Pharmacologically active pyridine derivatives and processes for

Details Pharmacologically active pyridine derivatives and processes for Pharmacologically active pyridine derivatives and processes for

1995-05-31

1998-03-17

Ford, John M.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514252, 5142358, 514 86, 544295, 544122, 544331, 544243, C07D40104, C07D40114, A61K 31505

Patent

active

057287082

DESCRIPTION:

BRIEF SUMMARY
This application is filed under 35 U.S.C. .sctn.371 as a national phase application of PCT/EP94/03148, filed Sep. 21, 1994.
The invention relates to N-phenyl-4-(4-pyridyl)2-pyrimidineamine derivatives, to processes for the preparation thereof, to medicaments comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals.
The invention relates to N-phenyl2-pyrimidineamine derivatives of formula I ##STR2## wherein R.sub.0 is hydrogen, halogen, lower alkoxy or lower alkyl, alkylamino, cyano, imidazolyl, guanidyl, amino, lower alkanoylamino, lower alkylamino-carbonylamino, amidino, di-lower alkylamino-cyclohexyl, carboxy, lower alkoxycarbonyl, carbamoyl, N-hydroxy-carbamoyl, hydroxy, lower alkoxy, dihydroxyphosphoryloxy, piperazinyl, lower alkanoyl-piperazinyl, formylpiperazinyl, prolylamido or by a radical of the formula H.sub.2 N--CH(R)--C(.dbd.O)--NH-- wherein R is hydrogen, C.sub.1 -C.sub.4 alkyl, benzyl, hydroxymethyl, 1-hydroxy-ethyl, mercaptomethyl, 2-methylthio-ethyl, indol-3-yl-methyl, phenyl-methyl, 4-hydroxy-phenyl-methyl, carbamoyl-methyl, 2-carbamoyl-ethyl, carboxy-methyl, 2-carboxy-ethyl, 4-amino-butyl, 3-guanidyl-propyl or R is 1H-imidazol-4-yl-methyl, and R.sub.2 is C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.3 alkoxy, chlorine, bromine, iodine, trifluoromethyl, hydroxy, phenyl, amino, mono(C.sub.1 -C.sub.3 alkyl)amino, di(C.sub.1 -C.sub.3 alkyl)amino, C.sub.2 -C.sub.4 alkanoyl, propenyloxy, carboxy, carboxy-methoxy, ethoxycarbonyl-methoxy, sulfanilamido, N,N-di-(C.sub.1 -C.sub.3 alkyl)sulfanilamido, N-methyl-piperazinyl, piperidinyl, 1H-imidazol-1-yl, 1H-triazol-1-yl, 1H-benzimidazol-2-yl, 1-naphthyl, cyclopentyl, 3,4-dimethyl-benzyl or a radical of one of the formulae: --C(.dbd.O)--R.sub.4, --O--(CH.sub.2).sub.n --N(R.sub.3)--R.sub.4, --C(.dbd.O)--NH--(CH.sub.2) .sub.n --N(R.sub.3)--R.sub.4, --CH(CH.sub.3)--NH--CHO, --NH.sub.2, --NH--CH.sub.2 --C(.dbd.O)--N(R.sub.3)--R.sub.4, ##STR3## wherein R.sub.3 and R.sub.4 are each independently of the other C.sub.1 -C.sub.3 alkyl, R.sub.4.sup.a is hydroxy, amino or imidazolyl, X is oxygen or sulfur, m is 1, 2 or 3, n is 2 or 3, R.sub.5 is hydrogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, chlorine, bromine, iodine or trifluoromethyl, R.sub.6 is 1H-imidazol-1-yl or morpholinyl and R.sub.7 is C.sub.1 -C.sub.3 alkyl or is phenyl that is unsubstituted or mono-substituted by C.sub.1 -C.sub.3 alkyl, halogen or by trifluoromethyl, and the salts thereof.
Halogen R.sub.0 is fluorine, bromine, iodine or preferably chlorine.
Lower alkoxy R.sub.0 is preferably methoxy.
Lower alkyl R.sub.0 is preferably methyl.
Amino-lower alkyl in a radical R.sub.1 is preferably .omega.-amino-C.sub.2 --C.sub.3 alkyl.
Hydroxy-lower alkyl in a radical R.sub.1 is preferably .omega.-hydroxy-C.sub.2 -C.sub.3 alkyl.
Cyclohexyl-amino R.sub.1 substituted by amino is preferably 4-amino-cyclohexyl-amino. Di-lower alkylamino-cyclohexyl as part of a substituted lower alkyl radical R.sub.1 is preferably 4-di-lower alkylamino-cyclohexyl, preferably 4-dimethylamino-cyclohexyl.
Piperazinyl R.sub.1 is preferably 1-piperazinyl. Piperazinyl R.sub.1 substituted by amino-lower alkyl is preferably 4-(2-amino-ethyl)-piperazin-1-yl.
Morpholinyl R.sub.1 and morpholinyl in a radical R.sub.1 are preferably 4-morpholinyl, wherein the free valency extends from the nitrogen. Lower alkylamino R.sub.1 substituted by morpholinyl is preferably 2-morpholin-4-yl-ethylamino.
Hydroxy-lower alkylamino in a radical R.sub.1 is preferably 2-hydroxy-ethylamino. Lower alkylamino substituted by hydroxy-lower alkylamino is preferably 3-(2-hydroxy-ethyl-amino)-prop-1-ylamino.
Imidazolyl R.sub.4.sup.a in a radical R.sub.2 is preferably 1H-imidazol-4-yl.
Lower alkanoylamino in a radical R.sub.1 is preferably acetylamino.
Lower alkylamino-carbonylamino in a radical R.sub.1 is preferably methylamino-carbonyl-amino.
Di-lower alkylamino in a radical R.sub.1 is preferably dimethylamino.
Formyl-piperazinyl in a radical R.sub.1 is preferably

REFERENCES:
patent: 4725600 (1988-02-01), Takaya et al.
patent: 4966622 (1990-10-01), Rempfler et al.
patent: 5159078 (1992-10-01), Rempfler et al.

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