EA036112B1 - 7-фенилэтиламино-4h-пиримидо[4,5-d][1,3]оксазин-2-оновые соединения в качестве ингибиторов мутантных idh1 и idh2 - Google Patents

7-фенилэтиламино-4h-пиримидо[4,5-d][1,3]оксазин-2-оновые соединения в качестве ингибиторов мутантных idh1 и idh2

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Publication number
EA036112B1
EA036112B1 EA201991161A EA201991161A EA036112B1 EA 036112 B1 EA036112 B1 EA 036112B1 EA 201991161 A EA201991161 A EA 201991161A EA 201991161 A EA201991161 A EA 201991161A EA 036112 B1 EA036112 B1 EA 036112B1
Authority
EA
Eurasian Patent Office
Prior art keywords
phenylethylamino
pyrimido
oxazin
compounds
mutant idh1
Prior art date
Application number
EA201991161A
Other languages
English (en)
Other versions
EA201991161A1 (ru
Inventor
Ренато Алехандро Бауэр
Серж Луи Буле
Тимоти Пол Беркхолдер
Реймонд Гилмор
Патрик Джеймс Хан
Зоран Ранкович
Original Assignee
Эли Лилли Энд Компани
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Эли Лилли Энд Компани filed Critical Эли Лилли Энд Компани
Publication of EA201991161A1 publication Critical patent/EA201991161A1/ru
Publication of EA036112B1 publication Critical patent/EA036112B1/ru

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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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Предложены соединение, такое как определено в настоящем документе, или фармацевтическая композиция, содержащая соединение, для применения в лечении рака, включающего мутантную IDH1 или мутантную IDH2, имеющее структуру
EA201991161A 2016-12-16 2017-12-08 7-фенилэтиламино-4h-пиримидо[4,5-d][1,3]оксазин-2-оновые соединения в качестве ингибиторов мутантных idh1 и idh2 EA036112B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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 (2)

Publication Number Publication Date
EA201991161A1 EA201991161A1 (ru) 2019-11-29
EA036112B1 true EA036112B1 (ru) 2020-09-29

Family

ID=60888651

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201991161A EA036112B1 (ru) 2016-12-16 2017-12-08 7-фенилэтиламино-4h-пиримидо[4,5-d][1,3]оксазин-2-оновые соединения в качестве ингибиторов мутантных idh1 и idh2

Country Status (37)

Country Link
US (3) US11001596B2 (ru)
EP (2) EP3555105B1 (ru)
JP (1) JP6793836B2 (ru)
KR (1) KR102276022B1 (ru)
CN (2) CN115109075B (ru)
AU (2) AU2017378060B2 (ru)
CA (1) CA3045303C (ru)
CL (1) CL2019001551A1 (ru)
CO (1) CO2019005287A2 (ru)
CR (1) CR20190252A (ru)
CY (1) CY1123577T1 (ru)
DK (1) DK3555105T3 (ru)
DO (1) DOP2019000163A (ru)
EA (1) EA036112B1 (ru)
EC (1) ECSP19042682A (ru)
ES (2) ES2835281T3 (ru)
HR (1) HRP20201882T1 (ru)
HU (1) HUE052067T2 (ru)
IL (1) IL267236B (ru)
JO (1) JOP20190142B1 (ru)
LT (1) LT3555105T (ru)
MA (2) MA53881A (ru)
MD (1) MD3555105T2 (ru)
MX (1) MX385562B (ru)
MY (1) MY197313A (ru)
NZ (1) NZ754115A (ru)
PE (1) PE20190977A1 (ru)
PH (1) PH12019501328B1 (ru)
PL (1) PL3555105T3 (ru)
PT (1) PT3555105T (ru)
RS (1) RS61108B1 (ru)
SA (1) SA519401897B1 (ru)
SI (1) SI3555105T1 (ru)
TN (1) TN2019000158A1 (ru)
UA (1) UA123640C2 (ru)
WO (1) WO2018111707A1 (ru)
ZA (1) ZA201903125B (ru)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9771349B2 (en) 2014-09-19 2017-09-26 Forma Therapeutics, Inc. Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
MX372986B (es) 2014-09-19 2020-03-31 Forma Therapeutics Inc Composiciones de pirimidin quinolinona como inhibidores de isocitrato deshidrogenasa mutante (mt-idh)
AU2015317322B2 (en) 2014-09-19 2020-09-17 Forma Therapeutics, Inc. Phenyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
LT3194376T (lt) 2014-09-19 2019-02-25 Forma Therapeutics, Inc. Piridin-2(1h)-ono chinolinono dariniai, kaip mutantinės izocitratdehidrogenazės inhibitoriai
US9624216B2 (en) 2015-04-21 2017-04-18 Forma Therapeutics, Inc. Quinolinone five-membered heterocyclic compounds 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
LT3640251T (lt) 2016-10-24 2022-03-10 Astrazeneca Ab 6,7,8,9-tetrahidro-3h-pirazolo[4,3-f]izochinolino dariniai, tinkami vėžio gydymui
AU2017377069B2 (en) 2016-12-16 2020-07-23 Janssen Pharmaceutica Nv Small molecule inhibitors of the JAK family of kinases
JOP20190144A1 (ar) 2016-12-16 2019-06-16 Janssen Pharmaceutica Nv إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز
EP3555105B1 (en) * 2016-12-16 2020-10-28 Eli Lilly and Company 7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant idh1 and idh2 inhibitors
MX2019008438A (es) 2017-01-30 2019-10-30 Astrazeneca Ab Moduladores del receptor de estrogeno.
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)
US20210196701A1 (en) 2018-05-16 2021-07-01 Forma Therapeutics, Inc. Inhibiting mutant idh-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
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
US12521395B2 (en) 2019-11-08 2026-01-13 Nerviano Medical Sciences S.R.L. Gem-disubstituted heterocyclic compounds and their use as IDH inhibitors
WO2021194953A1 (en) 2020-03-23 2021-09-30 Eli Lilly And Company 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
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
IL297216A (en) 2020-04-24 2022-12-01 Astrazeneca Ab Dosage regimen for the treatment of cancer
JP7719796B2 (ja) 2020-04-24 2025-08-06 アストラゼネカ・アクチエボラーグ 医薬製剤
US12559505B2 (en) 2020-06-28 2026-02-24 Wigen Biomedicine Technology (shanghai) Co., Ltd. IDH mutant inhibitor and use thereof
EP4181927A1 (en) * 2020-07-20 2023-05-24 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
CA3217608A1 (en) 2021-06-15 2022-12-22 Yuli Xie Idh mutant inhibitor and use thereof
WO2023018955A1 (en) 2021-08-13 2023-02-16 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

Citations (4)

* Cited by examiner, † Cited by third party
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
WO2017213910A1 (en) * 2016-06-06 2017-12-14 Eli Lilly And Company Mutant idh1 inhibitors

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
EP3555105B1 (en) * 2016-12-16 2020-10-28 Eli Lilly and Company 7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant idh1 and idh2 inhibitors

Patent Citations (4)

* Cited by examiner, † Cited by third party
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
WO2017213910A1 (en) * 2016-06-06 2017-12-14 Eli Lilly And Company Mutant idh1 inhibitors

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Publication number Publication date
PH12019501328A1 (en) 2020-02-24
PT3555105T (pt) 2020-12-21
PL3555105T3 (pl) 2021-05-17
EA201991161A1 (ru) 2019-11-29
CN110072867A (zh) 2019-07-30
MY197313A (en) 2023-06-13
ECSP19042682A (es) 2019-06-30
AU2020260493A1 (en) 2020-11-26
CN110072867B (zh) 2022-07-08
MX385562B (es) 2025-03-18
MA47399B1 (fr) 2021-02-26
AU2017378060A1 (en) 2019-05-30
CL2019001551A1 (es) 2019-10-25
RS61108B1 (sr) 2020-12-31
AU2020260493B2 (en) 2021-09-09
CA3045303C (en) 2022-05-17
EP3555105B1 (en) 2020-10-28
HUE052067T2 (hu) 2021-04-28
HRP20201882T1 (hr) 2021-01-22
ES2941631T3 (es) 2023-05-24
CY1123577T1 (el) 2022-03-24
JOP20190142A1 (ar) 2019-06-13
JP2020502157A (ja) 2020-01-23
US20200079791A1 (en) 2020-03-12
US20210230185A1 (en) 2021-07-29
MD3555105T2 (ro) 2021-01-31
IL267236A (en) 2019-08-29
PH12019501328B1 (en) 2023-05-12
CA3045303A1 (en) 2018-06-21
CR20190252A (es) 2019-08-26
SA519401897B1 (ar) 2022-07-28
KR102276022B1 (ko) 2021-07-13
DK3555105T3 (da) 2020-11-09
WO2018111707A1 (en) 2018-06-21
EP3763717B1 (en) 2023-03-08
EP3763717A1 (en) 2021-01-13
JP6793836B2 (ja) 2020-12-02
US11629156B2 (en) 2023-04-18
EP3555105A1 (en) 2019-10-23
CO2019005287A2 (es) 2019-05-31
CN115109075A (zh) 2022-09-27
US11649247B2 (en) 2023-05-16
PE20190977A1 (es) 2019-07-09
IL267236B (en) 2020-08-31
TN2019000158A1 (en) 2020-10-05
UA123640C2 (uk) 2021-05-05
ES2835281T3 (es) 2021-06-22
SI3555105T1 (sl) 2020-12-31
JOP20190142B1 (ar) 2023-03-28
NZ754115A (en) 2021-07-30
CN115109075B (zh) 2024-09-20
DOP2019000163A (es) 2019-07-15
ZA201903125B (en) 2024-08-28
MA47399A (fr) 2019-10-23
MX2019006830A (es) 2019-08-22
LT3555105T (lt) 2021-01-11
BR112019009648A2 (pt) 2019-09-10
MA53881A (fr) 2022-04-27
US11001596B2 (en) 2021-05-11
US20210206780A1 (en) 2021-07-08
KR20190077539A (ko) 2019-07-03
AU2017378060B2 (en) 2020-09-03

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AZ BY KG TJ TM