JP2016520645A5 - - Google Patents
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- Publication number
- JP2016520645A5 JP2016520645A5 JP2016517732A JP2016517732A JP2016520645A5 JP 2016520645 A5 JP2016520645 A5 JP 2016520645A5 JP 2016517732 A JP2016517732 A JP 2016517732A JP 2016517732 A JP2016517732 A JP 2016517732A JP 2016520645 A5 JP2016520645 A5 JP 2016520645A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- methyl
- amino
- pyrido
- dione
- 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.)
- Ceased
Links
- -1 heterocycloalkyloxy- Chemical group 0.000 claims 67
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 47
- 125000001072 heteroaryl group Chemical group 0.000 claims 29
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 28
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 26
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 21
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 19
- 150000001875 compounds Chemical class 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 13
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 12
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 12
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 12
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 11
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 9
- 229910052757 nitrogen Inorganic materials 0.000 claims 9
- 125000004093 cyano group Chemical group *C#N 0.000 claims 8
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 150000001602 bicycloalkyls Chemical group 0.000 claims 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 3
- 125000006625 (C3-C8) cycloalkyloxy group Chemical group 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- 125000005466 alkylenyl group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000005842 heteroatom Chemical group 0.000 claims 3
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000004043 oxo group Chemical group O=* 0.000 claims 3
- 229910052760 oxygen Inorganic materials 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 229910052717 sulfur Chemical group 0.000 claims 3
- 239000011593 sulfur Chemical group 0.000 claims 3
- 125000006564 (C4-C8) cycloalkyl group Chemical group 0.000 claims 2
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 2
- 125000000000 cycloalkoxy group Chemical group 0.000 claims 2
- 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 2
- 125000002933 cyclohexyloxy group Chemical group C1(CCCCC1)O* 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- OKUFKPFKQQFJJN-GQCTYLIASA-N (13E)-17-[ethyl(piperidin-4-yl)amino]-8-methyl-3,7-diazatricyclo[14.4.0.05,10]icosa-1(16),5(10),8,13,17,19-hexaene-2,6-dione Chemical compound C=1C=CC(C(NCC=2C(=O)NC(C)=CC=2CC/C=C/C2)=O)=C2C=1N(CC)C1CCNCC1 OKUFKPFKQQFJJN-GQCTYLIASA-N 0.000 claims 1
- 125000006526 (C1-C2) alkyl group Chemical group 0.000 claims 1
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000012609 Cowden disease Diseases 0.000 claims 1
- 201000002847 Cowden syndrome Diseases 0.000 claims 1
- 206010014967 Ependymoma Diseases 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 208000005726 Inflammatory Breast Neoplasms Diseases 0.000 claims 1
- 206010021980 Inflammatory carcinoma of the breast Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 208000008770 Multiple Hamartoma Syndrome Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical group C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000002541 furyl group Chemical group 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 201000004653 inflammatory breast carcinoma Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 201000008026 nephroblastoma Diseases 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 1
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 230000002861 ventricular Effects 0.000 claims 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361831649P | 2013-06-06 | 2013-06-06 | |
| US61/831,649 | 2013-06-06 | ||
| US201461949399P | 2014-03-07 | 2014-03-07 | |
| US61/949,399 | 2014-03-07 | ||
| US201461977666P | 2014-04-10 | 2014-04-10 | |
| US61/977,666 | 2014-04-10 | ||
| PCT/IB2014/062025 WO2014195919A1 (en) | 2013-06-06 | 2014-06-06 | Enhancer of zeste homolog 2 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016520645A JP2016520645A (ja) | 2016-07-14 |
| JP2016520645A5 true JP2016520645A5 (OSRAM) | 2017-07-13 |
Family
ID=50980343
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016517732A Ceased JP2016520645A (ja) | 2013-06-06 | 2014-06-06 | Ｚｅｓｔｅホモログ２エンハンサー阻害剤 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20160122342A1 (OSRAM) |
| EP (1) | EP3004096A1 (OSRAM) |
| JP (1) | JP2016520645A (OSRAM) |
| KR (1) | KR20160018594A (OSRAM) |
| CN (1) | CN105452246A (OSRAM) |
| AU (1) | AU2014276417B2 (OSRAM) |
| BR (1) | BR112015030515A2 (OSRAM) |
| CA (1) | CA2914414A1 (OSRAM) |
| RU (1) | RU2015155595A (OSRAM) |
| WO (1) | WO2014195919A1 (OSRAM) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2013331368A1 (en) | 2012-10-15 | 2015-04-30 | Epizyme, Inc. | Methods of treating cancer |
| 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 |
| US20190070188A1 (en) * | 2015-11-06 | 2019-03-07 | Epizyme, Inc. | Pediatric dosing for treatment of cancer with an ezh2 inhibitor |
| US10266542B2 (en) | 2017-03-15 | 2019-04-23 | Mirati Therapeutics, Inc. | EZH2 inhibitors |
| CN111344290B (zh) * | 2017-11-01 | 2023-12-01 | 无锡智康弘义生物科技有限公司 | 作为Wee1抑制剂的大环类化合物及其应用 |
| CN108117564B (zh) * | 2017-12-20 | 2020-09-04 | 苏州百灵威超精细材料有限公司 | 一种制备穴醚222的工艺方法 |
| PT3746446T (pt) | 2018-01-31 | 2022-07-18 | Mirati Therapeutics Inc | Inibidores de prc2 |
| CN110229151B (zh) * | 2018-03-06 | 2021-09-10 | 上海海和药物研究开发股份有限公司 | 吲嗪类化合物、其制备方法及用途 |
| EP3823671B1 (en) | 2018-07-09 | 2024-02-07 | Fondation Asile Des Aveugles | Inhibition of prc2 subunits to treat eye disorders |
| CA3106589A1 (en) * | 2018-07-27 | 2020-01-30 | Suzhou Sinovent Pharma Co., Ltd. | Polysubstituted benzene compound and preparation method and use thereof |
| US12180184B2 (en) | 2018-10-26 | 2024-12-31 | Wuxi Biocity Biopharmaceutics Co., Ltd. | Pyrimidopyrazolone derivative as Wee1 inhibitor and use thereof |
| EP3959214A1 (en) | 2019-04-22 | 2022-03-02 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as prc2 inhibitors |
| CN111909157B (zh) | 2019-05-07 | 2023-02-03 | 南京药石科技股份有限公司 | Ezh2抑制剂及其用途 |
| EP3980422A1 (en) | 2019-06-05 | 2022-04-13 | Mirati Therapeutics, Inc. | Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2566327T (pt) * | 2010-05-07 | 2017-05-26 | Glaxosmithkline Llc | Indoles |
| EP2646020B1 (en) * | 2010-12-01 | 2016-09-21 | Glaxosmithkline LLC | Indoles |
| JO3438B1 (ar) * | 2011-04-13 | 2019-10-20 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| PT2710018T (pt) * | 2011-05-19 | 2022-03-01 | Fundacion Del Sector Publico Estatal Centro Nac De Investigaciones Oncologicas Carlos Iii F S P Cnio | Compostos macrocíclicos como inibidores de proteína quinases |
| WO2013173441A2 (en) * | 2012-05-16 | 2013-11-21 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
-
2014
- 2014-06-06 KR KR1020157037025A patent/KR20160018594A/ko not_active Withdrawn
- 2014-06-06 WO PCT/IB2014/062025 patent/WO2014195919A1/en not_active Ceased
- 2014-06-06 RU RU2015155595A patent/RU2015155595A/ru not_active Application Discontinuation
- 2014-06-06 CN CN201480043421.0A patent/CN105452246A/zh active Pending
- 2014-06-06 CA CA2914414A patent/CA2914414A1/en not_active Abandoned
- 2014-06-06 EP EP14732021.2A patent/EP3004096A1/en not_active Withdrawn
- 2014-06-06 JP JP2016517732A patent/JP2016520645A/ja not_active Ceased
- 2014-06-06 BR BR112015030515A patent/BR112015030515A2/pt not_active IP Right Cessation
- 2014-06-06 AU AU2014276417A patent/AU2014276417B2/en not_active Ceased
- 2014-06-06 US US14/895,947 patent/US20160122342A1/en not_active Abandoned
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