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公开(公告)号：US10407446B2
公开(公告)日：2019-09-10
申请号：US15846679
申请日：2017-12-19
Applicant: AstraZeneca AB , Cancer Research Technology Limited
IPC: A61K31/522 , C07D473/32 , C07D519/00 , C07D473/18 , A61P35/00 , A61K31/502 , A61K45/06
Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where 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 DNA-PK mediated disease, including cancer. The specification further relates to 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 DNA-PK mediated disease, including cancer, using such compounds and salts.
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公开(公告)号：US10040789B2
公开(公告)日：2018-08-07
申请号：US15362989
申请日：2016-11-29
Applicant: AstraZeneca AB , Cancer Research Technology Limited
Inventor： David Robert Perkins , Maurice Raymond Verschoyle Finlay , Johannes Wilhelmus Maria Nissink , Piotr Antoni Raubo , Peter Duncan Smith , Andrew Bailey
IPC: C07D417/14 , A61K31/433 , A61K31/501
Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, is described. Q can be pyridazin-3-yl, 6-fluoropyridazin-3-yl; R1 can be H; R2 and R3 can each independently be C1-C6 alkyl, or R2 and R3 taken together are —(CH2)3—; or R1 and R2 taken together can be —(CH2)2— and R3 can be —CH3; R4 halo, —CH3, —OCH3, —OCHF2, —OCF3, or —CN; and n can be 0, 1, or 2. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
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公开(公告)号：US10196382B2
公开(公告)日：2019-02-05
申请号：US15360332
申请日：2016-11-23
Applicant: AstraZeneca AB , Cancer Research Technology Limited
Inventor： Maurice Raymond Verschoyle Finlay
IPC: C07D403/14
Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, where R1 can be hydro, methoxy, difluoromethoxy or trifluoromethoxy; R2 can be hydro, methoxy, trifluoromethoxy or trifluoromethyl; and R3 can be hydro or methoxy. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
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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：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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Patent Agency Ranking
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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公开(公告)号：US20170152254A1
公开(公告)日：2017-06-01
申请号：US15363018
申请日：2016-11-29
Applicant: AstraZeneca AB , Cancer Research Technology Limited
Inventor： Johannes Wilhelmus Maria Nissink , Maurice Raymond Verschoyle Finlay , Mark David Charles , Matt Wood
IPC: C07D417/14
CPC classification number: C07D417/14 , A61K31/501 , A61K31/53
Abstract: A compound of Formula (I): or a pharmaceutically acceptable salt thereof, where: Q can be 5-methylpyridazin-3-yl, 5-chloropyridazin-3-yl, 6-methylpyridazin-3-yl, or 6-fluoropyridazin-3-yl; R can be hydrogen, fluoro, or methoxy; R1 can be hydrogen, methoxy, difluoromethoxy, or trifluoromethoxy; and R2 can be methyl or ethyl. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
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公开(公告)号：US20210246131A1
公开(公告)日：2021-08-12
申请号：US17231164
申请日：2021-04-15
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：US20190169172A1
公开(公告)日：2019-06-06
申请号：US16266361
申请日：2019-02-04
Applicant: AstraZeneca AB , Cancer Research Technology Limited
Inventor： Maurice Raymond Verschoyle Finlay
IPC: C07D403/14
Abstract: A compound of Formula (I): or a pharmaceutically where R1 can be hydro, methoxy, difluoromethoxy or trifluoromethoxy; R2 can be hydro, methoxy, trifluoromethoxy or trifluoromethyl; and R3 can be hydro or methoxy. The compound of formula (I) can inhibit glutaminase, e.g., GLS1.
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