unbranched hydrocarbon group having 1 to 4 or 6 or 8 carbon atoms, which may optionally be substituted by one or more halogen atoms, preferably fluorine, which may be the same or different from one another. The following hydrocarbon groups are mentioned by way of example:
methyl, ethyl, propyl, 1-methylethyl(isopropyl), n-butyl, 1-methylpropyl, 2-methylpropyl, 1,1-dimethylethyl, pentyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, 1,1-dimethylpropyl, 1,2-dimethylpropyl, 2,2-dimethylpropyl, 1-ethylpropyl, hexyl, 1-methylpentyl, 2-methylphenyl, 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.
Aryl generally denotes an aromatic group having 6 to 10 carbon atoms, also 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 - which may be identical or

REFERENCES:
patent: 5246965 (1993-09-01), Main
patent: 5686496 (1997-11-01), Anderskewitz et al.
International Preliminary Examination Report for International Application No. PCT/EP96/05529, Dated Jul. 10, 1998.

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