Glaxo Group Limited

Allen Hanburys Limited

Allen & Hansbury, Limited

Barry J Price

John Bradshaw

John W Clitherow

Michael Martin-Smith

Duncan B Judd

Roger Hayes

John W MacKinnon

Linda Carey

Ian H Coates

David E Bays

David C Humber

George B Ewan

James A Bell

William L Mitchell

Alexander W Oxford

Peter C North

Michael D Dowle

Philip Blatcher

John W Mackinnon

Colin Frederick Webb

William D Ollis

The invention relates to compounds of the general formula (I): ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 ;

Tricyclic ketones useful as HT.sub.3 -receptor antagonists

The invention provides potent and selective antagonists of 5-HT at 5-HT.sub.3 receptors which are tricyclic lactams of the formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl, phenylC.sub.1-3 alkyl, --CO.sub.2 R.sup.5, --COR.sup.5, --CONR.sup.5 R.sup.6 or --SO.sub.2 R.sup.5 ;

Lactam derivatives

The invention relates to compounds of the general formula (I): ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and the various substituents are defined hereinbelow. The compounds are potent and selective antagonists of the effect of 5-HT at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety, and nausea and vomiting.

Tetrahydro-imidazolylmethylcarbazolones and analogs thereof for treating

The invention provides compounds of the general formula ##STR1## and physiologically acceptable salts and hydrates thereof, in which one of R.sub.1 and R.sub.2 represents hydrogen, halogen or a C.sub.1-4 alkyl group which may be optionally substituted by hydroxy or C.sub.1-4 alkoxy, and the other represents the group R.sub.4 R.sub.5 NAlk-- in which Alk represents a straight or branched alkylene chain of 1 to 6 carbon atoms;

Heterocyclic derivatives, processes for the use thereof and

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

Compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof have been found to show pharmacological activity as selective histamine H.sub.2 -antagonists. The substituents in the compounds of formula (I) are defined in the main body of the disclosure.

1,2,4-Triazole-3-amines and their pharmaceutical use

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 the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which

Heterocyclic derivatives

The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, hydrates and bioprecursors thereof, in which one of R.sub.1 and R.sub.2 represents hydrogen, halogen or a C.sub.1-4 alkyl group which may be optionally substituted by hydroxy or C.sub.1-4 alkoxy, and the other represents the group R.sub.4 R.sub.5 NAlk-- in which R.sub.4 represents hydrogen, C.sub.1-10 alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, heteroaralkyl, trifluoroalkyl, or alkyl substituted by hydroxy, alkoxy, amino, alkylamino, dialkylamino or cycloalkyl, and R.sub.5 represents hydrogen or a C.sub.1-4 alkyl group or R.sub.4 and R.sub.5 may, 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 C.sub.1-3 alkyl groups or a hydroxy group and/or may contain another heteroatom selected from oxygen and sulphur;

Thiophene derivatives and their pharmaceutical compositions and method

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

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Hertford, United Kingdom

Barry J Price