Glaxo Group Limited

Smithkline Beecham Corporation

David E Bays

Roger Hayes

Colin F Webb

Alexander W Oxford

Ian H Coates

John W Clitherow

Michael D Dowle

Hazel Joan Dyke

Richard Peter Charles Cousins

John W Mackinnon

John Bradshaw

Peter C North

Colin David Eldred

Philip Blatcher

Linda Carey

Keith Mills

David J Cavalla

Barry J Price

Duncan B Judd

Chuen Chan

Stephen Swanson

Brian Cox

Frank Ellis

Caroline Mary Cook

Martin Pass

Andrew Michael Kenneth Pennell

Joanna Victoria Geden

Brian David Judkins

Eric W Collington

Suzanne Elaine Keeling

William L Mitchell

Michael Martin-Smith

David I Scopes

Alison Judith Redgrave

David George Allen

Caroline Whitworth

Heather Hobbs

Charanjit Bountra

Darko Butina

Andrew Pearce

A method of treating a patient suffering from or susceptible to ischemic heart disease, peripheral vascular disease or stroke or which subject is suffering pain, a CNS disorder or sleep apnea which comprises administering a therapeutically effective amount of an adenosine derivative which is an agonist at the adenosine A1 receptor and which exhibits little or no agonist activity of the A3 receptor. The adenosine derivative has a general formula (I) as follows:

Adenosine derivatives and methods of administration

There are disclosed according to the invention, compounds of formula (I) wherein R , R and R are defined in the specification. Additionally, processes of preparing the compounds of formula (I), formulations containing same, and the administration of said compounds or formulations thereof in the treatment of inflammatory diseases are also disclosed.

2-(purin-9-yl)-tetrahydrofuran-3, 4-diol derivatives

A series of 2-(Purin-9-yl)-tetrahydrofuran-3,4-diol derivatives with broad anti-inflammatory properties which inhibit leukocyte recruitment and activation and which are agonists of the adenosine 2a receptor are described.

2-(purin-9-yl)-Tetrahydrofuran-3,4-diol derivatives

A compound of formula (I) which is an agonist at the adenosine Al receptor, wherein Y, Z, and W represent heteroatoms, and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof for use in therapy.

Adenosine derivatives

Use for GABA agonists for treating emesis

Compounds are disclosed of general formula: ##STR1## wherein R.sup.1 is H, C.sub.1-6 alkyl or C.sub.3-6 alkenyl; R.sup.2 is H, C.sub.1-3 alkyl, C.sub.3-6 alkenyl, aryl, ar(C.sub.1-4)-alkylene, or C.sub.5-7 cycloalkyl;

Indole derivatives

The invention relates to a salt of a basic histamine H.sub.2 -receptor antagonist of formula (I) ##STR1## and a complex of bismuth with a carboxylic acid selected from tartaric acid, citric acid and alkyl citric acids, or a solvate of such a salt, wherein

Carboxylic acid derivatives

The invention provides amide derivatives of the general formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom or a C.sub.1-6 alkyl group; Y represents a group --(CH.sub.2).sub.m --, where m represents 2, 3 or 4 or a group --X(CH.sub.2).sub.p, where p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.5, where R.sup.5 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.2, R.sup.3 and R.sup.4 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; and physiologically acceptable salts and solvates thereof. The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.3 receptors and are useful, for example, in the treatment of psychotic disorders, anxiety and nausea and vomiting.

5,6-dihydro-N-[(imidazol-4(or

The invention relates to tetracyclic ketones of the general formula (I) ##STR1## wherein n represents 1, 2 or 3;

[(Imidazol-4(and 5)-yl)methyl] tetracyclic ketones having 5-HT.sub.3

The invention provides lactam derivatives of the general formula (I) ##STR1## wherein n represents 2 or 3; Im represents an imidazolyl group of the formula: ##STR2## wherein one of the groups represented by R.sup.1, R.sup.2 and R.sup.3 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl- group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group; Y represents a group --(CH.sub.2).sub.m --, wherein m represents 2, 3 or 4; or Y represents a group --X(CH.sub.2).sub.p --, wherein p represents 2 or 3, X represents an oxygen or a sulphur atom or a group NR.sup.4, where R.sup.4 is a C.sub.1-6 alkyl group, and X is attached to the benzene ring moiety of the molecule; and physiologically acceptable salts and solvates thereof. The compounds of formula (I) are potent and selective antagonists of 5-hydroxytryptamine at 5-HT.sub.3 receptors and are useful, for example in the treatment of psychotic disorders, anxiety and nausea and vomiting.

Lactam derivatives

The invention relates to compounds of the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene chain and R.sup.3 is a hydrogen atom; or

Ketone derivatives which are antagonists of 5-HT at 5-HT.sub.3

Compounds are disclosed of formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and are C.sub.1-6 alkyl or C.sub.3-6 alkenyl; or --NR.sub.1 R.sub.2 forms a 5-membered (optionally containing an oxygen atom adjacent to the nitrogen) or a 6-membered ring, which ring optionally contains one unit of unsaturation and which is unsubstituted or substituted by hydroxy, oxo, optionally substituted methylidene, --COR.sub.3 (where R.sub.6 represents C.sub.1-6 alkyl, OR.sub.4 or --NHR.sub.4, and R.sub.4 represents hydrogen, C.sub.1-6 alkyl, aryl, ar(C.sub.1-6)alkyl) or .dbd.NOR.sub.5 (where R.sub.5 represents C.sub.1-6 alkyl);

Morpholine derivatives, pharmaceutical compositions and use

Indole derivatives are disclosed of the formula (I): ##STR1## wherein R.sub.1 represents H, or C.sub.1-6 alkyl or C.sub.3-6 Alkenyl;

5-Aminosulphoryl substituted indole derivatives

Indoles are disclosed of formula (I): ##STR1## wherein R.sub.1 represents R.sub.5 R.sub.6 NCOCH.sub.2 --, R.sub.5 CONH(CH.sub.2).sub.p --,

5-substituted 3-aninoalkyl indoles

Compounds are disclosed of formula (I): ##STR1## wherein R.sub.1 is halogen, a C.sub.1-3 alkoxy, R.sub.6 R.sub.7 NCO(CH.sub.2).sub.p --, R.sub.6 CONH(CH.sub.2).sub.p --, R.sub.6 R.sub.7 NSO.sub.2 (CH.sub.2).sub.p --, or R.sub.8 SO.sub.2 NH(CH.sub.2).sub.p -- (where R.sub.6 and R.sub.7 each represents hydrogen or C.sub.1-3 alkyl, R.sub.8 represents C.sub.1-3 alkyl and p is zero or 1);

Growing community of inventors

Ware, United Kingdom

David E Bays