C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 487/04 (2006.01) A61K 31/505 (2006.01)
Patent
CA 2053626
ABSTRACT HETEROCYCLIC COMPOUNDS This invention concerns novel heterocyclic compounds of formula I (and pharmaceutically-acceptable salts thereof): Image I wherein: R1 is hydrogen, (1-8C)alkyl or phenyl(1-4C)alkyl; R2 is (1-6C)alkyl, phenyl(1-4C)alkyl, (3-6C)cycloalkyl, (3-6C)cycloalkyl(1-4C)alkyl or phenyl; R3 is hydrogen, (1-6C)alkyl, phenyl(1-4C)alkyl, (3-6C)cycloalkyl, (3-6C)cycloalkyl(1-4C)alkyl, phenyl or (3-6C)alkenyl; R4 and R5 are independently selected from hydrogen and (1-6C)alkyl; and wherein the phenyl ring and/or one or more of said phenyl or benzene moieties may optionally be unsubstituted or substituted by one or more substituents independently selected from halogeno, (1-4C)alkyl, (3-6C)alkenyl, (1-4C)alkoxy, cyano, trifluoromethyl, nitro, carboxy, (1-4C)alkylamino, dialkylamino of up to six carbon atoms, (1-4C)alkylthio, (1-4C)alkylsulphinyl, (1-4C)alkylsulphonyl and (1-4C)alkylsulphonyl and (1-4C)alkylenedioxy; but excluding the compound in which R1, R3, R4 and R5 are each methyl, the phenyl ring is unsubstituted and R2 is ethyl, and its pharmaceutically-acceptable salt. The compound of formula I (and pharmaceutically-acceptable salts thereof) possess beneficial effects on the cardiovascular system, and in particular beneficial effects modulated via the sino-atrial node. Also included are processes for the manufacture of compounds of the formula I (or a pharmaceutically-acceptable salt), and pharmaceutical compositions.
Imperial Chemical Industries Plc
Smart & Biggar
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