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：US20220017516A1

公开(公告)日：2022-01-20

申请号：US17293970

申请日：2019-11-15

Applicant: THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL

Inventor： Mohammed ALJARAH ,  Dan NICULESCU-DUVAZ ,  Leo LEUNG ,  Deborah SMITHEN ,  Michael BROWN ,  Lawrence Christopher DAVIES ,  Caroline SPRINGER

IPC: C07D471/08 ,  C07D487/08 ,  C07D295/088 ,  C07D487/04 ,  C07D239/48 ,  C07D295/108 ,  C07D487/10 ,  A61P35/00

Abstract: The disclosure relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, Formula (I) 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.

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.

公开(公告)号：US20210238179A1

公开(公告)日：2021-08-05

申请号：US16972335

申请日：2019-06-05

Applicant: THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL

Inventor： Leo LEUNG ,  Kiri NORTH ,  Deborah SMITHEN ,  Mohammed ALJARAH ,  Michael BROWN ,  Ben AYERS ,  Dan NICULESCU-DUVAZ ,  Caroline SPRINGER

IPC: C07D487/04 ,  A61P35/00

Abstract: The disclosure relates to compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein X1 and X5 is each selected from CR1 or N; X2, X3 and X4 is each selected from CR1, CR2 or N, provided at least one of X2, X3 and X4 is CR2 and provided only one of X1, X2, X3, X4 and X5 can be N. R1, R2, R3, R4, R5, L1, L2 and L3 are 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.