Pharmacologically active pyrimidineamine derivatives and process

Details Pharmacologically active pyrimidineamine derivatives and process Pharmacologically active pyrimidineamine derivatives and process

1995-05-31

1998-01-06

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, 544295, 544296, 544238, 544331, C07D23942, A61K 31505

Patent

active

057055025

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 published as WO95/09851, Apr. 13, 1995.
The invention relates to N-phenyl-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-phenyl-2-pyrimidineamine derivatives of formula I ##STR2## wherein R.sub.1 is a substituted cyclic radical, the cyclic radical being bonded to a ring carbon atom in each case and being selected from phenyl, pyridyl, pyrazinyl, thiazolyl, pyrimidinyl, pyridazinyl and imidazolyl, and the substituents of the above-mentioned cyclic radical being selected from one or more of the groups halogen, cyano, carbamoyl, --C(.dbd.O)--OR.sub.3, --C(.dbd.O)--R.sub.4, --SO.sub.2 --N(R.sub.5)--R.sub.6, --N(R.sub.7)--R.sub.8, --OR.sub.9 and fluorine-substituted lower alkyl, wherein independently of the others hydrogen or lower alkyl that is unsubstituted or substituted by mono- or di-lower alkylamino; and --C(.dbd.O)--R.sub.11, --SO.sub.2 --N(R.sub.12)--R.sub.13, --N(R.sub.14)--R.sub.15, --OR.sub.16 and fluorine-substituted lower alkyl, wherein each independently of the others hydrogen or lower alkyl that is unsubstituted or substituted by mono- or di-lower alkylamino, and to salts of such compounds having at least one salt-forming group.
A substituted cyclic radical R.sub.1, such as, for example, a substituted phenyl radical R.sub.1, can have several substituents, but especially not more than 3 and, especially in the case of relatively large substituents, preferably only one substituent, which substituents are principally in the para- (or 4-position) and/or preferably meta-position (or 3-position) with respect to the bonding site of the cyclic radical R.sub.l. The above-mentioned substituted cyclic radicals R.sub.1 other than phenyl generally have up to two and preferably only one substituent, which is/are especially in the para-position and/or preferably meta-position with respect to the bonding site of the cyclic radical R.sub.1.
Pyridyl bonded to a ring carbon atom is 2- or preferably 4- or 3-pyridyl, especially 4-pyridyl. In a mono-substituted pyridyl radical R.sub.1, the substituent is preferably in the ortho-position with respect to the pyridine nitrogen.
Halogen in a radical R.sub.1 is preferably chlorine or fluorine.
Halogen-substituted phenyl R.sub.1 is preferably 2-, 3- or 4-chloro-phenyl, 2,4-, 3,4- or 2,5-dichloro-phenyl or 2,3,4-trichloro-phenyl.
Fluorine-substituted lower alkyl R.sub.2 is lower alkyl that carries at least one, but preferably several, fluorine substituents, especially 1,1,2,2-tetrafluoro-ethyl or more especially tri-fluoromethyl.
Mono- or di-lower alkylamino is, for example, methylamino or dimethylamino.
Within the scope of this text, the term "lower" denotes radicals having up to and including 7, preferably up to and including 4, carbon atoms.
Unless otherwise indicated in the context concerned, lower alkyl is preferably methyl or ethyl.
R.sub.3 and R.sub.7 are preferably hydrogen. R.sub.8 is preferably lower alkyl, such as especially n-propyl. R.sub.9 is preferably hydrogen or methyl.
Salt-forming groups in a compound of formula I are groups or radicals having basic or acidic properties. Compounds having at least one basic group or at least one basic radical, for example a mono-lower alkylamino group, a pyrazinyl radical or a pyridyl radical, can form acid addition salts, for example with inorganic acids, such as hydrochloric acid, sulfuric acid or a phosphoric acid, or with suitable organic carboxylic or sulfonic acids, for example aliphatic mono- or di-carboxylic acids, such as trifluoroacetic acid, acetic acid, propionic acid, glycolic acid, succinic acid, maleic acid, fumaric acid, hydroxymaleic acid, malic acid, tartaric acid, citric acid, oxalic acid or amino acids, such as arginine or lysine, aromatic carboxylic acids, such a

REFERENCES:
patent: 5612340 (1997-03-01), Zimmermann

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