Azura Ophthalmics Ltd.

The University of Manchester

Domainex Limited

The University of Leeds

St Georges Hospital Medical School

St George's Hosptial Medical School

Mark Richard Stewart

Yair Alster

Omer Rafaeli

Charles Bosworth

Marc Gleeson

Gary Karl Newton

Jonathan Dunn

Ian Holmes

Hila Barash

Robert M Burk

Trevor Robert Perrior

Kerry Jenkins

Clive Robinson

Jihui Zhang

David Ronald Garrod

Nicholas Chapman

Meriel Ruth Major

Alan Naylor

Philip Spencer Fallon

Rehan Aqil

Rebekah Elisabeth Key

Richard James Foster

Anna Hopkins

Natalie Louise Winfield

Ian Yule

Roger Taylor

Rebekah Elisabeth Beevers

Alexander James Nicholls

Colin Fishwick

Charlotte Revill

Helen Philippou

Lucie Juliette Guetzoyan

Stuart Crosby

Alistair James Macnair

Gabriel Negoita-giras

Stuart Richard Crosby

Meriel Ruth Mayor

This invention relates to compounds of formula (I) and methods of treatment using the compounds. The invention also relates to processes and methods for producing the compounds of the invention. The compounds of the invention are modulators of Factor XII (e.g. Factor XIIa). In particular, the compounds are inhibitors of Factor XIIa and may be useful as anticoagulants.

Factor XIIA inhibitors

Described herein are compositions and methods for the treatment of ocular surface disorders including meibomian gland dysfunction, blepharitis, dry eye disease and other inflammatory/infections disease of the anterior surface of the eye. Said compositions and methods comprise keratolytic conjugate which demonstrate keratolytic activity, and anti-inflammatory or other desirable activities. Topical administration of said compositions to the eye, ocular surface or surrounding areas provides therapeutic benefit to patients suffering from ocular surface disorders.

Compounds and methods for the treatment of ocular disorders

Described herein are compositions and methods for the treatment of ocular surface disorders including meibomian gland dysfunction, blepharitis, dry eye disease and other inflammatory and/or infectious disease of the anterior surface of the eye. Said compositions and methods comprise keratolytic conjugates which demonstrate keratolytic activity, and anti-inflammatory or other desirable activities. Topical administration of said compositions to the eyelid margin or surrounding areas provides therapeutic benefit to patients suffering from ocular surface disorders.

Described herein are compositions and methods for the treatment or prevention of ocular surface disorders including meibomian gland dysfunction, blepharitis, dry eye disease and other inflammatory and/or infectious diseases of the anterior surface of the eye(s). Said compositions and methods comprise keratolytic conjugates which demonstrate keratolytic activity, and anti-inflammatory or other desirable activities. Topical administration of said compositions to the eyelid margin or surrounding areas provides therapeutic benefit to patients suffering from ocular surface disorders.

The invention provides compounds of formula (I) wherein R is &#x2014;CHor &#x2014;CHCHand pharmaceutically acceptable salts thereof. The compounds of formula (I) are useful in the treatment of diseases or disorders mediated by IKK, TBK1 and/or SIK2 mechanisms in a subject, for example cancer and inflammatory and tissue repair disorders. The invention also provides uses of the compounds of formula (I) and compositions containing them. (Formula (I)) 

5-(pyrimidin-4-yl)-2-(pyrrolidin-1-yl)nicotinonitrile compounds as IKKE, TBK1 and/or SIK2 kinases inhibitors

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, 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 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.

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Cambridge, United Kingdom

Mark Richard Stewart