Heterocyclic derivatives as histamine h.sub.2- antagonists

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 257/06 (2006.01) C07C 279/28 (2006.01) C07D 239/46 (2006.01) C07D 249/14 (2006.01) C07D 295/096 (2006.01) C07D 401/12 (2006.01) C07D 413/12 (2006.01) C07D 471/04 (2006.01)

Patent

CA 1192545

ABSTRACT The invention relates to compounds of the general formula (I) Image and physiologically acceptable salts, hydrates and bioprecursors thereof, in which R1 represents hydrogen, C1-14 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl, heteroaralkyl or alkyl substituted by cycloalkyl, hydroxy, alkoxy, amino, alkylamino or dialkylamino; and R2 represents hydrogen or C1-4 alkyl group; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 to 10 membered ring which may be saturated or may contain at least one double bond, may be unsubstituted or may be substituted by one or more C1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom selected from oxygen or sulphur; Alk represents a straight or branched alkylene chain of 1 to 3 carbon atoms; Q represents a benzene ring in which incorporation into the rest of the molecule is through bonds at the 1- and 3- or 1- and 4- positions; R5 represents hydrogen or acyl; n and m, which may be the same or different; are each 1 or 2; and R3 represents hydrogen, alkyl, alkenyl, aralky ? hydroxy C2-6 alkyl, alkoxy C2-6 alkyl or C1-4 alkanoyl- oxy C2-6 alkyl The compounds show pharmacological activity as selective histamine H2-antagonists.

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