公开(公告)号：US20220289757A1

公开(公告)日：2022-09-15

申请号：US17712541

申请日：2022-04-04

Applicant: The Institute of Cancer Research: Royal Cancer Hospital

Inventor： Richard Marais ,  Caroline Springer ,  Dan Niculescu-Duvaz ,  Natalie Miller ,  Mohammed Aljarah ,  Alfonso Zambon ,  Leo Leung ,  Deborah Smithen ,  Michael Brown ,  Haoran Tang

IPC: C07D487/08 ,  A61P35/00

Abstract: 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.

公开(公告)号：US20200331922A1

公开(公告)日：2020-10-22

申请号：US16755739

申请日：2018-10-12

Applicant: The Institute of Cancer Research: Royal Cancer Hospital

Inventor： Richard Marais ,  Caroline Springer ,  Dan Niculescu-Duvaz ,  Natalie Miller ,  Mohammed Aljarah ,  Alfonso Zambon ,  Leo Leung ,  Deborah Smithen ,  Michael Brown ,  Haoran Tang

IPC: C07D487/08 ,  A61P35/00

Abstract: 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.

公开(公告)号：US12060360B2

公开(公告)日：2024-08-13

申请号：US17712541

申请日：2022-04-04

Applicant: The Institute of Cancer Research: Royal Cancer Hospital

Inventor： Richard Marais ,  Caroline Springer ,  Dan Niculescu-Duvaz ,  Natalie Miller ,  Mohammed Aljarah ,  Alfonso Zambon ,  Leo Leung ,  Deborah Smithen ,  Michael Brown ,  Haoran Tang

IPC: C07D471/08 ,  A61K31/439 ,  A61P35/00 ,  C07D487/08

CPC classification number: C07D487/08 ,  A61P35/00

Abstract: 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.

公开(公告)号：US12018029B2

公开(公告)日：2024-06-25

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: A61P35/00 ,  C07D487/04

CPC classification number: 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.

公开(公告)号：US11325915B2

公开(公告)日：2022-05-10

申请号：US16755739

申请日：2018-10-12

Applicant: The Institute of Cancer Research: Royal Cancer Hospital

Inventor： Richard Marais ,  Caroline Springer ,  Dan Niculescu-Duvaz ,  Natalie Miller ,  Mohammed Aljarah ,  Alfonso Zambon ,  Leo Leung ,  Deborah Smithen ,  Michael Brown ,  Haoran Tang

IPC: C07D471/08 ,  A61K31/439 ,  A61P35/00 ,  C07D487/08

Abstract: 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.