JP7784041B2 - がんの治療のためのｅｎｔ阻害剤としての大環状ジアミン誘導体、及びそれとアデノシン受容体拮抗薬との組合せ - Google Patents

がんの治療のためのｅｎｔ阻害剤としての大環状ジアミン誘導体、及びそれとアデノシン受容体拮抗薬との組合せ

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JP7784041B2
JP7784041B2 JP2022561072A JP2022561072A JP7784041B2 JP 7784041 B2 JP7784041 B2 JP 7784041B2 JP 2022561072 A JP2022561072 A JP 2022561072A JP 2022561072 A JP2022561072 A JP 2022561072A JP 7784041 B2 JP7784041 B2 JP 7784041B2
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oxo
benzenacyclotetradecaphan
diazepan
dimethoxy
dioxa
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JP2023521351A (ja
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ミカエル ドゥリニィ，
ステファノ クロシニャーニ，
エリカ ヨーケ カテライネ ヘレーン ハウトハイス，
マイケル ローリー，
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アイテオ ベルギウム エスエー
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4995—Pyrazines or piperazines forming part of bridged ring 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
    • C07D273/08—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and more than one oxygen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/18—Bridged systems
    • 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
    • C07D498/08—Bridged systems
    • 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
    • C07D498/12—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 three hetero rings
    • C07D498/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (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)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2022561072A 2020-04-07 2021-04-07 がんの治療のためのｅｎｔ阻害剤としての大環状ジアミン誘導体、及びそれとアデノシン受容体拮抗薬との組合せ Active JP7784041B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202063006629P 2020-04-07 2020-04-07
US63/006,629 2020-04-07
PCT/EP2021/059096 WO2021204896A1 (en) 2020-04-07 2021-04-07 Macrocyclic diamine derivatives as ent inhibitors for the treatment of cancers, and combination thereof with adenosine receptor antagonists

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JP2023521351A JP2023521351A (ja) 2023-05-24
JP2023521351A5 JP2023521351A5 (https=) 2024-04-17
JP7784041B2 true JP7784041B2 (ja) 2025-12-11

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US (1) US20230203058A1 (https=)
EP (1) EP4132933A1 (https=)
JP (1) JP7784041B2 (https=)
KR (1) KR20230007369A (https=)
CN (2) CN116535365A (https=)
AR (1) AR121777A1 (https=)
AU (1) AU2021253634A1 (https=)
BR (1) BR112022020324A2 (https=)
CA (1) CA3179526A1 (https=)
CL (1) CL2022002772A1 (https=)
IL (1) IL297127A (https=)
MX (1) MX2022012558A (https=)
PH (1) PH12022552981A1 (https=)
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CN118076610A (zh) * 2021-10-06 2024-05-24 Iteos比利时公司 具有ent1抑制活性的大环化合物
KR20240089211A (ko) * 2021-10-06 2024-06-20 아이테오스 벨지움 에스에이 Ent1 억제 활성을 갖는 마크로시클릭 화합물의 제조 방법
US20260069604A1 (en) * 2022-06-01 2026-03-12 Duke University Novel equilibrative nucleoside transporter inhibitors and methods of making and using same
CN115417766B (zh) * 2022-08-31 2024-05-17 天津药明康德新药开发有限公司 一种3-羟基-4,5二甲氧基苯甲酸叔丁酯的合成方法
CN115650936B (zh) * 2022-10-26 2024-11-01 天津药明康德新药开发有限公司 一种(叔丁基(3)-1,4-二氮杂卓-1-丙基)氨基甲酸酯的制备方法
TW202444377A (zh) * 2023-03-22 2024-11-16 比利時商艾托斯比利時公司 包括ent1抑制劑之鹽、結晶形式及水合物與溶劑合物的硫酸氫複合物
TW202523332A (zh) 2023-11-14 2025-06-16 比利時商艾托斯比利時公司 Ｅｎｔ１抑制劑與檢查點抑制劑組合
WO2025126110A1 (en) 2023-12-15 2025-06-19 iTeos Belgium SA Ent1 inhibitors in combination with bispecific antibodies
WO2025163520A1 (en) 2024-01-30 2025-08-07 iTeos Belgium SA Ent1 inhibitors for use in the treatment of diseases with increased adenosine levels
WO2025202864A1 (en) 2024-03-25 2025-10-02 iTeos Belgium SA Ent1 inhibitors in combination with oncolytic viruses and their use in the treatment of cancer
WO2026038162A1 (en) 2024-08-15 2026-02-19 iTeos Belgium SA Pharmaceutical compositions of ent1 inhibitors

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JP2017509687A (ja) 2014-04-03 2017-04-06 ヤンセン ファーマシューティカ エヌ．ベー． 大環状ピリミジン誘導体
JP2019508397A (ja) 2016-02-04 2019-03-28 ザ・ジョンズ・ホプキンス・ユニバーシティ ラパドシン（Ｒａｐａｄｏｃｉｎｓ）、受動拡散型ヌクレオシド輸送体１阻害剤及びその使用

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CN116535365A (zh) 2023-08-04
BR112022020324A2 (pt) 2023-03-07
AU2021253634A1 (en) 2022-11-03
WO2021204896A1 (en) 2021-10-14
TW202204365A (zh) 2022-02-01
CN115768773A (zh) 2023-03-07
PH12022552981A1 (en) 2024-02-26
KR20230007369A (ko) 2023-01-12
EP4132933A1 (en) 2023-02-15
CA3179526A1 (en) 2021-10-14
IL297127A (en) 2022-12-01
AR121777A1 (es) 2022-07-06
CL2022002772A1 (es) 2023-06-16
JP2023521351A (ja) 2023-05-24
MX2022012558A (es) 2023-02-22
US20230203058A1 (en) 2023-06-29

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