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公开(公告)号：US20220289757A1
公开(公告)日：2022-09-15
申请号：US17712541
申请日：2022-04-04
发明人： Richard Marais , Caroline Springer , Dan Niculescu-Duvaz , Natalie Miller , Mohammed Aljarah , Alfonso Zambon , Leo Leung , Deborah Smithen , Michael Brown , Haoran Tang
IPC分类号： C07D487/08 , A61P35/00
摘要： 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.
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公开(公告)号：US20200331922A1
公开(公告)日：2020-10-22
申请号：US16755739
申请日：2018-10-12
发明人： Richard Marais , Caroline Springer , Dan Niculescu-Duvaz , Natalie Miller , Mohammed Aljarah , Alfonso Zambon , Leo Leung , Deborah Smithen , Michael Brown , Haoran Tang
IPC分类号： C07D487/08 , A61P35/00
摘要： 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.
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公开(公告)号：US11608330B2
公开(公告)日：2023-03-21
申请号：US17221549
申请日：2021-04-02
发明人： Caroline Springer , Richard Marais , Dan Niculescu-Duvaz , Leo Leung , Deborah Smithen , Cedric Callens , Haoran Tang
IPC分类号： C07D417/12 , A61P35/00 , C07D263/46 , C07D277/26 , C07D277/36 , C07D333/18 , C07D333/34 , C07D409/12 , C12Q1/37
摘要： 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.
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公开(公告)号：US10807974B2
公开(公告)日：2020-10-20
申请号：US15999458
申请日：2017-02-17
发明人： Caroline Springer , Richard Marais , Dan Niculescu-Duvaz , Leo Leung , Deborah Smithen , Cedric Callens , Haoran Tang
IPC分类号： C07D417/12 , A61P35/00 , C07D333/18 , C07D277/26 , C12Q1/37 , C07D333/34 , C07D277/36 , C07D263/46 , C07D409/12
摘要： 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.
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公开(公告)号：US12060360B2
公开(公告)日：2024-08-13
申请号：US17712541
申请日：2022-04-04
发明人： Richard Marais , Caroline Springer , Dan Niculescu-Duvaz , Natalie Miller , Mohammed Aljarah , Alfonso Zambon , Leo Leung , Deborah Smithen , Michael Brown , Haoran Tang
IPC分类号： C07D471/08 , A61K31/439 , A61P35/00 , C07D487/08
CPC分类号： C07D487/08 , A61P35/00
摘要： 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.
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公开(公告)号：US11325915B2
公开(公告)日：2022-05-10
申请号：US16755739
申请日：2018-10-12
发明人： Richard Marais , Caroline Springer , Dan Niculescu-Duvaz , Natalie Miller , Mohammed Aljarah , Alfonso Zambon , Leo Leung , Deborah Smithen , Michael Brown , Haoran Tang
IPC分类号： C07D471/08 , A61K31/439 , A61P35/00 , C07D487/08
摘要： 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.
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公开(公告)号：US10995088B2
公开(公告)日：2021-05-04
申请号：US16908487
申请日：2020-06-22
发明人： Caroline Springer , Richard Marais , Dan Niculescu-Duvaz , Leo Leung , Deborah Smithen , Cedric Callens , Haoran Tang
IPC分类号： C07D417/12 , A61P35/00 , C07D263/46 , C07D277/46 , C07D277/36 , C07D333/18 , C07D333/34 , C07D409/12 , C12Q1/37 , C07D277/26
摘要： 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.
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