Darwin Discovery Limited

Chiroscience, Ltd.

Janssen Pharmaceutica Nv

Pulmagen Therapeutics (asthma) Limited

Genentech, Inc.

Other

Zafgen, Inc.

Gboo1, Inc.

Pulmagen Therapeutics Limited

John Gary Montana

Andrew Douglas Baxter

David Alan Owen

Hazel Joan Dyke

George Hynd

Robert John Watson

Stephen Colin Price

Christopher Lowe

Alan Findlay Haughan

Samuel Edward Mann

Patrizia Tisselli

Janusz Jozef Kulagowski

Calum Macleod

Steven Colin Beasley

Verity Margaret Sabin

Harry Finch

Calum MacLeod

Terry Aaron Panchal

George Martin Buckley

John Fraser Keily

Hannah Jayne Kendall

Rosa Arienzo

Andrew Sharpe

Duncan Robert Hannah

David Thomas Manallack

Michael Colin Cramp

David Edward Clark

Mark S Stanley

Karen Williams

Liang Bao

Neil Phillipson

Karen Ann Runcie

Robert James Maxey

Fabien Jean Ghislain Roussel

Neville McLean

Robert Zahler

Hazel Joan Hunt

Nicholas Charles Ray

Wendy Lee

Thomas David Pallin

Simon Charles Goodacre

Susan Mary Cramp

Richard John Davenport

Pascal Savy

Donald John Daley

Takahiro Ito

Hazel John Dyke

Yukari Perrella

Jonathan Dickens

Louise Picken

Barbara Avitabile-Woo

Richard John Taylor

Mathias Domostoj

Catherine Louise Picken

Ruth Elizabeth Wills

John Bird

Mitsuru Teramoto

Trevor Keith Harrison

Yann Griffon

Elizabeth Jane Reed Nicholson

Peter Crackett

Paul Vincent Murphy

Stephen Price

Janusz Kulagowski

Pascal Pierre Savy

Pierre Pascal Savy

The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-&#x3ba;B-inducing kinase (NIK&#x2014;also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.

Pyrazolopyrimidine derivatives as NIK inhibitors

Crystals of [8-chloro-3-(4-chlorobenzyl)-4-difluoromethoxy-2-ethylquinolin-5-yloxy]acetic acid L-lysine salt, i.e., a crystal A which has peaks at diffraction angles 2&#x3b8;=6.0&#xb0;, 10.0&#xb0;, 10.7&#xb0;, 12.1&#xb0;, 18.4&#xb0;, 19.2&#xb0; and 20.1&#xb0; in powder X-ray diffraction spectra and a crystal B which has peaks at diffraction angles 2&#x3b8;=6.0&#xb0;, 11.7&#xb0;, 12.4&#xb0;, 15.2&#xb0;, 16.4&#xb0;, 20.3&#xb0; and 22.6&#xb0; in powder X-ray diffraction spectra. These crystals are chemically stable and have excellent thermal stability and physical properties, and are therefore suitable as medicinal substances.

Quinoline derivative in crystal form

Thienopyrimidine derivatives as NIK inhibitors

Compounds as NIK inhibitors

[object Object]

Pyrazole derivatives as NIK inhibitors

The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-&#x3ba;B-inducing kinase (NIK&#x2014;also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders. 

3-(2-aminopyrimidin-4-yl)-5-(3-hydroxypropynyl)-1H-pyrrolo[2,3-C]pyridine derivatives as NIK inhibitors for the treatment of cancer

The invention provides sulphone compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various sulphone compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.

Sulphone compounds and methods of making and using same

In general, the present invention relates to small molecule inhibitors of the heat shock protein 90 family of chaperone proteins. The invention also features pharmaceutical compositions and kits that include the compounds and compositions of the invention. The invention further relates to the medical use of these compounds and compositions for the treatment of neurodegenerative diseases.

Adenine inhibitors of HSP90

Compound of formula (I) are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions. Wherein X is &#x2014;SO&#x2014; or *&#x2014;SONR&#x2014; wherein the bond marked with an asterisk is attached to Ar; Ris hydrogen, fluoro, chloro, CN or CF; Ris hydrogen, fluoro or chloro; Ris hydrogen, CCalkyl or C-Ccycloalkyl; Aris phenyl or a 5- or 6-membered heteroaryl group selected from furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C-Ccycloalkyl, &#x2014;O(C-Calkyl) or CCalkyl, the latter two groups being optionally substituted by one or more fluoro atoms; and Aris phenyl or 5- or 6-membered heteroaryl group selected from pyrrolyl, furanyl, thienyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, pyridinyl, pyridazinyl, pyrimidinyl and pyrazinyl, wherein the phenyl or heteroaryl groups are optionally substituted by one or more substituents independently selected from fluoro, chloro, CN, C-C-Ccycloalkyl, &#x2014;O(C-Calkyl) or CCalkyl, the latter two groups being optionally substituted by one or more fluoro atoms. 

Indoles and their therapeutic use

Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: Ris halogen or cyano; Ris hydrogen or methyl; Rand Rare independently &#x2014;OR, C-Calkyl or C-Ccycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; Ris hydrogen or halogen; Ris CCalkyl or C-Ccycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is &#x2014;CH&#x2014;, &#x2014;S&#x2014;, or &#x2014;O&#x2014;; one of Y and Yis hydrogen and the other is OR, &#x2014;C(&#x2550;O)R, NRSORor a heterocyclic group selected from those referred to in the specification; and R, Rand Rare as defined in the specification.

Quinolines and their therapeutic use

Compounds of formula (I) are CRTH2 ligands, useful in the treatment of, for example, asthma and COPD wherein: Ris halogen or cyano; Ris hydrogen or methyl; Rand Rare independently &#x2014;OR, C-Calkyl or C-Ccycloalkyl, the latter two groups being optionally substituted by one or more halogen atoms; Ris hydrogen or halogen; Ris C-Calkyl or C-Ccycloalkyl, either of which being optionally substituted by one or more halogen atoms; X is &#x2014;CH&#x2014;, &#x2014;S&#x2014;, or &#x2014;O&#x2014;; one of Y and Yis hydrogen and the other is OR, &#x2014;C(&#x2550;O)R, NRSORor a heterocyclic group selected from those referred to in the specification; and R, Rand Rare as defined in the specification. 

The invention relates to azabenzothiophenyl compounds of Formula I with anti-cancer and/or anti-inflammatory activity and more specifically to azabenzothiophenyl compounds which inhibit MEK kinase activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth or treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions. 

Aza-benzothiophenyl compounds and methods of use

Growing community of inventors

Cambridge, United Kingdom

John Gary Montana