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US 5,684,005 AGranted
Pharmacologically active CNS compounds
AssigneeGlaxo Wellcome Inc.
InventorsAlistair Ainslie Miller, Malcolm Stuart Nobbs, Richard Martin Hyde, Michael John Leach
Life of this patent
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Abstract
A class of substituted phenylpyrimidine compounds are disclosed which are potent inhibitors of the excitatory amino acid, glutamate. Such compounds are useful in the treatment or prevention of a range of CNS disorders including cerebral ischaemic damage and epilepsy.
Claims23
A pyrimidine of formula (I):
- ##STR7## wherein R.sub.1 is N-morpholino or N-(C.sub.1 -C.sub.6 alkyl)-piperazino;
- R.sub.2 is amino;
- R.sub.3 is selected rom the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl, trifluoromethyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, (C.sub.1 -C.sub.6 alkyl)thio(C.sub.1 -C.sub.6 alkyl), di(C.sub.1 -C.sub.6 alkyl)oxy!(C.sub.1 -C.sub.6 alkyl), and --CH.sub.2 X wherein X is selected from the group consisting of C.sub.1 -C.sub.6 alkoxy, phenoxy and benzyloxy except that R.sub.3 is not hydrogen or C.sub.1 -C.sub.6 alkyl when R.sub.1 is N-morpholino;
- each of R.sub.4, R.sub.5, R.sub.7 and R.sub.8 is the same or different and is hydrogen or halo or R.sub.4 and R.sub.5 together denote --CH.dbd.CH--CH.dbd.CH--;
- R.sub.6 is selected from the group consisting of hydrogen, halo, nitro and amino except that R.sub.6 is not chloro when R.sub.1 is morpholino or N-methylpiperazino, R.sub.2 is amino, R.sub.3 is ethyl and each of R.sub.4, R.sub.5, R.sub.7 and R.sub.8 is hydrogen;
- and pharmaceutically acceptable acid addition salts thereof.
3 more elements
A compound which is
- 2-N-morpholino-4-amino-5-(2,3,5-trichlorophenyl)-6-trifluoromethylpyrimidin e;
- and pharmaceutically acceptable acid addition salts thereof.
A pharmaceutical formulation comprising a pyrimidine of formula (I):
- ##STR8## wherein:
- R.sub.1 is N-morpholino or N-(C.sub.1 -C.sub.6 alkyl)-piperazino;
- R.sub.2 is amino;
- R.sub.3 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl, trifluoromethyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, (C.sub.1 -C.sub.6 alkyl)thio(C.sub.1 -C.sub.6 alkyl), di(C.sub.1 -C.sub.6 alkyl)oxy!(C.sub.1 -C.sub.6 alkyl), and --CH.sub.2 X wherein X is selected from the group consisting of C.sub.1 -C.sub.6 alkoxy, phenoxy and benzyloxy;
- each of R.sub.4, R.sub.5, R.sub.7 and R.sub.8 is the same or different and is hydrogen or halo or R.sub.4 and R.sub.5 together denote --CH.dbd.CH--CH.dbd.CH--;
- R.sub.6 is selected from the group consisting of hydrogen, halo, nitro and amino except that R.sub.6 is not chloro when R.sub.1 is morpholino or N-methylpiperazino, R.sub.2 is amino, R.sub.3 is ethyl and each of R.sub.4, R.sub.5, R.sub.7 and R.sub.8 is hydrogen;
- or a pharmaceutically acceptable acid addition salt thereof;
- and one or more acceptable carriers therefor.
5 more elements
2-N-morpholino-4-amino-5-(2,3,5-trichlorophenyl)pyrimidine;
- and pharmaceutically acceptable acid addition salts thereof.
Dependencies are inferred from the claim text.