The Institute of Cancer Research: Royal Cancer Hospital

Deborah Smithen

Caroline Joy Springer

Dan Niculescu-Duvaz

Leo Leung

Richard Marais

Haoran Tang

Mohammed Aljarah

Michael Brown

Cedric Callens

Natalie Miller

Alfonso Zambon

Kiri North

Ben Ayers

This invention relates to compounds useful as lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family member (LOXL1, LOXL2, LOXL3, LOXL4) inhibitors. In addition there are contemplated pharmaceutical compositions comprising the compounds and the use of the compounds in the treatment of conditions mediated by LOX and LOXL, for example cancer. In particular a LOX inhibitor such as the present compounds may be for use in the treatment of a cancer associated with EGFR. The present invention also contemplates the identification of biomarkers that predict responsiveness to a LOX inhibitor.

Lysyl oxidase inhibitors

The disclosure relates to compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein Xand Xis each selected from CRor N; X, Xand Xis each selected from CR, CRor N, provided at least one of X, Xand Xis CRand provided only one of X, X, X, Xand Xcan be N. R, R, R, R, R, L, Land Lare as defined herein. Compounds according to Formula (I) are pharmacologically effective as lysyl oxidase (LOX) inhibitors and are believed to be useful in the treatment of, for instance, cancer.

Hexahydropyrrolo[3,4-c]pyrrole derivatives useful as LOX inhibitors

Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof: wherein W, X, Y, Z, x, R, R, R, x and n are defined in the specification. The compounds are inhibitors of lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family members (LOXL1, LOXL2, LOXL3, LOXL4) and are useful in therapy, particularly in the treatment of cancer. Also disclosed are LOX inhibitors for use in the treatment of a cancer associated with EGFR and biomarkers that predict responsiveness to a LOX inhibitor.

Methylamine derivatives as lysysl oxidase inhibitors for the treatment of cancer

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Sutton, United Kingdom

Deborah Smithen