JP2016523955A5 - - Google Patents
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- Publication number
- JP2016523955A5 JP2016523955A5 JP2016524931A JP2016524931A JP2016523955A5 JP 2016523955 A5 JP2016523955 A5 JP 2016523955A5 JP 2016524931 A JP2016524931 A JP 2016524931A JP 2016524931 A JP2016524931 A JP 2016524931A JP 2016523955 A5 JP2016523955 A5 JP 2016523955A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- heterocycloalkyl
- cycloalkyl
- aryl
- heteroaryl
- 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.)
- Pending
Links
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 58
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 47
- 125000003118 aryl group Chemical group 0.000 claims 44
- 125000001072 heteroaryl group Chemical group 0.000 claims 44
- 229910052736 halogen Inorganic materials 0.000 claims 28
- 150000002367 halogens Chemical class 0.000 claims 28
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 27
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 25
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 25
- 125000004093 cyano group Chemical group *C#N 0.000 claims 21
- 229910052739 hydrogen Inorganic materials 0.000 claims 19
- 239000001257 hydrogen Substances 0.000 claims 19
- 125000000217 alkyl group Chemical group 0.000 claims 17
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 17
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 16
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 16
- 229910052757 nitrogen Inorganic materials 0.000 claims 16
- 150000003839 salts Chemical class 0.000 claims 15
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 14
- 150000001602 bicycloalkyls Chemical group 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 14
- 125000003545 alkoxy group Chemical group 0.000 claims 11
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 10
- 229910052760 oxygen Inorganic materials 0.000 claims 9
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 9
- 229910052717 sulfur Inorganic materials 0.000 claims 8
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims 7
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 6
- 125000006625 (C3-C8) cycloalkyloxy group Chemical group 0.000 claims 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 6
- 125000006564 (C4-C8) cycloalkyl group Chemical group 0.000 claims 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 5
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 4
- 125000005842 heteroatom Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 125000004043 oxo group Chemical group O=* 0.000 claims 4
- 239000001301 oxygen Substances 0.000 claims 4
- 239000011593 sulfur Chemical group 0.000 claims 4
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 3
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims 3
- -1 heterocycloalkyloxy- Chemical group 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 claims 1
- VKVMZGLDNBSRKZ-WGSAOQKQSA-N CC=1NC(=CC(C=1CNC(=O)C1=CSC(=C1C)N(CC)[C@@H]1CC[C@H](CC1)N(C)C)=O)C Chemical compound CC=1NC(=CC(C=1CNC(=O)C1=CSC(=C1C)N(CC)[C@@H]1CC[C@H](CC1)N(C)C)=O)C VKVMZGLDNBSRKZ-WGSAOQKQSA-N 0.000 claims 1
- HCMUWTBQKZLUDM-UHFFFAOYSA-N N-[(2,6-dimethyl-4-oxo-3H-pyridin-3-yl)methyl]-5-[ethyl(oxan-4-yl)amino]-4-methylthiophene-3-carboxamide Chemical compound CCN(C1CCOCC1)c1scc(C(=O)NCC2C(C)=NC(C)=CC2=O)c1C HCMUWTBQKZLUDM-UHFFFAOYSA-N 0.000 claims 1
- SCTVKSNCBUACPT-UHFFFAOYSA-N N-[(5-amino-2,6-dimethyl-4-oxo-3H-pyridin-3-yl)methyl]-5-[[4-(dimethylamino)cyclohexyl]-ethylamino]-4-methylthiophene-3-carboxamide Chemical compound CCN(C1CCC(CC1)N(C)C)c1scc(C(=O)NCC2C(C)=NC(C)=C(N)C2=O)c1C SCTVKSNCBUACPT-UHFFFAOYSA-N 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
- 0 *c1c(*)[s]c(C(NCC2=C(*)NC(*)=C(*)C2=O)=O)c1* Chemical compound *c1c(*)[s]c(C(NCC2=C(*)NC(*)=C(*)C2=O)=O)c1* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361844540P | 2013-07-10 | 2013-07-10 | |
| US61/844,540 | 2013-07-10 | ||
| PCT/IB2014/062983 WO2015004618A1 (en) | 2013-07-10 | 2014-07-09 | Enhancer of zeste homolog 2 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016523955A JP2016523955A (ja) | 2016-08-12 |
| JP2016523955A5 true JP2016523955A5 (enExample) | 2017-08-24 |
Family
ID=51212901
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016524931A Pending JP2016523955A (ja) | 2013-07-10 | 2014-07-09 | Ｚｅｓｔｅホモログ２エンハンサー阻害剤 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US9556157B2 (enExample) |
| EP (1) | EP3019494B1 (enExample) |
| JP (1) | JP2016523955A (enExample) |
| KR (1) | KR20160030221A (enExample) |
| CN (1) | CN105473580A (enExample) |
| AU (1) | AU2014288839B2 (enExample) |
| CA (1) | CA2917463A1 (enExample) |
| ES (1) | ES2640386T3 (enExample) |
| RU (1) | RU2016104044A (enExample) |
| WO (1) | WO2015004618A1 (enExample) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20190105669A (ko) | 2012-10-15 | 2019-09-17 | 에피자임, 인코포레이티드 | 암을 치료하는 방법 |
| CA2894222A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | 1,4-pyridone bicyclic heteroaryl compounds |
| MA40848A (fr) * | 2014-10-28 | 2021-05-05 | Glaxosmithkline Ip No 2 Ltd | Inhibiteurs d'ezh2 (enhancer of zeste homolog 2) |
| TW201636344A (zh) | 2014-12-05 | 2016-10-16 | 美國禮來大藥廠 | Ｅｚｈ２抑制劑 |
| TW201708210A (zh) * | 2015-06-30 | 2017-03-01 | 葛蘭素史克智慧財產（第二）有限公司 | Ｚｅｓｔｅ同源物２增強子之抑制劑 |
| WO2017035234A1 (en) | 2015-08-24 | 2017-03-02 | Epizyme, Inc. | Method for treating cancer |
| TW201718598A (zh) | 2015-08-27 | 2017-06-01 | 美國禮來大藥廠 | Ｅｚｈ２抑制劑 |
| WO2017079757A1 (en) * | 2015-11-06 | 2017-05-11 | Epizyme, Inc. | Pediatric dosing for treatment of cancer with an ezh2 inhibitor |
| AU2017330443B2 (en) | 2016-09-26 | 2023-08-24 | Dana-Farber Cancer Institute, Inc. | Chromobox protein inhibitors and uses thereof |
| BR112019014924A2 (pt) | 2017-01-19 | 2020-03-31 | St. Marianna University School Of Medicine | Composição farmacêutica usada para o tratamento de mielopatia associada ao htlv-1 |
| US10266542B2 (en) | 2017-03-15 | 2019-04-23 | Mirati Therapeutics, Inc. | EZH2 inhibitors |
| DK3746446T3 (da) | 2018-01-31 | 2022-06-27 | Mirati Therapeutics Inc | PRC2-inhibitorer |
| WO2020011607A1 (en) | 2018-07-09 | 2020-01-16 | Fondation Asile Des Aveugles | Inhibition of prc2 subunits to treat eye disorders |
| US12421228B2 (en) | 2019-04-22 | 2025-09-23 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as PRC2 inhibitors |
| CN114269748A (zh) | 2019-06-05 | 2022-04-01 | 米拉蒂医疗股份有限公司 | 作为用于治疗癌症的PRC2抑制剂的咪唑并[1,2-c]嘧啶衍生物 |
| CN110950834A (zh) * | 2019-11-26 | 2020-04-03 | 济南大学 | 新型eed-ezh2相互作用小分子抑制剂的确定和评价 |
| CA3249707A1 (en) | 2022-04-27 | 2023-11-02 | Daiichi Sankyo Company, Limited | COMBINATION OF AN ANTIBODY-DRUG CONJUGATE WITH AN EZH1 AND/OR EZH2 INHIBITOR |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6559145B2 (en) | 2000-07-12 | 2003-05-06 | Pharmacia & Upjohn Company | Heterocycle carboxamides as antiviral agents |
| JP4664597B2 (ja) | 2002-04-17 | 2011-04-06 | サイトキネティクス・インコーポレーテッド | 化合物、組成物および方法 |
| US7618981B2 (en) | 2004-05-06 | 2009-11-17 | Cytokinetics, Inc. | Imidazopyridinyl-benzamide anti-cancer agents |
| AU2006325746A1 (en) | 2005-12-14 | 2007-06-21 | Bristol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
| MX2012012966A (es) * | 2010-05-07 | 2013-01-22 | Glaxosmithkline Llc | Indoles. |
| US8846935B2 (en) | 2010-05-07 | 2014-09-30 | Glaxosmithkline Llc | Indazoles |
| WO2012005805A1 (en) | 2010-05-07 | 2012-01-12 | Glaxosmithkline Llc | Azaindazoles |
| EP2646020B1 (en) | 2010-12-01 | 2016-09-21 | Glaxosmithkline LLC | Indoles |
| WO2012118812A2 (en) | 2011-02-28 | 2012-09-07 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
| JO3363B1 (ar) | 2011-04-13 | 2019-03-13 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| TW201733984A (zh) * | 2011-04-13 | 2017-10-01 | 雅酶股份有限公司 | 經取代之苯化合物 |
| US9730925B2 (en) * | 2011-09-30 | 2017-08-15 | Glaxomithkline Llc | Methods of treating cancer |
| WO2013075084A1 (en) * | 2011-11-18 | 2013-05-23 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| US9085583B2 (en) | 2012-02-10 | 2015-07-21 | Constellation—Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| EP2836216B1 (en) | 2012-04-13 | 2022-06-08 | Epizyme, Inc. | Combination therapy for treating cancer |
| ES2617379T3 (es) | 2012-04-13 | 2017-06-16 | Epizyme, Inc. | Forma de sal de un inhibidor de histona metiltransferasa EZH2 humana |
| US9562041B2 (en) | 2012-05-16 | 2017-02-07 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
| BR112015008480A2 (pt) | 2012-10-15 | 2017-07-04 | Epizyme Inc | compostos de benzeno substituído |
| RU2015127822A (ru) | 2012-12-13 | 2017-01-16 | ГЛЭКСОСМИТКЛАЙН ЭлЭлСи | Ингибиторы энхансера гомолога 2 белка zeste |
| CA2894222A1 (en) * | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | 1,4-pyridone bicyclic heteroaryl compounds |
| HK1214815A1 (zh) | 2013-04-30 | 2016-08-05 | Glaxosmithkline Intellectual Property (No. 2) Limited | Zeste增强子同源物2的抑制剂 |
| EP3022184B1 (en) | 2013-07-19 | 2017-09-27 | Epizyme, Inc. | Substituted benzene compounds |
-
2014
- 2014-07-09 CA CA2917463A patent/CA2917463A1/en not_active Abandoned
- 2014-07-09 RU RU2016104044A patent/RU2016104044A/ru not_active Application Discontinuation
- 2014-07-09 US US14/898,178 patent/US9556157B2/en not_active Expired - Fee Related
- 2014-07-09 WO PCT/IB2014/062983 patent/WO2015004618A1/en not_active Ceased
- 2014-07-09 ES ES14741958.4T patent/ES2640386T3/es active Active
- 2014-07-09 AU AU2014288839A patent/AU2014288839B2/en not_active Ceased
- 2014-07-09 CN CN201480046665.4A patent/CN105473580A/zh active Pending
- 2014-07-09 JP JP2016524931A patent/JP2016523955A/ja active Pending
- 2014-07-09 KR KR1020167002906A patent/KR20160030221A/ko not_active Withdrawn
- 2014-07-09 EP EP14741958.4A patent/EP3019494B1/en active Active
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