The University of Edinburgh

The University of Manchester

Institute of Cancer Research: Royal Cancer Hospital (the)

St Georges Hospital Medical School

Hemocorm Limited

Domainex Limited

St George's Hosptial Medical School

The Institute of Cancer Research: Royal Cancer Hospital

Trevor Robert Perrior

Hazel Joan Dyke

Thomas David Pallin

Jonathan Robert Seckl

Brian Robert Walker

Peter Ward

Scott Peter Webster

Mark Richard Stewart

Gary Karl Newton

Rebekah Elisabeth Key

Rehan Aqil

Christopher Lord

Dan Niculescu-Duvaz

Alan Ashworth

Kerry Jenkins

Clive Robinson

Melanie Jayne Bayford

Stuart Firth-Clark

Ashley Nicholas Jarvis

Raymond John Boffey

Roderick Alan Porter

Jihui Zhang

David Ronald Garrod

Meriel Ruth Major

Roberto Angelo Motterlini

Brian Ernest Mann

Anna Hopkins

Christopher James Lord

Richard James Rowland Elliot

David Alistair Scapens

Tony Richard Johnson

Rebekah Elisabeth Beevers

Philip Alan Skone

Richard James Rowland Elliott

Gabriel Negoita-giras

Stuart Richard Crosby

Roderick Porter

Meriel Ruth Mayor

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, 3,3-disubstituted-(6-aza-bicyclo[3.1.1]hept-6-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, and 4,4-disubstituted piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds of the following formula that, inter alia, inhibit 11&#x3b2;-hydroxysteroid dehydrogenase type 1 (11&#x3b2;-HSD1). 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 inhibit 11&#x3b2;-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11&#x3b2;-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc. 

3,3-disubstituted-(8-aza-bicyclo[3.2.1]OCT-8-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanones as inhibitors of 11 (&#x3b2;)-HSD1

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2/-/-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. 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 inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc. 

3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, 3,3-disubstituted-(6-aza-bicyclo[3.1.1]hept-6-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone, and 4,4-disubstituted piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds of the following formula that, inter alia, inhibit 11&#x3b2;-hydroxysteroid dehydrogenase type 1 (11&#x3b2;-HSD1). 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 inhibit 11&#x3b2;-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11&#x3b2;-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.

3,3-disubstituted-(8-aza-bicyclo[3.2.1]oct-8-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanones as inhibitors of 11 (&#x3b2;)-HSD1

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted-2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. 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 inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc. 

C Compounds of the general formula (I) and salts thereof are useful in the treatment of diseases associated with aberrant activity of the protein kinases IKK&#x3b5; and/or TBK-1: in which: Rrepresents an aliphatic heterocyclyl group having 4, 5, 6 or 7 ring atoms, bonded to the phenyl group shown in formula I through a ring nitrogen atom, and optionally substituted by one or more substituents defined in the Specification; Rrepresents a phenyl or heteroaryl group which is optionally substituted by one or more substituents defined in the Specification; and each of Rand Rindependently represents a hydrogen atom or a Calkyl group. 

Pyrimidine compounds as inhibitors of protein kinases IKK epsilon and/or TBK-1, processes for their preparation, and pharmaceutical compositions containing them

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain (4-phenyl-piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds that, inter alia, inhibit 11&#x3b2;-hydroxysteroid dehydrogenase type 1 (11&#x3b2;-HSD1). 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 inhibit 11&#x3b2;-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11&#x3b2;-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.

(4-phenyl-piperidin-1-yl)-[5-(1H-pyrazol-4-yl)-thiophen-3-yl]-methanone compounds and their use

The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain pyruvamide compounds of the following formula (for convenience, collectively referred to herein as 'PVA compounds'), which, inter alia, inhibit a dust mite Group 1 peptidase allergen (e.g., Der p 1, Der f 1, Eur m 1). 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 inhibit a dust mite Group 1 peptidase allergen, and in the treatment of diseases and disorders that are mediated by a dust mite Group 1 peptidase allergen; that are ameliorated by the inhibition of a dust mite Group 1 peptidase allergen; asthma; rhinitis; allergic conjunctivitis; atopic dermatitis; an allergic condition which is triggered by dust mites; an allergic condition which is triggered by a dust mite Group 1 peptidase allergen; and canine atopy. 

Pyruvamide compounds as inhibitors of dust mite group 1 peptidase allergen and their use

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11&#x3b2;-hydroxysteroid dehydrogenase type 1 (11&#x3b2;-HSD1). 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 inhibit 11&#x3b2;-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11&#x3b2;-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.

Amido-thiophene compounds and their use

The present invention pertains generally to the field of therapeutic compounds and more specifically to certain pyruvamide compounds of the formula (X) (for convenience, collectively referred to herein as 'PVA compounds'), which, inter alia, inhibit a dust mite Group 1 peptidase allergen (e.g., Der p 1, Der f 1, Eur m 1). 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 inhibit a dust mite Group 1 peptidase allergen, and in the treatment of diseases and disorders that are mediated by a dust mite Group 1 peptidase allergen; that are ameliorated by the inhibition of a dust mite Group 1 peptidase allergen; asthma; rhinitis; allergic conjunctivitis; atopic dermatitis; an allergic condition which is triggered by dust mites; an allergic condition which is triggered by a dust mite Group 1 peptidase allergen; and canine atopy.

Compounds, pharmaceutical compositions and methods for the therapeutic delivery of carbon monoxide to humans and other mammals that employ transition metal complexes having at least a substituted cyclopentadienyl, indenyl or fluorenyl ligand and two or more carbonyl ligands.

Therapeutic delivery of carbon monoxide

Amido-thiophene compounds and their use as 11-beta-HSD1 inhibitors

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Cambridge, United Kingdom

Trevor Robert Perrior