CA3045303C - 7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant idh1 and idh2 inhibitors - Google Patents

7-phenylethylamino-4h-pyrimido[4,5-d][1,3]oxazin-2-one compounds as mutant idh1 and idh2 inhibitors Download PDF

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Publication number
CA3045303C
CA3045303C CA3045303A CA3045303A CA3045303C CA 3045303 C CA3045303 C CA 3045303C CA 3045303 A CA3045303 A CA 3045303A CA 3045303 A CA3045303 A CA 3045303A CA 3045303 C CA3045303 C CA 3045303C
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Prior art keywords
cancer
compound
ethyl
pyrimido
mmol
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CA3045303A
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English (en)
French (fr)
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CA3045303A1 (en
Inventor
Renato Alejandro BAUER
Serge Louis Boulet
Timothy Paul Burkholder
Raymond Gilmour
Patric James Hahn
Zoran Rankovic
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Eli Lilly and Co
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Bauer Renato Alejandro
Eli Lilly and Co
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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

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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)
CA3045303A 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 Active CA3045303C (en)

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
CA3045303A1 CA3045303A1 (en) 2018-06-21
CA3045303C true CA3045303C (en) 2022-05-17

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CA3045303A Active CA3045303C (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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US (3) US11001596B2 (enExample)
EP (2) EP3763717B1 (enExample)
JP (1) JP6793836B2 (enExample)
KR (1) KR102276022B1 (enExample)
CN (2) CN110072867B (enExample)
AU (2) AU2017378060B2 (enExample)
CA (1) CA3045303C (enExample)
CL (1) CL2019001551A1 (enExample)
CO (1) CO2019005287A2 (enExample)
CR (1) CR20190252A (enExample)
CY (1) CY1123577T1 (enExample)
DK (1) DK3555105T3 (enExample)
DO (1) DOP2019000163A (enExample)
EA (1) EA036112B1 (enExample)
EC (1) ECSP19042682A (enExample)
ES (2) ES2835281T3 (enExample)
HR (1) HRP20201882T1 (enExample)
HU (1) HUE052067T2 (enExample)
IL (1) IL267236B (enExample)
JO (1) JOP20190142B1 (enExample)
LT (1) LT3555105T (enExample)
MA (2) MA47399B1 (enExample)
MD (1) MD3555105T2 (enExample)
MX (1) MX385562B (enExample)
MY (1) MY197313A (enExample)
NZ (1) NZ754115A (enExample)
PE (1) PE20190977A1 (enExample)
PH (1) PH12019501328B1 (enExample)
PL (1) PL3555105T3 (enExample)
PT (1) PT3555105T (enExample)
RS (1) RS61108B1 (enExample)
SA (1) SA519401897B1 (enExample)
SI (1) SI3555105T1 (enExample)
TN (1) TN2019000158A1 (enExample)
UA (1) UA123640C2 (enExample)
WO (1) WO2018111707A1 (enExample)
ZA (1) ZA201903125B (enExample)

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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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WO2018111707A1 (en) 2018-06-21
PH12019501328A1 (en) 2020-02-24
TN2019000158A1 (en) 2020-10-05
PL3555105T3 (pl) 2021-05-17
KR20190077539A (ko) 2019-07-03
JP6793836B2 (ja) 2020-12-02
EA036112B1 (ru) 2020-09-29
HUE052067T2 (hu) 2021-04-28
ECSP19042682A (es) 2019-06-30
IL267236A (en) 2019-08-29
HRP20201882T1 (hr) 2021-01-22
US20200079791A1 (en) 2020-03-12
LT3555105T (lt) 2021-01-11
PH12019501328B1 (en) 2023-05-12
BR112019009648A2 (pt) 2019-09-10
UA123640C2 (uk) 2021-05-05
MX385562B (es) 2025-03-18
CN110072867A (zh) 2019-07-30
US11629156B2 (en) 2023-04-18
EA201991161A1 (ru) 2019-11-29
PE20190977A1 (es) 2019-07-09
CA3045303A1 (en) 2018-06-21
DOP2019000163A (es) 2019-07-15
US11649247B2 (en) 2023-05-16
JP2020502157A (ja) 2020-01-23
AU2017378060B2 (en) 2020-09-03
CN115109075A (zh) 2022-09-27
ES2941631T3 (es) 2023-05-24
RS61108B1 (sr) 2020-12-31
CY1123577T1 (el) 2022-03-24
MX2019006830A (es) 2019-08-22
NZ754115A (en) 2021-07-30
ES2835281T3 (es) 2021-06-22
JOP20190142B1 (ar) 2023-03-28
US20210230185A1 (en) 2021-07-29
MA47399A (fr) 2019-10-23
MY197313A (en) 2023-06-13
MA53881A (fr) 2022-04-27
EP3763717A1 (en) 2021-01-13
EP3763717B1 (en) 2023-03-08
PT3555105T (pt) 2020-12-21
KR102276022B1 (ko) 2021-07-13
DK3555105T3 (da) 2020-11-09
MA47399B1 (fr) 2021-02-26
AU2020260493B2 (en) 2021-09-09
US11001596B2 (en) 2021-05-11
US20210206780A1 (en) 2021-07-08
SI3555105T1 (sl) 2020-12-31
CN115109075B (zh) 2024-09-20
CL2019001551A1 (es) 2019-10-25
MD3555105T2 (ro) 2021-01-31
CO2019005287A2 (es) 2019-05-31
SA519401897B1 (ar) 2022-07-28
AU2017378060A1 (en) 2019-05-30
IL267236B (en) 2020-08-31
JOP20190142A1 (ar) 2019-06-13
CN110072867B (zh) 2022-07-08
EP3555105B1 (en) 2020-10-28
CR20190252A (es) 2019-08-26
AU2020260493A1 (en) 2020-11-26
ZA201903125B (en) 2024-08-28
EP3555105A1 (en) 2019-10-23

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