Cancer Research Technology Limited

Newcastle University Ventures Limited

Astex Therapeutics Limited

Kudos Pharmaceuticals Limited

Shire LLC

Cancer Research Campaign Technology Limited

Other

Osi Pharmaceuticals, Inc.

Cobra Therapeutics Limited

Alan Hilary Calvert

Nicola Jane Curtin

David Richard Newell

Bernard Thomas Golding

Roger John Griffin

Ian Robert Hardcastle

Alan H Calvert

Roger J Griffin

Nicola J Curtin

Niall Morrison Barr Martin

Graeme Cameron Murray Smith

Nicola Curtin

Celine Florence Cano

Hilary Alan Calvert

Duncan Charles Miller

Christopher Norbert Johnson

Steven Howard

Gianni Chessari

Ildiko Maria Buck

David Charles Rees

Kim Louise Hirst

Emiliano Tamanini

Laurent Jean Martin Rigoreau

James Daniel Osborne

Jeffrey David St Denis

Dale Robert Mitchell

Rhian Sara Holvey

Benjamin David Cons

Joanne Peach

Arwel Lewis

Benjamin Paul Whittaker

David Wyn Watson

Keith Allan Menear

Eric Valeur

Marc Geoffrey Hummersone

Paul Workman

Florence Irene Raynaud

Bernard Paul Nutley

Xiao-ling Fan Cockcroft

Francis Thomas Boyle

Eric W Collington

Angus Macleod

Martin Edward Mäntylä Noble

Martin Noble

Kappusamy Saravanan

Christiane Riedinger

Anna Frances Watson

Martin E M Noble

Jonathan G Williams

Vincent Junior Ming-lai Loh

Richard Franklin

Jane A Endicott

Philip J Jewsbury

John Kitchin

Mark Frigerio

Daniel Lee Rathbone

Jane Nicola Curtain

David R Houck

David Charles Billington

David Edward Smith

Nicholas Rich

Jane Nicola Curtin

Peter A Cicala

Hendrika Maria Gerarda Willems

Per Kallblad

John Lunec

Marine Desage-El Murr

Tristan Reuillon

Stephanie Myers

Lauren Molyneux

Laurent Rigoreau

Charmaine Paulina Quarterman

John Alfred Slack

Peter Cicala

Sarah Cully

The invention provides a compound of formula (I): or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.

Isoindolinone inhibitors of the MDM2-P53 interaction having anticancer activity

Isoindolinone inhibitors of the MDM2-p53 interaction having anticancer activity

A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.

Therapeutic agents

The invention provides compounds of formula (I) or a tautomer, stereoisomer, N-oxide, pharmaceutically acceptable salt or solvate thereof. The compounds are useful for the prophylaxis or treatment of a disease state or condition mediated by ERK5, in particular cancers.

Pyrrolcarboxamide derivatives for the inhibition of ERK5

A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53. 

The present invention relates to a novel process for producing quinazoline compounds which are useful in therapy. More specifically, the compounds produced by the process of the invention are useful in the treatment of a number of cardiovascular diseases. The process of the invention provides 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin 2(3H)-one, more commonly known as anagrelide and its analogues in a clean and efficient manner.

Process for the preparation of anagrelide and analogues

This invention relates to the discovery of prodrugs of 3-or 5-substituted analogues of the selective platelet lowering agent anagrelide which have reduced potential for cardiovascular side-effects and which should therefore lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to prodrugs of certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting the formation of blood platelets. An example of a compound of the present invention is methyl 2-(2-amino-5,6- dichloroquinazolin-3 (4H)-yl)-2-methylpropanoate or the 3,3-demethyl anagrelide open-ringed analog.

Substituted quinazolines for reducing platelet count

A compound of formula or a prodrug and/or a pharmaceutically acceptable salt thereof, wherein X is O, N or S; Ris hydrogen, halo, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyalkyl, substituted or unsubstituted alkylamine, alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroaralkyl; Ris hydrogen, halo, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyalkyl substituted or unsubstituted alkylamine, alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroalkyl; Ris hydrogen, halo, hydroxy, substituted or unsubstituted alloy substituted or unsubstituted hydroxyalkyl, substituted or unsubstituted alkylamine alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroalkyl; and R-R, is used to represent groups R, R, Rand Rwhich are H, OH, alkyl, alkoxy, alkylamine, hydroxyalkyl, halo, CF, NH, NO, COOH, C&#x2550;O.

Isoindolin-1-one derivatives

This invention relates to the discovery of 3- and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets.

Substituted quinazolines

A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: Rand Rare independently selected from hydrogen, an optionally substituted Calkyl group, Cheterocyclyl group, or Caryl group, or may together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; Q is &#x2014;NH&#x2014;C(&#x2550;O)&#x2014; or &#x2014;O&#x2014;; Y is an optionally substituted Calkylene group; X is selected from SRor NRR, wherein, R, or Rand Rare independently selected from hydrogen, optionally substituted Calkyl, Caryl, or Cheterocyclyl groups, or Rand Rmay together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; if Q is &#x2014;O&#x2014;, X is additionally selected from &#x2014;C(&#x2550;O)&#x2014;NRR, wherein Rand Rare independently selected from hydrogen, optionally substituted Calkyl, Caryl, or Cheterocyclyl groups, or Rand Rmay together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and if Q is &#x2014;NH&#x2014;C(&#x2550;O)&#x2014;, &#x2014;Y&#x2014;X may additionally be selected from Calkyl.

DNA-PK inhibitors

Compounds of formula I: wherein A, B and D are respectively selected from the group consisting of:

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Newcastle upon Tyne, United Kingdom

Bernard Thomas Golding