Astrazeneca Ab

Zeneca Limited

Imperial Chemical Industries Limited

Roger James

Robert Hugh Bradbury

Rodney Brian Hargreaves

Peter William Rodney Caulkett

Craig Johnstone

Roger John Butlin

Clifford David Jones

Michael Howard Block

Suzanne Saxon Bowker

Scott Boyd

John B Glen

Darren McKerrecher

Rodney B Hargreaves

Peter Warner

Geraint Jones

Darren Mckerrecher

Thorsten Nowak

Stuart Eric Pearson

Gordon Stuart Currie

Anthony Michael Slater

Paul J Phillips

Rolf Peter Walker

Barry Raymond Hayter

Peter Wr Caulkett

Peter Grahame Ballard

The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R, R, R, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).

Compounds effecting glucokinase

The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R, R, R, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes.  The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).

The invention relates to novel compounds of Formula (I) or a salt, solvate or prodrug thereof, wherein A, R, R, R, n and m are described in the specification, useful in the treatment of  a disease or condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to methods for preparing compounds of Formula (I) and their use as medicaments in the treatment of diseases mediated by glucokinase.

Vinyl phenyl derivatives as GLK activators

The invention relates to heterocyclic derivatives of formula (I), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.

Heterocyclic derivatives which inhibit factor Xa

The invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and more accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, formula (I).

The invention concerns pharmaceutically useful compounds of the formula I, in which A,, A,, A,, A,, B,, m, Ar, W, X, Y, Z and R,have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

Substituted pyrazin-2-yl-sulphonamide (-3-pyridyl) compounds and uses thereof

The invention concerns pharmaceutically useful compounds of the formula I, in which A.sup.1, A.sup.2, A.sup.3, A.sup.4, B.sup.1, m, Ar, W, X, Y, Z and R.sup.1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.

Substituted pyrazin-2-yl-sulphonamide-(3-pyridyl) compounds and uses

Heterocyclic compounds

The invention concerns pharmaceutically useful compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, n, m and Het have any of the meanings defined herein, and their pharmaceutically-acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processess for the manufacture of the novel compounds and the use of the compounds in medical treatment.

N-heterocyclic sulfonamides having endothelin receptor activity

Compounds of the formula I: ##STR1## wherein: X is O, S or NH; n is O or an integer of from 1 to 3; R.sup.1 is hydrogen, (1-6C)alkyl, or (1-4C)alkanoyl; R.sup.2 is CH.sub.2 R.sup.3, NHR.sup.4, SO.sub.2 NR.sup.5 YNR.sup.6 R.sup.7 or R.sup.8, in which R.sup.3 is hydroxy, (1-4C)alkoxy or (1-4C)alkylsulphonyl; R.sup.4 is (1-4C)alkylsulphonyl, (1-4C)haloalkylsulphonyl, formyl, carbamoyl or 2,6-dichloro-4-(2-(1,1-dimethylethyl)amino-1-hydroxyethyl)phenyl; R.sup.5 is hydrogen or (1-4C)alkyl; Y is CO or (1-6C)alkylene; R.sup.6 and R.sup.7 are independently (1-4C)alkyl, or R.sup.6 is hydrogen and R.sup.7 is (1-4C)alkyl, (1-4C)haloalkyl, phenyl(1-4C)alkyl or, when Y is (1-6C)alkylene, is (1-4C)alkylaminocarbonyl or (5-6C)cycloalkylaminocarbonyl; and R.sup.8 is a sugar residue of formula II in which R.sup.9 represents hydrogen, methyl or hydroxymethyl and m is 2 or 3; A is N or CT in which T is hydrogen or (1-4C)alkyl; or a pharmaceutically acceptable salt thereof, processes for their manufacture and pharmaceutical compounds containing them. The compounds are useful as adenosine antagonists.

2-furyl-triazalo [1,5-a]-[1,3,5]triazines and pyrazolo

Sterile pharmaceutical compositions for parenteral administration containing the compound 2,6-diisopropylphenol, and a method for producing anaesthesia in a warm-blooded animal by parenteral administration of said compound.

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Cheshire, United Kingdom

Roger James