C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 471/08 (2006.01) A61K 31/495 (2006.01) A61K 31/53 (2006.01)
Patent
CA 2088454
The invention relates to diazabicyclo derivatives of formula (I) and pharmaceutically acceptable salts thereof: Image wherein R1 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, alkoxyalkyl, oxoalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, acyl, dialkylaminoalkyl, hydroxyalkyl, haloalkyl, cyanoalkyl, heterocycloalkyl, aryl, heteroarylalkyl or arylalkyl; R2 is hydrogen or alkyl; R3 and R4 are the same or different and each represents hydrogen, alkyl, alkenyl, acyl, alkoxyalkyl or arylalkyl, wherein the aryl moiety is optionally substituted by alkoxy, nitro, alkyl, amino or halo; with the proviso that: when R2 is hydrogen and both R3 and R4 are methyl, R1 does not represent hydrogen, C1- C10alkyl, unsubstituted benzyl or dimethylaminoethyl, when R2 is hydrogen and both R3 and R4 are C1-C4alkyl, R1 does not represent hydrogen, C1-C6alkyl or benzyl, and when R2 is hydrogen, R3 is hydrogen or methyl and R4 is C1- C10alkyl, phenyl or naphthyl (C1-C4) alkyl, R1 does not represent hydrogen or C1-C10alkyl. The compounds of the invention have 5-HT3 receptor antagonist activity.
Arai Takeo
Fukutomi Ruta
Hagihara Koichiro
Hayakawa Toru
Kikuchi Haruhiko
Nisshin Flour Milling Co. Ltd.
Nisshin Seifun Group Inc.
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
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