JP2025508702A - キナゾリン化合物、及び変異ｋｒａｓタンパク質の阻害剤としてのその使用 - Google Patents
キナゾリン化合物、及び変異ｋｒａｓタンパク質の阻害剤としてのその使用 Download PDFInfo
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- JP2025508702A JP2025508702A JP2024547690A JP2024547690A JP2025508702A JP 2025508702 A JP2025508702 A JP 2025508702A JP 2024547690 A JP2024547690 A JP 2024547690A JP 2024547690 A JP2024547690 A JP 2024547690A JP 2025508702 A JP2025508702 A JP 2025508702A
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- Prior art keywords
- cancer
- fluoro
- amino
- compound
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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
- A61K31/495—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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
-
- 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
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
-
- 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
- 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
- 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
- C07D491/10—Spiro-condensed systems
-
- 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
- C07D495/10—Spiro-condensed 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
- C07D498/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202263310915P | 2022-02-16 | 2022-02-16 | |
| US63/310,915 | 2022-02-16 | ||
| PCT/US2023/062687 WO2023159086A1 (en) | 2022-02-16 | 2023-02-15 | Quinazoline compounds and use thereof as inhibtors of mutant kras proteins |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2025508702A true JP2025508702A (ja) | 2025-04-10 |
| JP2025508702A5 JP2025508702A5 (https=) | 2026-02-25 |
| JPWO2023159086A5 JPWO2023159086A5 (https=) | 2026-02-25 |
Family
ID=85685573
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024547690A Pending JP2025508702A (ja) | 2022-02-16 | 2023-02-15 | キナゾリン化合物、及び変異ｋｒａｓタンパク質の阻害剤としてのその使用 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20250163064A1 (https=) |
| EP (1) | EP4479401A1 (https=) |
| JP (1) | JP2025508702A (https=) |
| CN (1) | CN118974055A (https=) |
| AU (1) | AU2023222076A1 (https=) |
| CA (1) | CA3251001A1 (https=) |
| MX (1) | MX2024010045A (https=) |
| WO (1) | WO2023159086A1 (https=) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20210006356A (ko) | 2018-04-04 | 2021-01-18 | 아비나스 오퍼레이션스, 인코포레이티드 | 단백질분해 조절제 및 연관된 사용 방법 |
| WO2024112654A1 (en) | 2022-11-21 | 2024-05-30 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| CN121419983A (zh) | 2023-01-26 | 2026-01-27 | 阿尔维纳斯运营股份有限公司 | 基于小脑蛋白的kras降解protac及其相关用途 |
| EP4687905A1 (en) | 2023-03-30 | 2026-02-11 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| IL326136A (en) | 2023-08-07 | 2026-03-01 | Revolution Medicines Inc | RMC-6291 for use in the treatment of a disease or disorder associated with the RAS protein |
| AU2024323424A1 (en) | 2023-08-17 | 2026-03-05 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| AU2024337913A1 (en) | 2023-09-08 | 2026-03-26 | Gilead Sciences, Inc. | Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds |
| TW202528315A (zh) | 2023-09-21 | 2025-07-16 | 美商樹線生物科學公司 | 螺環二氫哌喃并吡啶ＫＲａｓ抑制劑 |
| WO2025076288A1 (en) | 2023-10-06 | 2025-04-10 | Amgen Inc. | Combination therapy for cancer treatment |
| AU2024357850A1 (en) | 2023-10-09 | 2026-04-23 | Incyte Corporation | Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor |
| US20250114339A1 (en) | 2023-10-09 | 2025-04-10 | Incyte Corporation | Combination therapy comprising a kras g12d inhibitor and an egfr inhibitor |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| US20250375445A1 (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 |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026035947A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload |
| WO2026035945A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026064527A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload |
| WO2026064520A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017172979A1 (en) * | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| KR102598895B1 (ko) | 2016-07-12 | 2023-11-07 | 레볼루션 메디슨즈, 인크. | 다른자리 입체성 shp2 억제제로서의 2,5-이치환 3-메틸 피라진 및 2,5,6-3치환 3-메틸 피라진 |
| MX2019008695A (es) | 2017-01-23 | 2019-09-11 | Revolution Medicines Inc | Compuestos biciclicos como inhibidores alostericos de shp2. |
| MX2019008696A (es) | 2017-01-23 | 2019-09-13 | Revolution Medicines Inc | Compuestos de piridina como inhibidores de shp2 alostericos. |
| EA201992781A1 (ru) | 2017-05-22 | 2020-04-01 | Эмджен Инк. | Ингибиторы g12c kras и способы их применения |
| MA50077A (fr) | 2017-09-08 | 2020-07-15 | Amgen Inc | Inhibiteurs de kras g12c et leurs procédés d'utilisation |
| MX2020003579A (es) | 2017-10-12 | 2020-07-22 | Revolution Medicines Inc | Compuestos de piridina, pirazina, y triazina como inhibidores de shp2 alostericos. |
| TWI844602B (zh) | 2018-12-20 | 2024-06-11 | 美商安進公司 | Kif18a抑制劑 |
| EP3898616B1 (en) | 2018-12-20 | 2024-10-02 | Amgen Inc. | Heteroaryl amides useful as kif18a inhibitors |
| WO2020132651A1 (en) | 2018-12-20 | 2020-06-25 | Amgen Inc. | Kif18a inhibitors |
| JP7676308B2 (ja) | 2018-12-20 | 2025-05-14 | アムジエン・インコーポレーテツド | Ｋｉｆ１８ａ阻害剤として有用なヘテロアリールアミド |
| CN116368130A (zh) * | 2020-08-28 | 2023-06-30 | 金橘生物科技公司 | 杂环化合物及其用途 |
| CN113999226B (zh) * | 2020-12-22 | 2023-01-06 | 上海科州药物研发有限公司 | 作为kras抑制剂的杂环化合物的制备及其应用方法 |
| WO2022173870A1 (en) * | 2021-02-09 | 2022-08-18 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| AU2022224511A1 (en) * | 2021-02-16 | 2023-08-10 | Lawrence Livermore National Security, Llc | Compositions and methods for inhibition of ras |
| WO2022184178A1 (en) * | 2021-03-05 | 2022-09-09 | Jacobio Pharmaceuticals Co., Ltd. | Kras g12d inhibitors |
| JP2024520791A (ja) * | 2021-06-10 | 2024-05-24 | レデックス・ファーマ・パブリック・リミテッド・カンパニー | 化合物 |
-
2023
- 2023-02-15 AU AU2023222076A patent/AU2023222076A1/en active Pending
- 2023-02-15 WO PCT/US2023/062687 patent/WO2023159086A1/en not_active Ceased
- 2023-02-15 EP EP23711641.3A patent/EP4479401A1/en active Pending
- 2023-02-15 CA CA3251001A patent/CA3251001A1/en active Pending
- 2023-02-15 CN CN202380032897.3A patent/CN118974055A/zh active Pending
- 2023-02-15 US US18/838,954 patent/US20250163064A1/en active Pending
- 2023-02-15 MX MX2024010045A patent/MX2024010045A/es unknown
- 2023-02-15 JP JP2024547690A patent/JP2025508702A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CA3251001A1 (en) | 2023-08-24 |
| MX2024010045A (es) | 2024-08-26 |
| WO2023159086A1 (en) | 2023-08-24 |
| EP4479401A1 (en) | 2024-12-25 |
| US20250163064A1 (en) | 2025-05-22 |
| AU2023222076A1 (en) | 2024-08-15 |
| CN118974055A (zh) | 2024-11-15 |
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Legal Events
| Date | Code | Title | Description |
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| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20260216 |
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| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20260216 |