Glaxo Group Limited

Glaxo Inc.

Cellzome Limited

Fovea Pharmaceuticals

Sanofi

Nuada, LLC

Atopix Therapeutics Limited

David Middlemiss

Alan Naylor

Michael D Dowle

Barry C Ross

Harry Finch

Lawrence H Lunts

David I Scopes

Kevin S Cardwell

Torquil I Jack

Ian F Skidmore

Stephen Paul Watson

Charles Willbe

Duncan B Judd

Caroline Leriche

John G Montana

Francis Gerard Fang

Colin David Eldred

Stephen V Frye

Neil Anthony Pegg

Andrew David Cansfield

John Thomas Feutrill

Pritom Shah

Brian Evans

Nigel Ramsden

Mihiro Sunose

Michael Menteith Hann

Jess Taylor

Kathryn Bell

Duncan Robert Armour

Gerard Martin Giblin

Xiao-Qing Lewell

Tania Hubbard

Maria Victoria Vinader

Frederick Arthur Brookfield

Susan Marie Royalty

Ian B Campbell

Mark Whittaker

Robert J Foglesong

Eric Roy Pettipher

Svenja Burckhardt

Jan Jozef Scicinski

Francis Wilson

Valerie Reader

James Ford Burns

Gitte Neubauer

Gunnar Erik Jagdmann, Jr

Carsten Hopf

Martin Pass

Gerard Drewes

Tatyana Dyakonov

Kellee Griffin Ring

Eric Auclair

Jacques Le Roux

Jan Josef Scicinski Scicinski

Gunnar Erik Jagdmann Jr Jr

Kellee Griffin Ring Ring

James Ford Burns Burns

Robert James Foglesong Foglesong

Susan Marie Royalty Royalty

Marcus Bantscheff

Bernhard Kuester

Manfred Raida

John Feutrill

Dirk Eberhard

Ulrich Kruse

Mick Hunter

Christopher Palmer

Mark Richard Ashton

The present invention relates to therapeutic applications of aniline derivatives of formula (I), for example in treating glaucoma: Formula (I), R1a represents H, an halogen, a (C-C)alkyl or a CN; R1b represents H, an halogen or a (C-C)alkyl; R1c represents H or a (C-C)alkyl; R2 represents H, an halogen, an OH, an O&#x2014;(C-C)alkyl or (C-C)alkyl; R3 represents H, an halogen, a (C-C)alkyl, an OH, an O&#x2014;(C-C)alkyl, a CONHor CN; R4 represents H, an halogen or a (C-C)alkyl; R5 represents H or F: R7 represents H or F; R8 represents H or F; R9 represents H or (C-C)alkyl, or one of its enantiomers. 

Aniline derivatives, their preparation and their therapeutic application

The present invention relates to aniline derivatives of formula (I), to their preparation and to their therapeutic application, for example in treating glaucoma: Formula (I), R1a represents H, an halogen, a (C-C)alkyl or a CN; R1b represents H, an halogen or a (C-C)alkyl; R1c represents H or a (C-C)alkyl; R2 represents H, an halogen, an OH, an O&#x2014;(C-C)alkyl or (C-C)alkyl; R3 represents H, an halogen, a (C-C)alkyl, an OH, an O&#x2014;(C-C)alkyl, a CONHor CN; R4 represents H, an halogen or a (C-C)alkyl; R5 represents H or F: R7 represents H or F; R8 represents H or F; R9 represents H or (C-C)alkyl, or one of its enantiomers. 

The invention relates to compounds of formula (I); wherein X and Rto Rhave the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of Itk or PI3K, for the treatment or prophylaxis of immunological, inflammatory or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments. 

Triazole derivatives as kinase inhibitors

The invention relates to compounds of formula (I) wherein X, Tand Rto Rhave the meaning as cited in the description and the claims. Said compounds are useful as protein kinase inhibitors, especially inhibitors of PI3K, for the treatment or prophylaxis of immunological, inflammatory, autoimmune, or allergic disorders. The invention also relates to pharmaceutical compositions including said compounds, the preparation of such compounds as well as the production of and use as medicaments.

Amino triazoles as PI3K inhibitors

The invention is directed to certain novel compounds, methods for producing them and methods for treating or ameliorating a kinase-mediated disorder. More particularly, this invention is directed to substituted quinazoline compounds useful as selective kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase-mediated disorder, In particular, the methods relate to treating or ameliorating a kinase-mediated disorder including cardiovascular diseases, diabetes, diabetes-associated disorders, inflammatory diseases, immunological disorders, cancer and diseases of the eye such as retinopathies or macular degeneration or other vitreoretinal diseases, and the like.

Substituted quinazoline compounds

The present invention relates to a series of novel compounds having the formula (I) wherein: X is NRor O; n is 1 or 2; A is a bicyclic carbocycle and R1 and R2 are as described herein. The compounds are useful as DPP-IV inhibitors, such as for the treatment of diabetes. 

Peptidase inhibitors

The present invention relates to piperidine derivatives of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-4 alkoxy group; R.sup.2 is ##STR2## R.sup.3 is a hydrogen or halogen atom; R.sup.4 and R.sup.5 may each independently represent a hydrogen or halogen atom, or a C.sub.1-4 alkyl, C.sub.1-4 alkoxy or trifluoromethyl group;

Piperidine derivatives

The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof wherein the R groups are defined in the specification. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

Benzofuran derivatives

There are disclosed preparation and compounds of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower alkyl or taken together are a --CH.sub.2 -- group to form a cyclopropane ring.

17 .beta.acyl 6 azaandrost-4,6 diazo-4-ene-3-ones

The invention provides compounds of the general formula (I): ##STR1## or a physiologically acceptable salt, solvate (e.g. hydrate) or a metabolically labile ester thereof. The compounds may be used in the treatment or prophylaxis of hypertension and diseases associated with cognitive disorders.

C-linked pyrazole derivatives

The invention provides compounds of the general formula (I) ##STR1## and physiologically acceptable salts, solvates or non-toxic metabolically labile esters thereof where R.sup.1 represents a halogen atom; Ar represents the group ##STR2## R.sup.3 represents a C-linked tetrazolyl group; R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a halogen atom or a C.sub.1-6 alkyl group; and

The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt, solvate or metabolically labile ester thereof wherein

The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are

Heterocyclic inhibitors of 5-.alpha.-testosterone reductase

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Bishops Stortford, United Kingdom

David Middlemiss