Condensed diazepinones, processes for preparing them and...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/55 (2006.01) C07D 243/38 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 487/04 (2006.01) C07D 495/04 (2006.01)

Patent

CA 1320197

Abstract There are descried new compounds of formula (I) Image (wherein B represents any one of the groups Image (S) (T) (U)'(V) (W); I D represents any one of the groups Image (i) (ii) (iii) Image and Image (iv) (v); X1 and X2 each represents a =CH- group or, if B represents a group S, U or W, either or both of X1 and X2 may also represent a nitrogen atom; A1 represents a straight-chained or branched saturated C2-7 alkylene group; A2 represents a straight-chained or branched saturated C1-5 alkylene group or, if in the 3-position relative to the nitrogen of the saturated heterocyclic ring, A2 may also represent a single bond; Z represent a single bond, or an oxygen or sulphur atom, or a methylene or 1,2-ethylene group R represents a hydrogen atom or a methyl group; R1 represents a branched or unbranched C1-4 alkyl group, and R2 represents a branched or unbranched C1-7 alkyl group optionally substituted by a hydroxy group at its second to seventh carbon atoms, or a cyclo- C3-7-alkyl or cyclo-C3-7-alkylmethyl group, optionally substituted on the cycloalkyl ring by a hydroxy group, or R1 and R2, together with the nitrogen atom between them, form a 4- to 7-membered saturated, monocyclic, heterocyclic ring optionally including in the ring an oxygen atom or Image group; R3 represents a C1-4 alkyl group or a chlorine or hydrogen atom R4 represents a hydrogen atom or a methyl group; R5 and R6 each represents a hydrogen, fluorine, chlorine or bromine atom or a C1-4 alkyl group; R7 represents a hydrogen or chlorine atom or a methyl group; R8 represents a hydrogen atom or a C1-4 alkyl group; R9 represents a hydrogen or halogen atom or a C1-4 alkyl group; R10 represents a hydrogen atom or a methyl group; and R12 represents a branched or unbranched C1-6 alkyl group; with the proviso that if B represents the group T and R7 represents a hydrogen atom, then R3 represents other than a chlorine atom and Z represents other than a sulphur atom), and stereoisomers and salts thereof. The compounds and their salts may be used as vagal pacemakers for the treatment of bradycardia and bradyarrhythmia.

554792

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