Beecham Group Plc

Smithkline Beecham Corporation

Other

Derek R Buckle

Harry Smith

Barrie C Cantello

David Glynn Smith

David G Smith

Andrew J Williams

Frank Peter Doyle

Barry Christian Cantello

Frederick Cassidy

Stuart Bailey

Andrew Faller

Ruth Judik Mayer

John M Tedder

Stephen T Carpenter

Gary Christie

Ivan L Pinto

Ashley E Fenwick

Ariane Elizabeth Marolewski

Inhibitors of the Production of s-CD23 and the secretion of TNF are provided.

Inhibitors of the production of S-CD23 and the secretion of TNF

The present invention is to the discovery of a novel CD23 processing enzyme which is of importance in the human immune response and regulation of IgE production, and is a protein expressed on the surface of a variety of cells.

CD23 processing enzyme preparation

A method for the treatment and/or prophylaxis of disorders associated with pulmonary hypertension and/or disorders associated with right heart failure, in mammals, such as humans, which method comprises administering to the mammal in need of such treatment and/or prophylaxis an effective and/or prophylactic amount of a vasodilator selected from the group consisting of ganglion blockers, sympathetic nerve blockers, and direct vasodilators; or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof.

Inhalational treatment of pulmonary hypertension and related conditions

Novel Compounds A compound of formula (I): ##STR1## where the substituents are defined later in the specification. The compounds are useful as muscle relaxants and as such have a number of pharmaceutical uses.

Benzopyranols

##STR1## A compound of formula (I) or, if appropriate, a pharmaceutically acceptable salt thereof, wherein R.sup.1 and R.sup.2 each independently represent an alkyl group or a moiety of formula (a): --(CH.sub.2).sub.m --A, wherein m represents zero or an integer 1, 2 or 3 and A represents a substituted or unsubstituted cyclic hydrocarbon radical; R.sup.3 represents hydrogen, NO.sub.2 or a halogen atom, an alkoxy group or a group of formula NR.sup.s R.sup.t wherein R.sup.s and R.sup.t each independently represent hydrogen or alkyl or R.sup.s and R.sup.t together with the nitrogen to which they are attached form a phthalimido group, the phthalimido group being substituted or unsubstituted in the phenylene moiety or R.sup.3 represents a moiety of formula (b), wherein R.sup.5 represents substituted or unsubstituted alkyl or a substituted or unsubstituted aryl group; and R.sup.6 represents hydrogen or a group SO.sub.2 R.sup.7 wherein R.sup.7 represents substituted or unsubstituted alkyl, a substituted or unsubstituted aryl group; R.sup.4 represents SO.sub.2 R.sup.8, wherein R.sup. 8 represents substituted or unsubstituted alkyl or a substituted or unsubstituted aryl group, or, when R.sup.3 represents a moiety of the above-defined formula (b), then R.sup.4 represents hydrogen or a substituted or unsubstituted alkyl group or a benzyl group substituted or unsubstituted in the phenyl ring a process for preparing such a compound, a composition comprising such a compound and the use of such a compound and composition in medicine.

Xanthine derivatives

A compound of formula (IA) in the form of a pharmaceutically acceptable microfine powder is disclosed. ##STR1##

Compound and treatment

A method for the treatment and/or prophylaxis of disorders associated with pulmonary hypertension and/or disorders associated with right heart failure, in mammals, such as humans, which method comprises administering to the mammal in need of such treatment and/or prophylaxis an effective and/or prophylactic amount of pinacidil; or a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof.

Novel treatment

A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sub.1 is a hydrogen atom or a C.sub.1-6 alkyl group, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are selected from hydrogen, hydroxyl, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy and C.sub.1-4 alkanoyl; G is a hydrogen atom or a hydroxyl group, and m and n are independently integers of from 1 to 3, with the proviso that when G is a hydroxyl grup, m or n is 1; is useful in the treatment of asthma.

Dioxonaphthotriazoles having antiallergic activity

Compounds of formula (I): ##STR1## in which R.sub.1 is hydrogen or C.sub.1-6 alkyl;

Certain pyridyl, thienyl or furyl propenoic acids or esters having

A compound of formula (I): ##STR1## or a salt, ester or amide thereof, in which

Novel compounds

A compound of formula (I): ##STR1## or a salt thereof, in which Y is a group--O(CH.sub.2).sub.m CH&lt;, --(CH.sub.2).sub.m CH&lt;, or --CH.dbd.C&lt; where

Arachidonic acid analogues, processes for their preparation and their

A process for preparing a compound of formula (I) ##STR1## wherein X phenyl optionally substituted by one halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy; or pyridyl; R.sup.1 is hydrogen or C.sub.1-6 alkyl; and n is an integer of from 1 to 6; which process comprises, cyclizing a compound of formula (II): ##STR2## wherein X, R.sup.1 and n are as defined in relation to formula (I); Y is an hydroxy or an acid activating group and R.sup.x is hydrogen or an N- protecting group and thereafter if desired carrying out one or more of the following steps: (i) removing any protecting group R.sup.x, (ii) preparing a salt of the compound of formula (I).

Process for preparing benzopyrano (2,3-d) triazoles

Compounds of the formula (I): ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is hydrogen or C.sub.1-6 alkyl, and R.sub.2 is hydroxy, C.sub.1-4 alkylsulphonyloxy or p-toluenesulphonyloxy are useful for the prophylaxis and treatment of diseases due to allergic response in mammals. Processes for their preparation are described.

Substituted benzopyranotriazoles and antiallergic use

A compound of the formula (I): ##STR1## wherein R.sub.1 is hydrogen or C.sub.1-6 alkyl;

Pharmacologically active benzopyranotriazole compounds

Compounds of the formula (I), or pharmaceutically acceptable salts thereof ##STR1## wherein X is phenyl, optionally substituted by one halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy; or pyridyl; R.sub.1 is hydrogen or C.sub.1-6 alkyl; and n is 1 to 6, pharmaceutical compositions containing them and a process for their preparation. These compounds are useful in the prophylaxis or treatment of diseases due to a histamine-mediated allergic response.

Growing community of inventors

Redhill, United Kingdom

Derek R Buckle