公开(公告)号：US10995088B2

公开(公告)日：2021-05-04

申请号：US16908487

申请日：2020-06-22

Applicant: The Institute of Cancer Research: Royal Cancer Hospital

Inventor： Caroline Springer ,  Richard Marais ,  Dan Niculescu-Duvaz ,  Leo Leung ,  Deborah Smithen ,  Cedric Callens ,  Haoran Tang

IPC: C07D417/12 ,  A61P35/00 ,  C07D263/46 ,  C07D277/46 ,  C07D277/36 ,  C07D333/18 ,  C07D333/34 ,  C07D409/12 ,  C12Q1/37 ,  C07D277/26

Abstract: Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof: wherein W, X, Y, Z, x, R1, R2, R3, 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.

公开(公告)号：US11608330B2

公开(公告)日：2023-03-21

申请号：US17221549

申请日：2021-04-02

Applicant: The Institute of Cancer Research: Royal Cancer Hospital

Inventor： Caroline Springer ,  Richard Marais ,  Dan Niculescu-Duvaz ,  Leo Leung ,  Deborah Smithen ,  Cedric Callens ,  Haoran Tang

IPC: C07D417/12 ,  A61P35/00 ,  C07D263/46 ,  C07D277/26 ,  C07D277/36 ,  C07D333/18 ,  C07D333/34 ,  C07D409/12 ,  C12Q1/37

Abstract: Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof: wherein W, X, Y, Z, x, R1, R2, R3, 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.

公开(公告)号：US10807974B2

公开(公告)日：2020-10-20

申请号：US15999458

申请日：2017-02-17

Applicant: The Institute of Cancer Research: Royal Cancer Hospital

Inventor： Caroline Springer ,  Richard Marais ,  Dan Niculescu-Duvaz ,  Leo Leung ,  Deborah Smithen ,  Cedric Callens ,  Haoran Tang

IPC: C07D417/12 ,  A61P35/00 ,  C07D333/18 ,  C07D277/26 ,  C12Q1/37 ,  C07D333/34 ,  C07D277/36 ,  C07D263/46 ,  C07D409/12

Abstract: Provided are compounds of the Formula (I), or a pharmaceutically acceptable salt thereof: wherein W, X, Y, Z, x, R1, R2, R3, 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.