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
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- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 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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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 (enExample) | 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 (enExample) |
| EP (1) | EP3464643A4 (enExample) |
| JP (1) | JP7121660B2 (enExample) |
| AU (1) | AU2017273726B2 (enExample) |
| CA (1) | CA3025933A1 (enExample) |
| WO (1) | WO2017210395A1 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3438B1 (ar) | 2011-04-13 | 2019-10-20 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| MX376008B (es) | 2012-10-15 | 2025-03-07 | Epizyme Inc | Inhibidor de ezh2 para usarse en el tratamiento de sarcoma epiteloide. |
| CA3025933A1 (en) | 2016-06-01 | 2017-12-07 | Epizyme, Inc. | Use of ezh2 inhibitors for treating cancer |
| JP2019521988A (ja) | 2016-06-17 | 2019-08-08 | エピザイム，インコーポレイティド | 癌を処置するためのｅｚｈ２阻害剤 |
| WO2018102687A2 (en) * | 2016-12-02 | 2018-06-07 | 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 |
| JP2020522687A (ja) * | 2017-06-02 | 2020-07-30 | エピザイム，インコーポレイティド | 癌を処置するためのｅｚｈ２阻害剤の使用 |
| EP3678663A4 (en) * | 2017-09-05 | 2021-06-02 | Epizyme, Inc. | POLYTHERAPY FOR CANCER TREATMENT |
| PT4043466T (pt) | 2018-01-31 | 2024-10-14 | Mirati Therapeutics Inc | Inibidores de prc2 |
| WO2019241742A1 (en) * | 2018-06-14 | 2019-12-19 | Board Of Regents, The University Of Texas System | Combination of ezh2 inhibitor and checkpoint therapy for the treatment of cancer |
| EP3959214A1 (en) | 2019-04-22 | 2022-03-02 | 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 |
| EP4267136A4 (en) * | 2020-12-23 | 2025-02-05 | Cascade Prodrug Inc. | Combination therapy with a vinca alkaloid n-oxide and an immune checkpoint inhibitor |
| EP4643863A1 (en) * | 2022-12-30 | 2025-11-05 | Tsinghua University | Pharmaceutical composition and use thereof |
| WO2024238381A1 (en) * | 2023-05-12 | 2024-11-21 | Taipei Medical University | Dual ezh2-hsp90 inhibitors |
Family Cites Families (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| PL2614369T3 (pl) * | 2010-09-10 | 2016-08-31 | Epizyme Inc | Sposób określania przydatności inhibitorów ludzkiego ezh2 w leczeniu |
| JP2014511389A (ja) | 2011-02-28 | 2014-05-15 | エピザイム インコーポレイテッド | 置換６，５−縮合二環式ヘテロアリール化合物 |
| TW201733984A (zh) | 2011-04-13 | 2017-10-01 | 雅酶股份有限公司 | 經取代之苯化合物 |
| JO3438B1 (ar) * | 2011-04-13 | 2019-10-20 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| EP2825161B1 (en) | 2012-03-12 | 2019-01-02 | Epizyme, Inc. | Inhibitors of human ezh2, and methods of use thereof |
| CN104768555B (zh) | 2012-04-13 | 2018-10-30 | Epizyme股份有限公司 | 用于治疗癌症的联合治疗 |
| PL3628670T3 (pl) * | 2012-04-13 | 2023-02-20 | Epizyme, Inc. | Postać soli dla inhibicji ezh2 |
| US9856320B2 (en) | 2012-05-15 | 2018-01-02 | Bristol-Myers Squibb Company | Cancer immunotherapy by disrupting PD-1/PD-L1 signaling |
| CN104756597A (zh) * | 2012-08-06 | 2015-07-01 | 美国博通公司 | 与自主拒绝禁止机制的改进相关的设备、方法、和计算机程序产品 |
| US20140062720A1 (en) * | 2012-09-06 | 2014-03-06 | John Murray Spruth | Remote Pipeline Corrosion Protection and Valve Monitoring Apparatus |
| MX376008B (es) | 2012-10-15 | 2025-03-07 | Epizyme Inc | Inhibidor de ezh2 para usarse en el tratamiento de sarcoma epiteloide. |
| SG10201705989YA (en) | 2012-10-15 | 2017-08-30 | Epizyme Inc | Substituted benzene compounds |
| US20150283142A1 (en) * | 2013-03-15 | 2015-10-08 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| WO2014100080A1 (en) * | 2012-12-19 | 2014-06-26 | Glaxosmithkline Llc | Combination |
| CA2894222A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | 1,4-pyridone bicyclic heteroaryl compounds |
| AU2013361060B2 (en) | 2012-12-21 | 2018-04-19 | Epizyme, Inc. | 1,4-pyridone compounds |
| US20160031907A1 (en) | 2013-03-15 | 2016-02-04 | Epizyme, Inc. | Substituted Benzene Compounds |
| US9776996B2 (en) | 2013-03-15 | 2017-10-03 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| US20160084839A1 (en) | 2013-04-02 | 2016-03-24 | Marisa Dolled-Filhart | Immunohistochemical assay for detecting expression of programmed death ligand 1 (pd-l1) in tumor tissue |
| WO2015010049A1 (en) | 2013-07-19 | 2015-01-22 | Epizyme, Inc. | Substituted benzene compounds |
| EP3022195A2 (en) | 2013-07-19 | 2016-05-25 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| SI3057962T1 (sl) | 2013-10-16 | 2024-01-31 | Epizyme, Inc. | Oblika hidrokloridne soli za ezh2 inhibicijo |
| AU2014337121A1 (en) | 2013-10-18 | 2016-04-14 | Epizyme, Inc. | Method of treating cancer |
| KR20220165809A (ko) | 2013-12-06 | 2022-12-15 | 에피자임, 인코포레이티드 | 암 치료를 위한 병용 요법 |
| US20150320754A1 (en) | 2014-04-16 | 2015-11-12 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| PL3157527T3 (pl) | 2014-06-17 | 2023-08-07 | Epizyme, Inc. | Inhibitory ezh2 do leczenia chłoniaka |
| EP3160940A4 (en) | 2014-06-25 | 2018-05-02 | Epizyme, Inc. | Substituted benzene and 6,5-fused bicyclic heteroaryl compounds |
| CA2963149A1 (en) * | 2014-10-16 | 2016-04-21 | Epizyme, Inc. | Method for treating cancer |
| HUE062159T2 (hu) | 2014-11-17 | 2023-10-28 | Epizyme Inc | Módszer a rák kezelésére N-((4,6-dimetil-2-oxo-l,2-dihidropiridin-3-il)metil)-5-(etil(tetrahidro-2H -pirán-4-il)amino)-4-metil-4'-(morfolinmetil)-[1,1'-bifenil]-3-karboxamiddal |
| ES2722048T3 (es) * | 2014-12-23 | 2019-08-07 | Novartis Ag | Compuestos de triazolopirimidina y usos de los mismos |
| MX391720B (es) | 2015-04-20 | 2025-03-21 | Epizyme Inc | Terapia combinada para tratar cáncer. |
| JP6890097B2 (ja) | 2015-06-10 | 2021-06-18 | エピザイム，インコーポレイティド | リンパ腫を処置するためのｅｚｈ２阻害剤 |
| CN108136011A (zh) | 2015-08-03 | 2018-06-08 | 星座制药公司 | Ezh2抑制剂和调节性t细胞功能的调制 |
| MX2018002344A (es) | 2015-08-24 | 2018-07-06 | Epizyme Inc | Metodo para tratar el cancer. |
| AU2016325643B2 (en) | 2015-09-25 | 2022-07-21 | Epizyme, Inc. | Method of treating malignant rhabdoid tumor or small cell cancer of the ovary of the hypercalcemic type |
| KR20180058829A (ko) | 2015-10-06 | 2018-06-01 | 에피자임, 인코포레이티드 | Ezh2 억제제로 수모세포종을 치료하는 방법 |
| JP2018532761A (ja) | 2015-11-06 | 2018-11-08 | エピザイム，インコーポレイティド | Ｅｚｈ２阻害剤を用いた癌の処置のための小児投与 |
| CN108697716A (zh) | 2015-12-07 | 2018-10-23 | Epizyme股份有限公司 | Ezh2抑制剂及其使用方法 |
| EP3407978A4 (en) | 2016-01-29 | 2020-01-15 | Epizyme Inc | POLYTHERAPY FOR THE TREATMENT OF CANCER |
| WO2017139404A1 (en) | 2016-02-08 | 2017-08-17 | Epizyme, Inc. | Methods of treating cancer |
| CA3025933A1 (en) | 2016-06-01 | 2017-12-07 | Epizyme, Inc. | Use of ezh2 inhibitors for treating cancer |
| JP2019521988A (ja) | 2016-06-17 | 2019-08-08 | エピザイム，インコーポレイティド | 癌を処置するためのｅｚｈ２阻害剤 |
| WO2018102687A2 (en) | 2016-12-02 | 2018-06-07 | Epizyme, Inc. | Combination therapy for treating cancer |
| EP3576729A4 (en) | 2017-02-02 | 2021-04-14 | Epizyme, Inc. | CANCER TREATMENT MODALITIES |
| US11642346B2 (en) | 2017-03-31 | 2023-05-09 | Epizyme, Inc. | Combination therapy for treating cancer |
| JP2020522687A (ja) | 2017-06-02 | 2020-07-30 | エピザイム，インコーポレイティド | 癌を処置するためのｅｚｈ２阻害剤の使用 |
-
2017
- 2017-06-01 CA CA3025933A patent/CA3025933A1/en active Pending
- 2017-06-01 AU AU2017273726A patent/AU2017273726B2/en not_active Expired - Fee Related
- 2017-06-01 EP EP17807460.5A patent/EP3464643A4/en not_active Withdrawn
- 2017-06-01 JP JP2018562564A patent/JP7121660B2/ja active Active
- 2017-06-01 US US16/306,182 patent/US11786533B2/en active Active
- 2017-06-01 WO PCT/US2017/035391 patent/WO2017210395A1/en not_active Ceased
-
2023
- 2023-09-06 US US18/462,229 patent/US20240139203A1/en not_active Abandoned
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