Piperidine and piperazine derivatives and their use as...

C - Chemistry – Metallurgy – 07 – D

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C07D 405/14 (2006.01) A61K 31/445 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/53 (2006.01) C07D 405/12 (2006.01) C07D 409/14 (2006.01) C07D 413/14 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2261725

Di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R1, R2, R3, R4, R21, R22, R28, X, Y and Z 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 of compounds of the above formula with acetylcholinesterase inhibitors.

Composés pipérazines Di-N substituées ou pipéridines 1,4 di-substituées de formule I (comprenant tous les isomères, sels, esters et solvates), formule dans laquelle R, R<1>, R<2>, R<3>, R<4>, R<21>, R<27>, R<28>, X, Y et Z sont tels que définis dans la description. Lesdits composés sont des antagonistes muscariniques utiles pour le traitement de troubles cognitifs tels que la maladie d'Alzheimer. Des compositions pharmaceutiques et des procédés de préparation sont décrits ainsi que des combinaisons synergiques de composés de ladite formule et d'inhibiteurs de l'acétylcholinestérase.

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