JP2013544846A5 - - Google Patents
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- JP2013544846A5 JP2013544846A5 JP2013542201A JP2013542201A JP2013544846A5 JP 2013544846 A5 JP2013544846 A5 JP 2013544846A5 JP 2013542201 A JP2013542201 A JP 2013542201A JP 2013542201 A JP2013542201 A JP 2013542201A JP 2013544846 A5 JP2013544846 A5 JP 2013544846A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- halo
- cycloalkyl
- alkoxyl
- alkylamino
- 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 18
- 150000001875 compounds Chemical class 0.000 claims 17
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 16
- 125000003118 aryl group Chemical group 0.000 claims 13
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 11
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 10
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 10
- 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 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims 9
- -1 cyano, hydroxyl Chemical group 0.000 claims 9
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 8
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 239000000203 mixture Substances 0.000 claims 5
- 238000000034 method Methods 0.000 claims 4
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 3
- 208000032839 leukemia Diseases 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 102100039489 Histone-lysine N-methyltransferase, H3 lysine-79 specific Human genes 0.000 claims 1
- 101000963360 Homo sapiens Histone-lysine N-methyltransferase, H3 lysine-79 specific Proteins 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 210000000349 chromosome Anatomy 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 230000019639 protein methylation Effects 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 230000005945 translocation Effects 0.000 claims 1
- LXFOLMYKSYSZQS-LURJZOHASA-N CC(C)N(C[C@H]([C@H]([C@H]1O)O)O[C@H]1[n]1c(ncnc2N)c2nc1)[C@H]1C[C@@H](CCc2nc3cc(C(C)(C)C)ccc3[nH]2)C1 Chemical compound CC(C)N(C[C@H]([C@H]([C@H]1O)O)O[C@H]1[n]1c(ncnc2N)c2nc1)[C@H]1C[C@@H](CCc2nc3cc(C(C)(C)C)ccc3[nH]2)C1 LXFOLMYKSYSZQS-LURJZOHASA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41966110P | 2010-12-03 | 2010-12-03 | |
| US61/419,661 | 2010-12-03 | ||
| PCT/US2011/063044 WO2012075381A1 (en) | 2010-12-03 | 2011-12-02 | Substituted purine and 7 - deazapurine compounds as modulators of epigenetic enzymes |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013544846A JP2013544846A (ja) | 2013-12-19 |
| JP2013544846A5 true JP2013544846A5 (enExample) | 2015-01-15 |
| JP5931905B2 JP5931905B2 (ja) | 2016-06-08 |
Family
ID=45444712
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013542201A Expired - Fee Related JP5931905B2 (ja) | 2010-12-03 | 2011-12-02 | 置換プリン及び７‐デアザプリン化合物 |
Country Status (18)
| Country | Link |
|---|---|
| US (5) | US8580762B2 (enExample) |
| EP (1) | EP2646444B1 (enExample) |
| JP (1) | JP5931905B2 (enExample) |
| KR (1) | KR101923746B1 (enExample) |
| CN (1) | CN103391939B (enExample) |
| AR (1) | AR084408A1 (enExample) |
| AU (1) | AU2011336415B2 (enExample) |
| BR (1) | BR112013013659B8 (enExample) |
| CA (1) | CA2819648C (enExample) |
| DK (1) | DK2646444T3 (enExample) |
| ES (1) | ES2577027T3 (enExample) |
| HR (1) | HRP20160655T1 (enExample) |
| IL (1) | IL226651A (enExample) |
| MX (1) | MX2013006251A (enExample) |
| RU (1) | RU2606514C2 (enExample) |
| SI (1) | SI2646444T1 (enExample) |
| TW (1) | TWI537271B (enExample) |
| WO (1) | WO2012075381A1 (enExample) |
Families Citing this family (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2011341441A1 (en) | 2010-12-03 | 2013-06-20 | Epizyme, Inc. | Modulators of histone methyltransferase, and methods of use thereof |
| US9394310B2 (en) | 2010-12-03 | 2016-07-19 | Epizyme, Inc. | Carbocycle-substituted purine and 7-deazapurine compounds |
| CN103391939B (zh) * | 2010-12-03 | 2016-03-09 | Epizyme股份有限公司 | 作为表观遗传酶调节剂的经取代的嘌呤和7-氮杂嘌呤化合物 |
| EP2646454B1 (en) | 2010-12-03 | 2015-07-08 | Epizyme, Inc. | 7-deazapurine modulators of histone methyltransferase, and methods of use thereof |
| WO2013055397A1 (en) | 2011-10-14 | 2013-04-18 | Children's Medical Center Corporation | Inhibition and enhancement of reprogramming by chromatin modifying enzymes |
| KR102072041B1 (ko) | 2011-12-22 | 2020-01-31 | 앨리오스 바이오파마 인크. | 치환된 뉴클레오사이드, 뉴클레오타이드 및 그의 유사체 |
| US9441007B2 (en) | 2012-03-21 | 2016-09-13 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| USRE48171E1 (en) | 2012-03-21 | 2020-08-25 | Janssen Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| WO2014026198A1 (en) | 2012-08-10 | 2014-02-13 | Epizyme, Inc. | Inhibitors of protein methyltransferase dot1l and methods of use thereof |
| EP2892536B1 (en) * | 2012-09-06 | 2019-12-18 | Epizyme, Inc. | Method of treating leukemia |
| JP2016510316A (ja) * | 2012-12-21 | 2016-04-07 | エピザイム，インコーポレイティド | 白血病の治療に使用するためのｄｏｔ１ｌ阻害剤 |
| EA027879B1 (ru) | 2013-02-22 | 2017-09-29 | Пфайзер Инк. | ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-РОДСТВЕННЫХ КИНАЗ (JAK) |
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| WO2014152261A1 (en) * | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Substituted 7-deazapurine compounds |
| US9394258B2 (en) | 2013-03-14 | 2016-07-19 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| EP2970181B1 (en) | 2013-03-14 | 2017-06-07 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| EP3363434A1 (en) | 2013-03-14 | 2018-08-22 | Epizyme Inc | Arginine methyltransferase inhibitors and uses thereof |
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| US9120757B2 (en) | 2013-03-14 | 2015-09-01 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| US9446064B2 (en) * | 2013-03-14 | 2016-09-20 | Epizyme, Inc. | Combination therapy for treating cancer |
| CA2903394C (en) | 2013-03-14 | 2021-08-31 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| JP2016517434A (ja) * | 2013-03-14 | 2016-06-16 | エピザイム，インコーポレイティド | 癌を処置するための併用療法 |
| US20160039767A1 (en) | 2013-03-14 | 2016-02-11 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| JP2016514164A (ja) | 2013-03-14 | 2016-05-19 | エピザイム，インコーポレイティド | アルギニンメチルトランスフェラーゼ阻害剤としてのピラゾール誘導体およびその使用 |
| WO2014153172A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| WO2014152566A2 (en) | 2013-03-15 | 2014-09-25 | Epizyme, Inc. | Methods of synthesizing substituted purine compounds |
| US20160022725A1 (en) * | 2013-03-15 | 2016-01-28 | Epizyme, Inc. | Injectable formulations for treating cancer |
| WO2015003131A1 (en) * | 2013-07-03 | 2015-01-08 | Epizyme, Inc. | Substituted purine compounds |
| US9535067B2 (en) | 2013-07-29 | 2017-01-03 | Dana-Farber Cancer Institute, Inc. | DOT1L probes |
| US10407732B2 (en) | 2013-08-02 | 2019-09-10 | Memorial Sloan Kettering Cancer Center | Methods for the detection and treatment of leukemias that are responsive to DOT1L inhibition |
| WO2015073706A1 (en) * | 2013-11-13 | 2015-05-21 | Epizyme, Inc. | Methods for treating cancer |
| WO2015200680A2 (en) * | 2014-06-25 | 2015-12-30 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| WO2016024185A1 (en) | 2014-08-12 | 2016-02-18 | Pfizer Inc. | Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase |
| US20170232030A1 (en) * | 2014-08-13 | 2017-08-17 | Epizyme, Inc. | Combination therapy for treating cancer |
| US9458165B2 (en) | 2014-08-27 | 2016-10-04 | Dana-Farber Cancer Institute, Inc. | DOT1L inhibitors |
| US20190083521A1 (en) * | 2014-09-17 | 2019-03-21 | Epizyme, Inc. | Combination therapy for treating cancer |
| AU2015317509A1 (en) * | 2014-09-17 | 2017-03-16 | Epizyme, Inc. | Injectable formulations for treating cancer |
| WO2016051396A1 (en) * | 2014-09-30 | 2016-04-07 | Susan Eve Vecht-Lifshitz | Pharmaceutical compositions for treating ebola virus disease |
| US20180028552A1 (en) * | 2015-01-30 | 2018-02-01 | Epizyme, Inc. | Combination therapy for treating cancer |
| US11453697B1 (en) | 2015-08-13 | 2022-09-27 | Merck Sharp & Dohme Llc | Cyclic di-nucleotide compounds as sting agonists |
| AU2017212572A1 (en) | 2016-01-26 | 2018-08-23 | Memorial Sloan-Kettering Cancer Center | Targeting chromatin regulators inhibits leukemogenic gene expression in NPM1 mutant leukemia |
| SG10201913290QA (en) * | 2016-03-15 | 2020-03-30 | Oryzon Genomics Sa | Combinations of lsd1 inhibitors for the treatment of hematological malignancies |
| CN120661674A (zh) | 2016-03-15 | 2025-09-19 | 奥莱松基因组股份有限公司 | 用于治疗实体瘤的lsd1抑制剂的组合 |
| CN106432095B (zh) * | 2016-09-09 | 2019-04-16 | 东南大学 | 匹莫苯丹关键中间体6-(3,4-二氨基苯基)-5-甲基-4,5-二氢哒嗪-3(2h)-酮的制备 |
| CN110691779B (zh) | 2017-03-24 | 2023-10-10 | 库拉肿瘤学公司 | 治疗血液系统恶性肿瘤和尤因肉瘤的方法 |
| CN109748944B (zh) * | 2017-11-03 | 2021-12-10 | 中国科学院上海药物研究所 | 5’-脱氧-5’-异丙基取代氨基核苷类化合物、其制备方法和用途 |
| CN109748943A (zh) * | 2017-11-03 | 2019-05-14 | 中国科学院上海药物研究所 | 2’-c-甲基取代核苷类化合物及其制备与用途 |
| AU2018381004B2 (en) * | 2017-12-05 | 2021-04-29 | Angex Pharmaceutical, Inc. | Heterocyclic compounds as PRMT5 inhibitors |
| KR102118891B1 (ko) | 2018-10-04 | 2020-06-04 | 성균관대학교산학협력단 | 매소니아노사이드 b를 유효성분으로 포함하는 혼합 직계성 백혈병 유전자 재배열 동반 백혈병 예방 및 치료용 약학적 조성물 |
| WO2020146561A1 (en) | 2019-01-09 | 2020-07-16 | Dana-Farber Cancer Institute, Inc. | Dot1l degraders and uses thereof |
| CN113631535B (zh) * | 2019-03-11 | 2024-04-12 | 协同医药发展有限公司 | 治疗铁死亡相关紊乱的杂芳基和双杂环芳基衍生物 |
| CN110092804A (zh) * | 2019-03-29 | 2019-08-06 | 广州盈升生物科技有限公司 | 一种含双环基团的嘌呤化合物及其制备方法 |
| JP2022522534A (ja) | 2019-04-02 | 2022-04-19 | アリゴス セラピューティクス インコーポレイテッド | Ｐｒｍｔ５を標的にする化合物 |
| CN113024620B (zh) * | 2021-03-11 | 2023-02-28 | 沈阳药科大学 | 一种嘌呤衍生物及其制备方法和用途 |
| WO2022271540A1 (en) * | 2021-06-21 | 2022-12-29 | Mayo Foundation For Medical Education And Research | Inhibitors of dot1l |
| TW202317546A (zh) | 2021-07-09 | 2023-05-01 | 美商普萊克斯姆公司 | 調節ikzf2之芳基化合物及醫藥組合物 |
| US20240335438A1 (en) * | 2021-07-19 | 2024-10-10 | Dana-Farber Cancer Institute, Inc. | Targeting dot1l and smarca4/2 for the treatment of mllr leukemia |
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| EP2646454B1 (en) | 2010-12-03 | 2015-07-08 | Epizyme, Inc. | 7-deazapurine modulators of histone methyltransferase, and methods of use thereof |
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-
2011
- 2011-12-02 CN CN201180066760.7A patent/CN103391939B/zh not_active Expired - Fee Related
- 2011-12-02 US US13/310,157 patent/US8580762B2/en not_active Expired - Fee Related
- 2011-12-02 CA CA2819648A patent/CA2819648C/en active Active
- 2011-12-02 SI SI201130856A patent/SI2646444T1/sl unknown
- 2011-12-02 ES ES11804836.2T patent/ES2577027T3/es active Active
- 2011-12-02 HR HRP20160655TT patent/HRP20160655T1/hr unknown
- 2011-12-02 JP JP2013542201A patent/JP5931905B2/ja not_active Expired - Fee Related
- 2011-12-02 EP EP11804836.2A patent/EP2646444B1/en active Active
- 2011-12-02 DK DK11804836.2T patent/DK2646444T3/da active
- 2011-12-02 WO PCT/US2011/063044 patent/WO2012075381A1/en not_active Ceased
- 2011-12-02 RU RU2013130250A patent/RU2606514C2/ru active
- 2011-12-02 BR BR112013013659A patent/BR112013013659B8/pt not_active IP Right Cessation
- 2011-12-02 KR KR1020137017337A patent/KR101923746B1/ko not_active Expired - Fee Related
- 2011-12-02 MX MX2013006251A patent/MX2013006251A/es active IP Right Grant
- 2011-12-02 AU AU2011336415A patent/AU2011336415B2/en not_active Ceased
- 2011-12-05 TW TW100144669A patent/TWI537271B/zh not_active IP Right Cessation
- 2011-12-05 AR ARP110104537A patent/AR084408A1/es active IP Right Grant
-
2013
- 2013-05-30 IL IL226651A patent/IL226651A/en active IP Right Grant
- 2013-10-16 US US14/055,510 patent/US9096634B2/en active Active
-
2015
- 2015-06-26 US US14/752,023 patent/US20150366893A1/en not_active Abandoned
-
2017
- 2017-11-03 US US15/802,979 patent/US20180280422A1/en not_active Abandoned
-
2020
- 2020-06-10 US US16/897,690 patent/US20210252035A1/en not_active Abandoned
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