Proximagen Limited

Cadlink Technology Corporation

Nhs Blood and Transplant

Bio Products Laboratory Limited

David Evans

Iain Simpson

Edward Savory

Lee Patient

Max Espensen

Ronald Veck

Michael Higginbottom

Marianne Nilsson

Tobias Koolmeister

Martin Haraldsson

Alison Stewart

Allison Carley

Peter Feldman

Erik Nordling

Michelle Georgiou

Derek Wheeler

Christopher Hardway

Sarah Kingsland

Robert Clemmitt

Paul St-Pierre

James Ramsden

Trevor Simmonds

Gordon Reynen

Allison Powell

Caroline Connolly

Torkil Menne

Johan Selmer

Jesper Lange

Compound of formula (I) or a pharmaceutically acceptable salt, or N-oxide thereof, that are inhibitors of SSAO activity: where V, W, X, Y, Z, R, and Rare as defined herein.

Substituted imidazo[4,5-c]pyridine compounds and compositions thereof

A process for the preparation of a compound of formula (Ia) or a pharmaceutically acceptable salt, or N-oxide thereof that includes reacting a compound of formula (IIIa) or (Va) with a compound of formula (IX) to form the compound of formula (Ia) 

Imidazo[4,5-c]pyridine and pyrrolo[2,3-c]pyridine derivatives as SSAO inhibitors

The compounds of formula (I) are inhibitors of SSAO activity wherein V, W, X, Y, Z, Rand Rare as defined in the claims.

The present invention relates to compounds which are inhibitors of SSAO activity. The invention also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.

Compounds

Imidazo[4,5-C]pyridine and pyrrolo[2,3-C]pyridine derivatives as SSAO inhibitors

The compounds of formula (I) are inhibitors of semicarbazide-sensitive amine oxidase (SSAO) activity useful in the treatment of inflammation, an inflammatory disease, an immune or an autoimmune disorder, or inhibition of tumor growth. 

The compound of formula (I) are inhibitors of SSAO activity (Formula (I)) wherein the terms Y, Z, W, Rand Rare defined in the claims. 

Disclosed are compounds which inhibit SSAO enzyme activity. Also disclosed are pharmaceutical compositions comprising these compounds and the use of these compounds in the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases, immune disorders and the inhibition of tumor growth.

Inhibitor compounds of semicarbazide-sensitive amine oxidases

2-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}ethan-1-amine; 3-aminopropyl 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxylate; 1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}-4-(dimethylamino)butan-1-one; 5-amino-1-{4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}pentan-1-one; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; N-(3-aminopropyl)-4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidine-1-carboxamide; 4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-N-[3-(dimethylamino)propyl]piperidine-1-carboxamide; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)piperazine; 4-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)morpholine; 1-({4-[1-(4-chlorophenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]piperidin-1-yl}carbonyl)-1,4-diazepane; ethyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; ethyl 1-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylate; 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxylic acid; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-4-carboxamide; 4-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4yl}carbonyl)morpholine; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-4-yl}carbonyl)piperazine; {4-[1-(4-methylphenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}methanol; {4-[1-(4-methyl-phenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-2-yl}methanol; [(3R)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl]methanol; methyl 4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxylate; N-(2-aminoethyl)-4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholine-3-carboxamide; 2-{4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]morpholin-3-yl}ethan-1-ol; methyl 1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxylate; N-(2-aminoethyl)-1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidine-2-carboxamide; 1-({1-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-2-yl}carbonyl)piperazine; 4-[1-(4-methylphenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]morpholine; 1-(4-chlorophenyl)-3-(piperidin-4-yl)-1H-pyrrolo[2,3-c]pyridin-4-ol; N-butyl-1-(4-chlorophenyl)-N-methyl-1H-pyrazolo[3,4-c]pyridin-3-amine; 1-[4-(fluoromethyl)phenyl]-3-(oxan-4-yl)-1H-pyrazolo[3,4-c]pyridine; and 3-({4-[1-(4-chlorophenyl)-1H-pyrazolo[3,4-c]pyridin-3-yl]piperidin-1-yl}methyl)pyridine are useful for the inhibition of SSAO activity.

Enzyme inhibitor compounds

The present invention relates to processes for the preparation of virus inactivated thrombin, and to the products prepared by these processes.

Process for producing a virus-inactivated thrombin preparation

A method for enabling a program that communicates a document description from a composition system to a printing system to manage variable-dot halftones for use with variable-dot printing devices, comprising the steps of creating a set of strings, each string defining a halftone cell intensity value and comprising at least one pixel imbution value, wherein said pixel imbution value is in the range of 0 to P, wherein P is the number of physical appearances that a painted pixel can have; using a selected halftone cell intensity value to directly choose a string from said set of strings; and painting at least one pixel within a halftone cell according to a pixel imbution value within the chosen string.

Variable-dot halftoning

The present invention relates to processes for the purification of fibrinogen, and to readily solubilised fibrinogen preparations.

Processes for the preparation of fibrinogen

A method for enabling a program that communicates a document description from a composition system to a printing system to manage variable-dot halftones for use with variable-dot printing devices, comprising the steps of using a selected halftone cell size to choose an array comprising at least one string defining a halftone cell intensity value, said string comprising at least one pixel imbution value, wherein said pixel imbution value is in the range of 0 to P, wherein P is the number of physical appearances that a painted pixel can have; using a selected halftone cell intensity value to choose a string; and painting at least one pixel within a halftone cell according to a pixel imbution value within the chosen string.

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Royston, United Kingdom

David Evans