Astrazeneca Ab

Zeneca Limited

Astra Zeneca U.k. Limited

Andrew Stocker

John Preston

Paul Robert Owen Whittamore

Michael J Smithers

Alan Wellington Faull

James Stewart Scott

Martin John Packer

John Wall Rayner

Colette Marie Mayo

Andrew David Morley

Paul Turner

Alan Martin Birch

Paul Schofield

Paul Michael Murray

Gary Peter Tomkinson

Michael Butters

Jeremy Stephen Parker

Paul Ro Whittamore

Nowak Thorsten

A compound of formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11&#x3b2;HSD1, processes for making them and pharmaceutical compositions comprising them are also described.

Pyrazole derivatives as 11-beta-HSD1 inhibitors

New crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]benzoic acid; their use in the inhibition of 11&#x3b2;HSD1, processes for making them and pharmaceutical compositions comprising them are also described.

Crystalline forms of 4-[4-(2-adamantylcarbamoyl)-5-tert-butyl-pyrazol-1-yl]Benzoic acid 471

Chemical compounds

A process for preparing a compound of formula (I) where Rand Rare as defined in the specification; and Ris hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R, Rand Rare as defined in relation to formula (I), and Ris nitrogen-protecting group, and removing the group R&#x2014;, and thereafter if desired or necessary, removing any protecting group Rto obtain the corresponding carboxylic acid. Novel intermediates and the use of the products in the preparation of pharmaceutical compounds is also described and claimed. 

Process and intermediates for the preparation of the thienopyrrole derivatives

Heterocyclic amides of formula (1) and pharmaceutically acceptable salts or pro-drugs thereof wherein variable groups are as described herein; which possess glycogen phosphorylase inhibitory activity and accordingly have value in the treatment of disease states associated with increased glycogen phosphorylase activity are described. Processes for the manufacture of said heterocyclic amide derivatives and pharmaceutical compositions containing them are also described.

Indole-amid derivatives which possess glycogen phosphorylase inhibitory activity

Novel Process and Intermediates. A process for preparing a compound of formula (I) where Rand Rare as defined in the specification; and Ris hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where Rand Rand Rare as defined in relation to formula (I), and Ris nitrogen protecting group, and removing the group R, and thereafter if desired, removing any protecting group R. Novel intermediates and the use of these in the formation of pharmaceutical compounds is also described and claimed 

Process and intermediates for the preparation of thienopyrrole derivatives

Heterocyclic amides of formula (1) wherein:

Heterocyclic amide derivatives as inhibitors of glycogen phosphorylase

Compounds of formula (I), wherein Gis CH or N; Gis CH or N; Ris a variety of optional substituents; Lis (1-4C)alkylene; Tis CH or N; Rand Rare independently hydrogen or (1-4C)alkyl or are joined to form a ring; Xand Xrepresent various linking groups; Ar is phenylene or certain heteroaryl rings and Q represents a variety of aromatic or heterocyclic rings systems, and pharmaceutically acceptable salts thereof are described as useful antithrombotic and anticoagulant agents, and are selective Factor Xa inhibitors. Processes for their preparation and pharmaceutical compositions containing them are also described.

Aminoheterocyclic derivatives as antithrombotic or anticoagulant agents

Heterocyclic amide derivatives as inhibitors of glycogen phoshorylase

The invention relates to heterocyclic derivatives of formula (I)A&#x2014;B&#x2014;X&#x2014;T(R)&#x2014;L&#x2014;T(R)&#x2014;X&#x2014;Q&#x2003;&#x2003;(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

(Hetero) aryl-sulfonamide derivatives, their preparation and their use as factor XA inhibitors

The invention relates to heterocyclic derivatives of formula (I) and (Ia), 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 of the formula (I): A&mdash;B&mdash;X,&mdash;T,(R,)&mdash;L,&mdash;T,(R,)&mdash;X,&mdash;Q or pharmaceutically acceptable salts thereof, which possess antithrombotic and anticoagulant properties due to their inhibition of Factor Xa 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.

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Macclesfield, United Kingdom

Andrew Stocker