JP2013544846A5 - - Google Patents
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- Publication number
- 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 |
|---|---|---|---|---|
| US8580762B2 (en) * | 2010-12-03 | 2013-11-12 | Epizyme, Inc. | Substituted purine and 7-deazapurine compounds |
| CA2819620A1 (en) | 2010-12-03 | 2012-06-21 | Epizyme, Inc. | Modulators of histone methyltransferase, and methods of use thereof |
| CA2819625A1 (en) | 2010-12-03 | 2012-06-07 | Epizyme, Inc. | 7-deazapurine modulators of histone methyltransferase, and methods of use thereof |
| AU2011336264A1 (en) | 2010-12-03 | 2013-06-20 | Epizyme, Inc. | Carbocycle-substituted purine and 7-deazapurine compounds |
| WO2013055397A1 (en) | 2011-10-14 | 2013-04-18 | Children's Medical Center Corporation | Inhibition and enhancement of reprogramming by chromatin modifying enzymes |
| SI2794627T1 (sl) | 2011-12-22 | 2019-02-28 | Alios Biopharma, Inc. | Substituirani nukleozidi, nukleotidi in njihovi analogi |
| USRE48171E1 (en) | 2012-03-21 | 2020-08-25 | Janssen Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| US9441007B2 (en) | 2012-03-21 | 2016-09-13 | Alios 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 |
| CA2883781A1 (en) | 2012-09-06 | 2014-03-13 | Epizyme, Inc. | Method of treating leukemia |
| WO2014100662A1 (en) * | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | Dot1 l inhibitors for use in the treatment of leukemia |
| EP2958921B1 (en) | 2013-02-22 | 2017-09-20 | Pfizer Inc | Pyrrolo [2, 3 -d]pyrimidine derivatives as inhibitors of janus kinases (jak) |
| US9394258B2 (en) | 2013-03-14 | 2016-07-19 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| AU2014260433A1 (en) | 2013-03-14 | 2015-09-10 | Epizyme, Inc. | Pyrazole derivatives as arginine methyltransferase inhibitors and uses thereof |
| US9120757B2 (en) | 2013-03-14 | 2015-09-01 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| EP2970136A1 (en) | 2013-03-14 | 2016-01-20 | Epizyme, Inc. | Arginine methyl transferase inhibtors and uses thereof |
| EP2970133B1 (en) | 2013-03-14 | 2018-10-24 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| SG11201506972PA (en) | 2013-03-14 | 2015-10-29 | Epizyme Inc | Arginine methyltransferase inhibitors and uses thereof |
| WO2014153208A1 (en) | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| EP2970134B1 (en) | 2013-03-14 | 2018-02-28 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| US9446064B2 (en) * | 2013-03-14 | 2016-09-20 | Epizyme, Inc. | Combination therapy for treating cancer |
| 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 |
| US20160031839A1 (en) | 2013-03-14 | 2016-02-04 | Epizyme, Inc. | Arginine methyltransferase inhibitors and uses thereof |
| WO2014152261A1 (en) * | 2013-03-14 | 2014-09-25 | Epizyme, Inc. | Substituted 7-deazapurine compounds |
| WO2014144659A1 (en) | 2013-03-14 | 2014-09-18 | Epizyme, Inc. | Pyrazole derivatives as prmt1 inhibitors and uses thereof |
| AU2014239516B2 (en) * | 2013-03-15 | 2019-01-24 | Epizyme, Inc. | Injectable formulations for treating cancer |
| CA2903303A1 (en) | 2013-03-15 | 2014-09-25 | Epizyme, Inc. | Methods of synthesizing substituted purine compounds |
| 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 |
| US20170198006A1 (en) * | 2014-06-25 | 2017-07-13 | Epizyme, Inc. | Prmt5 inhibitors and uses thereof |
| EP3180344B1 (en) | 2014-08-12 | 2019-09-18 | Pfizer Inc | Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase |
| WO2016025635A2 (en) * | 2014-08-13 | 2016-02-18 | Epizyme, Inc. | Combination therapy for treating cancer |
| US9458165B2 (en) | 2014-08-27 | 2016-10-04 | Dana-Farber Cancer Institute, Inc. | DOT1L inhibitors |
| AU2015317509A1 (en) * | 2014-09-17 | 2017-03-16 | Epizyme, Inc. | Injectable formulations for treating cancer |
| WO2016043874A2 (en) * | 2014-09-17 | 2016-03-24 | Epizyme, Inc. | Combination therapy for treating cancer |
| EP3200826B1 (en) * | 2014-09-30 | 2021-04-21 | Vecht-lifshitz, Susan Eve | 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 |
| CA3012649A1 (en) | 2016-01-26 | 2017-08-03 | Memorial Sloan-Kettering Cancer Center | Targeting chromatin regulators inhibits leukemogenic gene expression in npm1 mutant leukemia |
| KR102646126B1 (ko) | 2016-03-15 | 2024-03-11 | 오리존 지노믹스 에스.에이. | 혈액 악성 종양의 치료를 위한 lsd1 억제제의 조합물 |
| AU2017233898B2 (en) | 2016-03-15 | 2022-12-15 | Oryzon Genomics, S.A. | Combinations of LSD1 inhibitors for use in the treatment of solid tumors |
| 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 |
| US11944627B2 (en) | 2017-03-24 | 2024-04-02 | Kura Oncology, Inc. | Methods for treating hematological malignancies and Ewing's sarcoma |
| 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 |
| WO2019112719A1 (en) * | 2017-12-05 | 2019-06-13 | 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 |
| EP3908583A4 (en) | 2019-01-09 | 2022-08-10 | Dana-Farber Cancer Institute, Inc. | Dot1l degraders and uses thereof |
| JP2022523860A (ja) * | 2019-03-11 | 2022-04-26 | コラボレイティブ メディシナル デベロップメント， エルエルシー | フェロトーシス関連障害の処置のための複素芳香族およびヘテロ二環式芳香族誘導体 |
| 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 |
| US11198699B2 (en) | 2019-04-02 | 2021-12-14 | Aligos Therapeutics, Inc. | Compounds targeting PRMT5 |
| 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 |
| CA3226162A1 (en) | 2021-07-09 | 2023-01-12 | Plexium, Inc. | Aryl compounds and pharmaceutical compositions that modulate ikzf2 |
| AU2022316195A1 (en) * | 2021-07-19 | 2024-01-04 | Dana-Farber Cancer Institute, Inc. | Targeting dot1l and smarca4/2 for the treatment of mllr leukemia |
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| EP1138689A1 (en) | 2000-03-28 | 2001-10-04 | Roche Diagnostics GmbH | N8- and C8-linked purine bases as universal nucleosides used for oligonucleotide hybridization |
| EP1138688A1 (en) | 2000-03-28 | 2001-10-04 | Roche Diagnostics GmbH | N8- and C8- linked purine bases as universal nucleosides used for oligonucleotide hybridization |
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| US8580762B2 (en) * | 2010-12-03 | 2013-11-12 | Epizyme, Inc. | Substituted purine and 7-deazapurine compounds |
| AU2011336264A1 (en) | 2010-12-03 | 2013-06-20 | Epizyme, Inc. | Carbocycle-substituted purine and 7-deazapurine compounds |
| CA2819625A1 (en) | 2010-12-03 | 2012-06-07 | Epizyme, Inc. | 7-deazapurine modulators of histone methyltransferase, and methods of use thereof |
| CA2819620A1 (en) | 2010-12-03 | 2012-06-21 | Epizyme, Inc. | Modulators of histone methyltransferase, and methods of use thereof |
| CA2883781A1 (en) * | 2012-09-06 | 2014-03-13 | Epizyme, Inc. | Method of treating leukemia |
| US9446064B2 (en) * | 2013-03-14 | 2016-09-20 | Epizyme, Inc. | Combination therapy for treating cancer |
| CA2903303A1 (en) | 2013-03-15 | 2014-09-25 | Epizyme, Inc. | Methods of synthesizing substituted purine compounds |
| 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 |
-
2011
- 2011-12-02 US US13/310,157 patent/US8580762B2/en not_active Expired - Fee Related
- 2011-12-02 RU RU2013130250A patent/RU2606514C2/ru active
- 2011-12-02 KR KR1020137017337A patent/KR101923746B1/ko not_active Expired - Fee Related
- 2011-12-02 JP JP2013542201A patent/JP5931905B2/ja not_active Expired - Fee Related
- 2011-12-02 DK DK11804836.2T patent/DK2646444T3/da active
- 2011-12-02 MX MX2013006251A patent/MX2013006251A/es active IP Right Grant
- 2011-12-02 ES ES11804836.2T patent/ES2577027T3/es active Active
- 2011-12-02 EP EP11804836.2A patent/EP2646444B1/en active Active
- 2011-12-02 CA CA2819648A patent/CA2819648C/en active Active
- 2011-12-02 SI SI201130856A patent/SI2646444T1/sl unknown
- 2011-12-02 BR BR112013013659A patent/BR112013013659B8/pt not_active IP Right Cessation
- 2011-12-02 CN CN201180066760.7A patent/CN103391939B/zh not_active Expired - Fee Related
- 2011-12-02 WO PCT/US2011/063044 patent/WO2012075381A1/en not_active Ceased
- 2011-12-02 HR HRP20160655TT patent/HRP20160655T1/hr unknown
- 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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