Ucbbiopharma Srl

Astex Therapeutics Limited

Cancer Research Technology Limited

Ucb Biopharma Sprl

The Institute of Cancer Research: Royal Cancer Hospital

The Wellcome Trust Limited

Richard David Taylor

Zhaoning Zhu

Adrian Liam Gill

Malcolm Maccoss

Fabien Claude Lecomte

Martin Alexander Lowe

Gareth Neil Brace

Teresa De Haro Garcia

Miles Stuart Congreve

Andrew Madin

Christopher William Murray

Valerio Berdini

Gordon Saxty

Caroline Joy Springer

Richard Marais

Charlotte Mary Griffiths-Jones

Michael Alistair O'Brien

Maria Grazia Carr

Gilbert Besong

Matthew Duncan Selby

James Thomas Reuberson

Elizabeth Pearl Jones

Anne Marie Foley

Emma Vickerstaffe

Gregory Foulkes

Owen Callaghan

Rajdeep Kaur Nijjar

Andrew Pike

Esteban Roman Vela

Terence Seward Baker

Dan Niculescu-Duvaz

Ion Niculescu-Duvaz

Delphine Menard

Joanna Rachel Quincey

Helen Tracey Horsley

Xiaofeng Liu

Harmen Dijkstra

Robert James Townsend

Michael Alistair O'brien

Hervé Jean Claude Deboves

Monika-Sarah Elisabeth Dorothea Schulze

Rebecca Louise Charlton

Catherine Gaulon

Rose Elizabeth Bardell-Cox

James Richard Frost

Rose Elizabeth Chappell

Monika-Sarah Elizabeth Dorothea Schulze

Adam Peter Smalley

Trevor Morgan

Wei Tsung Yau

Lloyd Malcolm King

Jiye Shi

Paul Jonathan Hickford

Richard Malcolm Marais

Herv Jean Claude Deboves

Gilbert Ebai Besong

A series of substituted fused bicyclic imidazole derivatives, including imidazo[1,2-a]pyridine derivatives and analogues thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.

Imidazopyridine derivatives as IL-17 modulators

Computer-implemented methods of designing an antibody that will bind to a target epitope are disclosed. In one arrangement, the method comprises identifying one or more hotspot residues that will each bind to a corresponding one of one or more hotspot sites on the target epitope. Candidate antibody structures are selected from a database such that characteristic atoms within the antibody structure and hotspot characteristic atoms can be superimposed computationally with an averaged spatial deviation less than a predetermined threshold. A designed antibody is generated by replacing matching residues with different residues such that a predicted affinity is increased.

De novo antibody design

The application relates to a series of 2-imino-6-methylhexahydropyrimidin-4-one derivatives and 3-imino-5-methyl-1,2,4-thiadiazinane 1,1-dioxide derivatives of formula (I), substituted by an arylaminophenyl or heteroarylaminophenyl moiety. The compounds are potent inhibitors of the growth and propagation of theparasite in human blood and thus useful as pharmaceutical agents for the treatment of malaria. 

Antimalarial hexahydropyrimidine analogues

A series of substituted fused bicyclic imidazole derivatives, including benzimidazole derivatives and analogues thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders.

Fused imidazole derivatives as IL-17 modulators

A series of 2-imino-6-methyltetrahydropyrimidin-4(1H)-one derivatives, substituted in the 6-position by a phenyl moiety which in turn is meta-substituted by an optionally substituted unsaturated fused bicyclic ring system containing at least one nitrogen atom, being selective inhibitors of plasmepsin V activity, are beneficial as pharmaceutical agents, especially in the treatment of malaria.

Iminotetrahydropyrimidinone derivatives as plasmepsin V inhibitors

A series of substituted spirocyclic 2-oxoindoline derivatives, and analogues thereof, being potent modulators of human IL-17 activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including inflammatory and autoimmune disorders. 

Spirocyclic indolines as IL-17 modulators

A series of 3-imino-5-methyl-1,2,4-thiadiazinane 1,1-dioxide derivatives of formula (I), substituted in the 5-position by a phenyl moiety NH which in turn is meta-substituted by an optionally substituted fused bicyclic heteroaromatic ring system containing at least one nitrogen atom, being selective inhibitors of plasmepsin V activity, are beneficial as pharmaceutical agents, especially in the treatment of malaria. 

Iminothiadiazinane dioxide derivatives as plasmepsin V inhibitors

The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.

Bicyclic heterocyclic compounds as FGFR inhibitors

The invention relates to new bicyclic heterocyclic derivative compounds of Formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. The compounds of Formula (I) are inhibitors of FGFR, VEGFR or PDGFR.

Imidazo[1,2-a]pyridine compounds for use in treating cancer

The present invention pertains to certain 6-carboaryloxy-pyrazin-2-yl-carboaryl-amines of the following formula, and pharmaceutically acceptable salts thereof, which, inter alia, inhibit RAF (e.g., B-RAF) activity, inhibit cell proliferation, treat cancer, etc., wherein Q is independently &#x2014;N&#x2550;; Ris independently a group of the formula -J-L-Z; -JL-Z is independently &#x2014;NH&#x2014;Z; Z is independently Ccarboaryl and is independently unsubstituted or substituted; Ris independently &#x2014;H; Ris independently a group of the formula &#x2014;W&#x2014;Y; W is independently &#x2014;O&#x2014;; Y is independently Ccarboaryl and is independently unsubstituted or substituted; and Ris independently &#x2014;H. The present invention also pertains to pharmaceutical compositions comprising such compounds. 

6-carboaryl-oxy-pyrazin-2-yl-carboaryl-amines and compositions comprising said compounds

The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B-RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formula (I): wherein: J is independently &#x2014;O&#x2014; or &#x2014;NR&#x2014;; R, if present, is independently &#x2014;H or a substituent; Ris independently &#x2014;H or a substituent; Y is independently &#x2014;CH&#x2550; or &#x2014;N&#x2550;; Q is independently &#x2014;(CH)&#x2014;M&#x2014;(CH)&#x2014; wherein: j is independently 0, 1 or 2; k is independently 0, 1, or 2; j+k is 0, 1, or 2; M is independently &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;NH&#x2014;, &#x2014;NMe&#x2014;, or &#x2014;CH&#x2014;; each of R, R, R, and Ris independently &#x2014;H or a substituent; and additionally Rand Rtaken together may be &#x2014;CH&#x2550;CH&#x2014;CH&#x2550;CH&#x2014;; L is independently: a linker group formed by a chain of 2, 3, or 4 linker moieties; each linker moiety is independently &#x2014;CH&#x2014;, &#x2014;NR&#x2014;, &#x2014;C(&#x2550;X)&#x2014;, or &#x2014;S(&#x2550;O)&#x2014;; exactly one linker moiety is &#x2014;NR&#x2014;, or: exactly two linker moieties are &#x2014;NR&#x2014;; exactly one linker moiety is &#x2014;C(&#x2550;X)&#x2014;, and no linker moiety is &#x2014;S(&#x2550;O)&#x2014;; or: exactly one linker moiety is &#x2014;S(&#x2550;O)&#x2014;, and no linker moiety is &#x2014;C(&#x2550;X)&#x2014;; no two adjacent linker moieties are &#x2014;NR&#x2014;; X is independently &#x2550;O or &#x2550;S; each Ris independently &#x2014;H or a substituent; A is independently: Ccarboaryl, Cheteroaryl, Ccarbocyclic, Cheterocyclic; and is independently unsubstituted or substituted; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. 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 RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc. 

Imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof as therapeutic compounds

Growing community of inventors

Slough, United Kingdom

Richard David Taylor