JP7756069B6 - 四環式化合物、その調製と使用の方法 - Google Patents
四環式化合物、その調製と使用の方法Info
- Publication number
- JP7756069B6 JP7756069B6 JP2022506075A JP2022506075A JP7756069B6 JP 7756069 B6 JP7756069 B6 JP 7756069B6 JP 2022506075 A JP2022506075 A JP 2022506075A JP 2022506075 A JP2022506075 A JP 2022506075A JP 7756069 B6 JP7756069 B6 JP 7756069B6
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- JP
- Japan
- Prior art keywords
- compound
- minutes
- mmol
- stirred
- crude product
- 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.)
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Classifications
-
- 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
- A61K31/435—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
- A61K31/47—Quinolines; Isoquinolines
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero rings
-
- 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
- C07D487/16—Peri-condensed 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
- C07D487/22—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 four or more hetero rings
-
- 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
- C07D498/16—Peri-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
- C07D498/22—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 four or more hetero rings
-
- 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
- C07D513/12—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 three hetero rings
- C07D513/16—Peri-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
- C07D513/22—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 four or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201910712388 | 2019-08-02 | ||
| CN201910712388.0 | 2019-08-02 | ||
| CN201910899724 | 2019-09-23 | ||
| CN201910899724.7 | 2019-09-23 | ||
| CN201911157922.2 | 2019-11-22 | ||
| CN201911157922 | 2019-11-22 | ||
| CN202010054185 | 2020-01-17 | ||
| CN202010054185.X | 2020-01-17 | ||
| PCT/CN2020/106573 WO2021023154A1 (zh) | 2019-08-02 | 2020-08-03 | 四并环类化合物及其制备方法和应用 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022543767A JP2022543767A (ja) | 2022-10-14 |
| JP2022543767A5 JP2022543767A5 (enExample) | 2023-08-16 |
| JP7756069B2 JP7756069B2 (ja) | 2025-10-17 |
| JP7756069B6 true JP7756069B6 (ja) | 2025-11-27 |
Family
ID=74483410
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022506075A Active JP7756069B6 (ja) | 2019-08-02 | 2020-08-03 | 四環式化合物、その調製と使用の方法 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20220298174A1 (enExample) |
| EP (1) | EP4011886A4 (enExample) |
| JP (1) | JP7756069B6 (enExample) |
| KR (1) | KR20220079521A (enExample) |
| CN (1) | CN112300195B (enExample) |
| AU (1) | AU2020325477A1 (enExample) |
| CA (1) | CA3149403A1 (enExample) |
| IL (1) | IL290276B2 (enExample) |
| MX (1) | MX2022001421A (enExample) |
| WO (1) | WO2021023154A1 (enExample) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019217307A1 (en) | 2018-05-07 | 2019-11-14 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| CA3112043A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| AU2019338207B2 (en) | 2018-09-10 | 2025-01-02 | Mirati Therapeutics, Inc. | Combination therapies |
| SMT202500028T1 (it) | 2018-09-10 | 2025-03-12 | Mirati Therapeutics Inc | Terapie combinate |
| US12208099B2 (en) | 2018-09-10 | 2025-01-28 | Mirati Therapeutics, Inc. | Combination therapies |
| WO2020085504A1 (ja) | 2018-10-26 | 2020-04-30 | 大鵬薬品工業株式会社 | 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法 |
| US12377101B2 (en) | 2018-12-05 | 2025-08-05 | Mirati Therapeutics, Inc. | Combination therapies |
| WO2020146613A1 (en) | 2019-01-10 | 2020-07-16 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| CN112390818B (zh) * | 2019-08-12 | 2023-08-22 | 劲方医药科技(上海)有限公司 | 取代的杂芳环并二氢嘧啶酮衍生物，其制法与医药上的用途 |
| CN114615981B (zh) | 2019-08-29 | 2024-04-12 | 米拉蒂治疗股份有限公司 | Kras g12d抑制剂 |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| CN114761012B (zh) | 2019-09-24 | 2025-03-21 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| MD4051678T2 (en) | 2019-10-28 | 2026-07-31 | Merck Sharp & Dohme Llc | Small molecule inhibitors of the KRAS G12C mutant |
| WO2021085653A1 (en) | 2019-10-31 | 2021-05-06 | Taiho Pharmaceutical Co., Ltd. | 4-aminobut-2-enamide derivatives and salts thereof |
| EP4067343A4 (en) | 2019-11-29 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | NEW PHENOLIC COMPOUND OR SALT THEREOF |
| PH12022551513A1 (en) | 2019-12-20 | 2023-04-24 | Mirati Therapeutics Inc | Sos1 inhibitors |
| US12702658B2 (en) | 2020-04-24 | 2026-08-11 | Taiho Pharmaceutical Co., Ltd. | Anticancer combination therapy with N-(1-acryloyl-azetidin-3-yl)-2-((1H-indazol-3-yl)amino)methyl)-1H-imidazole-5-carboxamide inhibitor of KRAS-G12C |
| WO2021215544A1 (en) | 2020-04-24 | 2021-10-28 | Taiho Pharmaceutical Co., Ltd. | Kras g12d protein inhibitors |
| CN113929676A (zh) * | 2020-07-14 | 2022-01-14 | 浙江海正药业股份有限公司 | 吡啶并杂环类衍生物及其制备方法和用途 |
| CN113980032B (zh) * | 2020-07-27 | 2023-06-16 | 江苏恒瑞医药股份有限公司 | 稠合四环类衍生物、其制备方法及其在医药上的应用 |
| US12655160B2 (en) | 2020-08-04 | 2026-06-16 | Mirati Therapeutics, Inc. | KRAS G12D inhibitors |
| EP4210833A4 (en) | 2020-09-11 | 2024-09-11 | Mirati Therapeutics, Inc. | CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR |
| EP4216951B1 (en) | 2020-09-22 | 2026-04-01 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| WO2022109487A1 (en) | 2020-11-23 | 2022-05-27 | Merck Sharp & Dohme Corp. | Spirocyclic-substituted 6,7-dihydro-pyrano[2,3-d]pyrimidine inhibitors of kras g12c mutant |
| EP4262807A4 (en) | 2020-12-15 | 2025-04-23 | Mirati Therapeutics, Inc. | Azachinazoline pan-KRAS inhibitors |
| WO2022133038A1 (en) | 2020-12-16 | 2022-06-23 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| CN114716435A (zh) * | 2021-01-04 | 2022-07-08 | 广州百霆医药科技有限公司 | Kras g12c突变抑制剂 |
| US20240199644A1 (en) * | 2021-03-07 | 2024-06-20 | Jacobio Pharmaceuticals Co., Ltd. | Fused Ring Derivatives Useful as KRAS G12D Inhibitors |
| CA3226720A1 (en) * | 2021-07-23 | 2023-01-26 | Suzhou Zanrong Pharma Limited | Kras g12d inhibitors and uses thereof |
| US20240374571A1 (en) | 2021-09-01 | 2024-11-14 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
| CN118019746A (zh) * | 2021-09-27 | 2024-05-10 | 北京加科思新药研发有限公司 | 多环稠环衍生物及其用途 |
| KR20240089594A (ko) * | 2021-10-22 | 2024-06-20 | 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 | 질소 함유 테트라시클릭 화합물, 이의 제조 방법 및 이의 의학적 응용 |
| WO2023072297A1 (zh) * | 2021-11-01 | 2023-05-04 | 江苏恒瑞医药股份有限公司 | 含氮的四环化合物、其制备方法及其在医药上的应用 |
| WO2023103906A1 (zh) * | 2021-12-07 | 2023-06-15 | 贝达药业股份有限公司 | Kras g12d抑制剂及其在医药上的应用 |
| AU2023299635A1 (en) * | 2022-06-27 | 2025-01-02 | Cspc Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd | Tricyclic compounds and uses thereof |
| AU2023320565A1 (en) | 2022-08-05 | 2025-01-23 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| WO2024032703A1 (en) * | 2022-08-11 | 2024-02-15 | Beigene, Ltd. | Heterocyclic compounds, compositions thereof, and methods of treatment therewith |
| US20260137665A1 (en) | 2022-10-11 | 2026-05-21 | Aadi Bioscience, Inc. | Combination therapies for the treatment of cancer |
| WO2024197503A1 (en) * | 2023-03-27 | 2024-10-03 | Nikang Therapeutics , Inc. | Tricyclic derivatives as kras inhibitors |
| KR20250174948A (ko) * | 2023-04-21 | 2025-12-15 | 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 | 질소 함유 테트라시클릭 화합물의 결정 형태 및 이의 제조 방법 |
| US20250109147A1 (en) | 2023-09-08 | 2025-04-03 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| KR20260104082A (ko) | 2023-09-29 | 2026-07-03 | 디3 바이오 (우씨) 컴퍼니, 리미티드 | 암의 치료에 사용하기 위한 wx-001 또는 그의 유도체와 kras g12c 억제제의 조합물 |
| KR20260096846A (ko) | 2023-10-20 | 2026-06-24 | 머크 샤프 앤드 돔 엘엘씨 | Kras 단백질의 소분자 억제제 |
| US20250304556A1 (en) * | 2024-04-02 | 2025-10-02 | Mirati Therapeutics, Inc. | Processes for preparation of prmt5 inhibitors and intermediates for making the same |
| WO2026064527A1 (en) * | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018206539A1 (en) | 2017-05-11 | 2018-11-15 | Astrazeneca Ab | Heteroaryl compounds that inhibit g12c mutant ras proteins |
| WO2018217651A1 (en) | 2017-05-22 | 2018-11-29 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| WO2019051291A1 (en) | 2017-09-08 | 2019-03-14 | Amgen Inc. | Inhibitors of kras g12c and methods of using the same |
| WO2019099524A1 (en) | 2017-11-15 | 2019-05-23 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| JP2022531196A (ja) | 2019-04-28 | 2022-07-06 | ジェンフリート セラピューティクス（シャンハイ）インコーポレイテッド | オキサアザキナゾリン－７（８ｈ）－ケトン化合物、その調製方法及びその医薬用途 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6441910B2 (ja) * | 2013-09-30 | 2018-12-19 | シャンハイ インリ ファーマシューティカル カンパニー リミティド | 縮合ピリミジン化合物、中間体、その調製方法、組成物及び使用 |
| CR20190338A (es) * | 2016-12-22 | 2019-09-09 | Amgen Inc | Inhibidores de kras g12c y métodos para su uso |
| CN112390818B (zh) * | 2019-08-12 | 2023-08-22 | 劲方医药科技(上海)有限公司 | 取代的杂芳环并二氢嘧啶酮衍生物，其制法与医药上的用途 |
-
2020
- 2020-08-03 IL IL290276A patent/IL290276B2/en unknown
- 2020-08-03 MX MX2022001421A patent/MX2022001421A/es unknown
- 2020-08-03 KR KR1020227006959A patent/KR20220079521A/ko not_active Ceased
- 2020-08-03 CN CN202010769535.0A patent/CN112300195B/zh active Active
- 2020-08-03 US US17/632,167 patent/US20220298174A1/en not_active Abandoned
- 2020-08-03 CA CA3149403A patent/CA3149403A1/en active Pending
- 2020-08-03 AU AU2020325477A patent/AU2020325477A1/en not_active Abandoned
- 2020-08-03 EP EP20850862.2A patent/EP4011886A4/en active Pending
- 2020-08-03 WO PCT/CN2020/106573 patent/WO2021023154A1/zh not_active Ceased
- 2020-08-03 JP JP2022506075A patent/JP7756069B6/ja active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018206539A1 (en) | 2017-05-11 | 2018-11-15 | Astrazeneca Ab | Heteroaryl compounds that inhibit g12c mutant ras proteins |
| WO2018217651A1 (en) | 2017-05-22 | 2018-11-29 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| WO2019051291A1 (en) | 2017-09-08 | 2019-03-14 | Amgen Inc. | Inhibitors of kras g12c and methods of using the same |
| WO2019099524A1 (en) | 2017-11-15 | 2019-05-23 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| JP2022531196A (ja) | 2019-04-28 | 2022-07-06 | ジェンフリート セラピューティクス（シャンハイ）インコーポレイテッド | オキサアザキナゾリン－７（８ｈ）－ケトン化合物、その調製方法及びその医薬用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| US20220298174A1 (en) | 2022-09-22 |
| CA3149403A1 (en) | 2021-02-11 |
| JP7756069B2 (ja) | 2025-10-17 |
| IL290276B1 (en) | 2026-01-01 |
| IL290276A (en) | 2022-04-01 |
| JP2022543767A (ja) | 2022-10-14 |
| EP4011886A1 (en) | 2022-06-15 |
| WO2021023154A1 (zh) | 2021-02-11 |
| CN112300195A (zh) | 2021-02-02 |
| IL290276B2 (en) | 2026-05-01 |
| AU2020325477A1 (en) | 2022-03-17 |
| EP4011886A4 (en) | 2023-07-26 |
| MX2022001421A (es) | 2022-06-08 |
| KR20220079521A (ko) | 2022-06-13 |
| CN112300195B (zh) | 2021-12-24 |
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