ES2835281T3 - Compuestos de 7-feniletilamino-4H-pirimido[4,5-d][1,3]oxazin-2-ona como inhibidores de IDH1 e IDH2 mutantes - Google Patents
Compuestos de 7-feniletilamino-4H-pirimido[4,5-d][1,3]oxazin-2-ona como inhibidores de IDH1 e IDH2 mutantes Download PDFInfo
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- ES2835281T3 ES2835281T3 ES17822882T ES17822882T ES2835281T3 ES 2835281 T3 ES2835281 T3 ES 2835281T3 ES 17822882 T ES17822882 T ES 17822882T ES 17822882 T ES17822882 T ES 17822882T ES 2835281 T3 ES2835281 T3 ES 2835281T3
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- Prior art keywords
- ethyl
- compound
- phenyl
- oxazin
- pyrimido
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- 101000599886 Homo sapiens Isocitrate dehydrogenase [NADP], mitochondrial Proteins 0.000 title claims description 38
- 102100037845 Isocitrate dehydrogenase [NADP], mitochondrial Human genes 0.000 title claims description 38
- 239000003112 inhibitor Substances 0.000 title description 18
- USFRTQXJZLVVJL-UHFFFAOYSA-N 7-(2-phenylethylamino)-1,4-dihydropyrimido[4,5-d][1,3]oxazin-2-one Chemical class C1(=CC=CC=C1)CCNC=1N=CC2=C(NC(OC2)=O)N=1 USFRTQXJZLVVJL-UHFFFAOYSA-N 0.000 title description 2
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- 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 description 11
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- 150000004714 phosphonium salts Chemical class 0.000 description 1
- 230000026731 phosphorylation Effects 0.000 description 1
- 238000006366 phosphorylation reaction Methods 0.000 description 1
- 229960005235 piperonyl butoxide Drugs 0.000 description 1
- 229920000136 polysorbate Polymers 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 239000002244 precipitate Substances 0.000 description 1
- 238000002953 preparative HPLC Methods 0.000 description 1
- VVWRJUBEIPHGQF-UHFFFAOYSA-N propan-2-yl n-propan-2-yloxycarbonyliminocarbamate Chemical compound CC(C)OC(=O)N=NC(=O)OC(C)C VVWRJUBEIPHGQF-UHFFFAOYSA-N 0.000 description 1
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- 238000012827 research and development Methods 0.000 description 1
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- AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 description 1
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- GDMNPKKOWQLMCK-DJZRFWRSSA-N tert-butyl 4-[1-[4-[(1S)-1-aminoethyl]phenyl]-2-cyclopropylethyl]piperazine-1-carboxylate Chemical compound C[C@H](N)c1ccc(cc1)C(CC1CC1)N1CCN(CC1)C(=O)OC(C)(C)C GDMNPKKOWQLMCK-DJZRFWRSSA-N 0.000 description 1
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Classifications
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- 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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
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| US201662435283P | 2016-12-16 | 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 (1)
| Publication Number | Publication Date |
|---|---|
| ES2835281T3 true ES2835281T3 (es) | 2021-06-22 |
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| ES17822882T Active ES2835281T3 (es) | 2016-12-16 | 2017-12-08 | Compuestos de 7-feniletilamino-4H-pirimido[4,5-d][1,3]oxazin-2-ona como inhibidores de IDH1 e IDH2 mutantes |
| ES20189241T Active ES2941631T3 (es) | 2016-12-16 | 2017-12-08 | Compuestos de Pirido[4,3-d][1,3]oxazin-2-ona como inhibidores de IDH1 e IDH2 mutantes |
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| ES20189241T Active ES2941631T3 (es) | 2016-12-16 | 2017-12-08 | Compuestos de Pirido[4,3-d][1,3]oxazin-2-ona como inhibidores de IDH1 e IDH2 mutantes |
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| HUE062424T2 (hu) | 2014-09-19 | 2023-11-28 | Forma Therapeutics Inc | Piridin-2(1H)-on kinolinon származékok mint mutáns izocitrát dehidrogenáz inhibitorok |
| CA2961807A1 (en) | 2014-09-19 | 2016-03-24 | Forma Therapeutics, Inc. | Phenyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| WO2016044781A1 (en) | 2014-09-19 | 2016-03-24 | Forma Therapeutics, Inc. | Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors |
| WO2016044787A1 (en) | 2014-09-19 | 2016-03-24 | Forma Therapeutics, Inc. | Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| US9624175B2 (en) | 2015-04-21 | 2017-04-18 | Forma Therapeutics, Inc. | Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| US10407419B2 (en) | 2015-04-21 | 2019-09-10 | Forma Therapeutics, Inc. | Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors |
| UA125824C2 (uk) | 2016-10-24 | 2022-06-15 | Астразенека Аб | 6,7,8,9-ТЕТРАГІДРО-3H-ПІРАЗОЛО[4,3-f]ІЗОХІНОЛІНОВІ ПОХІДНІ, ЗАСТОСОВНІ В ЛІКУВАННІ РАКУ |
| JP6793836B2 (ja) * | 2016-12-16 | 2020-12-02 | イーライ リリー アンド カンパニー | 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 |
| MX2022004474A (es) | 2016-12-16 | 2023-08-15 | Janssen Pharmaceutica Nv | Inhibidores de moléculas pequeñas de la familia de quinasas jak. |
| JOP20190144A1 (ar) | 2016-12-16 | 2019-06-16 | Janssen Pharmaceutica Nv | إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز |
| CR20190379A (es) | 2017-01-30 | 2019-10-21 | Astrazeneca Ab | Moduladores del receptor de estrógeno |
| US11013734B2 (en) | 2018-05-16 | 2021-05-25 | 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) |
| US11311527B2 (en) | 2018-05-16 | 2022-04-26 | Forma Therapeutics, Inc. | Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-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 |
| SMT202300073T1 (it) | 2018-05-16 | 2023-05-12 | Forma Therapeutics Inc | Inibizione di idh-1 mutante |
| 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 |
| WO2021089395A1 (en) * | 2019-11-08 | 2021-05-14 | Nerviano Medical Sciences S.R.L. | Gem-disubstituted heterocyclic compounds and their use as idh inhibitors |
| MX2022011846A (es) * | 2020-03-23 | 2023-01-04 | Lilly Co Eli | Metodo para el tratamiento de sujetos resistentes al inhibidor idh1. |
| AU2021242260B2 (en) * | 2020-03-23 | 2023-12-14 | Eli Lilly And Company | Combination therapy with a mutant IDH inhibitor |
| EP4125917B1 (en) * | 2020-03-23 | 2024-04-17 | Eli Lilly and Company | Combination therapy with a mutant idh inhibitor and a bcl-2 inhibitor |
| US20210330653A1 (en) | 2020-04-24 | 2021-10-28 | Astrazeneca Ab | Dosage Regimen for the Treatment of Cancer |
| PE20221838A1 (es) | 2020-04-24 | 2022-11-29 | 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 |
| CA3186786A1 (en) * | 2020-07-20 | 2022-01-27 | David Michael HYMAN | Combination therapy with a mutant idh1 inhibitor, a deoxyadenosine analog, and a platinum agent |
| US12390451B2 (en) | 2021-03-11 | 2025-08-19 | Janssen Pharmaceutica Nv | Small molecule inhibitor of the JAK family of kinases |
| 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 |
| US20240261294A1 (en) * | 2021-06-09 | 2024-08-08 | 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 |
| EP4384273A1 (en) | 2021-08-13 | 2024-06-19 | 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 |
| US20250049809A1 (en) * | 2023-07-31 | 2025-02-13 | Board Of Regents, The University Of Texas System | Inhibitors of mutant idh1 and idh2 |
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| MX342326B (es) * | 2011-09-27 | 2016-09-26 | Novartis Ag | 3-pirimidin-4-il-oxazolidin-2-onas como inhibidoras de idh mutante. |
| MX2015012822A (es) * | 2013-03-14 | 2016-05-31 | Novartis Ag | 3-pirimidin-4-il-oxazolidin-2-onas- como inhibidores del 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 |
| US9624175B2 (en) * | 2015-04-21 | 2017-04-18 | Forma Therapeutics, Inc. | Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| GB2552283A (en) * | 2015-04-24 | 2018-01-17 | 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 |
| JP6682043B2 (ja) * | 2016-06-06 | 2020-04-15 | イーライ リリー アンド カンパニー | 変異体ｉｄｈ１阻害剤 |
| JP6793836B2 (ja) * | 2016-12-16 | 2020-12-02 | イーライ リリー アンド カンパニー | 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 |
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2017
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