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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
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.
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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
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.
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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
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.
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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
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.
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公开(公告)号：US20200216818A1
公开(公告)日：2020-07-09
申请号：US16592187
申请日：2019-10-03
Inventor： Richard Marais , Caroline Springer , Serena Tommasini
IPC: C12N7/00 , C12N9/48 , A61K31/136 , A61K35/768 , A61K47/54 , A61K31/135 , A61K38/48
Abstract: Methods of making vaccinia viruses for gene-directed prodrug therapy are disclosed and their use in the treatment of disease is provided. In particular, the anti-tumour effects of vaccinia viruses that are modified to express a prodrug activating enzyme are disclosed.
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Patent Agency Ranking
6.发明申请公开(公告)号：US20160130564A1
公开(公告)日：2016-05-12
申请号：US14898284
申请日：2014-06-18
Inventor： Richard Marais , Caroline Springer , Serena Tommasini
IPC: C12N7/00 , C12N9/48 , A61K31/136 , A61K35/768 , A61K47/48
CPC classification number: C12N7/00 , A61K31/135 , A61K31/136 , A61K35/768 , A61K38/48 , A61K47/542 , C12N9/485 , C12N2710/24132 , C12N2710/24143 , C12Y304/16 , C12Y304/17021
Abstract: Methods of making vaccinia viruses for gene-directed prodrug therapy are disclosed and their use in the treatment of disease is provided. In particular, the anti-tumor effects of vaccinia viruses that are modified to express a prodrug-activating enzyme are disclosed.
Abstract translation: 公开了用于基因导向的前药治疗的痘苗病毒的方法，并提供其在治疗疾病中的用途。 特别地，公开了修饰以表达前体药物活化酶的痘苗病毒的抗肿瘤作用。
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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
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.
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![Hexahydropyrrolo[3,4-c]pyrrole derivatives useful as LOX inhibitors](/abs-image/US/2024/06/25/US12018029B2/abs.jpg.150x150.jpg)
公开(公告)号：US12018029B2
公开(公告)日：2024-06-25
申请号：US16972335
申请日：2019-06-05
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.
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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
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.
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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
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.
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