5,6,7,8-tetrahydro-4h-isoxazolo [4,5-c] azepine derivatives

C - Chemistry – Metallurgy – 07 – D

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167/209, 260/241

C07D 498/04 (2006.01) A61K 31/55 (2006.01)

Patent

CA 1319688

ABSTRACT OF THE INVENTION The present invention relates to novel compounds of the following formula: I Image wherein Rl is alkyl, alkenyl, alkynyl, branched or unbranched, with 1 - 6 carbonatoms either unsubstituted or optionally substituted with fluoro, hydroxy or phenyl, in which the phenyl group may be substituted with halogen, trifluoro- methyl, lower alkyl, hydroxy or lower alkoxy; R2 is hydrogen or lower alkyl (1-6 C-atoms); R3 and R4 are the same or different, and each represents hydrogen, alkyl (1-6 C-atoms) or cycloalkyl (3-6 C-atoms), or phenyl optionally substituted with halogen, trifluoromethyl, lower alkyl (1-6 C-atoms), hydroxy, or lower alkoxy (1- 6 C-atoms) or phenyl-lower alkyl (7-10 C-atoms), in which the phenyl group may be substituted with halogen, trifluoromethyl, lower alkyl (1-6 C-atoms), hydroxyor lower alkoxy (1-6 C-atoms); as well as individual isomers and pharmaceutically-acceptable acid addition salts thereof. The invention moreover relates to methods for the preparation of the compounds of formula I, to novel intermediates, to pharmaceutical compositions containing same and to methods for the treatment of disorders, caused by malfunction of the acetylcholine (AcCh) or muscarinic system, by administering a non-toxic effective amount of a compound of formula I.

583657

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