KR102276022B1 - 돌연변이체 idh1 및 idh2 억제제로서의 7-페닐에틸아미노-4h-피리미도[4,5-d][1,3]옥사진-2-온 화합물 - Google Patents
돌연변이체 idh1 및 idh2 억제제로서의 7-페닐에틸아미노-4h-피리미도[4,5-d][1,3]옥사진-2-온 화합물 Download PDFInfo
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- KR102276022B1 KR102276022B1 KR1020197016855A KR20197016855A KR102276022B1 KR 102276022 B1 KR102276022 B1 KR 102276022B1 KR 1020197016855 A KR1020197016855 A KR 1020197016855A KR 20197016855 A KR20197016855 A KR 20197016855A KR 102276022 B1 KR102276022 B1 KR 102276022B1
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- South Korea
- Prior art keywords
- ethyl
- compound
- phenyl
- oxazin
- mmol
- 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.)
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- OJAJQPPNSPNCIA-UHFFFAOYSA-N CSc1ncc(COC(N2)=O)c2n1 Chemical compound CSc1ncc(COC(N2)=O)c2n1 OJAJQPPNSPNCIA-UHFFFAOYSA-N 0.000 description 1
- SHSKNAGOEXFZER-LURJTMIESA-N C[C@@H](c(cc1)ccc1Br)NC(C(F)(F)F)=O Chemical compound C[C@@H](c(cc1)ccc1Br)NC(C(F)(F)F)=O SHSKNAGOEXFZER-LURJTMIESA-N 0.000 description 1
- JUHDQPLVTZBONJ-DQUNLGLBSA-N C[C@@H](c1ccc(C(CC2CC2)N(CC2)CCN2C(OC(C)(C)C)=O)cc1)Nc1ncc(COC(N2C)=O)c2c1 Chemical compound C[C@@H](c1ccc(C(CC2CC2)N(CC2)CCN2C(OC(C)(C)C)=O)cc1)Nc1ncc(COC(N2C)=O)c2c1 JUHDQPLVTZBONJ-DQUNLGLBSA-N 0.000 description 1
- GDMNPKKOWQLMCK-JXFKEZNVSA-N C[C@@H](c1ccc([C@H](CC2CC2)N(CC2)CCN2C(OC(C)(C)C)=O)cc1)N Chemical compound C[C@@H](c1ccc([C@H](CC2CC2)N(CC2)CCN2C(OC(C)(C)C)=O)cc1)N GDMNPKKOWQLMCK-JXFKEZNVSA-N 0.000 description 1
- PSHNPAKOZYNOJK-JXFKEZNVSA-N C[C@@H](c1ccc([C@H](CC2CC2)N(CC2)CCN2C(OC(C)(C)C)=O)cc1)NC(C(F)(F)F)=O Chemical compound C[C@@H](c1ccc([C@H](CC2CC2)N(CC2)CCN2C(OC(C)(C)C)=O)cc1)NC(C(F)(F)F)=O PSHNPAKOZYNOJK-JXFKEZNVSA-N 0.000 description 1
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
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- 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 (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 (2)
| Publication Number | Publication Date |
|---|---|
| KR20190077539A KR20190077539A (ko) | 2019-07-03 |
| KR102276022B1 true KR102276022B1 (ko) | 2021-07-13 |
Family
ID=60888651
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020197016855A Active KR102276022B1 (ko) | 2016-12-16 | 2017-12-08 | 돌연변이체 idh1 및 idh2 억제제로서의 7-페닐에틸아미노-4h-피리미도[4,5-d][1,3]옥사진-2-온 화합물 |
Country Status (37)
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2961807A1 (en) | 2014-09-19 | 2016-03-24 | Forma Therapeutics, Inc. | Phenyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| CA2961811C (en) | 2014-09-19 | 2021-11-02 | Forma Therapeutics, Inc. | Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| ES2768694T3 (es) | 2014-09-19 | 2020-06-23 | Forma Therapeutics Inc | Composiciones de quinolinona pirimidinas como inhibidores de isocitrato dehidrogenasa mutante |
| WO2016044789A1 (en) | 2014-09-19 | 2016-03-24 | Forma Therapeutics, Inc. | Pyridin-2(1h)-one 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 |
| US10294206B2 (en) | 2015-04-21 | 2019-05-21 | Forma Tm2, Inc. | Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors |
| TWI735681B (zh) | 2016-10-24 | 2021-08-11 | 瑞典商阿斯特捷利康公司 | 化合物 |
| KR102276022B1 (ko) * | 2016-12-16 | 2021-07-13 | 일라이 릴리 앤드 캄파니 | 돌연변이체 idh1 및 idh2 억제제로서의 7-페닐에틸아미노-4h-피리미도[4,5-d][1,3]옥사진-2-온 화합물 |
| LT3555097T (lt) | 2016-12-16 | 2022-08-25 | Janssen Pharmaceutica Nv | Imidazo[4,5-d]pirolo[2,3-b]piridino junginiai kaip janus kinazės inhibitoriai |
| JOP20190144A1 (ar) | 2016-12-16 | 2019-06-16 | Janssen Pharmaceutica Nv | إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز |
| PT3494116T (pt) | 2017-01-30 | 2020-01-28 | Astrazeneca Ab | Moduladores de recetores de estrogénio |
| 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 |
| WO2019222553A1 (en) | 2018-05-16 | 2019-11-21 | Forma Therapeutics, Inc. | Inhibiting mutant idh-1 |
| 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) |
| 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 |
| CN115443137B (zh) * | 2020-03-23 | 2024-05-31 | 伊莱利利公司 | 使用突变idh抑制剂和bcl-2抑制剂的组合疗法 |
| CN115335060B (zh) * | 2020-03-23 | 2024-11-12 | 伊莱利利公司 | 使用突变idh抑制剂的组合疗法 |
| AU2021241471B2 (en) * | 2020-03-23 | 2023-12-14 | Eli Lilly And Company | Method for treating IDH1 inhibitor-resistant subjects |
| WO2021214253A1 (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 |
| WO2022001916A1 (zh) * | 2020-06-28 | 2022-01-06 | 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 |
| US20230255973A1 (en) * | 2020-07-20 | 2023-08-17 | Eli Lilly And Company | Combination therapy with a mutant idh1 inhibitor, a deoxyadenosine analog, and a platinum agent |
| BR112023018286A2 (pt) | 2021-03-11 | 2023-10-31 | Janssen Pharmaceutica Nv | Lorpucitinib para uso no tratamento de distúrbios mediados por jak |
| 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 |
| MX2023013664A (es) | 2021-06-15 | 2024-01-08 | Wigen Biomedicine Tech Shanghai Co Ltd | Inhibidor de mutante de idh y uso del mismo. |
| 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 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013046136A1 (en) | 2011-09-27 | 2013-04-04 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-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 |
| 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 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105209460A (zh) * | 2013-03-14 | 2015-12-30 | 诺华股份有限公司 | 作为突变idh抑制剂的3-嘧啶-4-基-噁唑烷-2-酮化合物 |
| WO2014147586A1 (en) * | 2013-03-22 | 2014-09-25 | Novartis Ag | 1-(2-(ethylamino)pyrimidin-4-yl)pyrrolidin-2-ones as inhibitors of mutant idh |
| CN107405687A (zh) * | 2015-04-24 | 2017-11-28 | 哈利伯顿能源服务公司 | 制作陶瓷或金属间化合物零件的方法 |
| ES2814290T3 (es) * | 2016-06-06 | 2021-03-26 | Lilly Co Eli | Inhibidores de IDH1 mutante |
| KR102276022B1 (ko) * | 2016-12-16 | 2021-07-13 | 일라이 릴리 앤드 캄파니 | 돌연변이체 idh1 및 idh2 억제제로서의 7-페닐에틸아미노-4h-피리미도[4,5-d][1,3]옥사진-2-온 화합물 |
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2017
- 2017-12-08 KR KR1020197016855A patent/KR102276022B1/ko active Active
- 2017-12-08 HU HUE17822882A patent/HUE052067T2/hu unknown
- 2017-12-08 WO PCT/US2017/065246 patent/WO2018111707A1/en not_active Ceased
- 2017-12-08 DK DK17822882.1T patent/DK3555105T3/da active
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- 2017-12-08 AU AU2017378060A patent/AU2017378060B2/en active Active
- 2017-12-08 TN TNP/2019/000158A patent/TN2019000158A1/en unknown
- 2017-12-08 EA EA201991161A patent/EA036112B1/ru not_active IP Right Cessation
- 2017-12-08 PL PL17822882T patent/PL3555105T3/pl unknown
- 2017-12-08 MX MX2019006830A patent/MX385562B/es unknown
- 2017-12-08 MD MDE20191188T patent/MD3555105T2/ro unknown
- 2017-12-08 JP JP2019532088A patent/JP6793836B2/ja active Active
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- 2017-12-08 LT LTEP17822882.1T patent/LT3555105T/lt unknown
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- 2017-12-08 CN CN201780078017.0A patent/CN110072867B/zh active Active
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- 2017-12-08 JO JOP/2019/0142A patent/JOP20190142B1/ar active
- 2017-12-08 SI SI201730488T patent/SI3555105T1/sl 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
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- 2019-06-06 CL CL2019001551A patent/CL2019001551A1/es unknown
- 2019-06-11 IL IL267236A patent/IL267236B/en active IP Right Grant
- 2019-06-11 DO DO2019000163A patent/DOP2019000163A/es unknown
- 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 US17/202,867 patent/US11629156B2/en active Active
- 2021-03-16 US US17/202,515 patent/US11649247B2/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013046136A1 (en) | 2011-09-27 | 2013-04-04 | Novartis Ag | 3-pyrimidin-4-yl-oxazolidin-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 |
| 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 |
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| EP3328866B1 (en) | 7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds and theit use as mutant idh1 inhibitors | |
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