Astrazeneca Ab

Zeneca Limited

Other

Astra Zeneca U.k. Limited

Zeneca Pharma S. A.

Ucbbiopharma Srl

Craig Johnstone

John Robert Porter

Andrew Peter Thomas

Rikki Peter Alexander

Laurent Francois Andre Hennequin

Daniel Christopher Brookings

Alan Wellington Faull

Elaine Sophie Elizabeth Stokes

Andrew David Morley

Rodney Brian Hargreaves

Peter William Rodney Caulkett

Scott Boyd

David R Brittain

Thomas McInally

Kurt G Pike

Michael S Large

Julien Alistair Brown

Boris Kroeplien

Andrew John Barker

Gareth Morse Davies

Martin Clive Hutchings

James Andrew Johnson

Suzanne Saxon Bowker

Darren McKerrecher

Michael James Waring

James Thomas Reuberson

Matthew Duncan Selby

Jean-Jacques Marcel Lohmann

Roger James

Clifford David Jones

Michael Howard Block

Edward Clayton

Darren Mckerrecher

Stephen Brough

Elizabeth Pearl Jones

Andrew Baxter

Fabien Claude Lecomte

Helen Tracey Horsley

Martin Alexander Lowe

Joanna Rachel Quincey

Jeffrey Philip Poyser

Alleyn Thomas Plowright

Gareth Neil Brace

Anne Marie Foley

Michael Alan Shaw

Ellen Olivia Gallimore

David Griffiths

Philip Jeffrey Poyser

Alexander Heifetz

Laura Jane Gleave

Jonathan Mark Bentley

Zhaoning Zhu

Herve Jean Deboves

Ian Andrew Yule

Craig Adrian Miller

Compounds of formula (I), or salts thereof, which inhibit acetyl CoA (acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein:

1,3,4-oxadiazole derivatives as DGAT1 inhibitors

The invention relates to thiophene carboxamides of formula (I), wherein A, R, R, R, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy. 

Phenyl thiophene carboxamide compounds as inhibitors of the enzyme IKK-2

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 quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; Rrepresents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, Calkyl, Calkoxy, Calkylthio, or &#x2014;NRR(wherein Rand R, which may be the same or different, each represents hydrogen or Calkyl); Rrepresents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; Rrepresents hydroxy, halogeno, Calkyl, Calkoxy, Calkanoyloxy, trifluoromethyl, cyano, amino or nitro; Xrepresents &#x2014;O&#x2014;, &#x2014;CH&#x2014;, &#x2014;S&#x2014;, &#x2014;SO&#x2014;, &#x2014;SO&#x2014;, &#x2014;NRCO&#x2014;, &#x2014;CONR&#x2014;, &#x2014;SONR&#x2014;, &#x2014;NRSO&#x2014; or &#x2014;NR&#x2014; (wherein R, R, R, Rand Reach independently represents hydrogen, Calkyl or CalkoxyCalkyl); Rrepresents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

Quinazoline derivatives and pharmaceutical compositions containing them

Compounds of Formula (I) wherein: Ris hydroxymethyl; Ris selected from &#x2014;C(O)NRR, SONRR, S(O)Rand HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; Ris selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; Ris selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; Ris hydrogen or (1-4C)alkyl; or Rand Rtogether with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro drug or solvate thereof, are described. Their use as GLK activators, pharmaceutical compositions containing them, and processes for their preparation are also described. 

Heteroaryl benzamide derivatives as GLK activators

The invention relates to thiophene carboxamides of formula (I), wherein A, R, R, R, R, Rand X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy. 

Thiophene-carboxamide derivatives and their use as inhibitors of the enzyme IKK-2

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 heteroaromatic carboxamides of formula (I), wherein A, R, Rand X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.

Substituted Thiophene compounds

The invention relates to thiophene carboxanmides of formula (I), wherein A, R, R, R, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy. 

Thiophene carboxamide compounds as inhibitors of enzyme IKK-2

The invention relates to thiophene carboxamides of formula (I), wherein R, R, R, A, n and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy 

Compounds

The invention concerns quinazoline derivatives of the formula I

Quinazoline derivatives

The invention relates to quinazoline derivatives of formula (I) wherein m is an integer from 1 to 2; Rrepresents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, Calkyl, Calkoxy, Calkylthio, or &#x2014;NRR(wherein Rand R, which may be the same or different, each represents hydrogen or Calkyl); Rrepresents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; Rrepresents hydroxy, halogeno, Calkyl, Calkoxy, Calkanoyloxy, trifluoromethyl, cyano, amino or nitro; Xrepresents &#x2014;O&#x2014;, &#x2014;CH&#x2014;, &#x2014;S&#x2014;, &#x2014;SO&#x2014;, &#x2014;SO&#x2014;, &#x2014;NRCO&#x2014;, &#x2014;CONR&#x2014;, &#x2014;SONR&#x2014;, &#x2014;NRSO&#x2014; or &#x2014;NR&#x2014; (wherein R, R, R, Rand Reach independently represents hydrogen, Calkyl or CalkoxyCalkyl); Rrepresents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, and salts thereof; processes for their preparation, pharmaceutical compostions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGP, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

Chemical compounds

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Macclesfield, United Kingdom

Craig Johnstone