AU2021253634A1 - Macrocyclic diamine derivatives as ENT inhibitors for the treatment of cancers, and combination thereof with adenosine receptor antagonists - Google Patents
Macrocyclic diamine derivatives as ENT inhibitors for the treatment of cancers, and combination thereof with adenosine receptor antagonists Download PDFInfo
- Publication number
- AU2021253634A1 AU2021253634A1 AU2021253634A AU2021253634A AU2021253634A1 AU 2021253634 A1 AU2021253634 A1 AU 2021253634A1 AU 2021253634 A AU2021253634 A AU 2021253634A AU 2021253634 A AU2021253634 A AU 2021253634A AU 2021253634 A1 AU2021253634 A1 AU 2021253634A1
- Authority
- AU
- Australia
- Prior art keywords
- oxo
- diazepana
- benzenacyclotetradecaphane
- dimethoxy
- dioxa
- Prior art date
- Legal status (The legal status 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 status listed.)
- Pending
Links
Classifications
-
- 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
- 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
-
- 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
- C07D498/12—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
Landscapes
- 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)
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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AU2021253634A1 true AU2021253634A1 (en) | 2022-11-03 |
Family
ID=75441913
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2021253634A Pending AU2021253634A1 (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 |
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=) |
Families Citing this family (11)
| 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 |
| 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 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1646390B1 (en) * | 2003-07-22 | 2008-10-08 | Cv Therapeutics, Inc. | A1 adenosine receptor antagonists |
| JO3126B1 (ar) * | 2007-11-14 | 2017-09-20 | Janssen Pharmaceutica Nv | مثبطات ناقل نيوكليوسيد متوازن اي ان تي 1 |
| 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. |
| US10131670B2 (en) * | 2016-12-16 | 2018-11-20 | Cystic Fibrosis Foundation Therapeutics, Inc. | Bicyclic heteroaryl derivatives as CFTR potentiators |
| 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 |
-
2021
- 2021-04-07 KR KR1020227038825A patent/KR20230007369A/ko active Pending
- 2021-04-07 AU AU2021253634A patent/AU2021253634A1/en active Pending
- 2021-04-07 BR BR112022020324A patent/BR112022020324A2/pt unknown
- 2021-04-07 MX MX2022012558A patent/MX2022012558A/es unknown
- 2021-04-07 CA CA3179526A patent/CA3179526A1/en active Pending
- 2021-04-07 JP JP2022561072A patent/JP7784041B2/ja active Active
- 2021-04-07 CN CN202310367239.1A patent/CN116535365A/zh active Pending
- 2021-04-07 IL IL297127A patent/IL297127A/en unknown
- 2021-04-07 PH PH1/2022/552981A patent/PH12022552981A1/en unknown
- 2021-04-07 WO PCT/EP2021/059096 patent/WO2021204896A1/en not_active Ceased
- 2021-04-07 EP EP21717829.2A patent/EP4132933A1/en active Pending
- 2021-04-07 AR ARP210100908A patent/AR121777A1/es unknown
- 2021-04-07 CN CN202180040635.2A patent/CN115768773A/zh active Pending
- 2021-04-07 TW TW110112556A patent/TW202204365A/zh unknown
- 2021-04-07 US US17/917,462 patent/US20230203058A1/en active Pending
-
2022
- 2022-10-07 CL CL2022002772A patent/CL2022002772A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN116535365A (zh) | 2023-08-04 |
| BR112022020324A2 (pt) | 2023-03-07 |
| 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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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| DA3 | Amendments made section 104 |
Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE NAME OF THE INVENTOR TO READ DELIGNY, MICHAEL; CROSIGNANI, STEFANO; HOUTHUYS, ERICA JOKE KATELIJNE HELEEN AND ROWLEY, MICHAEL |