JP2019533650A5 - - Google Patents
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- Publication number
- JP2019533650A5 JP2019533650A5 JP2019517090A JP2019517090A JP2019533650A5 JP 2019533650 A5 JP2019533650 A5 JP 2019533650A5 JP 2019517090 A JP2019517090 A JP 2019517090A JP 2019517090 A JP2019517090 A JP 2019517090A JP 2019533650 A5 JP2019533650 A5 JP 2019533650A5
- Authority
- JP
- Japan
- Prior art keywords
- halo
- membered
- alkyl
- hydroxyl
- 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.)
- Granted
Links
- 125000005843 halogen group Chemical group 0.000 claims 128
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 92
- 125000005842 heteroatom Chemical group 0.000 claims 69
- -1 cyano, hydroxyl Chemical group 0.000 claims 61
- 125000000753 cycloalkyl group Chemical group 0.000 claims 61
- 229910052760 oxygen Inorganic materials 0.000 claims 59
- 229910052717 sulfur Inorganic materials 0.000 claims 55
- 150000001875 compounds Chemical class 0.000 claims 43
- 125000003118 aryl group Chemical group 0.000 claims 41
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 40
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 36
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 35
- 125000004093 cyano group Chemical group *C#N 0.000 claims 34
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 27
- 125000001072 heteroaryl group Chemical group 0.000 claims 26
- 125000004043 oxo group Chemical group O=* 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 13
- 229910052757 nitrogen Inorganic materials 0.000 claims 10
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 8
- 125000000217 alkyl group Chemical group 0.000 claims 7
- 125000005647 linker group Chemical group 0.000 claims 7
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 6
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- 102000004190 Enzymes Human genes 0.000 claims 3
- 108090000790 Enzymes Proteins 0.000 claims 3
- 108091000080 Phosphotransferase Proteins 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 230000005764 inhibitory process Effects 0.000 claims 3
- 102000020233 phosphotransferase Human genes 0.000 claims 3
- 208000019838 Blood disease Diseases 0.000 claims 2
- 102100035042 Histone-lysine N-methyltransferase EHMT2 Human genes 0.000 claims 2
- 101000877312 Homo sapiens Histone-lysine N-methyltransferase EHMT2 Proteins 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000014951 hematologic disease Diseases 0.000 claims 2
- 208000018706 hematopoietic system disease Diseases 0.000 claims 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- KRQUFUKTQHISJB-YYADALCUSA-N 2-[(E)-N-[2-(4-chlorophenoxy)propoxy]-C-propylcarbonimidoyl]-3-hydroxy-5-(thian-3-yl)cyclohex-2-en-1-one Chemical compound CCC\C(=N/OCC(C)OC1=CC=C(Cl)C=C1)C1=C(O)CC(CC1=O)C1CCCSC1 KRQUFUKTQHISJB-YYADALCUSA-N 0.000 claims 1
- SWKAVEUTKGKHSR-UHFFFAOYSA-N 3-(benzylsulfamoyl)-4-bromo-n-(4-bromophenyl)benzamide Chemical compound C1=CC(Br)=CC=C1NC(=O)C1=CC=C(Br)C(S(=O)(=O)NCC=2C=CC=CC=2)=C1 SWKAVEUTKGKHSR-UHFFFAOYSA-N 0.000 claims 1
- 108010055196 EphA2 Receptor Proteins 0.000 claims 1
- 102100030340 Ephrin type-A receptor 2 Human genes 0.000 claims 1
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 claims 1
- 101710182396 Fibroblast growth factor receptor 3 Proteins 0.000 claims 1
- 102100035043 Histone-lysine N-methyltransferase EHMT1 Human genes 0.000 claims 1
- 101000877314 Homo sapiens Histone-lysine N-methyltransferase EHMT1 Proteins 0.000 claims 1
- 101000977771 Homo sapiens Interleukin-1 receptor-associated kinase 4 Proteins 0.000 claims 1
- 101000777293 Homo sapiens Serine/threonine-protein kinase Chk1 Proteins 0.000 claims 1
- 101001059443 Homo sapiens Serine/threonine-protein kinase MARK1 Proteins 0.000 claims 1
- 101000934996 Homo sapiens Tyrosine-protein kinase JAK3 Proteins 0.000 claims 1
- 102100023533 Interleukin-1 receptor-associated kinase 4 Human genes 0.000 claims 1
- 101150028321 Lck gene Proteins 0.000 claims 1
- 101710138999 MAP kinase-interacting serine/threonine-protein kinase 2 Proteins 0.000 claims 1
- 102100033610 MAP kinase-interacting serine/threonine-protein kinase 2 Human genes 0.000 claims 1
- 108060004795 Methyltransferase Proteins 0.000 claims 1
- 102000016397 Methyltransferase Human genes 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 229940124639 Selective inhibitor Drugs 0.000 claims 1
- 102100031081 Serine/threonine-protein kinase Chk1 Human genes 0.000 claims 1
- 102100028921 Serine/threonine-protein kinase MARK1 Human genes 0.000 claims 1
- 208000018020 Sickle cell-beta-thalassemia disease syndrome Diseases 0.000 claims 1
- 206010043391 Thalassaemia beta Diseases 0.000 claims 1
- 102100025387 Tyrosine-protein kinase JAK3 Human genes 0.000 claims 1
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 claims 1
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 208000007056 sickle cell anemia Diseases 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022192370A JP2023022230A (ja) | 2016-09-30 | 2022-11-30 | Ｅｈｍｔ２阻害剤としての置換された融合二環式または三環式複素環化合物 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662402863P | 2016-09-30 | 2016-09-30 | |
| US62/402,863 | 2016-09-30 | ||
| US201762509620P | 2017-05-22 | 2017-05-22 | |
| US62/509,620 | 2017-05-22 | ||
| PCT/US2017/054468 WO2018064557A1 (en) | 2016-09-30 | 2017-09-29 | Substituted fused bi- or tri- heterocyclic compounds as ehmt2 inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022192370A Division JP2023022230A (ja) | 2016-09-30 | 2022-11-30 | Ｅｈｍｔ２阻害剤としての置換された融合二環式または三環式複素環化合物 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2019533650A JP2019533650A (ja) | 2019-11-21 |
| JP2019533650A5 true JP2019533650A5 (enExample) | 2020-11-12 |
| JPWO2018064557A5 JPWO2018064557A5 (enExample) | 2022-10-11 |
| JP7187449B2 JP7187449B2 (ja) | 2022-12-12 |
Family
ID=60043417
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019517090A Active JP7187449B2 (ja) | 2016-09-30 | 2017-09-29 | Ｅｈｍｔ２阻害剤としての置換された融合二環式または三環式複素環化合物 |
| JP2022192370A Pending JP2023022230A (ja) | 2016-09-30 | 2022-11-30 | Ｅｈｍｔ２阻害剤としての置換された融合二環式または三環式複素環化合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022192370A Pending JP2023022230A (ja) | 2016-09-30 | 2022-11-30 | Ｅｈｍｔ２阻害剤としての置換された融合二環式または三環式複素環化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US20200039961A1 (enExample) |
| EP (2) | EP4105203A1 (enExample) |
| JP (2) | JP7187449B2 (enExample) |
| AU (3) | AU2017336074A1 (enExample) |
| CA (1) | CA3037587A1 (enExample) |
| WO (1) | WO2018064557A1 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11672800B2 (en) | 2017-04-21 | 2023-06-13 | Epizyme, Inc. | Combination therapies with EHMT2 inhibitors |
| WO2020097398A1 (en) | 2018-11-07 | 2020-05-14 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof |
| US12522583B2 (en) | 2018-11-07 | 2026-01-13 | Dana-Farber Cancer Institute, Inc. | Benzimidazole derivatives and aza-benzimidazole derivatives as Janus kinase 2 inhibitors and uses thereof |
| WO2020097400A1 (en) | 2018-11-07 | 2020-05-14 | Dana-Farber Cancer Institute, Inc. | Imidazopyridine derivatives and aza-imidazopyridine derivatives as janus kinase 2 inhibitors and uses thereof |
| US11691963B2 (en) | 2020-05-06 | 2023-07-04 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as JAK2 inhibitors |
| EP4267574B1 (en) | 2020-12-23 | 2025-04-23 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| CA3234638A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| US12162881B2 (en) | 2021-11-09 | 2024-12-10 | Ajax Therapeutics, Inc. | Forms and compositions of inhibitors of JAK2 |
| CN116425642B (zh) * | 2023-04-06 | 2025-06-10 | 浙江科聚生物医药有限公司 | 2-甲氧基-4-氟-5-胺基苯酚的制备方法 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SE8604566D0 (sv) | 1986-10-27 | 1986-10-27 | Haessle Ab | Novel compunds |
| GB8820231D0 (en) | 1988-08-25 | 1988-09-28 | Fujisawa Pharmaceutical Co | New benzazole compounds processes for preparation thereof & pharmaceutical composition comprising same |
| US5763263A (en) | 1995-11-27 | 1998-06-09 | Dehlinger; Peter J. | Method and apparatus for producing position addressable combinatorial libraries |
| AU2207897A (en) | 1996-03-11 | 1997-10-01 | Eli Lilly And Company | Methods of treating or preventing interstitial cystitis |
| US6391907B1 (en) | 1999-05-04 | 2002-05-21 | American Home Products Corporation | Indoline derivatives |
| HUP0200993A3 (en) | 1999-05-04 | 2003-05-28 | Wyeth Corp | Thio-oxindole derivatives, use of them for producing pharmaceutical compositions and pharmaceutical compositions containing them |
| TW593278B (en) | 2001-01-23 | 2004-06-21 | Wyeth Corp | 1-aryl-or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands |
| ES2327418T3 (es) * | 2003-10-16 | 2009-10-29 | Novartis Vaccines And Diagnostics, Inc. | Benzazoles sustituidos y uso de los mismos como inhibidores de la quinasa raf. |
| US8214439B2 (en) | 2005-12-06 | 2012-07-03 | Microsoft Corporation | Document object model API for MIME |
| FR2897061B1 (fr) * | 2006-02-03 | 2010-09-03 | Sanofi Aventis | Derives de n-heteroaryl-carboxamides tricycliques contenant un motif benzimidazole, leur preparation et leur application en therapeutique. |
| CN103172637B (zh) | 2013-03-13 | 2015-05-27 | 上海大学 | 嘧啶并[1,2-a]苯并咪唑类化合物及其制备方法 |
| US9284272B2 (en) | 2014-03-28 | 2016-03-15 | Abbvie Inc. | Inhibitors of histone methyltransferase G9a |
| WO2015200329A1 (en) | 2014-06-23 | 2015-12-30 | Genentech, Inc. | Methods of treating cancer and preventing cancer drug resistance |
| TWI808067B (zh) * | 2016-12-19 | 2023-07-11 | 美商雅酶股份有限公司 | 作為ehmt2抑制劑之胺取代的雜環化合物及其使用方法 |
| AU2018243749A1 (en) * | 2017-03-31 | 2019-11-21 | Epizyme, Inc. | Methods of using EHMT2 inhibitors |
| WO2019079596A1 (en) * | 2017-10-18 | 2019-04-25 | Epizyme, Inc. | METHODS OF USING EHMT2 INHIBITORS IN IMMUNOTHERAPIES |
| KR20200101332A (ko) * | 2017-10-18 | 2020-08-27 | 에피자임, 인코포레이티드 | 혈액 장애 예방 또는 치료에 있어서의 ehmt2 저해제의 사용 방법 |
-
2017
- 2017-09-29 EP EP22173440.3A patent/EP4105203A1/en not_active Withdrawn
- 2017-09-29 JP JP2019517090A patent/JP7187449B2/ja active Active
- 2017-09-29 AU AU2017336074A patent/AU2017336074A1/en not_active Abandoned
- 2017-09-29 CA CA3037587A patent/CA3037587A1/en active Pending
- 2017-09-29 EP EP17781368.0A patent/EP3519393B1/en active Active
- 2017-09-29 WO PCT/US2017/054468 patent/WO2018064557A1/en not_active Ceased
- 2017-09-29 US US16/338,093 patent/US20200039961A1/en not_active Abandoned
-
2021
- 2021-11-30 AU AU2021277619A patent/AU2021277619B2/en active Active
- 2021-12-23 US US17/560,545 patent/US20220274961A1/en not_active Abandoned
-
2022
- 2022-11-30 JP JP2022192370A patent/JP2023022230A/ja active Pending
-
2024
- 2024-02-08 AU AU2024200781A patent/AU2024200781A1/en active Pending
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