University of Dundee

Medivir Ab

Merck Patent Gmbh

Glaxosmithkline Intellectual Property Development Limited

Ian Gilbert

Neil Norcross

Gian Filippo Ruda

Stephen Brand

Nils-Gunnar Johansson

Corinne Nguyen

Ganasan Kasinathan

Alessandro Schipani

Dolores Gonzalez Pacanowska

Laura Cleghorn

Paul Graham Wyatt

Stephen Thompson

Victoria Smith

Tracy Bayliss

Justin Harrison

Ruth Brenk

Christopher Walpole

Jeremy Besnard

Timothy James Miles

Susan Davis

Michael George Thomas

Andrew Lee Hopkins

Maria Marco Martin

Lars Henrik Sandberg

Eun Jung Ko

Beatriz Baragana Ruibal

Achim Porzelle

Elisabet Viayna Gaza

Keren Abecassis

Barbara Forte

Chimed Jansen

Beatriz Baragana

The present invention relates to a novel class of chromene-2-carboxamide compounds inhibitors of general formula I wherein R, R, R, R, R, R, R, Rand X are as defined herein, to their use in medicine, and their use as anti-infective agents in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes.

Anti-infective agents

A compound of Formula (I), or a salt thereof, compositions comprising the compound, processes for its preparation and its use in therapy, for example in the treatment of parasitic diseases such as Chagas disease, Human African Trypanosomiasis (HAT) and leishmaniasis, particularly visceral leishmaniasis (VL).

Imidazo[1,2-B][1,2,4]triazine derivatives as antiparasitic agents

The present invention relates to N-heterocyclic sulphonamide compounds, in particular pyrazole sulphonamide compounds, and their use as N-myristoyl transferase inhibitors.

N-myristoyl transferase inhibitors

The present invention relates to a novel class of quinolone-4-carboxamide Pf3D7 inhibitors of general formula (I) (Formula (I)) wherein R, R, R, R, R, R, R, Rand X are as defined herein, to their use in medicine, and in the treatment of malaria in particular, to compositions containing them, to processes for their preparation and to intermediates used in such processes. 

Anti-malarial agents

The invention relates to morpholino-derivatives according to Formula (I) or stereoisomers or pharmaceutically acceptable salts or solvate thereof, wherein R, R, R, R, R, R, R, R, R, m and n are as defined in the specification. The compounds are antagonists, reverse agonists or agonists of G-protein coupled receptors, such as dopamine D4 and 5HT1a. The inventions also relates to pharmaceutical compositions comprising the compounds and methods involving the compounds and compositions. The compounds and compositions of the invention may in particular be used in the treatment of diseases and disorders, such as neurological and neurodegenerative diseases; or as lead compounds for the design and selection of further therapeutic compounds. 

Morpholino compounds, uses and methods

Deoxyuridine derivatives of the formula where

Dutpase inhibitors

Deoxyuridine derivatives of the formula (I) where Ris H or various substituents; D is &#x2014;NHCO&#x2014;, &#x2014;CONH&#x2014;, -0-, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;CH&#x2550;CH, &#x2014;C&#x2261;C&#x2014;, &#x2014;NR&#x2014;; Ris hydrogen or various substituents; Ris H, C-Calkyl, C-Calkanoyl; E is Si or C; R, Rand Rare independently selected from C-Calkyl, C-Calkenyl, C-Calkynyl or a stable monocyclic, bicyclic or tricyclic ring system; G is &#x2014;O&#x2014;, &#x2014;S&#x2014;, &#x2014;CHR&#x2014;, &#x2014;C(&#x2550;O)&#x2014;; J is &#x2014;CH&#x2014;, or when G is CHRmay also be &#x2014;O&#x2014; or &#x2014;NH&#x2014;; Ris H, F, &#x2014;CH, &#x2014;CHNH, &#x2014;CHOH; &#x2014;OHRis H, F, &#x2014;CH, &#x2014;CHNH, &#x2014;CHOH, &#x2014;CH(OH)CH, CH(NH)CH; or Rand Rtogether define an olefinic bond, or together form a &#x2014;CH-group, thereby defining a cis or trans cyclopropyl group; have utility in the prophylaxis or treatment of protozoal diseases such as malaria. 

DUTPase inhibitors

Deoxyuridine derivatives of Formula (I'); where A is O, S or CH; B is O, S or CHR; Ris H, or various substituents; Ris H, F; Ris H, F, OH, NH; or Rand Rtogether form a chemical bond; D is &#x2014;NHCO&#x2014;, &#x2014;CONH&#x2014;, &#x2014;O&#x2014;, &#x2014;C(&#x2550;O)&#x2014;, &#x2014;CH&#x2550;CH, &#x2014;C&#x2261;C&#x2014;, &#x2014;NR&#x2014;; Ris hydrogen or various substituents; Ris H, C-Calkyl, C-Calkanoyl; E is Si or C; R, Rand Rare independently selected from C-Calkyl, C-Calkenyl, C-Calkynyl, or a stable monocyclic, bicyclic or tricyclic ring system have utility in the prophylaxis of treatment of parasitic diseases such as malaria. 

Dutpase Inhibitors

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Dundee, United Kingdom

Ian Gilbert