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 PDF

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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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ethyl
compound
phenyl
oxazin
mmol
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KR20190077539A (ko
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레나토 알레한드로 바우어
서지 루이즈 불레
티모시 폴 버크홀더
레이몬드 길모어
패트릭 제임스 한
조란 란코빅
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일라이 릴리 앤드 캄파니
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/5365Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic 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)
KR1020197016855A 2016-12-16 2017-12-08 돌연변이체 idh1 및 idh2 억제제로서의 7-페닐에틸아미노-4h-피리미도[4,5-d][1,3]옥사진-2-온 화합물 Active KR102276022B1 (ko)

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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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KR20190077539A KR20190077539A (ko) 2019-07-03
KR102276022B1 true KR102276022B1 (ko) 2021-07-13

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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

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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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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
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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

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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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AU2017378060B2 (en) 2020-09-03
CN110072867B (zh) 2022-07-08
MX385562B (es) 2025-03-18
JOP20190142B1 (ar) 2023-03-28
SI3555105T1 (sl) 2020-12-31
AU2020260493B2 (en) 2021-09-09
KR20190077539A (ko) 2019-07-03
JOP20190142A1 (ar) 2019-06-13
ECSP19042682A (es) 2019-06-30
EP3763717B1 (en) 2023-03-08
US11001596B2 (en) 2021-05-11
US20210206780A1 (en) 2021-07-08
EP3555105B1 (en) 2020-10-28
ES2941631T3 (es) 2023-05-24
CN110072867A (zh) 2019-07-30
PL3555105T3 (pl) 2021-05-17
US11649247B2 (en) 2023-05-16
CN115109075A (zh) 2022-09-27
RS61108B1 (sr) 2020-12-31
SA519401897B1 (ar) 2022-07-28
EP3763717A1 (en) 2021-01-13
MA53881A (fr) 2022-04-27
CY1123577T1 (el) 2022-03-24
NZ754115A (en) 2021-07-30
HUE052067T2 (hu) 2021-04-28
MY197313A (en) 2023-06-13
JP6793836B2 (ja) 2020-12-02
EA036112B1 (ru) 2020-09-29
LT3555105T (lt) 2021-01-11
BR112019009648A2 (pt) 2019-09-10
AU2017378060A1 (en) 2019-05-30
MD3555105T2 (ro) 2021-01-31
CA3045303A1 (en) 2018-06-21
US11629156B2 (en) 2023-04-18
EA201991161A1 (ru) 2019-11-29
ES2835281T3 (es) 2021-06-22
CN115109075B (zh) 2024-09-20
ZA201903125B (en) 2024-08-28
TN2019000158A1 (en) 2020-10-05
HRP20201882T1 (hr) 2021-01-22
WO2018111707A1 (en) 2018-06-21
CA3045303C (en) 2022-05-17
US20200079791A1 (en) 2020-03-12
PH12019501328A1 (en) 2020-02-24
IL267236B (en) 2020-08-31
IL267236A (en) 2019-08-29
US20210230185A1 (en) 2021-07-29
MA47399A (fr) 2019-10-23
DOP2019000163A (es) 2019-07-15
PE20190977A1 (es) 2019-07-09
CL2019001551A1 (es) 2019-10-25
DK3555105T3 (da) 2020-11-09
EP3555105A1 (en) 2019-10-23
MX2019006830A (es) 2019-08-22
CR20190252A (es) 2019-08-26
PH12019501328B1 (en) 2023-05-12
MA47399B1 (fr) 2021-02-26
UA123640C2 (uk) 2021-05-05
CO2019005287A2 (es) 2019-05-31
PT3555105T (pt) 2020-12-21
JP2020502157A (ja) 2020-01-23
AU2020260493A1 (en) 2020-11-26

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