Anticonvulsive substituted-9-benzyl-9H-purines

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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Details

514262, 544264, 544265, 544276, 544277, 544326, A61K 3152, C07D47316

Patent

active

051108186

ABSTRACT:
The invention relates to novel 9H-purine derivatives, especially to the novel substituted 9-benzyl-9H-purines of the general formula ##STR1## in which Ph is a phenyl radical substituted by halogen, R.sub.1 is hydrogen or a free amino group or an amino group that is substituted aliphatically, cycloaliphatically, cycloaliphatically-aliphatically and/or by acyl, and R.sub.2 is halogen, lower alkoxy, lower alkyl, a free amino group, or an amino group that is substituted aliphatically, cycloaliphatically, cycloaliphatically-aliphatically and/or by acyl, with the proviso that R.sub.2 is other than halogen when Ph is 2-fluorophenyl or 2,5- or 2,6-difluorophenyl and R.sub.1 is a radical of the formula --N(R.sub.11)(R.sub.12) (Ia) in which either R.sub.11 is hydrogen, methyl or ethyl and R.sub.12 is hydrogen, methyl, hydroxymethyl, ethyl, n-propyl, isopropyl, cyclopropyl, cyclopenthyl or cyclopropylmethyl, or R.sub.11 is hydrogen and R.sub.12 is methoxymethyl, and with the further proviso that R.sub.2 is other than chlorine when Ph is 3-chlorophenyl, 4-chlorophenyl or 3,4-dichlorophenyl and R.sub.1 is N,N-dimethylamino, and to the novel compounds of formula I in which Ph is 2-fluorophenyl or 2,6-difluorophenyl, R.sub.1 is N-methylamino or N,N-dimethylamino and R.sub.2 is chlorine, and to the salts thereof in each case. These compounds and the salts thereof can be used as pharmaceutical active ingredients and can be manufactured in a manner known per se.

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Kelley, et al., J. Med. Chem., 1988, 31, 606-612.
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