JP2019517491A5 - - Google Patents
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- JP2019517491A5 JP2019517491A5 JP2018562564A JP2018562564A JP2019517491A5 JP 2019517491 A5 JP2019517491 A5 JP 2019517491A5 JP 2018562564 A JP2018562564 A JP 2018562564A JP 2018562564 A JP2018562564 A JP 2018562564A JP 2019517491 A5 JP2019517491 A5 JP 2019517491A5
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- Prior art keywords
- cancer
- alkyl
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- halo
- cyano
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- -1 cyano, hydroxyl Chemical group 0.000 claims 31
- 125000005843 halogen group Chemical group 0.000 claims 30
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 25
- 125000004093 cyano group Chemical group *C#N 0.000 claims 24
- 206010028980 Neoplasm Diseases 0.000 claims 22
- 125000003118 aryl group Chemical group 0.000 claims 22
- 239000003112 inhibitor Substances 0.000 claims 21
- 102100038970 Histone-lysine N-methyltransferase EZH2 Human genes 0.000 claims 19
- 101000882127 Homo sapiens Histone-lysine N-methyltransferase EZH2 Proteins 0.000 claims 19
- 229940076838 Immune checkpoint inhibitor Drugs 0.000 claims 19
- 102000037984 Inhibitory immune checkpoint proteins Human genes 0.000 claims 19
- 108091008026 Inhibitory immune checkpoint proteins Proteins 0.000 claims 19
- 201000011510 cancer Diseases 0.000 claims 19
- 239000012274 immune-checkpoint protein inhibitor Substances 0.000 claims 19
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 18
- 239000000203 mixture Substances 0.000 claims 18
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 17
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 17
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 14
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 13
- 125000005842 heteroatom Chemical group 0.000 claims 9
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims 8
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 8
- 229910052799 carbon Inorganic materials 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 7
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 7
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 6
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- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 2
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- 125000000217 alkyl group Chemical group 0.000 claims 2
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- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
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- 229940121656 pd-l1 inhibitor Drugs 0.000 claims 2
- GJVFBWCTGUSGDD-UHFFFAOYSA-L pentamethonium bromide Chemical compound [Br-].[Br-].C[N+](C)(C)CCCCC[N+](C)(C)C GJVFBWCTGUSGDD-UHFFFAOYSA-L 0.000 claims 2
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- OVSQVDMCBVZWGM-QSOFNFLRSA-N quercetin 3-O-beta-D-glucopyranoside Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C(C=2C=C(O)C(O)=CC=2)OC2=CC(O)=CC(O)=C2C1=O OVSQVDMCBVZWGM-QSOFNFLRSA-N 0.000 claims 2
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- 125000000582 cycloheptyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662344338P | 2016-06-01 | 2016-06-01 | |
| US62/344,338 | 2016-06-01 | ||
| PCT/US2017/035391 WO2017210395A1 (en) | 2016-06-01 | 2017-06-01 | Use of ezh2 inhibitors for treating cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019517491A JP2019517491A (ja) | 2019-06-24 |
| JP2019517491A5 true JP2019517491A5 (https=) | 2020-07-09 |
| JP7121660B2 JP7121660B2 (ja) | 2022-08-18 |
Family
ID=60477941
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018562564A Active JP7121660B2 (ja) | 2016-06-01 | 2017-06-01 | 癌を処置するためのｅｚｈ２阻害剤の使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US11786533B2 (https=) |
| EP (1) | EP3464643A4 (https=) |
| JP (1) | JP7121660B2 (https=) |
| AU (1) | AU2017273726B2 (https=) |
| CA (1) | CA3025933A1 (https=) |
| WO (1) | WO2017210395A1 (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3363B1 (ar) | 2011-04-13 | 2019-03-13 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| CA2887243C (en) | 2012-10-15 | 2024-04-09 | Epizyme, Inc. | Methods of treating cancer |
| WO2017210395A1 (en) | 2016-06-01 | 2017-12-07 | Epizyme, Inc. | Use of ezh2 inhibitors for treating cancer |
| EP3471830A4 (en) | 2016-06-17 | 2020-02-26 | Epizyme Inc | EZH2 INHIBITORS TO TREAT CANCER |
| EP3548032A2 (en) * | 2016-12-02 | 2019-10-09 | Epizyme, Inc. | Combination therapy for treating cancer |
| US10266542B2 (en) | 2017-03-15 | 2019-04-23 | Mirati Therapeutics, Inc. | EZH2 inhibitors |
| US11642346B2 (en) | 2017-03-31 | 2023-05-09 | Epizyme, Inc. | Combination therapy for treating cancer |
| EP3630080A4 (en) * | 2017-06-02 | 2021-03-10 | Epizyme, Inc. | USE OF EZH2 INHIBITORS TO TREAT CANCER |
| WO2019050924A1 (en) | 2017-09-05 | 2019-03-14 | Epizyme, Inc. | POLY THERAPY FOR THE TREATMENT OF CANCER |
| MX2020007974A (es) | 2018-01-31 | 2020-09-07 | Mirati Therapeutics Inc | Inhibidores de complejo represivo polycomb 2 (prc2). |
| US20210260051A1 (en) * | 2018-06-14 | 2021-08-26 | Board Of Regents, The University Of Texas System | Combination of ezh2 inhibitor and checkpoint therapy for the treatment of cancer |
| US12421228B2 (en) | 2019-04-22 | 2025-09-23 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as PRC2 inhibitors |
| EP3980422A1 (en) | 2019-06-05 | 2022-04-13 | Mirati Therapeutics, Inc. | Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer |
| WO2021063331A1 (zh) * | 2019-09-30 | 2021-04-08 | 江苏恒瑞医药股份有限公司 | EZH2抑制剂与含有TGF-β受体的融合蛋白联合在制备治疗肿瘤的药物中的用途 |
| EP4053122B1 (en) | 2019-10-31 | 2024-10-09 | Daegu-Gyeongbuk Medical Innovation Foundation | Compound comprising ezh2 inhibitor and e3 ligase binder and pharmaceutical composition for preventing or treating ezh2-associated disease comprising same as active ingredient |
| CN111303133A (zh) * | 2020-03-25 | 2020-06-19 | 清华大学 | 降解ezh2蛋白的小分子化合物 |
| WO2022140661A1 (en) * | 2020-12-23 | 2022-06-30 | Cascade Prodrug Inc. | Combination therapy with a vinca alkaloid n-oxide and an immune checkpoint inhibitor |
| CN119136808A (zh) * | 2022-12-30 | 2024-12-13 | 清华大学 | 药物组合物及其应用 |
| KR20260030731A (ko) * | 2023-05-12 | 2026-03-06 | 타이페이 메디컬 유니이버시티 | Ezh2-hsp90 이중 억제제 |
Family Cites Families (48)
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|---|---|---|---|---|
| GB2482903A (en) * | 2010-08-19 | 2012-02-22 | Software Imaging Technology Ltd | A print engine |
| US9175331B2 (en) * | 2010-09-10 | 2015-11-03 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
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-
2017
- 2017-06-01 WO PCT/US2017/035391 patent/WO2017210395A1/en not_active Ceased
- 2017-06-01 CA CA3025933A patent/CA3025933A1/en active Pending
- 2017-06-01 US US16/306,182 patent/US11786533B2/en active Active
- 2017-06-01 EP EP17807460.5A patent/EP3464643A4/en not_active Withdrawn
- 2017-06-01 AU AU2017273726A patent/AU2017273726B2/en not_active Expired - Fee Related
- 2017-06-01 JP JP2018562564A patent/JP7121660B2/ja active Active
-
2023
- 2023-09-06 US US18/462,229 patent/US20240139203A1/en not_active Abandoned
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