Glaxo Group Limited

Glaxosmithkline Intellectual Property Development Limited

Esther Pilar Fernandez Velando

Julia Castro Pichel

Raquel Fernandez Menendez

Silvia Gonzalez Del Valle

David Matthew Wilson

Alfonso Mendoza Losana

Lluis Ballell Pages

Jose-Miguel Coteron Lopez

Jorge Fernandez-Molina

Maria Luisa Leon-Diaz

Araceli Mallo-Rubio

Matthew James Wolfendale

The present invention relates to a compound of Formula (I) having pharmacological activity, processes for its preparation, pharmaceutical compositions and their use in the treatment of certain parasitic certain parasitic protozoal infections such as malaria, in particular infection by. (S)&#x2014;N-(2-fluoropyridin-4-yl)-3-methyl-2-(5-methyl-2,4-dioxo-1,2-dihydropyrido[3,4-d]pyrimidin-3(4H)-yl)butanamide.

Compound (S) and (R)-N-(2-fluoropyridin-4-yl)-3-methyl-2-(5-methyl-2,4-dioxo-1,2-dihydropyrido[3,4-d]pyrimidin-3(4H)-yl)butanamide and use

A compound of Formula (I) or a pharmaceutically acceptable salt thereof: Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR; or X is C and Y is S; Z is selected from N and CH; Ris selected from H and Calkyl; Ris selected from H, Calkyl, OH, &#x2014;CHOH and Calkoxy; Each Ris independently selected from OH, Calkyl, F, Cl, Br, NH, and Calkoxy; Ris selected from Calkyl and haloCalkyl; Ris selected from H, Calkyl and haloCalkyl; Rand Rare either i) each independently selected from H, Calkyl and Calkoxy; or ii) Rand Rtogether with the ring to which they are attached form a 9-membered bicyclic ring; p is 0-3; and Ris selected from H and Calkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.

3-amino-pyrazole derivatives useful against tuberculosis

A compound of Formula (I) or a pharmaceutically acceptable salt thereof: Wherein: Het is a 5 to 10-membered heteroaromatic ring; Either X is N and Y is CR; or X is C and Y is S; Z is selected from N and CH; Ris selected from H and Calkyl; Ris selected from H, Calkyl, OH, &#x2014;CHOH and Calkoxy; Each Ris independently selected from OH, Calkyl, F, Cl, Br, NH, and Calkoxy; Ris selected from Calkyl and haloCalkyl; Ris selected from H, Calkyl and haloCalkyl; Rand Rare either i) each independently selected from H, Calkyl and Calkoxy; or ii) Rand Rtogether with the ring to which they are attached form a 9-membered bicylic ring; p is 0-3; and Ris selected from H and Calkyl, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.

A compound of Formula (I) wherein: either X is N and Y is CRor X is C and Y is S; Z is selected from N and CH; Ris selected from H and Me; Ris selected from H, OH, OMe and Me; each Ris independently selected from Calkyl, F, Cl, Br, CFand NH; Ris selected from Me, CF, NOand CHF; Ris selected from H, Me and CHF; Ris selected from H and Me; and p is 0-3, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.

(Pyrazol-3-yl)-1,3,4-thiadiazol-2-amine and (pyrazol-3-yl)-1,3,4-thiazol-2-amine compounds

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Madrid, Spain

Esther Pilar Fernandez Velando