Astrazeneca Ab

Zeneca Limited

Thorsten Nowak

Roger John Butlin

Jeremy Nicholas Burrows

Michael Howard Block

Janet Elizabeth Pease

David Stephen Clarke

Andrew Peter Thomas

Peter Warner

Roger James

Alleyn Thomas Plowright

William McCoull

Alan Martin Birch

Craig Samuel Donald

Suzanne Saxon Bowker

Paul Ro Whittamore

The present invention relates to compounds that inhibit HSP90 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as for treatment of solid tumors.

5,6,7,8-tetrahydropteridine derivatives as HSP90 inhibitors

Compounds of formula (I), and salts and pro-drugs thereof: Formula (I) wherein for example Ris optionally substituted aryl or heteroaryl; Y is a linking group selected from, for example, a direct bond, and a (substituted) alkyl chain; Ris an optionally substituted aryl, an optionally substituted cycloalkyl or an optionally substituted heterocyclic group; are described. Processes to make such compounds and their use as DGAT inhibitors, for example in the treatment of obesity, are also described. 

Oxadiazole derivative as DGAT inhibitors

A compound of Formula (I); wherein the substituents are as defined in the text for use in modulating insulin-like growth factor 1 receptor activity in a warm blooded animal such as man. 

4-(pyrazol-3-ylamino) pyrimidine derivatives for use in the treatment of cancer

The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; Ris an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; Rand Rare as defined within; Ris hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are also described

Use of compounds for the elevation of pyruvate dehydrogenase activity

Amides as inhibitors for pyruvate dehydrogenase

A compound of formula (I) wherein: n is 1 or 2; R is chloro, fluoro, bromo, methyl or methoxy; R is as defined within; R is as defined within; and R is hydrogen or fluoro; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.

Substituted N-phenyl 2-hydroxy-2-methyl-3,3,3-trifluoropropanamide derivatives which elevate pyruvate dehydrogenase activity

Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N-oxide; R and R are substituents as defined within; R and R are defined within and are alkyl or halo alkyl or together form a halocycloalkyl ring; R is a substituent as defined within; Y&mdash;Z is a linking group as defined within; are useful in the production of a elevation of PDH activity in a warm-blooded animal such as a human being. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are described.

Benzenesulfonamide-derivatives and their use as medicaments

A compound of formula (I) wherein: R , R , R , R , R , R and R are as defined within; or a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof is described. The use of compounds of formula (I) in the production of an elevation of PDH activity in a warm-blooded animal such as a human being are also described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are detailed.

Chemical compounds

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).

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Macclesfield, United Kingdom

Thorsten Nowak