2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives

Details 2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives 2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives

1998-02-27

2000-06-27

Cerstl, Robert

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

544354, C07D24144, A61K 31495

Patent

active

060807431

DESCRIPTION:

BRIEF SUMMARY
The invention relates to the use of 2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula I ##STR2## wherein one of the radicals R.sub.1 and R.sub.2 is a group R.sub.5 and the other is a group of formula --CH(R.sub.6)--alk--R.sub.7 (Ia), --alk--CH(R.sub.6)-R.sub.7 (Ib), --alk--N(R.sub.8)--X--R.sub.7 (Ic), --alk--N.sup.+ (R.sub.8)(R.sub.9)--X--R.sub.7 A (Id), --alk--O--X--R.sub.7 (Ie) or --alk--S--X--R.sub.7 (If), lower alkyl, halogen, trifluoromethyl, cyano or nitro, amino, radical; cyano; acyl derived from carbonic acid or from a semiester or semiamide of carbonic acid, from sulfuric acid or from an aliphatic or aromatic sulfonic acid or from phosphoric acid or from a phosphonic acid ester; amino that is unsubstituted or aliphatically or araliphatically substituted and/or substituted by aliphatic, araliphatic or aromatic acyl; or an aromatic or heteroaromatic radical, from an aliphatic or araliphatic carboxylic acid or from an aliphatic or araliphatic semiester of carbonic acid, or and X, form an unsubstituted or substituted mono- or di-azacycloalkyl, azoxacycloalkyl, azathiacycloalkyl or optionally oxidized thiacycloalkyl radical bonded via a nitrogen atom, or an unsubstituted or substituted, optionally partially hydrogenated aryl or heteroaryl radical, R.sub.8, R.sub.9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A.sup.- being the anion of a protonic acid, R.sub.8 and X or together with the nitrogen atom bonding R.sub.8, R.sub.9 and X, it forms part of one of the mentioned ring systems) is a divalent aliphatic, cycloaliphatic or araliphatic radical or a direct bond, of formula Ic, R.sub.2 and R.sub.3 are each independently of the other fluorine, chlorine, bromine, methyl, ethyl or trifluoromethyl and R.sub.4 is hydrogen, when alk is methylene, ethylidene or propylidene, the group --N(R.sub.8)--X--R.sub.7 is other than a 5-membered mono-, di-, tri- or tetra-azaheteroaryl radical that is bonded via a nitrogen atom and is optionally benzo-fused and/or substituted by alkyl having up to and including 6 carbon atoms or substituted in the .omega.-position by a group of the formula --N(R.sub.a)--R.sub.b wherein R.sub.a and R.sub.b are each independently of the other hydrogen, alkyl, cycloalkyl, phenyl-lower alkyl or pyridyl-lower alkyl or together with the nitrogen atom bonding them form a pyrrolidino, piperidino, piperazino, N'-lower alkylpiperazino, morpholino or azepino group, medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor, and R.sub.4 are hydrogen and R.sub.2 is a group of formula Ib, when alk is methylene, R.sub.6 is other than amino or R.sub.7 is other than carboxy, R.sub.3 and R.sub.4 are hydrogen and R.sub.2 is a group of formula Ic, when alk is methylene, the group --N(R.sub.8)--X--R.sub.7 is other than 1-imidazolyl or when alk is ethylene the group --N(R.sub.8)--X--R.sub.7 is other than amino, dipropylamino, N-(2-phenylethyl)-N-propyl-amino and N'-(2-chlorophenyl)piperazino, is a group of formula Ic, chlorine, bromine, methyl, ethyl or trifluoromethyl and R.sub.4 is hydrogen, when alk is methylene, ethylidene or propylidene the group --N(R.sub.8)--X--R.sub.7 is other than a 5-membered mono-, di-, tri- or tetra-azaheteroaryl radical that is bonded via a nitrogen atom and is optionally benzo-fused and/or substituted by alkyl having up to and including 6 carbon atoms or substituted in the .omega.-position by a group of the formula --N(R.sub.a)--R.sub.b wherein R.sub.a and R.sub.b are each independently of the other hydrogen, alkyl, cycloalkyl, phenyl-lower alkyl or pyridyl-lower alkyl or together with the nitrogen atom bonding them form a pyrrolidino, piperidino, piperazino, N'-lower alkylpiperazino, morpholino or azepino group, pharmaceutical compositions comprising them.
Unsubstituted or lower alkylated and/or lower alkanoylated amino is, for example, amino, lower alkylamino, lower alkanoylamino, N-lower alkyl-N

REFERENCES:
patent: 4156734 (1979-05-01), Stone

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