JP2020502157A5 - - Google Patents
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- Publication number
- JP2020502157A5 JP2020502157A5 JP2019532088A JP2019532088A JP2020502157A5 JP 2020502157 A5 JP2020502157 A5 JP 2020502157A5 JP 2019532088 A JP2019532088 A JP 2019532088A JP 2019532088 A JP2019532088 A JP 2019532088A JP 2020502157 A5 JP2020502157 A5 JP 2020502157A5
- Authority
- JP
- Japan
- Prior art keywords
- ethyl
- pharmaceutically acceptable
- cancer
- glioblastoma
- enoylpiperazin
- 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
- 208000005017 glioblastoma Diseases 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 5
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 4
- 208000025324 B-cell acute lymphoblastic leukemia Diseases 0.000 claims 4
- 101001042041 Bos taurus Isocitrate dehydrogenase [NAD] subunit beta, mitochondrial Proteins 0.000 claims 4
- 201000008808 Fibrosarcoma Diseases 0.000 claims 4
- 208000032612 Glial tumor Diseases 0.000 claims 4
- 206010018338 Glioma Diseases 0.000 claims 4
- 101000960234 Homo sapiens Isocitrate dehydrogenase [NADP] cytoplasmic Proteins 0.000 claims 4
- 101000599886 Homo sapiens Isocitrate dehydrogenase [NADP], mitochondrial Proteins 0.000 claims 4
- 102100039905 Isocitrate dehydrogenase [NADP] cytoplasmic Human genes 0.000 claims 4
- 102100037845 Isocitrate dehydrogenase [NADP], mitochondrial Human genes 0.000 claims 4
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 206010002449 angioimmunoblastic T-cell lymphoma Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- -1 2 -cyclopropyl Chemical group 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 206010003571 Astrocytoma Diseases 0.000 claims 2
- 208000005243 Chondrosarcoma Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 201000010915 Glioblastoma multiforme Diseases 0.000 claims 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 2
- 201000010133 Oligodendroglioma Diseases 0.000 claims 2
- 206010061332 Paraganglion neoplasm Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 2
- 201000007450 intrahepatic cholangiocarcinoma Diseases 0.000 claims 2
- 201000001441 melanoma Diseases 0.000 claims 2
- 208000007312 paraganglioma Diseases 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 201000002510 thyroid cancer Diseases 0.000 claims 2
- JVTRZJXFAOQMRA-UHFFFAOYSA-N 1,3-oxazin-2-one Chemical compound O=C1N=CC=CO1 JVTRZJXFAOQMRA-UHFFFAOYSA-N 0.000 claims 1
- BASWGFWYCDZRSM-HXBUSHRASA-N 1-ethyl-7-[[(1S)-1-[4-[1-(4-prop-2-enoylpiperazin-1-yl)propyl]phenyl]ethyl]amino]-4H-pyrimido[4,5-d][1,3]oxazin-2-one Chemical compound CCC(N1CCN(CC1)C(=O)C=C)C1=CC=C(C=C1)[C@H](C)NC1=NC2=C(COC(=O)N2CC)C=N1 BASWGFWYCDZRSM-HXBUSHRASA-N 0.000 claims 1
- AFGYODUJVVOZAX-YADARESESA-N 7-[[(1S)-1-[4-[(1R)-2-cyclopropyl-1-(4-prop-2-enoylpiperazin-1-yl)ethyl]phenyl]ethyl]amino]-1-ethyl-4H-pyrimido[4,5-d][1,3]oxazin-2-one Chemical compound CCN1C(=O)OCc2cnc(N[C@@H](C)c3ccc(cc3)[C@@H](CC3CC3)N3CCN(CC3)C(=O)C=C)nc12 AFGYODUJVVOZAX-YADARESESA-N 0.000 claims 1
- AFGYODUJVVOZAX-CYFREDJKSA-N 7-[[(1S)-1-[4-[(1S)-2-cyclopropyl-1-(4-prop-2-enoylpiperazin-1-yl)ethyl]phenyl]ethyl]amino]-1-ethyl-4H-pyrimido[4,5-d][1,3]oxazin-2-one Chemical compound CCN1C(=O)OCC2=C1N=C(N[C@@H](C)C1=CC=C(C=C1)[C@H](CC1CC1)N1CCN(CC1)C(=O)C=C)N=C2 AFGYODUJVVOZAX-CYFREDJKSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662435283P | 2016-12-16 | 2016-12-16 | |
| US62/435,283 | 2016-12-16 | ||
| PCT/US2017/065246 WO2018111707A1 (en) | 2016-12-16 | 2017-12-08 | 7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant idh1 and idh2 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020502157A JP2020502157A (ja) | 2020-01-23 |
| JP2020502157A5 true JP2020502157A5 (enExample) | 2020-03-05 |
| JP6793836B2 JP6793836B2 (ja) | 2020-12-02 |
Family
ID=60888651
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019532088A Active JP6793836B2 (ja) | 2016-12-16 | 2017-12-08 | 変異体ｉｄｈ１およびｉｄｈ２阻害剤としての７−フェニルエチルアミノ−４ｈ−ピリミド［４，５−ｄ］［１，３］オキサジン−２−オン化合物 |
Country Status (37)
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3194375B1 (en) | 2014-09-19 | 2018-11-21 | Forma Therapeutics, Inc. | Phenyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| US9771349B2 (en) | 2014-09-19 | 2017-09-26 | Forma Therapeutics, Inc. | Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| PT3733662T (pt) | 2014-09-19 | 2023-08-18 | Forma Therapeutics Inc | Derivados piridin-2(1h)-ona-quinolinona como inibidores de isocitrato desidrogenase mutante |
| ES2768694T3 (es) | 2014-09-19 | 2020-06-23 | Forma Therapeutics Inc | Composiciones de quinolinona pirimidinas como inhibidores de isocitrato dehidrogenasa mutante |
| US9624216B2 (en) | 2015-04-21 | 2017-04-18 | Forma Therapeutics, Inc. | Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors |
| US10294206B2 (en) | 2015-04-21 | 2019-05-21 | Forma Tm2, Inc. | Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| PT3433256T (pt) | 2016-10-24 | 2019-10-31 | Astrazeneca | Derivados de 6,7,8,9-tetrahidro-3h-pirazolo[4,3-f]isoquinolina úteis no tratamento do cancro |
| JOP20190144A1 (ar) | 2016-12-16 | 2019-06-16 | Janssen Pharmaceutica Nv | إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز |
| ES2922379T3 (es) | 2016-12-16 | 2022-09-14 | Janssen Pharmaceutica Nv | Compuestos de imidazo[4,5,D]pirrolo[2,3,B]piridina como inhibidores de Janus quinasas |
| CN110072867B (zh) * | 2016-12-16 | 2022-07-08 | 伊莱利利公司 | 作为突变体idh1和idh2抑制剂的7-苯基乙基氨基-4h-嘧啶并[4,5-d][1,3]噁嗪-2-酮化合物 |
| KR102246668B1 (ko) | 2017-01-30 | 2021-04-29 | 아스트라제네카 아베 | 에스트로겐 수용체 조절인자 |
| US11013733B2 (en) | 2018-05-16 | 2021-05-25 | Forma Therapeutics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mlDH-1) |
| US11013734B2 (en) | 2018-05-16 | 2021-05-25 | Forma Therapeutics, Inc. | Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation |
| US11311527B2 (en) | 2018-05-16 | 2022-04-26 | Forma Therapeutics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-1) |
| US10532047B2 (en) | 2018-05-16 | 2020-01-14 | Forma Therapeutics, Inc. | Solid forms of ((S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile |
| EP3720442B1 (en) | 2018-05-16 | 2022-12-28 | Forma Therapeutics, Inc. | Inhibiting mutant idh-1 |
| TW202016110A (zh) | 2018-06-15 | 2020-05-01 | 比利時商健生藥品公司 | Ｊａｋ激酶家族之小分子抑制劑 |
| JP7744336B2 (ja) * | 2019-11-08 | 2025-09-25 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | ｇｅｍ－二置換複素環式化合物及びＩＤＨ阻害剤としてのその使用 |
| EP4125917B1 (en) | 2020-03-23 | 2024-04-17 | Eli Lilly and Company | Combination therapy with a mutant idh inhibitor and a bcl-2 inhibitor |
| IL296094A (en) | 2020-03-23 | 2022-11-01 | Lilly Co Eli | Method for treating idh1 inhibitor-resistant subjects |
| BR112022017394A2 (pt) | 2020-03-23 | 2022-10-18 | Lilly Co Eli | Terapia de combinação com um inibidor de idh mutante |
| IL297216A (en) | 2020-04-24 | 2022-12-01 | Astrazeneca Ab | Dosage regimen for the treatment of cancer |
| PE20221838A1 (es) | 2020-04-24 | 2022-11-29 | Astrazeneca Ab | Formulaciones farmaceuticas |
| US20230174550A1 (en) * | 2020-06-28 | 2023-06-08 | Wigen Biomedicine Technology (shanghai) Co., Ltd. | Idh mutant inhibitor and use thereof |
| WO2022020281A1 (en) | 2020-07-20 | 2022-01-27 | Eli Lilly And Company | Combination therapy with a mutant idh1 inhibitor, a deoxyadenosine analog, and a platinum agent |
| AU2022233254A1 (en) | 2021-03-11 | 2023-10-26 | Janssen Pharmaceutica Nv | Lorpucitinib for use in the treatment of jak mediated disorders |
| CN113588768B (zh) * | 2021-05-18 | 2022-07-05 | 国家卫生健康委科学技术研究所 | 一种以分子图像方式定量组织内内源性代谢物的质谱方法 |
| EP4337217A1 (en) | 2021-06-09 | 2024-03-20 | Eli Lilly and Company | Method for treating idh inhibitor-resistant subjects |
| BR112023024454A2 (pt) * | 2021-06-15 | 2024-02-06 | Wigen Biomedicine Tech Shanghai Co Ltd | Composto de fórmula geral (1) ou um isômero, uma forma cristalina, um sal farmaceuticamente aceitável, um hidrato ou um solvato do mesmo; e; uso do composto ou do isômero |
| US11746115B2 (en) | 2021-08-13 | 2023-09-05 | Eli Lilly And Company | Solid forms of 7-[[(1S)-1-[4-[(1S)-2-cyclopropyl-1-(4-prop-2-enoylpiperazin-1-yl)ethyl]phenyl]ethyl]amino]-1-ethyl-4H-pyrimido[4,5-d][1,3]oxazin-2-one |
| WO2023141087A1 (en) | 2022-01-19 | 2023-07-27 | Eli Lilly And Company | Combination therapy with a mutant idh inhibitor |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6026544B2 (ja) * | 2011-09-27 | 2016-11-16 | ノバルティス アーゲー | 変異体ｉｄｈの阻害剤としての３−ピリミジン−４−イル−オキサゾリジン−２−オン類 |
| KR20150127197A (ko) * | 2013-03-14 | 2015-11-16 | 노파르티스 아게 | 돌연변이 idh의 억제제로서의 3-피리미딘-4-일-옥사졸리딘-2-온 |
| WO2014147586A1 (en) * | 2013-03-22 | 2014-09-25 | Novartis Ag | 1-(2-(ethylamino)pyrimidin-4-yl)pyrrolidin-2-ones as inhibitors of mutant idh |
| US10294206B2 (en) * | 2015-04-21 | 2019-05-21 | Forma Tm2, Inc. | Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| US10471507B2 (en) * | 2015-04-24 | 2019-11-12 | Halliburton Energy Services, Inc. | Methods of fabricating ceramic or intermetallic parts |
| WO2017019429A1 (en) * | 2015-07-27 | 2017-02-02 | Eli Lilly And Company | 7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds and theit use as mutant idh1 inhibitors |
| ES2814290T3 (es) * | 2016-06-06 | 2021-03-26 | Lilly Co Eli | Inhibidores de IDH1 mutante |
| CN110072867B (zh) * | 2016-12-16 | 2022-07-08 | 伊莱利利公司 | 作为突变体idh1和idh2抑制剂的7-苯基乙基氨基-4h-嘧啶并[4,5-d][1,3]噁嗪-2-酮化合物 |
-
2017
- 2017-12-08 CN CN201780078017.0A patent/CN110072867B/zh active Active
- 2017-12-08 TN TNP/2019/000158A patent/TN2019000158A1/en unknown
- 2017-12-08 ES ES20189241T patent/ES2941631T3/es active Active
- 2017-12-08 UA UAA201905584A patent/UA123640C2/uk unknown
- 2017-12-08 MD MDE20191188T patent/MD3555105T2/ro unknown
- 2017-12-08 MY MYPI2019003350A patent/MY197313A/en unknown
- 2017-12-08 WO PCT/US2017/065246 patent/WO2018111707A1/en not_active Ceased
- 2017-12-08 HR HRP20201882TT patent/HRP20201882T1/hr unknown
- 2017-12-08 CA CA3045303A patent/CA3045303C/en active Active
- 2017-12-08 EP EP20189241.1A patent/EP3763717B1/en active Active
- 2017-12-08 MA MA053881A patent/MA53881A/fr unknown
- 2017-12-08 PT PT178228821T patent/PT3555105T/pt unknown
- 2017-12-08 CN CN202210758386.7A patent/CN115109075B/zh active Active
- 2017-12-08 KR KR1020197016855A patent/KR102276022B1/ko active Active
- 2017-12-08 PE PE2019001077A patent/PE20190977A1/es unknown
- 2017-12-08 JP JP2019532088A patent/JP6793836B2/ja active Active
- 2017-12-08 EA EA201991161A patent/EA036112B1/ru not_active IP Right Cessation
- 2017-12-08 DK DK17822882.1T patent/DK3555105T3/da active
- 2017-12-08 NZ NZ754115A patent/NZ754115A/en unknown
- 2017-12-08 CR CR20190252A patent/CR20190252A/es unknown
- 2017-12-08 AU AU2017378060A patent/AU2017378060B2/en active Active
- 2017-12-08 HU HUE17822882A patent/HUE052067T2/hu unknown
- 2017-12-08 JO JOP/2019/0142A patent/JOP20190142B1/ar active
- 2017-12-08 MX MX2019006830A patent/MX385562B/es unknown
- 2017-12-08 EP EP17822882.1A patent/EP3555105B1/en active Active
- 2017-12-08 US US16/349,873 patent/US11001596B2/en active Active
- 2017-12-08 MA MA47399A patent/MA47399B1/fr unknown
- 2017-12-08 ES ES17822882T patent/ES2835281T3/es active Active
- 2017-12-08 LT LTEP17822882.1T patent/LT3555105T/lt unknown
- 2017-12-08 PL PL17822882T patent/PL3555105T3/pl unknown
- 2017-12-08 SI SI201730488T patent/SI3555105T1/sl unknown
- 2017-12-08 RS RS20201429A patent/RS61108B1/sr unknown
- 2017-12-08 PH PH1/2019/501328A patent/PH12019501328B1/en unknown
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2019
- 2019-05-17 ZA ZA2019/03125A patent/ZA201903125B/en unknown
- 2019-05-23 CO CONC2019/0005287A patent/CO2019005287A2/es unknown
- 2019-05-30 SA SA519401897A patent/SA519401897B1/ar unknown
- 2019-06-06 CL CL2019001551A patent/CL2019001551A1/es unknown
- 2019-06-11 DO DO2019000163A patent/DOP2019000163A/es unknown
- 2019-06-11 IL IL267236A patent/IL267236B/en active IP Right Grant
- 2019-06-14 EC ECSENADI201942682A patent/ECSP19042682A/es unknown
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2020
- 2020-10-29 AU AU2020260493A patent/AU2020260493B2/en active Active
- 2020-11-25 CY CY20201101122T patent/CY1123577T1/el unknown
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2021
- 2021-03-16 US US17/202,515 patent/US11649247B2/en active Active
- 2021-03-16 US US17/202,867 patent/US11629156B2/en active Active
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