公开(公告)号：US20190152966A1

公开(公告)日：2019-05-23

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 NICULES-CU-DUVAZ ,  Leo LEUNG ,  Deborah SMITHEN ,  Cedric CALLENS ,  Haoran TANG

IPC: C07D417/12 ,  A61P35/00 ,  C07D333/18 ,  C07D277/26 ,  C12Q1/37

CPC classification number: C07D417/12 ,  A61P35/00 ,  C07D263/46 ,  C07D277/26 ,  C07D277/36 ,  C07D333/18 ,  C07D333/34 ,  C07D409/12 ,  C12Q1/37 ,  C12Y304/21

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：US20210040078A1

公开(公告)日：2021-02-11

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 ,  C07D333/34 ,  C07D277/36 ,  C07D263/46 ,  C07D409/12 ,  A61P35/00 ,  C07D277/26 ,  C07D333/18 ,  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：US20220372028A1

公开(公告)日：2022-11-24

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 ,  C07D333/34 ,  C07D277/36 ,  C07D263/46 ,  C07D409/12 ,  A61P35/00 ,  C07D277/26 ,  C07D333/18 ,  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.