Substituted pyrido (2,3-b)(1,4)benzodiazepin-6-ones,...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/55 (2006.01)

Patent

CA 1311752

Abstract Substituted pyrido[2,3-b][1,4]benzodiazepin- 6-ones The invention relates to a new compound of formula I Image (I) (wherein R1 represents a C1-4 alkyl group, or a chlorine or hydrogen atom; R2 represents a hydrogen atom or a methyl group; R3 and R4 each represent a hydrogen, fluorine, chlorine or bromine atom, or a C1-4 alkyl group, with the proviso that at least one of the radicals R1, R2, R3 and R4 is other than hydrogen; R5 and R6, which are the same or different, each represents a C1-6 alkyl group, or R5 and R6, together with the nitrogen atom between them, represent a 4- to 7-membered saturated, monocyclic, heteroaliphatic ring optionally incorporating within the ring an oxygen atom or an -?-CH3 group; Z represents a single bond, an oxygen atom, or a methylene or 1,2-ethylene group; and A represents a methylene group attached at the 2- or 3-position of the heteroaliphatic ring or a single bond to the 3-position of the heteroaliphatic ring), or an acid addition salt thereof. The new compounds have favourable effects on the heart rate and, in view of the absence of effects inhibiting gastric acid secretion and inhibiting salivation and of mydriatic effects, as well as excellent absorption, are suitable as vagal pacemakers for the treatment of bradycardias and bradyarrhythmias in human beings or animals.

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