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David Michel Adrien Taddei

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Thomas Christopher Colley

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Garth Rapeport

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David Cousin

Rudy Broeckx

Walter Filliers

Stephen Thom

Christopher William Murray

Valerio Berdini

Steven Howard

Ildiko Maria Buck

Alison Jo-Anne Woolford

Iain Walters

Charlotte Mary Griffiths-Jones

Thomas Daniel Heightman

James Edward Harvey Day

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Michael Liam Cooke

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Marc O'Reilly

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Stephen John Davies

Angus Macleod

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Derek John Londesbrough

George Hardy

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Ian Strutt

Joseph William Wrigglesworth

Colin Peter Sambrook-Smith

Thomas Alanine

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Mohammed Abdul Quddus

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Lorna Duffy

David Charles Festus Moffat

Anil Patel

Jokin Carrillo Arregui

Daniel Hamza

Jonathon Gareth Williams

Jennifer Claire Thomas

David Michael Adrien Taddei

Hayley Tegan Angela Watson

Claire Anne Marie Cariou

Euan Alexander Fordyce

David Kenneth Mycock

Eric Sing Yuen Tse

Ito Kazuhiro

Ildiko Buck

Catherine Elizabeth Charron

Alex Copmans

Stephen Malcolm Thom

Jonathan Martin Shannon

A combination therapy including one or more compounds of formula (I): wherein R represents hydrogen, halo, cyano, Chaloalkyl, Chaloalkoxy, or SONRR, Rand Rindependently represent hydrogen or halo; Rrepresents hydrogen, halo, cyano, Calkyl, Calkoxy, or Chaloalkoxy; Rrepresents halo, cyano, Calkyl, or Chydroxyalkyl; Rrepresents hydrogen or Calkyl; X represents CH or N; Y represents N or CH which carbon atom may optionally be substituted by R, Ror R; Rand Rindependently represent hydrogen or Calkyl; or a pharmaceutically acceptable salt thereof; and a second or further active ingredient.

Process for preparing a compound useful to treat mycoses

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

A process for preparing a compound of formula (II): includes reacting a compound of formula (VIII): with a compound of formula (XIV): 

A compound has the following formula: The compound is a p38 MAP kinase inhibitor. The compound and its pharmaceutically acceptable salts can be used for treatment of conditions, such as inflammatory diseases.

Inhibitor of p38 MAP kinase

The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered nitrogen-containing heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is substituted with a nitrogen-containing group R' wherein Rcontains from 1 to 7 atoms other than hydrogen or halogen. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.

Sulfonylureas and sulfonylthioureas as NLRPinhibitors

The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is di-substituted at the 3- and 4-positions relative to the point of attachment of the sulfonyl group, wherein at least one of the di-substituents contains a nitrogen atom. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP.

Sulfonylureas and sulfonylthioureas as NLRP3 inhibitors

A compound which is an arylimidazolyl isoxazole of formula (I): (Formula (I)) or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer, particularly prostate cancer. 

Pharmaceutical compounds

There are provided compounds of formula (I) as defined in the specification which are p38 MAP kinase inhibitors for use as medicaments for the treatment inter alia of inflammatory diseases. 

Pyrazolyl-ureas as 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.

A process for preparing a compound of formula (II):  includes reacting a compound of formula (VIII):  with a compound of formula (XIV): 

There are provided compounds of formula (I) which are inhibitors of the family of p38 mitogen-activated protein kinase enzymes, and to their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.

1-pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl) oxy) napththalen-1-yl) ureas as P38 MAP knase inhibitors

A dry powder pharmaceutical formulation for inhalation including a compound of formula (I): that is 1-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(4-((2-((6-ethylpyrazin-2-yl)amino)pyridin-4-yl)methoxy)naphthalen-1-yl)urea or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof; and lactose as a topically acceptable diluent. An inhaler device containing the dry powder pharmaceutical formulation is also described.

The invention is directed to compounds of general formula (I) and pharmaceutical compositions containing such compounds. The compounds and compositions have valuable pharmaceutical properties. In particular, they may be used for the treatment of cancer. Novel intermediates and novel methods of preparation are also disclosed.

Pharmaceutically active compounds

There is provided a compound of formula (I) which is an inhibitor of the family of p38 mitogen-activated protein kinase enzymes, and to its use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as asthma and COPD.

1-pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl) oxy) napththalen-i-yl) ureas as P38 mapkinase inhibitors

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Nottingham, United Kingdom

Stuart Thomas Onions