Astrazeneca Ab

Jeremy Nicholas Burrows

Roger John Butlin

Thorsten Nowak

Michael Howard Block

Janet Elizabeth Pease

John Graham Cumming

David Stephen Clarke

Thomas McInally

Paul Ro Whittamore

Ulrika Yngve

Per I Arvidsson

Erica Tjerneld

Imidazole substituted pyrimidines and pharmaceutically acceptable salts thereof; pharmaceutical formulations containing such pyrimidines; the use of such compounds in therapy; the use of such compounds for the treatment of conditions associated with glycogen synthase kinase-3 related disorders, such as Alzheimer's disease, as well as methods of treatment of such disorders comprising administering to subjects in need of such treatment therapeutically effective amounts of such compounds.

Imidazole substituted pyrimidines

The invention concerns compounds of formula (I), wherein the variables are defined herein; processes for preparing them, compositions comprising them and their use in modulating CCR5 receptor activity.

Ccr5 modulators benzimidazoles or benzotriazoles

The invention provides a compound of formula (I): wherein R, R, R, R, R, R, R, and Rare as defined; or a pharmaceutically acceptable salt thereof or a solvate thereof; compositions containing these compounds, processes for preparing them and their use as modulators of chemokine activity (especially CCR5 activity)

Piperidine derivatives as modulators of chemokine receptors

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.

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Macclesfield, United Kingdom

Jeremy Nicholas Burrows