Glaxo Group Limited

Allen & Hansburys Limited

Michael Martin-Smith

John Bradshaw

John W Clitherow

Barry J Price

Duncan B Judd

John W MacKinnon

Roger Hayes

Linda Carey

David E Bays

Philip Blatcher

John W Mackinnon

Compounds of the general formula: ##STR1## and physiologically acceptable salts, and hydrates, N-oxides and bioprecursors of such compounds and such salts in which

Pharmacologically active aminoalkylphenyl compounds and their use

The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which the variables are as defined in the specification. The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists. Also disclosed are intermediates in the preparation of the compounds of the formula (I).

3-[3-[1-piperidinylmethyl]phenoxy]propanamine

The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, which show pharmacological activity as selective histamine H.sub.2 -antagonists.

Triazoleamine derivatives having histamine H.sub.2 -antagonist properties

Compounds of the formula (I) ##STR1## in which R.sub.1 and R.sub.2 each may represent hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, or alkyl, substituted by hydroxy, C.sub.1-3 alkoxy, amino, C.sub.1-3 alkylamino or di-C.sub.1-3 alkylamino or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form an alicyclic heterocyclic ring which may be unsubstituted or may be substituted by one or more C.sub.1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom are described.

Pyrimidone derivatives

The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which the substituents are defined later. The compounds show pharmacological activity as selective histamine H.sub.2 -antagonists.

1,2,4-Triazole-3-amine and 1,2,4 triazole-3,5-diamine compounds and

The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which

1H-1,2,4-Triazole-3,5-diamine derivatives and use as selective histamine

The invention provides compounds of general formula ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which

Amine derivatives

Triazole acylamines, pharmaceutical compositions thereof and method of

The invention relates to compounds of the formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which

1,2,4-Triazole-3,5-diamine derivatives

The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, N-oxides, hydrates and bioprecursors thereof, in which Y represents .dbd.O, .dbd.S, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 represents hydrogen, nitro, cyano, lower alkyl, aryl, lower alkylsulphonyl or arylsulphonyl; R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen lower alkyl, cycloalkyl, lower alkenyl, aralkyl, hydroxy, lower trifluoroalkyl, lower alkyl substituted by hydroxy, lower alkoxy, amine, lower alkylamino or dialkylamino, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring which may contain other heteroatoms or the group ##STR2## where R.sub.4 represents hydrogen or lower alkyl; Q represents a furan or thiophen ring in which incorporation into the rest of the molecule is through bonds at the 2- and 5-positions, or 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; X represents --CH.sub.2 --, --O-- or --S--; n represents zero, 1 or 2; m represents 2, 3 or 4; Alk represents a straight chain alkylene group of 1 to 3 carbon atoms; (except that n is not zero when X is oxygen and Q is a furan or thiophen ring system) q represents 2, 3 or 4 or can additionally represent zero or 1 when E is a --CH.sub.2 --group; p represents zero, 1 or 2; E represents --CH.sub.2 --, --O-- or --S--; and Z represents a monocyclic 5 or 6 membered carbocyclic or heterocyclic aromatic ring which may be optionally substituted by one or more groups or Z represents ##STR3## where Q' represents any of the rings defined for Q; Alk' represents any of the groups defined for Alk; and R.sub.5 and R.sub.6, which may be the same or different, each represent any of the groups defined for R.sub.1 and R.sub.2 ; (except that p is not zero when E is oxygen and Q' or Z is a furan or thiophen ring system) The compounds of formula (I) show pharmacological activity as selective histamine H.sub.2 -antagonists.

Aminoalkylthiophene derivatives as histamine H.sub.2 -antagonists

The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, N-oxides, hydrates and bioprecursors thereof, in which Y represents .dbd.O, .dbd.S, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 represents hydrogen, nitro, cyano, lower alkyl, aryl, lower alkylsulphonyl or arylsulphonyl; R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen lower alkyl, cycloalkyl, lower alkenyl, aralkyl, hydroxy, lower trifluoroalkyl, lower alkyl substituted by hydroxy, lower alkoxy, amine, lower alkylamino or dialkylamino, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring which may contain other heteroatoms or the group ##STR2## where R.sub.4 represents hydrogen or lower alkyl;

Amine derivatives and pharmaceutical compositions containing them

The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, N-oxides, hydrates and bioprecursors thereof, in which

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Ware, United Kingdom

Michael Martin-Smith