- 6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists
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A new set of quinazolinedione sulfonamide derivatives as competitive AMPA receptor antagonist with improved properties compared to 1 is disclosed. By modulating physico-chemical properties, compound 29 was identified with a low ED50 of 5.5 mg/kg in an animal model of anticonvulsant activity after oral dosage.
- Orain, David,Ofner, Silvio,Koller, Manuel,Carcache, David A.,Froestl, Wolfgang,Allgeier, Hans,Rasetti, Vittorio,Nozulak, Joachim,Mattes, Henri,Soldermann, Nicolas,Floersheim, Philipp,Desrayaud, Sandrine,Kallen, Joerg,Lingenhoehl, Kurt,Urwyler, Stephan
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p. 996 - 999
(2012/03/26)
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- 1H-QUINAZ0LINE-2,4-DIONES AND THEIR USE AS AMPA-RECEPTOR LIGANDS
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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.
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Page/Page column 13; 103
(2010/11/24)
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- QUINAZOLINE DERIVATIVES
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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.
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Page/Page column 61
(2010/02/15)
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