PROCESS FOR PREPARING HETEROCYCLIC DERIVATIVES

摘要

of formula (I) and their bioprecursors, hydrates and salts are new. (where R1 and R2 are each H, 1-10C alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, trifluoroalkyl or alkyl substd. by a hydroxy, alkoxy, amino, alkylamino, dialkylamino or cycloalkyl or together with the N atom form a 5-10 membered, aliphatic heterocyclic gp. which may be satd. may contain >=1 double bond and may be substd. by >=1 alkyl gp. or a hydroxy gp. and/or may contain a further heteroatom, Alk is opt. branched 1-6C alkylene, Q is a furan or thiophene ring joined to the remaining molecule at positions 2 and 5 or a benzene ring joined at positions 1, 3 or 1, 4, the furan ring may be substd. by a gp. R7 next to the R1R2N-Alk-gp. R7 is halo or 1-4C alkyl which may be substd. by hydroxy or 1-4 C alkoxy, X is -CH2-, -NR6-, -O- or -S-, R2 is H or methyl, n = 0, 1 or 2, m = 2,3, or 4, R3 is H, alkyl, alkenyl aralkyl, >=2C hydroxyalkyl, alkoxyalkyl or aryl, R4 and R5 are ach H, alkyl nopt. substd. by hydroxy or 1-3C alkoxy) alkenyl, aralkyl or heteroaralkyl or together with the N atom form a 5-7 membered satd. heterocyclic ring (which may contain a further heteroatom or -NR6-), or =CR8R9, R8 is alkyl or heteroaryl, and R9 is H or alkyl). These H2 histamine receptor blockers are used to treat gastric acid hypersecretion (e.g. treatment of gastric or peptic ulcers or hypersecretion during surgery) and allergic and inflammatory states where histamine is the mediator. The cpds. may bea dministered, opt. with other active cpds. e.g. H1-receptor antagonists, by buccal, topical, parenteral, rectal or pref. oral routes.