Otsuka Pharmaceutical Company, Limited

Astex Therapeutics Limited

Novartis Ag

Marc O'Reilly

Steven Howard

Alison Jo-Anne Woolford

Stuart Thomas Onions

Christopher William Murray

Valerio Berdini

Ildiko Maria Buck

Charlotte Mary Griffiths-Jones

Thomas Daniel Heightman

Jonathan Shannon

James Edward Harvey Day

David Norton

David Cousin

John Paul Watts

Michael Liam Cooke

Miles Stuart Congreve

Michael Luzzio

Gianni Chessari

Bharat Lagu

Paul Graham Wyatt

Lawrence Blas Perez

Andrew James Woodhead

Fan Yang

Christine Hiu-Tung Chen

Christopher Thomas Brain

Young Shin Cho

Yaping Wang

John William Giraldes

Sunkyu Kim

Claudio Dagostin

Steven Douglas Hiscock

Yipin Lu

Paul Mortenson

Harren Jhoti

Jonathan Martin Shannon

Michael Joseph Luzzio

Paul Neil Mortenson

John Grialdes

The invention provides a compound of formula (0): The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.

Benzolactam compounds as protein kinase inhibitors

The invention provides a compound of formula (0):  The compounds are inhibitors of ERK1/2 kinases and will be useful in the treatment of ERK1/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.

The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof;wherein Q is CH or N; X is N, N&#x2014;Oor CR; Y is N, N&#x2014;Oor CR; Rand Rare independently selected from hydrogen and various substituents as defined in the claims; or Rand Rtogether with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; Ris selected from hydrogen and various substituents; and Ris selected from hydrogen and various substituents 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. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.

Imidazole derivatives and their use as modulators of cyclin dependent kinases

A method for identifying a ligand of a target macromolecule is disclosed, comprising the steps of: soaking one or more crystals of the target macromolecule in a solution containing a collection of compounds generated in situ or separate from the crystal, where the solution has been prepared without the purification of the synthesized collection of compounds; obtaining an X-ray crystal diffraction pattern of the soaked macromolecule crystal; and using said X-ray crystal diffraction pattern to identify any compound bound to the macromolecule crystal, said compound being a ligand of the target macromolecule.

Synthesis and screening of ligands using X-ray crystallography

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Hereford, United Kingdom

Marc O'Reilly