2-(hetero)aryl-2-(N-((hetero)aryl)-amino)-acetic acid derivatives useful e.g. for treating anxiety, inflammation, allergy, depression, diarrhea or especially pain is NMDA antagonist
New 2-(aryl or heteroaryl)-2-(N-(aryl or heteroaryl)-amino)-acetic acid derivatives (I). New medicaments contain heteroaryl-aminoacetic acid derivative(s) of formula R 2>-CH(NHR 1>)-COOH (I), including their racemates, pure stereoisomers (specifically enantiomers or diastereomers), stereoisome...
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Zusammenfassung: | New 2-(aryl or heteroaryl)-2-(N-(aryl or heteroaryl)-amino)-acetic acid derivatives (I). New medicaments contain heteroaryl-aminoacetic acid derivative(s) of formula R 2>-CH(NHR 1>)-COOH (I), including their racemates, pure stereoisomers (specifically enantiomers or diastereomers), stereoisomer mixtures in all proportions, free acids or bases, salts (specifically sodium salts or hydrochlorides) and/or solvates (specifically hydrates). R 1>monocyclic aryl or heteroaryl (optionally substituted (os) and optionally fused with an os mono- or polycyclic ring (optionally containing heteroatom(s))); R 2>os monocyclic aryl, optionally fused with an os mono- or polycyclic ring system (optionally containing heteroatom(s)). ACTIVITY : Analgesic; tranquilizer; antiinflammatory; antiallergic; antidepressant; antiaddictive; antialcoholic; antidiarrheic; uropathic; antipruritic; cardiant; antitussive; anticonvulsant; neuroleptic; neuroprotective; nootropic; antiparkinsonian; cerebroprotective; vasotropic; anti-HIV; antidiabetic; auditory. In a formalin test for analgesic activity in mice, (3,5-dichlorophenylamino)-(2-methylsulfanyl-phenyl)-acetic acid (Ia) (as the sodium salt) inhibited nociception by 66% at a dose of 31.6 mg/kg. MECHANISM OF ACTION : N-Methyl-D-aspartate (NMDA) antagonist. In binding assays for the glycine B binding site of the NMDA receptor channel, (Ia) inhibited binding by 39% at a concentration of 10 MicroM.
Die vorliegende Erfindung betrifft Arzneimittel, enthaltend substituierte 2-Aryl-Aminoessigsäure-Verbindungen und/oder substituierte 2-Heteroaryl-Aminoessigsäure-Verbindungen sowie deren Verwendung zur Herstellung von Arzneimitteln. |
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