Isoquinolinone derivatives

C - Chemistry – Metallurgy – 07 – D

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C07D 401/06 (2006.01) A61K 31/47 (2006.01)

Patent

CA 2054091

ABSTRACT A NOVEL ISOQUINOLINONE DERIVATIVE Isoquinolinone derivatives of the formula: Image (I) wherein R1 is hydrogen, halogen C1-4 alkyl, C1-4 alkoxy or a group of formula: -NR4R5 wherein R4 is hydrogen, C1-4 alkyl or C2-4 alkanoyl and R5 is hydrogen, C1-4 alkyl. or benzyl; R2 is hydrogen or C1-4 alkyl; R3 is hydrogen or C1-4 alkyl; 1 is 1, 2, 3 or 4; m is 1 or 2; n is 1 or 2 and ? is a single bond or double bond and non-toxic acid addition salts thereof and hydrates thereof possess an antagonistic activity against 5-HT3 receptor, and are useful for the prevention and/or treatment of diseases induced when 5-HT acts on 5-HT3 receptors (especially vomiting induced by the administration of an anti-cancer agent).

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