Benzylpiperidines and piperazines as muscarinic antagonists

Details Benzylpiperidines and piperazines as muscarinic antagonists Benzylpiperidines and piperazines as muscarinic antagonists

C - Chemistry, Metallurgy

07

D

C07D 295/096 (2006.01) A61K 31/445 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/695 (2006.01) C07D 211/24 (2006.01) C07D 211/32 (2006.01) C07D 213/63 (2006.01) C07D 213/70 (2006.01) C07D 233/84 (2006.01) C07D 237/14 (2006.01) C07D 239/32 (2006.01) C07D 239/34 (2006.01) C07D 241/18 (2006.01) C07D 257/04 (2006.01) C07D 263/58 (2006.01) C07D 277/34 (2006.01) C07D 295/03 (2006.01) C07D 295/084 (2006.01) C07D 295/088 (2006.01) C07D 295/108 (2006.01) C07D 295/112 (2006.01) C07D 295/116 (2006.01)

Patent

CA 2212895

Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula (I) (including all isomers salts esters, and solvates) wherein R, R1, R2, R3, R4, R21, R27, R28, X, Y, 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 of compounds of the above formula or other compounds capable of enhan cing acetylcholine release with acetylcholinesterase inhibitors.

Les composés de pipérazine di-N-substituée ou de pipéradine 1,4 di-substituée de formule (I) (y compris tous les isomères, sels, esters et solvates) où R, R<1>, R<2>, R<3>, R<4>, R<21>, R<27>, R<28>, X, Y, et Z sont comme définis dans les spécifications, constituent des antagonistes muscariniques utiles au traitement des troubles cognitifs tels que la maladie d'Alzheimer. Des compositions pharmaceutiques et des méthodes de préparation sont également présentées. Sont également présentées des combinaisons synergiques de composés de formule (I), ou d'autres composés capables de favoriser la production d'acétylcholine avec des inhibiteurs d'acétylcholinestérase.

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