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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    • 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)
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) CN115109075B (enExample)
AU (2) AU2017378060B2 (enExample)
CA (1) CA3045303C (enExample)
CL (1) CL2019001551A1 (enExample)
CO (1) CO2019005287A2 (enExample)
CR (1) CR20190252A (enExample)
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DO (1) DOP2019000163A (enExample)
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HR (1) HRP20201882T1 (enExample)
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JO (1) JOP20190142B1 (enExample)
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PH (1) PH12019501328B1 (enExample)
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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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MX372964B (es) 2014-09-19 2020-03-27 Forma Therapeutics Inc Derivados de fenil quinolinona como inhibidores de isocitrato deshidrogenasa mutante (mt-idh)
AU2015317321B2 (en) 2014-09-19 2020-03-12 Forma Therapeutics, Inc. Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors
EP3201185B1 (en) 2014-09-19 2018-11-21 Forma Therapeutics, Inc. Pyridinyl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
WO2016171755A1 (en) 2015-04-21 2016-10-27 Forma Therapeutics, Inc. Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
US9624216B2 (en) 2015-04-21 2017-04-18 Forma Therapeutics, Inc. Quinolinone five-membered heterocyclic compounds as mutant-isocitrate dehydrogenase inhibitors
JOP20190090B1 (ar) 2016-10-24 2023-03-28 Astrazeneca Ab مشتقات 9،8،7،6-رابع هيدرو-3h-بيرازولو [4،3-f]أيزوكينولين مفيدة في علاج السرطان
JOP20190144A1 (ar) 2016-12-16 2019-06-16 Janssen Pharmaceutica Nv إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز
PH12019501328B1 (en) * 2016-12-16 2023-05-12 Lilly Co Eli 7-phenylethlamino-4h-pyrimido][4,5-d][1,3] oxazin-2-one compounds as mutant 1dh1 and 1dh2 inhibitors
JP7291077B2 (ja) 2016-12-16 2023-06-14 ヤンセン ファーマシューティカ エヌ.ベー. Jakファミリーのキナーゼの低分子阻害物質
EP3689873B1 (en) 2017-01-30 2022-09-14 Astrazeneca AB Estrogen receptor modulators
US20210196701A1 (en) 2018-05-16 2021-07-01 Forma Therapeutics, Inc. Inhibiting mutant idh-1
US11497743B2 (en) 2018-05-16 2022-11-15 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)
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
US11013734B2 (en) 2018-05-16 2021-05-25 Forma Therapeutics, Inc. Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation
US11738018B2 (en) 2018-05-16 2023-08-29 FORMA Therapeuetics, Inc. Inhibiting mutant isocitrate dehydrogenase 1 (mIDH-1)
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
ES3033669T3 (en) 2019-11-08 2025-08-06 Nerviano Medical Sciences Srl Gem-disubstituted heterocyclic compounds and their use as idh inhibitors
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
ES2981250T3 (es) * 2020-03-23 2024-10-08 Lilly Co Eli Terapia combinada con un inhibidor de IDH mutante
IL296094A (en) * 2020-03-23 2022-11-01 Lilly Co Eli Method for treating idh1 inhibitor-resistant subjects
JP7712955B2 (ja) 2020-04-24 2025-07-24 アストラゼネカ・アクチエボラーグ 癌の治療のための投薬レジメン
MX2022013258A (es) 2020-04-24 2022-11-14 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
JP2023534991A (ja) * 2020-07-20 2023-08-15 イーライ リリー アンド カンパニー 変異型idh1阻害剤、デオキシアデノシン類似体、及び白金剤を用いた併用療法
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
CN117460514A (zh) * 2021-06-09 2024-01-26 伊莱利利公司 用于治疗idh抑制剂耐药的对象的方法
US20240208978A1 (en) * 2021-06-15 2024-06-27 Wigen Biomedicine Technology (shanghai) Co., Ltd. Idh mutant inhibitor and use thereof
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

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AU2012313888B2 (en) * 2011-09-27 2016-03-31 Novartis Ag 3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH
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
WO2016171755A1 (en) * 2015-04-21 2016-10-27 Forma Therapeutics, Inc. Fused-bicyclic aryl quinolinone derivatives as mutant-isocitrate dehydrogenase inhibitors
WO2016171715A1 (en) * 2015-04-24 2016-10-27 Halliburton Energy Services, Inc. Methods of fabricating ceramic or intermetallic parts
JP6473270B2 (ja) * 2015-07-27 2019-02-20 イーライ リリー アンド カンパニー 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−オン化合物及び変異体idh1阻害剤としてのそれらの使用
ES2814290T3 (es) * 2016-06-06 2021-03-26 Lilly Co Eli Inhibidores de IDH1 mutante
PH12019501328B1 (en) * 2016-12-16 2023-05-12 Lilly Co Eli 7-phenylethlamino-4h-pyrimido][4,5-d][1,3] oxazin-2-one compounds as mutant 1dh1 and 1dh2 inhibitors

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

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