Respivert Limited

Cellcentric Limited

King's College London

David Michel Adrien Taddei

Stuart Thomas Onions

Neil Anthony Pegg

Kazuhiro Ito

John King-Underwood

Peter John Murray

Peter Strong

Catherine Elisabeth Charron

Jonathan Gareth Williams

William Garth Rapeport

Simon Christopher Hirst

Gareth Harbottle

Richard James Brown

Jonathan Shannon

Alex Herman Copmans

Rudy Laurent Maria Broeckx

Silvia Paoletta

Alun John Smith

Don Smyth

Alan D Borthwick

Sarkis Barret Kalindjian

David Cousin

David Wood

Jane Theresa Brown

Jonathan Patrick Thomas Corcoran

Jason John Shiers

Donald Alan Gilbert

Anil Patel

Colin Lindley

John Paul Madeley

James Vaughan Morey

Jonathan Trevorrow

Ting Qin

Eric Sing Yuen Tse

David Kenneth Mycock

David Reginald Adams

Paul Baguley

Catherine Elizabeth Charron

A process for producing a compound of the following formula (I) which process comprises: (a) treating a compound of the following formula (5) with a compound of the following formula (6) to generate an intermediate compound of the following formula (7); (b) treating a compound of formula (7) as defined above with a compound of the following formula (8); and (c) recovering a compound of formula (I) as defined above. The compound of formula (I) is a promising modulator of p300/CBP activity that has potential utility in treating cancers, including prostate cancer, haematological cancers, bladder cancer and lung cancer. 

Process for preparing modulators of p300 and/or CBP

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

A compound which is a benzimidazole of formula (I): wherein X is a 5-membered heteroaryl group selected from the following: 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. 

A compound which is an isoxazolyl imidazopyridine of formula (I): wherein: Rand R, which are the same or different, are each H or C alkyl; Rand R, which are the same or different, are each H or F; X is -(alk)-, -alk-C(&#x2550;O)&#x2014;NR&#x2014;, -alk-NR&#x2014;C(&#x2550;O)&#x2014; or -alk-C(&#x2550;O)&#x2014;; Ris selected from &#x2014;S(&#x2550;O)R' and a 4- to 7-membered heterocyclic group which is unsubstituted or substituted; Rand R, which are the same or different, are each H or Calkyl; or Rand Rform, together with the C atom to which they are attached, a Ccycloalkyl group; Rand R, which are the same or different, are each H, Calkyl, OH or F; Ris phenyl or a 5- to 12-membered N-containing heteroaryl group and is unsubstituted or substituted; alk is Calkylene; R&#x2032; is Calkyl; and n is 0 or 1; 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. 

Isoxazolyl substituted imidazopyridines

A compound which is a benzimidazolyl isoxazole of formula (I): wherein: Rand R, which are the same or different, are each H or Calkyl; R, Rand R, which are the same or different, are each H or F; X is -(alk-, -alk-C(&#x2550;O)&#x2014;NR&#x2014;, -alk-NR&#x2014;C(&#x2550;O)&#x2014; or -alk-C(&#x2550;O)&#x2014;; Ris selected from &#x2014;S(&#x2550;O)R'; a 4- to 6-membered, C-linked heterocyclic group which is unsubstituted or substituted; and an N-linked spiro group of the following formula: Rand R, which are the same or different, are each H or Calkyl, or Rand Rform, together with the C atom to which they are attached, a Ccycloalkyl group; Rand R, which are the same or different, are each H, Calkyl, OH or F; Ris phenyl or a 5- to 12-membered, N-containing heteroaryl group and is unsubstituted or substituted; alk is Calkylene; R&#x2032; is Calkyl; and n is 0 or 1; 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. 

Isoxazolyl substituted benzimidazoles

The present invention relates inter alia to a compound of formula (I) and to compositions comprising the same and to the use of the compounds and to compositions of the compounds in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making the said compounds. 

2-((4-amino-3-(3-fluoro-5-hydroxyphenyl)-1H-pyrazolo[3,4-D]pyrimidin-1-yl)methyl)-3-(2-(trifluoromethyl)benzyl) quinazolin-4(3H)-one derivatives and their use as phosphoinositide 3-kinase inhibitors

The present invention relates inter alia to a compound of formula (I) and to compositions comprising the same and to the use of the compounds and to compositions of the compounds in treatment, for example in the treatment of inflammatory diseases, in particular respiratory inflammatory disease. The invention also extends to methods of making the said compounds.

Phosphoinositide 3-kinase inhibitors

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as 'AAA compounds'), which, inter alia, are (selective) retinoic acid receptor &#x3b1; (RAR&#x3b1;) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RAR&#x3b1;, and in the treatment of diseases and conditions that are mediated by RAR&#x3b1;, that are ameliorated by the activation of RAR&#x3b1;, etc., including cognitive disorders, memory impairment, memory deficit, senile dementia, Alzheimer's disease, early stage Alzheimer's disease, intermediate stage Alzheimer's disease, late stage Alzheimer's disease, cognitive impairment, and mild cognitive impairment. 

Therapeutic aryl-amido-aryl compounds and their use

There are provided inter alia compounds of formula (I) wherein R, Ar, L, X, Rand Q are as defined in the specification for use in therapy, especially in the treatment of inflammatory diseases.

P38 MAP kinase inhibitors

The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, including all stereoisomers, tautomers and isotopic derivatives thereof, which are inhibitors of p38 mitogen-activated protein kinase enzymes (referred to herein as p38 MAP kinase inhibitors), particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPD.

p38 MAP kinase inhibitors

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Nottingham, United Kingdom

David Michel Adrien Taddei