N.v. Organon

Oxford University Innovation Ltd

Merck Sharp + Dohme B.v.

Philip Stephen Jones

David Jonathan Bennett

Jiaqiang Cai

Zoran Rankovic

Christopher Joseph Schofield

Jürgen Brem

Michael Arnold McDonough

Angus John Morrison

John Stephen Robinson

Xavier Fradera

Iain Cumming

Jonathan Gillespie

Anna M Rydzik

Joanne Hewitt

Andrew Pannifer

The present invention relates to certain compounds, in particular, indole derivatives that function as inhibitors of bacterial metallo-beta-lactamases. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of a bacterial infection.

Inhibitors of metallo-beta-lactamases

The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein Ris H or (C)alkyl; Ris halogen or (C)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the S. . . Ssubstites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain. 

1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derivatives

The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.

6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives

The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I wherein each of the substituents is given the definition as set forth in the specification and claims, pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S and/or cathepsin K related diseases such as osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.

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Newhouse, United Kingdom

Philip Stephen Jones