Astex Therapeutics Limited

Cancer Research Technology Limited

The Institute of Cancer Research: Royal Cancer Hospital

Glaxosmithkline Intellectual Property Development Limited

Marinus Leendert Verdonk

Valerio Berdini

Gordon Saxty

Ian James Collins

Paul Graham Wyatt

Robert George Boyle

Robert Downham

David Winter Walker

Steven Woodhead

Robin Arthur Ellis Carr

Hannah Fiona Sore

James Francis Callahan

Alison Jo-Anne Woolford

Charlotte Mary Griffiths-Jones

Thomas Daniel Heightman

Jeffrey K Kerns

David Norton

Brent W McCleland

Hong Nie

Joseph E Pero

Thomas Glanmor Davies

Tindy Li

Steven Howard

Maria Grazia Carr

Hendrika Maria Gerarda Willems

Peng Li

Steven John Woodhead

The present invention relates to biaryl pyrazole compounds of Formula (I) methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.

Biaryl pyrazoles as NRF2 regulators

The present invention relates to arylcyclohexyl pyrazole compounds of Formula (I) methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.

Arylcyclohexyl pyrazoles as NRF2 regulators

The invention provides compounds of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between Rand NRRand a maximum chain length of 4 atoms extending between E and NRR, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom &#x3b1; with respect to the NRRgroup and provided that the oxo group when present is located at a carbon atom &#x3b1; with respect to the NRRgroup; Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.

Pyrazole derivatives as protein kinase modulators

The invention provides compounds of the formula (I) having protein kinase B inhibiting activity:  Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.

The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between Rand NRRand a maximum chain length of 4 atoms extending between E and NRR, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NRRgroup and provided that the oxo group when present is located at a carbon atom a with respect to the NRRgroup; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; Ris an aryl or heteroaryl group; and R, R, Rand Rare as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents. 

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Burwell, United Kingdom

Marinus Leendert Verdonk