JP2021500334A5 - - Google Patents
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- Publication number
- JP2021500334A5 JP2021500334A5 JP2020521599A JP2020521599A JP2021500334A5 JP 2021500334 A5 JP2021500334 A5 JP 2021500334A5 JP 2020521599 A JP2020521599 A JP 2020521599A JP 2020521599 A JP2020521599 A JP 2020521599A JP 2021500334 A5 JP2021500334 A5 JP 2021500334A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- compound according
- pharmaceutically acceptable
- tautomer
- acceptable salt
- 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.)
- Withdrawn
Links
- 150000001875 compounds Chemical class 0.000 claims description 272
- 150000003839 salts Chemical class 0.000 claims description 70
- 229940126214 compound 3 Drugs 0.000 claims description 22
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 16
- 239000013078 crystal Substances 0.000 claims description 16
- 206010028980 Neoplasm Diseases 0.000 claims description 14
- 201000011510 cancer Diseases 0.000 claims description 14
- 208000019838 Blood disease Diseases 0.000 claims description 12
- AEMRFAOFKBGASW-UHFFFAOYSA-M Glycolate Chemical compound OCC([O-])=O AEMRFAOFKBGASW-UHFFFAOYSA-M 0.000 claims description 12
- 208000014951 hematologic disease Diseases 0.000 claims description 12
- 208000018706 hematopoietic system disease Diseases 0.000 claims description 12
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims description 10
- 229940125782 compound 2 Drugs 0.000 claims description 10
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims description 8
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 8
- 150000001278 adipic acid derivatives Chemical class 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 8
- 229940079593 drug Drugs 0.000 claims description 8
- 238000004519 manufacturing process Methods 0.000 claims description 8
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims description 8
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 8
- 102100035043 Histone-lysine N-methyltransferase EHMT1 Human genes 0.000 claims description 6
- 102100035042 Histone-lysine N-methyltransferase EHMT2 Human genes 0.000 claims description 6
- 101000877314 Homo sapiens Histone-lysine N-methyltransferase EHMT1 Proteins 0.000 claims description 6
- 101000877312 Homo sapiens Histone-lysine N-methyltransferase EHMT2 Proteins 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 6
- 230000002401 inhibitory effect Effects 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 6
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 4
- 206010025323 Lymphomas Diseases 0.000 claims description 4
- QIAFMBKCNZACKA-UHFFFAOYSA-N N-benzoylglycine Chemical compound OC(=O)CNC(=O)C1=CC=CC=C1 QIAFMBKCNZACKA-UHFFFAOYSA-N 0.000 claims description 4
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 claims description 4
- 229910019142 PO4 Inorganic materials 0.000 claims description 4
- 239000002253 acid Substances 0.000 claims description 4
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid Chemical compound OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 claims description 4
- 201000005787 hematologic cancer Diseases 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 4
- 239000010452 phosphate Substances 0.000 claims description 4
- 208000032839 leukemia Diseases 0.000 claims description 3
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 208000011691 Burkitt lymphomas Diseases 0.000 claims description 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims description 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 208000018020 Sickle cell-beta-thalassemia disease syndrome Diseases 0.000 claims description 2
- 206010043391 Thalassaemia beta Diseases 0.000 claims description 2
- 229940125904 compound 1 Drugs 0.000 claims description 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 201000003444 follicular lymphoma Diseases 0.000 claims description 2
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims description 2
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 2
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 2
- 201000005202 lung cancer Diseases 0.000 claims description 2
- 208000020816 lung neoplasm Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 208000007056 sickle cell anemia Diseases 0.000 claims description 2
- 150000003467 sulfuric acid derivatives Chemical class 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 17
- 230000002489 hematologic effect Effects 0.000 claims 1
- 0 CC(CCc(cccc1)c1IC)C*1CCC1 Chemical compound CC(CCc(cccc1)c1IC)C*1CCC1 0.000 description 46
- 238000000034 method Methods 0.000 description 13
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 description 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 description 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 description 2
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 description 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023002371A JP2023036991A (ja) | 2017-10-18 | 2023-01-11 | Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762573917P | 2017-10-18 | 2017-10-18 | |
| US62/573,917 | 2017-10-18 | ||
| PCT/US2018/056428 WO2019079540A1 (en) | 2017-10-18 | 2018-10-18 | AMINO-SUBSTITUTED HETEROCYCLIC COMPOUNDS AS INHIBITORS OF EHMT2, SALTS THEREOF, AND METHODS OF SYNTHESIS THEREOF |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023002371A Division JP2023036991A (ja) | 2017-10-18 | 2023-01-11 | Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2021500334A JP2021500334A (ja) | 2021-01-07 |
| JP2021500334A5 true JP2021500334A5 (https=) | 2021-10-07 |
Family
ID=66173899
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020521599A Withdrawn JP2021500334A (ja) | 2017-10-18 | 2018-10-18 | Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法 |
| JP2023002371A Pending JP2023036991A (ja) | 2017-10-18 | 2023-01-11 | Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023002371A Pending JP2023036991A (ja) | 2017-10-18 | 2023-01-11 | Ｅｈｍｔ２阻害剤としてのアミン置換複素環化合物、その塩、及びそれらの合成方法 |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US20200247790A1 (https=) |
| EP (1) | EP3697762A4 (https=) |
| JP (2) | JP2021500334A (https=) |
| KR (1) | KR20200101330A (https=) |
| CN (1) | CN111417628A (https=) |
| AU (2) | AU2018353122B2 (https=) |
| BR (1) | BR112020007632A2 (https=) |
| CA (1) | CA3079273A1 (https=) |
| CL (1) | CL2020001009A1 (https=) |
| CO (1) | CO2020005944A2 (https=) |
| EA (1) | EA202090959A1 (https=) |
| IL (2) | IL301746B2 (https=) |
| MA (1) | MA50418A (https=) |
| MX (2) | MX2020007152A (https=) |
| SG (1) | SG11202003225YA (https=) |
| WO (1) | WO2019079540A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN110446495B (zh) | 2017-02-17 | 2023-09-05 | 特维娜有限公司 | 含有7元氮杂杂环的δ阿片受体调节化合物及其使用和制备方法 |
| CN110621316B (zh) | 2017-04-21 | 2024-01-26 | Epizyme股份有限公司 | 用ehmt2抑制剂进行的组合疗法 |
| KR102717072B1 (ko) | 2017-10-18 | 2024-10-15 | 인사이트 코포레이션 | Pi3k-감마 저해제로서의 3차 하이드록시기로 치환된 축합된 이미다졸 유도체 |
| CR20250050A (es) | 2018-09-05 | 2025-03-19 | Incyte Corp | Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165) |
| CN114249785B (zh) * | 2020-09-23 | 2024-04-05 | 常州方圆制药有限公司 | 一种2-腺苷n-吡唑的衍生物瑞加德松的制备方法 |
| WO2022093904A1 (en) * | 2020-10-27 | 2022-05-05 | Trevena, Inc. | Crystalline and amorphous forms of a delta-opioid modulator |
| WO2025240956A1 (en) * | 2024-05-17 | 2025-11-20 | Yale University | G9a/ehmt2 inhibitor use for prader-willi syndrome |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20070105839A1 (en) * | 2003-09-18 | 2007-05-10 | Patricia Imbach | 2, 4-Di (phenylamino) pyrimidines useful in the treatment of proliferative disorders |
| JP5191391B2 (ja) * | 2005-11-01 | 2013-05-08 | ターゲジェン インコーポレーティッド | キナーゼのビ−アリールメタ−ピリミジン阻害剤 |
| US8604042B2 (en) * | 2005-11-01 | 2013-12-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
| US9284272B2 (en) * | 2014-03-28 | 2016-03-15 | Abbvie Inc. | Inhibitors of histone methyltransferase G9a |
| CN106536509B (zh) * | 2014-06-16 | 2020-06-09 | 基础应用医学研究基金会 | 作为组蛋白甲基转移酶和dna甲基转移酶的双重抑制剂的新型化合物 |
| EP3157524A4 (en) * | 2014-06-23 | 2017-12-06 | Genentech, Inc. | Methods of treating cancer and preventing cancer drug resistance |
| PL3442947T3 (pl) * | 2016-04-15 | 2023-10-02 | Epizyme, Inc. | Związki arylowe lub heteroarylowe podstawione aminą jako inhibitory ehmt1 i ehmt2 |
| US20200039998A1 (en) * | 2016-12-19 | 2020-02-06 | Epizyme, Inc. | Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof |
| US20200113901A1 (en) * | 2017-03-31 | 2020-04-16 | Epizyme, Inc. | Methods of using ehmt2 inhibitors |
| AU2018353139A1 (en) * | 2017-10-18 | 2020-06-04 | Epizyme, Inc. | Methods of using EHMT2 inhibitors in immunotherapies |
-
2018
- 2018-10-18 JP JP2020521599A patent/JP2021500334A/ja not_active Withdrawn
- 2018-10-18 AU AU2018353122A patent/AU2018353122B2/en active Active
- 2018-10-18 BR BR112020007632-5A patent/BR112020007632A2/pt unknown
- 2018-10-18 CN CN201880077022.4A patent/CN111417628A/zh active Pending
- 2018-10-18 EA EA202090959A patent/EA202090959A1/ru unknown
- 2018-10-18 WO PCT/US2018/056428 patent/WO2019079540A1/en not_active Ceased
- 2018-10-18 IL IL301746A patent/IL301746B2/en unknown
- 2018-10-18 KR KR1020207013781A patent/KR20200101330A/ko not_active Ceased
- 2018-10-18 EP EP18869308.9A patent/EP3697762A4/en not_active Withdrawn
- 2018-10-18 US US16/756,565 patent/US20200247790A1/en not_active Abandoned
- 2018-10-18 SG SG11202003225YA patent/SG11202003225YA/en unknown
- 2018-10-18 CA CA3079273A patent/CA3079273A1/en active Pending
- 2018-10-18 MX MX2020007152A patent/MX2020007152A/es unknown
- 2018-10-18 MA MA050418A patent/MA50418A/fr unknown
-
2020
- 2020-04-15 CL CL2020001009A patent/CL2020001009A1/es unknown
- 2020-04-16 IL IL273974A patent/IL273974B2/en unknown
- 2020-05-15 CO CONC2020/0005944A patent/CO2020005944A2/es unknown
- 2020-07-13 MX MX2024012124A patent/MX2024012124A/es unknown
-
2022
- 2022-03-24 US US17/703,155 patent/US20220324851A1/en not_active Abandoned
-
2023
- 2023-01-11 JP JP2023002371A patent/JP2023036991A/ja active Pending
-
2024
- 2024-02-22 AU AU2024201165A patent/AU2024201165A1/en active Pending
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