188699-41-4Relevant academic research and scientific papers
2,3-dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives
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, (2008/06/13)
PCT No. PCT/EP96/03644 Sec. 371 Date Feb. 27, 1998 Sec. 102(e) Date Feb. 27, 1998 PCT Filed Aug. 19, 1996 PCT Pub. No. WO97/08155 PCT Pub. Date Mar. 6, 19972,3-Dioxo-1,2,3,4-tetrahydro-quinoxalinyl derivatives of formula (I), wherein one of the radicals R1, and R2 is a group R5 and the other is a group of formula -CH(R6)-alk-R7 (Ia), -alk-CH(R6-R7 (Ib), -alk-N(R8)-X-R7 (Ic), -alk-N+(R8)(R9)-X-R7A- (Id), -alk-O-X-R7 (Ie) or -alk-S-X-R7 (If), R3, R4 and R5 are each independently of the others hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, R6 is unsubstituted or lower alkylated and/or lower alkanoylated amino, R7 is hydrogen; an aliphatic, cycloaliphatic or heterocycloaliphatic 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 unsubtituted or aliphatically or araliphatically substituted and/or substituted by aliphatic, araliphatic or aromatic acyl; or an aromatic or heteroaromatic radical, R8 is hydrogen; an aliphatic or araliphatic radical; or acyl derived from an aliphatic or araliphatic carboxylic acid or from an aliphatic or araliphatic semiester of carbonic acid, or R7 and R8, together with X and the nitrogen atom bonding R8 and X, form an unsubstitued or substituted mono- or di-azaxycloalkyl, azoxacycloalkyl, azathiacycloalkyl or optionally oxidised thiacycloalkyl radical bonded via a nitrogen atom, or an unsubstituted or substituted, optionally partially hxdrogenated aryl or heteroaryl radical, R9 is an aliphatic or araliphatic radical, or R7, R8 and R9 together with X and the nitrogen atom bonding R8, R9 and X, form an unsubstituted or substituted quaternary heteroaryl radical bonded via the quaternary nitrogen atom, with A- being the anion of a protonic acid, alk is lower alkylene, and X (unless, together with R7 and R8 and the nitrogen atom bonding R8 and X or together with the nitrogen atom bonding R8, R9 and X, it forms part of one of the mentioned ring systems) is a divalent aliphatic, cycloaliphatic or araliphatic radical or a direct bond, and the pharmaceutically acceptable salts thereof can be used in the preparation of a medicament for the treatment of pathological conditions that are responsive to blocking of AMPA, kainate and/or glycine binding sites of the NMDA receptor.
Substituted aminoalkane phosphonic acids
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, (2008/06/13)
PCT No. PCT/EP97/05843 Sec. 371 Date Apr. 23, 1999 Sec. 102(e) Date Apr. 23, 1999 PCT Filed Oct. 22, 1997 PCT Pub. No. WO98/17672 PCT Pub. Date Apr. 30, 1998Compounds of the formula I in which R1 is hydroxyl or an aliphatic, araliphatic or aromatic radical, X is a divalent aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical, R2 is hydrogen or an aliphatic or araliphatic radical, alk is lower alkylidene and R3, R4 and R5 independently of one another are hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro, and their salts can be used for the treatment of pathological conditions which respond to blockage of excitatory amino acid receptors, and for the production of pharmaceutical preparations.
5-aminomethylquinoxaline-2,3-diones. Part II: N-aryl derivatives as novel NMDA/glycine and AMPA antagonists
Auberson, Yves P.,Acklin, Pierre,Allgeier, Hans,Biollaz, Michel,Bischoff, Serge,Ofner, Silvio,Veenstra, Siem J.
, p. 71 - 74 (2007/10/03)
Potent antagonists at the glycine-binding site of NMDA receptors, as well as dual antagonists acting also at AMPA receptors have been identified in a series of 5-arylaminomethylquinoxaline-2,3-diones. A study of the structure-activity relationship of these compounds is reported here.
