JP6793836B2 - 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 - Google Patents
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 Download PDFInfo
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- JP6793836B2 JP6793836B2 JP2019532088A JP2019532088A JP6793836B2 JP 6793836 B2 JP6793836 B2 JP 6793836B2 JP 2019532088 A JP2019532088 A JP 2019532088A JP 2019532088 A JP2019532088 A JP 2019532088A JP 6793836 B2 JP6793836 B2 JP 6793836B2
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- idh1
- cancer
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- 101000960234 Homo sapiens Isocitrate dehydrogenase [NADP] cytoplasmic Proteins 0.000 title claims description 76
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- 101000599886 Homo sapiens Isocitrate dehydrogenase [NADP], mitochondrial Proteins 0.000 title claims description 47
- 102100037845 Isocitrate dehydrogenase [NADP], mitochondrial Human genes 0.000 title claims description 47
- JVTRZJXFAOQMRA-UHFFFAOYSA-N 1,3-oxazin-2-one Chemical class O=C1N=CC=CO1 JVTRZJXFAOQMRA-UHFFFAOYSA-N 0.000 title claims description 25
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 53
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 46
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- ORAKJUSEGHCLMU-UCFFOFKASA-N tert-butyl 4-[3-methoxy-1-[4-[(1S)-1-[(2,2,2-trifluoroacetyl)amino]ethyl]phenyl]propyl]piperazine-1-carboxylate Chemical compound COCCC(N1CCN(CC1)C(=O)OC(C)(C)C)c1ccc(cc1)[C@H](C)NC(=O)C(F)(F)F ORAKJUSEGHCLMU-UCFFOFKASA-N 0.000 description 1
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- 150000003628 tricarboxylic acids Chemical class 0.000 description 1
- 210000004881 tumor cell Anatomy 0.000 description 1
- 230000004565 tumor cell growth Effects 0.000 description 1
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Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5365—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
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| 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 |
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| JP2020502157A JP2020502157A (ja) | 2020-01-23 |
| JP2020502157A5 JP2020502157A5 (enExample) | 2020-03-05 |
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| KR102209667B1 (ko) | 2014-09-19 | 2021-01-29 | 포르마 세라퓨틱스 인크. | 돌연변이-아이소시트레이트 탈수소효소 저해제로서의 피리딘-2(1h)-온 퀴놀린 유도체 |
| MX372964B (es) | 2014-09-19 | 2020-03-27 | Forma Therapeutics Inc | Derivados de fenil quinolinona como inhibidores de isocitrato deshidrogenasa mutante (mt-idh) |
| AU2015317321B2 (en) | 2014-09-19 | 2020-03-12 | Forma Therapeutics, Inc. | Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors |
| EP3201185B1 (en) | 2014-09-19 | 2018-11-21 | Forma Therapeutics, Inc. | Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| WO2016171755A1 (en) | 2015-04-21 | 2016-10-27 | Forma Therapeutics, Inc. | Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| US9624216B2 (en) | 2015-04-21 | 2017-04-18 | Forma Therapeutics, Inc. | Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors |
| JOP20190090B1 (ar) | 2016-10-24 | 2023-03-28 | Astrazeneca Ab | مشتقات 9،8،7،6-رابع هيدرو-3h-بيرازولو [4،3-f]أيزوكينولين مفيدة في علاج السرطان |
| JOP20190144A1 (ar) | 2016-12-16 | 2019-06-16 | Janssen Pharmaceutica Nv | إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز |
| PH12019501328B1 (en) * | 2016-12-16 | 2023-05-12 | Lilly Co Eli | 7-phenylethlamino-4h-pyrimido][4,5-d][1,3] oxazin-2-one compounds as mutant 1dh1 and 1dh2 inhibitors |
| JP7291077B2 (ja) | 2016-12-16 | 2023-06-14 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｊａｋファミリーのキナーゼの低分子阻害物質 |
| EP3689873B1 (en) | 2017-01-30 | 2022-09-14 | Astrazeneca AB | Estrogen receptor modulators |
| US20210196701A1 (en) | 2018-05-16 | 2021-07-01 | Forma Therapeutics, Inc. | Inhibiting mutant idh-1 |
| US11497743B2 (en) | 2018-05-16 | 2022-11-15 | Forma Therapeutics, Inc. | Treating patients harboring an isocitrate dehydrogenase 1 (IDH-1) mutation |
| US11013733B2 (en) | 2018-05-16 | 2021-05-25 | Forma Therapeutics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mlDH-1) |
| WO2019222551A1 (en) | 2018-05-16 | 2019-11-21 | 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 |
| US11013734B2 (en) | 2018-05-16 | 2021-05-25 | Forma Therapeutics, Inc. | Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation |
| US11738018B2 (en) | 2018-05-16 | 2023-08-29 | FORMA Therapeuetics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-1) |
| US11311527B2 (en) | 2018-05-16 | 2022-04-26 | Forma Therapeutics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-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 |
| ES3033669T3 (en) | 2019-11-08 | 2025-08-06 | Nerviano Medical Sciences Srl | Gem-disubstituted heterocyclic compounds and their use as idh inhibitors |
| AU2021241470B2 (en) * | 2020-03-23 | 2023-12-14 | Board Of Regents, The University Of Texas System | Combination therapy with a mutant IDH inhibitor and a Bcl-2 inhibitor |
| ES2981250T3 (es) * | 2020-03-23 | 2024-10-08 | Lilly Co Eli | Terapia combinada con un inhibidor de IDH mutante |
| IL296094A (en) * | 2020-03-23 | 2022-11-01 | Lilly Co Eli | Method for treating idh1 inhibitor-resistant subjects |
| JP7712955B2 (ja) | 2020-04-24 | 2025-07-24 | アストラゼネカ・アクチエボラーグ | 癌の治療のための投薬レジメン |
| MX2022013258A (es) | 2020-04-24 | 2022-11-14 | Astrazeneca Ab | Formulaciones farmaceuticas. |
| CN115768775B (zh) * | 2020-06-28 | 2024-10-25 | 微境生物医药科技(上海)有限公司 | Idh突变体抑制剂及其用途 |
| JP2023534991A (ja) * | 2020-07-20 | 2023-08-15 | イーライ リリー アンド カンパニー | 変異型ｉｄｈ１阻害剤、デオキシアデノシン類似体、及び白金剤を用いた併用療法 |
| 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 |
| CN117460514A (zh) * | 2021-06-09 | 2024-01-26 | 伊莱利利公司 | 用于治疗idh抑制剂耐药的对象的方法 |
| US20240208978A1 (en) * | 2021-06-15 | 2024-06-27 | Wigen Biomedicine Technology (shanghai) Co., Ltd. | Idh mutant inhibitor and use thereof |
| CA3224704A1 (en) | 2021-08-13 | 2023-02-16 | David Andrew Coates | Solid forms of 7-[[(1s)-1-[4-[(1s)-2-cyclopropyl-1-(4-prop-2-enoylpiper azin-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 |
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| AU2012313888B2 (en) * | 2011-09-27 | 2016-03-31 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH |
| BR112015022483A2 (pt) * | 2013-03-14 | 2017-07-18 | Novartis Ag | 3-pirimidin-4-il-oxazolidin-2-onas como inibidores de idh mutante |
| WO2014147586A1 (en) * | 2013-03-22 | 2014-09-25 | Novartis Ag | 1-(2-(ethylamino)pyrimidin-4-yl)pyrrolidin-2-ones as inhibitors of mutant idh |
| WO2016171755A1 (en) * | 2015-04-21 | 2016-10-27 | Forma Therapeutics, Inc. | Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| WO2016171715A1 (en) * | 2015-04-24 | 2016-10-27 | Halliburton Energy Services, Inc. | Methods of fabricating ceramic or intermetallic parts |
| JP6473270B2 (ja) * | 2015-07-27 | 2019-02-20 | イーライ リリー アンド カンパニー | 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−オン化合物及び変異体ｉｄｈ１阻害剤としてのそれらの使用 |
| ES2814290T3 (es) * | 2016-06-06 | 2021-03-26 | Lilly Co Eli | Inhibidores de IDH1 mutante |
| PH12019501328B1 (en) * | 2016-12-16 | 2023-05-12 | Lilly Co Eli | 7-phenylethlamino-4h-pyrimido][4,5-d][1,3] oxazin-2-one compounds as mutant 1dh1 and 1dh2 inhibitors |
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