Oxa- and thia-diazole muscarinic receptor antagonists

Details Oxa- and thia-diazole muscarinic receptor antagonists Oxa- and thia-diazole muscarinic receptor antagonists

C - Chemistry, Metallurgy

07

D

C07D 413/04 (2006.01) A61K 31/445 (2006.01) A61K 31/505 (2006.01) C07D 413/14 (2006.01) C07D 417/04 (2006.01) C07D 417/14 (2006.01)

Patent

CA 2247164

A compound of formula (I) wherein RI is C1-C6 alkyl, halo-(C1-C6 alkyl), C3-C7 cycloalkyl, C2-C6 alkylnyl, hydroxy-<C2-C6 alkynyl), (C1-C4 alkoxy)-(C2-C6 alkynyl), aryl, aryl-(C1-C4 alkyl), heteroaryl or heteroaryl-(C1-C4 alkyl); R2 is H or C1-C4 alkyl; R3 is aryl, heteroaryl, 2,3- dihydrobenzofuranyl or C4-C7 cycloalkyl; X is O or S; and Y is a direct link, -CH2-, -(CH2)2- or -CH2O-; or a pharmaceutically acceptable salt thereof. The compounds are muscarinic receptor antagonists useful in the treatment of, e.g., irritable bowel syndrome and urinary incontinence. The compounds are also useful as cognition enhancers.

L'invention concerne un composé de la formule (I), ainsi que des sels de ce composé, acceptables sur le plan pharmaceutique. Dans cette formule, R<1> est un C1-C6 alkyle, halo-(C1-C6 alkyle), C3-C7 cycloalkyle, C2-C6 alcynyle, hydroxy-(C2-C6 alcynyle), (C1-C4 alcoxy)-(C2-C6 alcynyle), aryle, aryl-(C1-C4 alkyle), hétéroaryle ou hétéroaryle-(C1-C4 alkyle); R<2> est H ou C1-C4 alkyle; R<3> est aryle, hétéroaryle, 2,3-dihydrobenzofuranyle ou C4-C7 cycloalkyle; X est O ou S; et Y est une liaison directe, -CH2-, -(CH2)2- ou -CH2O-. Ces composés sont des antagonistes des récepteurs muscariniques et ils sont utiles, par exemple, pour le traitement du syndrome du côlon irritable et l'incontinence urinaire. Ils sont également utiles comme améliorants cognitifs.

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