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公开(公告)号:US11766434B2
公开(公告)日:2023-09-26
申请号:US17244171
申请日:2021-04-29
Applicant: Cancer Research Technology Limited
Inventor: Emma L. Carswell , Mark David Charles , Chukuemeka Tennyson Ekwuru , Frederic Elustondo , Katherine M. Fowler , Gregory R. Ott , Jonathan R. Roffey , Joanna L. Brookfield , Daniel James Ford , Mathew L. Calder
IPC: A61K31/506 , A61K31/437 , A61K31/551 , C07D403/14 , C07D413/14 , C07D417/14 , C07D471/04
CPC classification number: A61K31/506 , A61K31/437 , A61K31/551 , C07D403/14 , C07D413/14 , C07D417/14 , C07D471/04
Abstract: The present invention relates to compounds of formula I as defined herein, and salts and solvates thereof, that function as inhibitors of cell division cycle 7 (Cdc7) kinase enzyme activity. The present invention also relates to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which Cdc7 kinase activity is implicated.
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公开(公告)号:US20220079942A1
公开(公告)日:2022-03-17
申请号:US17244171
申请日:2021-04-29
Applicant: Cancer Research Technology Limited
Inventor: Emma L. Carswell , Mark David Charles , Chukuemeka Tennyson Ekwuru , Frederic Elustondo , Katherine M. Fowler , Gregory R. Ott , Jonathan R. Roffey , Joanna L. Brookfield , Daniel James Ford , Mathew L. Calder
IPC: A61K31/506 , A61K31/437 , A61K31/551 , C07D403/14 , C07D413/14 , C07D417/14 , C07D471/04
Abstract: The present invention relates to compounds of formula I as defined herein, and salts and solvates thereof, that function as inhibitors of cell division cycle 7 (Cdc7) kinase enzyme activity. The present invention also relates to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which Cdc7 kinase activity is implicated.
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公开(公告)号:US10981904B2
公开(公告)日:2021-04-20
申请号:US16402825
申请日:2019-05-03
Applicant: Cancer Research Technology Limited
IPC: C07D417/14
Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, where: Q can be 1,2,4-triazin-3-yl, pyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R1 can be hydrogen, methoxy, trifluoromethoxy, oxetan-3-yl, 3-fluoroazetidin-1-yl, 3-methoxyazetidin-1-yl, or 3,3-difluoroazetidin-1-yl; R2 can be hydrogen or fluoro; R3 can be hydrogen or methoxy; and R4 can be methoxy, ethoxy, or methoxymethyl; provided that when R1 is hydrogen, methoxy or trifluoromethoxy, then R3 is not hydrogen, and/or R4 is methoxymethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
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公开(公告)号:US20190389853A1
公开(公告)日:2019-12-26
申请号:US16402825
申请日:2019-05-03
Applicant: ASTRAZENECA AB , CANCER RESEARCH TECHNOLOGY LIMITED
IPC: C07D417/14
Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, where: Q can be 1,2,4-triazin-3-yl, pyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R1 can be hydrogen, methoxy, trifluoromethoxy, oxetan-3-yl, 3-fluoroazetidin-1-yl, 3-methoxyazetidin-1-yl, or 3,3-difluoroazetidin-1-yl; R2 can be hydrogen or fluoro; R3 can be hydrogen or methoxy; and R4 can be methoxy, ethoxy, or methoxymethyl; provided that when R1 is hydrogen, methoxy or trifluoromethoxy, then R3 is not hydrogen, and/or R4 is methoxymethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
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公开(公告)号:US20170197954A1
公开(公告)日:2017-07-13
申请号:US15314562
申请日:2015-05-27
Applicant: AstraZeneca AB , Cancer Research Technology Limited
Inventor: Maurice Raymond Verschoyle Finlay , Chukuemeka Tennyson Ekwuru , Mark David Charles , Piotr Antoni Raubo , Jonathan James Gordon Winter , Johannes Wilhelmus Maria Nissink
IPC: C07D417/14 , C07B59/00
CPC classification number: C07D417/14 , C07B59/002 , C07B2200/05 , C07B2200/13
Abstract: The specification relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where Q, R, R1 and R2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent GLS1 mediated disease, including cancer. The specification further relates to crystalline forms of compounds of Formula (I) and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating GLS1 kinase mediated disease, including cancer, using such compounds and salts.
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公开(公告)号:US11753405B2
公开(公告)日:2023-09-12
申请号:US17231164
申请日:2021-04-15
Applicant: Cancer Research Technology Limited
IPC: C07D417/14
CPC classification number: C07D417/14
Abstract: A compound of Formula (I):
or a pharmaceutically acceptable salt thereof, where: Q can be 1,2,4-triazin-3-yl, pyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R1 can be hydrogen, methoxy, trifluoromethoxy, oxetan-3-yl, 3-fluoroazetidin-1-yl, 3-methoxyazetidin-1-yl, or 3,3-difluoroazetidin-1-yl; R2 can be hydrogen or fluoro; R3 can be hydrogen or methoxy; and R4 can be methoxy, ethoxy, or methoxymethyl; provided that when R1 is hydrogen, methoxy or trifluoromethoxy, then R3 is not hydrogen, and/or R4 is methoxymethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.-
公开(公告)号:US11020396B2
公开(公告)日:2021-06-01
申请号:US16348073
申请日:2017-11-07
Applicant: Cancer Research Technology Limited
Inventor: Emma L. Carswell , Mark David Charles , Chukuemeka Tennyson Ekwuru , Frederic Elustondo , Katherine M. Fowler , Gregory R. Ott , Jonathan R. Roffey , Joanna L. Brookfield , Daniel James Ford , Mathew L. Calder
IPC: C07D403/14 , A61K31/506 , A61K31/437 , A61K31/551 , C07D413/14 , C07D417/14 , C07D471/04
Abstract: The present invention relates to compounds of formula I as defined herein, and salts and solvates thereof, that function as inhibitors of cell division cycle 7 (Cdc7) kinase enzyme activity. The present invention also relates to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which Cdc7 kinase activity is implicated.
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公开(公告)号:US10323028B2
公开(公告)日:2019-06-18
申请号:US15363030
申请日:2016-11-29
Applicant: AstraZeneca AB , Cancer Research Technology Limited
IPC: C07D417/14
Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, where: Q can be 1,2,4-triazin-3-yl, pyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R1 can be hydrogen, methoxy, trifluoromethoxy, oxetan-3-yl, 3-fluoroazetidin-1-yl, 3-methoxyazetidin-1-yl, or 3,3-difluoroazetidin-1-yl; R2 can be hydrogen or fluoro; R3 can be hydrogen or methoxy; and R4 can be methoxy, ethoxy, or methoxymethyl; provided that when R1 is hydrogen, methoxy or trifluoromethoxy, then R3 is not hydrogen, and/or R4 is methoxymethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
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公开(公告)号:US10294221B2
公开(公告)日:2019-05-21
申请号:US16025455
申请日:2018-07-02
Applicant: AstraZeneca AB , Cancer Research Technology Limited
Inventor: Maurice Raymond Verschoyle Finlay , Chukuemeka Tennyson Ekwuru , Mark David Charles , Piotr Antoni Raubo , Jonathan James Gordon Winter , Johannes Wilhelmus Maria Nissink
IPC: C07D417/14 , C07B59/00
Abstract: The specification relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R, R1 and R2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent GLS1 mediated disease, including cancer. The specification further relates to crystalline forms of compounds of Formula (I) and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating GLS1 kinase mediated disease, including cancer, using such compounds and salts.
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公开(公告)号:US10040788B2
公开(公告)日:2018-08-07
申请号:US15314562
申请日:2015-05-27
Applicant: AstraZeneca AB , Cancer Research Technology Limited
Inventor: Maurice Raymond Verschoyle Finlay , Chukuemeka Tennyson Ekwuru , Mark David Charles , Piotr Antoni Raubo , Jonathan James Gordon Winter , Johannes Wilhelmus Maria Nissink
IPC: C07D417/14 , C07B59/00
Abstract: The specification relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where Q, R, R1 and R2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent GLS1 mediated disease, including cancer. The specification further relates to crystalline forms of compounds of Formula (I) and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating GLS1 kinase mediated disease, including cancer, using such compounds and salts.
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