CN115811977A - 变构egfr抑制剂及其使用方法 - Google Patents
变构egfr抑制剂及其使用方法 Download PDFInfo
- Publication number
- CN115811977A CN115811977A CN202180041075.2A CN202180041075A CN115811977A CN 115811977 A CN115811977 A CN 115811977A CN 202180041075 A CN202180041075 A CN 202180041075A CN 115811977 A CN115811977 A CN 115811977A
- Authority
- CN
- China
- Prior art keywords
- group
- membered
- alkyl
- compound
- aryl
- 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
- 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)
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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN115811977A true CN115811977A (zh) | 2023-03-17 |
Family
ID=78846544
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202180041075.2A Pending CN115811977A (zh) | 2020-06-09 | 2021-06-09 | 变构egfr抑制剂及其使用方法 |
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 (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102005021963A1 (de) * | 2005-05-12 | 2006-11-23 | Aicuris Gmbh & Co. Kg | Substituierte Dihydropyrazolotriazinone |
| WO2008130581A1 (en) * | 2007-04-20 | 2008-10-30 | Schering Corporation | Pyrimidinone derivatives and methods of use thereof |
| US20180290975A1 (en) * | 2015-06-30 | 2018-10-11 | Dana-Farber Cancer Institute, Inc. | Inhibitors of egfr and methods of use thereof |
Family Cites Families (4)
| 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 |
| PE20211388A1 (es) * | 2018-06-29 | 2021-07-27 | Hoffmann La Roche | Compuestos |
| JP7086272B2 (ja) * | 2018-08-16 | 2022-06-17 | コリア リサーチ インスティテュート オブ ケミカル テクノロジー | イソインドリン－１－オン誘導体、同じものを調製する方法、およびがんを予防するまたは処置するための有効な構成要素として同じものを含む医薬組成物 |
-
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 (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102005021963A1 (de) * | 2005-05-12 | 2006-11-23 | Aicuris Gmbh & Co. Kg | Substituierte Dihydropyrazolotriazinone |
| WO2008130581A1 (en) * | 2007-04-20 | 2008-10-30 | Schering Corporation | Pyrimidinone derivatives and methods of use thereof |
| US20180290975A1 (en) * | 2015-06-30 | 2018-10-11 | Dana-Farber Cancer Institute, Inc. | Inhibitors of egfr and methods of use thereof |
Non-Patent Citations (2)
| Title |
|---|
| JIA, Y. 等: "Overcoming EGFR T790M and C797S resistance with mutantselective allosteric inhibitors", NATURE, vol. 534, no. 7605, 25 November 2016 (2016-11-25), pages 129 - 132 * |
| STNEXT REGISTRY: "CAS No: 1053671-46-7", Retrieved from the Internet <URL:STNext Registry> * |
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 |
| JP7785701B2 (ja) | 2025-12-15 |
| 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 |
| JP2023529701A (ja) | 2023-07-11 |
| AU2021289729A1 (en) | 2023-02-02 |
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| WO2023250321A1 (en) | Fused bicyclic egfr inhibitors and methods of use thereof | |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination |