JP7453989B2 - 抗癌剤として有用な縮合三環式化合物 - Google Patents
抗癌剤として有用な縮合三環式化合物 Download PDFInfo
- Publication number
- JP7453989B2 JP7453989B2 JP2021552640A JP2021552640A JP7453989B2 JP 7453989 B2 JP7453989 B2 JP 7453989B2 JP 2021552640 A JP2021552640 A JP 2021552640A JP 2021552640 A JP2021552640 A JP 2021552640A JP 7453989 B2 JP7453989 B2 JP 7453989B2
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- chloro
- pyrazino
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- tetrahydro
- fluoro
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Classifications
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- 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
- C07D498/04—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
- A61K31/55—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
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
-
- 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
- C07D498/14—Ortho-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
- 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)
- 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)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962813885P | 2019-03-05 | 2019-03-05 | |
| US62/813,885 | 2019-03-05 | ||
| US201962951146P | 2019-12-20 | 2019-12-20 | |
| US62/951,146 | 2019-12-20 | ||
| PCT/EP2020/055551 WO2020178282A1 (en) | 2019-03-05 | 2020-03-03 | Fused tricyclic compounds useful as anticancer agents |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022523981A JP2022523981A (ja) | 2022-04-27 |
| JPWO2020178282A5 JPWO2020178282A5 (https=) | 2023-02-08 |
| JP2022523981A5 JP2022523981A5 (https=) | 2023-02-08 |
| JP7453989B2 true JP7453989B2 (ja) | 2024-03-21 |
Family
ID=69740367
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021552640A Active JP7453989B2 (ja) | 2019-03-05 | 2020-03-03 | 抗癌剤として有用な縮合三環式化合物 |
Country Status (25)
| Country | Link |
|---|---|
| US (1) | US12410187B2 (https=) |
| EP (1) | EP3935060B1 (https=) |
| JP (1) | JP7453989B2 (https=) |
| KR (1) | KR102934231B1 (https=) |
| CN (1) | CN113508118B (https=) |
| AU (1) | AU2020231045B2 (https=) |
| BR (1) | BR112021017408A2 (https=) |
| CA (1) | CA3131156A1 (https=) |
| CL (1) | CL2021002296A1 (https=) |
| CO (1) | CO2021012381A2 (https=) |
| CR (1) | CR20210504A (https=) |
| DO (1) | DOP2021000183A (https=) |
| EC (1) | ECSP21073246A (https=) |
| ES (1) | ES3010507T3 (https=) |
| IL (1) | IL285761B2 (https=) |
| JO (1) | JOP20210241A1 (https=) |
| MA (1) | MA55198A (https=) |
| MX (1) | MX2021010674A (https=) |
| PE (1) | PE20220140A1 (https=) |
| PH (1) | PH12021552083A1 (https=) |
| SG (1) | SG11202109451TA (https=) |
| TW (1) | TW202100532A (https=) |
| UY (1) | UY38602A (https=) |
| WO (1) | WO2020178282A1 (https=) |
| ZA (1) | ZA202106192B (https=) |
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11932633B2 (en) | 2018-05-07 | 2024-03-19 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| SMT202500028T1 (it) | 2018-09-10 | 2025-03-12 | Mirati Therapeutics Inc | Terapie combinate |
| WO2020055761A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| CA3112043A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| JP2022500385A (ja) | 2018-09-10 | 2022-01-04 | ミラティ セラピューティクス， インコーポレイテッド | 組み合わせ療法 |
| 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 |
| CN113164418A (zh) | 2018-12-05 | 2021-07-23 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| WO2020146613A1 (en) | 2019-01-10 | 2020-07-16 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| WO2021041671A1 (en) | 2019-08-29 | 2021-03-04 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| CN114761012B (zh) | 2019-09-24 | 2025-03-21 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| CN114867726B (zh) | 2019-10-28 | 2023-11-28 | 默沙东有限责任公司 | Kras g12c突变体的小分子抑制剂 |
| EP4065231A1 (en) | 2019-11-27 | 2022-10-05 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| US12479834B2 (en) | 2019-11-29 | 2025-11-25 | Taiho Pharmaceutical Co., Ltd. | Phenol compound or salt thereof |
| ES2929700T3 (es) | 2019-12-11 | 2022-12-01 | Lilly Co Eli | Inhibidores de KRas g12c |
| PH12022551513A1 (en) | 2019-12-20 | 2023-04-24 | Mirati Therapeutics Inc | Sos1 inhibitors |
| TWI799871B (zh) * | 2020-05-27 | 2023-04-21 | 大陸商勁方醫藥科技(上海)有限公司 | 三環并環類化合物，其製法與醫藥上的用途 |
| IL299131A (en) | 2020-06-18 | 2023-02-01 | Revolution Medicines Inc | Methods for delaying, preventing and treating acquired resistance to RAS inhibitors |
| MX2023002248A (es) | 2020-09-03 | 2023-05-16 | Revolution Medicines Inc | Uso de inhibidores de sos1 para tratar neoplasias malignas con mutaciones de shp2. |
| WO2022056307A1 (en) | 2020-09-11 | 2022-03-17 | Mirati Therapeutics, Inc. | Crystalline forms of a kras g12c inhibitor |
| AU2021347232A1 (en) | 2020-09-23 | 2023-04-27 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| CN114437107B (zh) * | 2020-11-06 | 2025-04-04 | 江苏先声药业有限公司 | 哌嗪类化合物及其应用 |
| CN114539286B (zh) * | 2020-11-24 | 2024-02-02 | 成都百裕制药股份有限公司 | 哌嗪衍生物及其在医药上的应用 |
| TWI880049B (zh) | 2020-12-04 | 2025-04-11 | 美商美國禮來大藥廠 | Kras g12c抑制劑 |
| WO2022132200A1 (en) | 2020-12-15 | 2022-06-23 | Mirati Therapeutics, Inc. | Azaquinazoline pan-kras inhibitors |
| EP4262803A4 (en) | 2020-12-16 | 2025-03-12 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| WO2022133345A1 (en) | 2020-12-18 | 2022-06-23 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| WO2022216762A1 (en) * | 2021-04-08 | 2022-10-13 | Genentech, Inc. | Oxazepine compounds and uses thereof in the treatment of cancer |
| CA3224341A1 (en) | 2021-09-01 | 2023-03-09 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
| WO2023066371A1 (zh) | 2021-10-22 | 2023-04-27 | 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 |
| TW202325298A (zh) * | 2021-11-01 | 2023-07-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 含氮的四環化合物、其製備方法及其在醫藥上的應用 |
| CN118434422A (zh) | 2021-12-28 | 2024-08-02 | 阿斯利康(英国)有限公司 | 抗体-药物缀合物和rasg12c抑制剂的组合 |
| EP4486345A1 (en) | 2022-03-04 | 2025-01-08 | Eli Lilly and Company | Method of treatment including kras g12c inhibitors and shp2 inhibitors |
| CA3247183A1 (en) | 2022-04-08 | 2023-10-12 | Eli Lilly And Company | TREATMENT METHOD INCLUDING KRAS G12C INHIBITORS AND AURORA A INHIBITORS |
| EP4687905A1 (en) | 2023-03-30 | 2026-02-11 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AU2024251689A1 (en) | 2023-04-14 | 2025-11-27 | Astrazeneca Ab | Combinations of kras inhibitor and atr inhibitor for the treatment of cancer |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2024248123A1 (ja) | 2023-06-02 | 2024-12-05 | 第一三共株式会社 | 抗ｈｅｒ３抗体－薬物コンジュゲートとｒａｓｇ１２ｃ阻害剤の組み合わせ |
| 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 |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025085748A1 (en) | 2023-10-20 | 2025-04-24 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
| 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 |
| 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 |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| 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 |
| 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)
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| WO2008007661A1 (en) | 2006-07-11 | 2008-01-17 | Takeda Pharmaceutical Company Limited | Tricyclic heterocyclic compound and use thereof |
| WO2018206539A1 (en) | 2017-05-11 | 2018-11-15 | Astrazeneca Ab | Heteroaryl compounds that inhibit g12c mutant ras proteins |
| WO2019215203A1 (en) | 2018-05-08 | 2019-11-14 | Astrazeneca Ab | Tetracyclic heteroaryl compounds |
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| EP2836482B1 (en) | 2012-04-10 | 2019-12-25 | The Regents of The University of California | Compositions and methods for treating cancer |
| JP6473133B2 (ja) | 2013-03-15 | 2019-02-20 | アラクセス ファーマ エルエルシー | Ｋｒａｓｇ１２ｃの共有結合性阻害剤 |
| US9745319B2 (en) | 2013-03-15 | 2017-08-29 | Araxes Pharma Llc | Irreversible covalent inhibitors of the GTPase K-Ras G12C |
| AU2014331794C1 (en) | 2013-10-10 | 2019-09-12 | Araxes Pharma Llc | Inhibitors of KRAS G12C |
| NO2714752T3 (https=) * | 2014-05-08 | 2018-04-21 | ||
| GB201409624D0 (en) * | 2014-05-30 | 2014-07-16 | Astrazeneca Ab | 1,3,4-thiadiazole compounds and their use in treating cancer |
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| JP2018513853A (ja) | 2015-04-10 | 2018-05-31 | アラクセス ファーマ エルエルシー | 置換キナゾリン化合物およびその使用方法 |
| JP6789239B2 (ja) | 2015-04-15 | 2020-11-25 | アラクセス ファーマ エルエルシー | Ｋｒａｓの縮合三環系インヒビターおよびその使用の方法 |
| MX388781B (es) | 2015-07-22 | 2025-03-20 | Araxes Pharma Llc | Compuestos de quinazolina sustituido y su uso como inhibidores de proteínas kras, hras y/o nras mutantes g12c. |
| WO2017058902A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
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| EP3356353A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058915A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
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| KR20180081596A (ko) | 2015-11-16 | 2018-07-16 | 아락세스 파마 엘엘씨 | 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법 |
| JP7039489B2 (ja) | 2016-05-18 | 2022-03-22 | ミラティ セラピューティクス， インコーポレイテッド | Ｋｒａｓ ｇ１２ｃ阻害剤 |
| US10280172B2 (en) | 2016-09-29 | 2019-05-07 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| EP3523289A1 (en) | 2016-10-07 | 2019-08-14 | Araxes Pharma LLC | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
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| WO2019110751A1 (en) | 2017-12-08 | 2019-06-13 | Astrazeneca Ab | Tetracyclic compounds as inhibitors of g12c mutant ras protein, for use as anti-cancer agents |
| TW201942115A (zh) | 2018-02-01 | 2019-11-01 | 美商輝瑞股份有限公司 | 作為抗癌藥之經取代的喹唑啉和吡啶並嘧啶衍生物 |
| TW201942116A (zh) | 2018-02-09 | 2019-11-01 | 美商輝瑞股份有限公司 | 作為抗癌劑之四氫喹唑啉衍生物 |
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2020
- 2020-03-03 ES ES20708488T patent/ES3010507T3/es active Active
- 2020-03-03 MA MA055198A patent/MA55198A/fr unknown
- 2020-03-03 IL IL285761A patent/IL285761B2/en unknown
- 2020-03-03 PE PE2021001444A patent/PE20220140A1/es unknown
- 2020-03-03 KR KR1020217031298A patent/KR102934231B1/ko active Active
- 2020-03-03 SG SG11202109451TA patent/SG11202109451TA/en unknown
- 2020-03-03 WO PCT/EP2020/055551 patent/WO2020178282A1/en not_active Ceased
- 2020-03-03 MX MX2021010674A patent/MX2021010674A/es unknown
- 2020-03-03 US US17/436,137 patent/US12410187B2/en active Active
- 2020-03-03 CN CN202080018236.1A patent/CN113508118B/zh active Active
- 2020-03-03 PH PH1/2021/552083A patent/PH12021552083A1/en unknown
- 2020-03-03 JP JP2021552640A patent/JP7453989B2/ja active Active
- 2020-03-03 AU AU2020231045A patent/AU2020231045B2/en active Active
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008007661A1 (en) | 2006-07-11 | 2008-01-17 | Takeda Pharmaceutical Company Limited | Tricyclic heterocyclic compound and use thereof |
| WO2018206539A1 (en) | 2017-05-11 | 2018-11-15 | Astrazeneca Ab | Heteroaryl compounds that inhibit g12c mutant ras proteins |
| WO2019215203A1 (en) | 2018-05-08 | 2019-11-14 | Astrazeneca Ab | Tetracyclic heteroaryl compounds |
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