JP7785701B2 - アロステリックｅｇｆｒ阻害剤及びその使用方法 - Google Patents
アロステリックｅｇｆｒ阻害剤及びその使用方法Info
- Publication number
- JP7785701B2 JP7785701B2 JP2022576178A JP2022576178A JP7785701B2 JP 7785701 B2 JP7785701 B2 JP 7785701B2 JP 2022576178 A JP2022576178 A JP 2022576178A JP 2022576178 A JP2022576178 A JP 2022576178A JP 7785701 B2 JP7785701 B2 JP 7785701B2
- Authority
- JP
- Japan
- Prior art keywords
- compound
- egfr
- active agent
- alkyl
- pharmaceutically acceptable
- 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.)
- Active
Links
Classifications
-
- 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
- C07D487/04—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
- A61K31/435—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
-
- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2025137145A JP2025170326A (ja) | 2020-06-09 | 2025-08-20 | アロステリックｅｇｆｒ阻害剤及びその使用方法 |
| JP2025137144A JP2025168374A (ja) | 2020-06-09 | 2025-08-20 | アロステリックｅｇｆｒ阻害剤及びその使用方法 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063036622P | 2020-06-09 | 2020-06-09 | |
| US63/036,622 | 2020-06-09 | ||
| US202063111429P | 2020-11-09 | 2020-11-09 | |
| US63/111,429 | 2020-11-09 | ||
| PCT/US2021/036657 WO2021252661A1 (en) | 2020-06-09 | 2021-06-09 | Allosteric egfr inhibitors and methods of use thereof |
Related Child Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2025137145A Division JP2025170326A (ja) | 2020-06-09 | 2025-08-20 | アロステリックｅｇｆｒ阻害剤及びその使用方法 |
| JP2025137144A Division JP2025168374A (ja) | 2020-06-09 | 2025-08-20 | アロステリックｅｇｆｒ阻害剤及びその使用方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023529701A JP2023529701A (ja) | 2023-07-11 |
| JP2023529701A5 JP2023529701A5 (https=) | 2024-06-19 |
| JP7785701B2 true JP7785701B2 (ja) | 2025-12-15 |
Family
ID=78846544
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022576178A Active JP7785701B2 (ja) | 2020-06-09 | 2021-06-09 | アロステリックｅｇｆｒ阻害剤及びその使用方法 |
| JP2025137144A Pending JP2025168374A (ja) | 2020-06-09 | 2025-08-20 | アロステリックｅｇｆｒ阻害剤及びその使用方法 |
| JP2025137145A Pending JP2025170326A (ja) | 2020-06-09 | 2025-08-20 | アロステリックｅｇｆｒ阻害剤及びその使用方法 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2025137144A Pending JP2025168374A (ja) | 2020-06-09 | 2025-08-20 | アロステリックｅｇｆｒ阻害剤及びその使用方法 |
| JP2025137145A Pending JP2025170326A (ja) | 2020-06-09 | 2025-08-20 | アロステリックｅｇｆｒ阻害剤及びその使用方法 |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US20230212171A1 (https=) |
| EP (1) | EP4161516A4 (https=) |
| JP (3) | JP7785701B2 (https=) |
| KR (1) | KR20230033645A (https=) |
| CN (1) | CN115811977A (https=) |
| AU (1) | AU2021289729A1 (https=) |
| BR (1) | BR112022025139A2 (https=) |
| CA (1) | CA3181982A1 (https=) |
| CO (1) | CO2022019316A2 (https=) |
| EC (1) | ECSP22098041A (https=) |
| IL (1) | IL298935A (https=) |
| JO (1) | JOP20220332A1 (https=) |
| MX (1) | MX2022015739A (https=) |
| NZ (1) | NZ795548A (https=) |
| SA (1) | SA522441639B1 (https=) |
| WO (1) | WO2021252661A1 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2023289368A1 (en) * | 2022-06-21 | 2025-01-16 | Dana-Farber Cancer Institute, Inc. | Fused bicyclic egfr inhibitors and methods of use thereof |
| GB202216962D0 (en) | 2022-11-14 | 2022-12-28 | Addex Pharmaceuticals Sa | Novel compounds |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102005021963A1 (de) | 2005-05-12 | 2006-11-23 | Aicuris Gmbh & Co. Kg | Substituierte Dihydropyrazolotriazinone |
| JP2010524940A (ja) | 2007-04-20 | 2010-07-22 | シェーリング コーポレイション | ピリミジノン誘導体およびそれらの使用方法 |
| JP2018522879A (ja) | 2015-06-30 | 2018-08-16 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | Ｅｇｆｒ阻害剤およびその使用方法 |
| WO2020002487A1 (en) | 2018-06-29 | 2020-01-02 | F. Hoffmann-La Roche Ag | Compounds |
| WO2020036386A1 (ko) | 2018-08-16 | 2020-02-20 | 한국화학연구원 | 이소인돌린-1온 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 암의 예방 또는 치료용 약학적 조성물 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8163779B2 (en) * | 2006-12-20 | 2012-04-24 | Takeda San Diego, Inc. | Glucokinase activators |
| JP5746032B2 (ja) * | 2008-09-19 | 2015-07-08 | ネルビアーノ・メデイカル・サイエンシーズ・エツセ・エルレ・エルレ | ３，４−ジヒドロ−２Ｈ−ピロロ［１，２−ａ］ピラジン−１−オン誘導体 |
-
2021
- 2021-06-09 US US18/000,722 patent/US20230212171A1/en active Pending
- 2021-06-09 NZ NZ795548A patent/NZ795548A/en unknown
- 2021-06-09 AU AU2021289729A patent/AU2021289729A1/en active Pending
- 2021-06-09 CA CA3181982A patent/CA3181982A1/en active Pending
- 2021-06-09 IL IL298935A patent/IL298935A/en unknown
- 2021-06-09 BR BR112022025139A patent/BR112022025139A2/pt unknown
- 2021-06-09 EP EP21821203.3A patent/EP4161516A4/en active Pending
- 2021-06-09 KR KR1020227043942A patent/KR20230033645A/ko active Pending
- 2021-06-09 JP JP2022576178A patent/JP7785701B2/ja active Active
- 2021-06-09 WO PCT/US2021/036657 patent/WO2021252661A1/en not_active Ceased
- 2021-06-09 MX MX2022015739A patent/MX2022015739A/es unknown
- 2021-06-09 CN CN202180041075.2A patent/CN115811977A/zh active Pending
-
2022
- 2022-12-07 SA SA522441639A patent/SA522441639B1/ar unknown
- 2022-12-08 JO JOJO/P/2022/0332A patent/JOP20220332A1/ar unknown
- 2022-12-28 EC ECSENADI202298041A patent/ECSP22098041A/es unknown
- 2022-12-30 CO CONC2022/0019316A patent/CO2022019316A2/es unknown
-
2025
- 2025-08-20 JP JP2025137144A patent/JP2025168374A/ja active Pending
- 2025-08-20 JP JP2025137145A patent/JP2025170326A/ja active Pending
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102005021963A1 (de) | 2005-05-12 | 2006-11-23 | Aicuris Gmbh & Co. Kg | Substituierte Dihydropyrazolotriazinone |
| JP2010524940A (ja) | 2007-04-20 | 2010-07-22 | シェーリング コーポレイション | ピリミジノン誘導体およびそれらの使用方法 |
| JP2018522879A (ja) | 2015-06-30 | 2018-08-16 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | Ｅｇｆｒ阻害剤およびその使用方法 |
| WO2020002487A1 (en) | 2018-06-29 | 2020-01-02 | F. Hoffmann-La Roche Ag | Compounds |
| WO2020036386A1 (ko) | 2018-08-16 | 2020-02-20 | 한국화학연구원 | 이소인돌린-1온 유도체, 이의 제조방법 및 이를 유효성분으로 포함하는 암의 예방 또는 치료용 약학적 조성물 |
Non-Patent Citations (4)
| Title |
|---|
| Bioorganic & Medicinal Chemistry Letters，2015年，25，1580-1585 |
| Chem. Commun.，2014年，50，3220-3223 |
| Heterocycles，1977年，8，251-256 |
| Nature，2016年，534，129-132 |
Also Published As
| Publication number | Publication date |
|---|---|
| CA3181982A1 (en) | 2021-12-16 |
| SA522441639B1 (ar) | 2024-10-24 |
| KR20230033645A (ko) | 2023-03-08 |
| WO2021252661A1 (en) | 2021-12-16 |
| ECSP22098041A (es) | 2023-06-30 |
| IL298935A (en) | 2023-02-01 |
| MX2022015739A (es) | 2023-03-23 |
| NZ795548A (en) | 2026-01-30 |
| US20230212171A1 (en) | 2023-07-06 |
| CO2022019316A2 (es) | 2023-01-16 |
| JP2025170326A (ja) | 2025-11-18 |
| JOP20220332A1 (ar) | 2022-12-08 |
| EP4161516A4 (en) | 2024-08-07 |
| EP4161516A1 (en) | 2023-04-12 |
| JP2025168374A (ja) | 2025-11-07 |
| BR112022025139A2 (pt) | 2023-02-14 |
| CN115811977A (zh) | 2023-03-17 |
| JP2023529701A (ja) | 2023-07-11 |
| AU2021289729A1 (en) | 2023-02-02 |
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