Muscarinic antagonists

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 239/34 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) A61K 31/505 (2006.01) A61K 31/53 (2006.01) A61K 31/535 (2006.01) C07D 211/58 (2006.01) C07D 213/643 (2006.01) C07D 241/04 (2006.01) C07D 295/088 (2006.01) C07D 295/096 (2006.01) C07D 311/68 (2006.01) C07D 317/58 (2006.01) C07D 317/62 (2006.01) C07D 401/04 (2006.01) C07D 405/14 (2006.01) C07D 409/14 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2258044

Di-N-substituted piperazine or 1,4di-substituted piperidine compounds in accordance with formula (I) (including all isomers, salts, esters, and solvates), wherein Q, n, R, R1, R2, R3, R4, R21, R27, R28, X, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations with acetylcholinesterase inhibitors of compounds capable of enhancing acetylcholine release and having the above formula.

Composés de pipérazine di-N-substituée ou de pipéridine 1,4-disubstituée de formule (I) (y compris tous les isomères, sels, esters et solvates) dans laquelle Q, n, R, R<1>, R<2>, R<3>, R<4>, R<21>, R<27>, R<28>, X et Z sont tels que définis dans le descriptif, qui sont des antagonistes muscariniques utiles pour traiter des troubles cognitifs tels que la maladie d'Alzheimer. Des compositions pharmaceutiques et des procédés de préparation sont également décrits, ainsi que des combinaisons synergiques d'inhibiteurs d'acétylcholinestérase et de composés capables d'améliorer la libération d'acétylcholine et ayant la formule susmentionnée.

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