CN116535365A - 作为ent抑制剂用于治疗癌症的大环二胺衍生物以及其与腺苷受体拮抗剂的组合 - Google Patents

作为ent抑制剂用于治疗癌症的大环二胺衍生物以及其与腺苷受体拮抗剂的组合 Download PDF

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Publication number
CN116535365A
CN116535365A CN202310367239.1A CN202310367239A CN116535365A CN 116535365 A CN116535365 A CN 116535365A CN 202310367239 A CN202310367239 A CN 202310367239A CN 116535365 A CN116535365 A CN 116535365A
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China
Prior art keywords
oxo
benzocyclotetradec
ester
dimethoxy
dioxa
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CN202310367239.1A
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English (en)
Chinese (zh)
Inventor
M·德利格尼
S·克罗西格纳尼
E·J·K·H·胡图伊斯
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Iteos Belgium SA
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Iteos Belgium SA
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Publication of CN116535365A publication Critical patent/CN116535365A/zh
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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
    • 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
    • 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
    • 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)
CN202310367239.1A 2020-04-07 2021-04-07 作为ent抑制剂用于治疗癌症的大环二胺衍生物以及其与腺苷受体拮抗剂的组合 Pending CN116535365A (zh)

Applications Claiming Priority (4)

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
CN202180040635.2A CN115768773A (zh) 2020-04-07 2021-04-07 作为ent抑制剂用于治疗癌症的大环二胺衍生物以及其与腺苷受体拮抗剂的组合

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CN202180040635.2A Division CN115768773A (zh) 2020-04-07 2021-04-07 作为ent抑制剂用于治疗癌症的大环二胺衍生物以及其与腺苷受体拮抗剂的组合

Publications (1)

Publication Number Publication Date
CN116535365A true CN116535365A (zh) 2023-08-04

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CN202310367239.1A Pending CN116535365A (zh) 2020-04-07 2021-04-07 作为ent抑制剂用于治疗癌症的大环二胺衍生物以及其与腺苷受体拮抗剂的组合
CN202180040635.2A Pending CN115768773A (zh) 2020-04-07 2021-04-07 作为ent抑制剂用于治疗癌症的大环二胺衍生物以及其与腺苷受体拮抗剂的组合

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Country Status (15)

Country Link
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=)
TW (1) TW202204365A (https=)
WO (1) WO2021204896A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025126110A1 (en) * 2023-12-15 2025-06-19 iTeos Belgium SA Ent1 inhibitors in combination with bispecific antibodies

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050059683A1 (en) * 2003-07-22 2005-03-17 Jeff Zablocki A1 adenosine receptor antagonists
CN101855224A (zh) * 2007-11-14 2010-10-06 詹森药业有限公司 平衡型核苷转运蛋白ent1抑制剂
CN110300589A (zh) * 2016-12-16 2019-10-01 囊性纤维化基金会治疗公司 作为cftr增效剂的双环异杂芳基衍生物

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0906579D0 (en) 2009-04-16 2009-05-20 Vernalis R&D Ltd Pharmaceuticals, compositions and methods of making and using the same
US9291747B2 (en) 2010-02-08 2016-03-22 Essilor International (Compagnie Generale D'optique) Optical article comprising an anti-reflecting coating having anti-fogging properties
ES2365960B1 (es) 2010-03-31 2012-06-04 Palobiofarma, S.L Nuevos antagonistas de los receptores de adenosina.
MA39822A (fr) * 2014-04-03 2018-02-06 Janssen Pharmaceutica Nv Dérivés de pyrimidine bicycle
MX380313B (es) * 2016-02-04 2025-03-12 Univ Johns Hopkins Rapadocinas, inhibidores de transportador 1 de nucleósido equilibrador y usos de los mismos.
HUE064141T2 (hu) 2017-01-20 2024-02-28 Arcus Biosciences Inc Azolopirimidin rákkal összefüggõ rendellenességek kezelésére
TWI801372B (zh) 2017-03-30 2023-05-11 比利時商艾特歐斯比利時有限公司 作為a2a抑制劑的硫胺甲酸酯衍生物以及用於癌症治療的方法

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050059683A1 (en) * 2003-07-22 2005-03-17 Jeff Zablocki A1 adenosine receptor antagonists
CN101855224A (zh) * 2007-11-14 2010-10-06 詹森药业有限公司 平衡型核苷转运蛋白ent1抑制剂
CN110300589A (zh) * 2016-12-16 2019-10-01 囊性纤维化基金会治疗公司 作为cftr增效剂的双环异杂芳基衍生物

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2025126110A1 (en) * 2023-12-15 2025-06-19 iTeos Belgium SA Ent1 inhibitors in combination with bispecific antibodies

Also Published As

Publication number Publication date
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
JP7784041B2 (ja) 2025-12-11
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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