Cycloalkylpyrrole-3-carboxylic acid derivatives and...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 487/04 (2006.01) A61K 31/40 (2006.01) A61K 31/403 (2006.01) A61K 31/404 (2006.01) A61P 25/00 (2006.01) A61P 25/20 (2006.01) A61P 25/22 (2006.01) A61P 25/24 (2006.01) C07D 209/42 (2006.01) C07D 209/52 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2452211

This invention relates to cycloalkylpyrolle-3-carboxylic acid derivatives and heterocycloalkylpyrrole-3-carboxylic acid derivatives that bind with high selectively and/or high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in the treatment of central nervous system (CNS) diseases. This invention also relates to the use of these cycloalkylpyrolle-3-carboxylic acid derivatives and heterocycloalkylpyrrole-3-carboxylic acid derivatives in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the detection of GABAA receptors in tissue samples.

cette invention concerne des dérivés d'acide cycloalkylpyrolle-3 carboxylique et des dérivés d'acide hétérocycloalkylpyrrole-3 carboxylique qui se lient avec une sélectivtié et/ou une affinité élevées avec le site benzodiazépine de récepteurs GABA¿A?. L'invention concerne également des compositions pharmaceutiques renfermant de tels composés et l'utilisation de ces derniers pour le traitement de troubles du système nerveux central (SNC). Cette invention porte également sur l'utilisation de ces dérivés d'acide cycloalkylpyrolle-3-carboxylique et de ces dérivés d'acide hétérocycloalkylpyrrole-3-carboxylique en combinaison avec un ou plusieurs autres agents SNC dans le but de potentialiser les effets d'autres agents du SNC. De plus, l'invention concerne l'utilisation de tels composés comme sondes pour la détection de récepteurs GABA¿A? dans des échantillons de tissus.

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