摘要:
The present invention relates to 1H-Quinazoline-2,4-dione derivatives of formula (I) wherein the substituents are defined as in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them.
摘要:
Compounds have the formula (I), in which R1 stands for hydroxy or an aliphatic, araliphatic or aromatic radical; X stands for a bivalent aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical; R2 stands for hydrogen or an aliphatic or araliphatic radical; alk stands for lower alkylidene; and R3, R4 and R5 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro. These compounds and their salts may be used for treating pathological conditions which respond to the blocking of exciter amino acid receptors, and for producing pharmaceutical compositions.
摘要:
2,3-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-R¿7? (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 R¿7? 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.
摘要:
The present invention relates to l H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as AMPA-receptor ligands, in particular for the treatment of epilepsy or schizophrenia, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) and combinations comprising compounds of formula (I) are disclosed.
摘要:
Compounds of the formula (I), wherein X and R1 to R5 are as defined in the description, are useful for treating disorders mediated full or in part by mGluR5.
摘要:
The present invention relates to l H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as AMPA-receptor ligands, in particular for the treatment of epilepsy or schizophrenia, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) and combinations comprising compounds of formula (I) are disclosed.
摘要:
Compounds have the formula (I), in which R1 stands for hydroxy or an aliphatic, araliphatic or aromatic radical; X stands for a bivalent aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic, heteroarylaliphatic or aromatic radical; R2 stands for hydrogen or an aliphatic or araliphatic radical; alk stands for lower alkylidene; and R3, R4 and R5 independently represent hydrogen, lower alkyl, halogen, trifluoromethyl, cyano or nitro. These compounds and their salts may be used for treating pathological conditions which respond to the blocking of exciter amino acid receptors, and for producing pharmaceutical compositions.