KR102861303B1 - Kras g12c 억제제 - Google Patents
Kras g12c 억제제Info
- Publication number
- KR102861303B1 KR102861303B1 KR1020207016494A KR20207016494A KR102861303B1 KR 102861303 B1 KR102861303 B1 KR 102861303B1 KR 1020207016494 A KR1020207016494 A KR 1020207016494A KR 20207016494 A KR20207016494 A KR 20207016494A KR 102861303 B1 KR102861303 B1 KR 102861303B1
- Authority
- KR
- South Korea
- Prior art keywords
- mmol
- delete delete
- alkyl
- optionally substituted
- formula
- 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
- 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
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5355—Non-condensed oxazines and containing further 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
- 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)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762586775P | 2017-11-15 | 2017-11-15 | |
| US62/586,775 | 2017-11-15 | ||
| PCT/US2018/061060 WO2019099524A1 (en) | 2017-11-15 | 2018-11-14 | Kras g12c inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| KR20200100632A KR20200100632A (ko) | 2020-08-26 |
| KR102861303B1 true KR102861303B1 (ko) | 2025-09-17 |
Family
ID=66431793
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020207016494A Active KR102861303B1 (ko) | 2017-11-15 | 2018-11-14 | Kras g12c 억제제 |
Country Status (34)
| Country | Link |
|---|---|
| US (4) | US10689377B2 (https=) |
| EP (3) | EP3710439B1 (https=) |
| JP (2) | JP7322019B2 (https=) |
| KR (1) | KR102861303B1 (https=) |
| CN (2) | CN111989321B (https=) |
| AU (1) | AU2018369759B2 (https=) |
| BR (1) | BR112020009818A2 (https=) |
| CA (1) | CA3082579A1 (https=) |
| CL (1) | CL2020001271A1 (https=) |
| CO (1) | CO2020007244A2 (https=) |
| CY (2) | CY1125974T1 (https=) |
| DK (1) | DK3710439T3 (https=) |
| EA (1) | EA202091186A1 (https=) |
| ES (2) | ES2944547T3 (https=) |
| FI (2) | FI3710439T3 (https=) |
| FR (1) | FR24C1026I2 (https=) |
| HR (1) | HRP20230377T1 (https=) |
| HU (2) | HUE061599T2 (https=) |
| IL (1) | IL274601B2 (https=) |
| LT (2) | LT3710439T (https=) |
| MX (1) | MX2020005063A (https=) |
| MY (1) | MY200356A (https=) |
| NL (1) | NL301279I2 (https=) |
| PH (1) | PH12020550622A1 (https=) |
| PL (1) | PL3710439T3 (https=) |
| PT (1) | PT3710439T (https=) |
| RS (1) | RS64182B1 (https=) |
| SA (1) | SA520411982B1 (https=) |
| SG (1) | SG11202004427TA (https=) |
| SI (1) | SI3710439T1 (https=) |
| TW (1) | TWI809005B (https=) |
| UA (1) | UA125802C2 (https=) |
| WO (2) | WO2019099524A1 (https=) |
| ZA (1) | ZA202002105B (https=) |
Families Citing this family (217)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102444509B1 (ko) * | 2016-05-18 | 2022-09-19 | 미라티 테라퓨틱스, 인크. | Kras g12c 억제제 |
| LT3710439T (lt) * | 2017-11-15 | 2023-05-10 | Mirati Therapeutics, Inc. | Kras g12c inhibitoriai |
| CA3098574A1 (en) * | 2018-05-04 | 2019-11-07 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| WO2019217307A1 (en) | 2018-05-07 | 2019-11-14 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| TW202012415A (zh) | 2018-05-08 | 2020-04-01 | 瑞典商阿斯特捷利康公司 | 化學化合物 |
| ES2961253T3 (es) * | 2018-08-31 | 2024-03-11 | Mirati Therapeutics Inc | Inhibidores de KRas G12C |
| EP3849535A4 (en) | 2018-09-10 | 2022-06-29 | Mirati Therapeutics, Inc. | Combination therapies |
| ES3017461T3 (en) | 2018-09-10 | 2025-05-13 | Mirati Therapeutics Inc | Combination of dasatinib and adagrasib for use in the treatment of non-small cell lung cancer |
| EP3849537B1 (en) | 2018-09-10 | 2024-10-23 | 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 |
| EA202190749A1 (ru) * | 2018-09-10 | 2021-07-09 | Мирати Терапьютикс, Инк. | Способы комбинированной терапии |
| 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 |
| PE20260440A1 (es) | 2018-11-09 | 2026-02-19 | Hoffmann La Roche | Compuestos de anillo fusionado |
| MX2021002804A (es) * | 2018-12-05 | 2021-07-15 | Mirati Therapeutics Inc | Terapias de combinacion. |
| EP3908283A4 (en) | 2019-01-10 | 2022-10-12 | Mirati Therapeutics, Inc. | KRAS G12C INHIBITORS |
| US20220152026A1 (en) * | 2019-02-12 | 2022-05-19 | Novartis Ag | Pharmaceutical combination comprising tno155 and a krasg12c inhibitor |
| KR102934231B1 (ko) | 2019-03-05 | 2026-03-06 | 아스트라제네카 아베 | 항암제로 유용한 융합 삼환식 화합물 |
| TW202110837A (zh) * | 2019-05-24 | 2021-03-16 | 大陸商江蘇恆瑞醫藥股份有限公司 | 氫化吡啶并嘧啶類衍生物、其製備方法及其在醫藥上的應用 |
| WO2020239077A1 (zh) * | 2019-05-29 | 2020-12-03 | 上海翰森生物医药科技有限公司 | 含氮杂环类衍生物调节剂、其制备方法和应用 |
| CN112047939B (zh) * | 2019-06-06 | 2023-05-02 | 江苏先声药业有限公司 | 一种具有抗肿瘤活性的四氢吡啶并嘧啶类化合物 |
| CN112300153B (zh) * | 2019-07-26 | 2023-06-13 | 博瑞生物医药(苏州)股份有限公司 | 一种杂环化合物、药物组合物和用途 |
| JP7756069B6 (ja) * | 2019-08-02 | 2025-11-27 | 上海済▲ユウ▼医薬科技股▲フン▼有限公司 | 四環式化合物、その調製と使用の方法 |
| CN112341457A (zh) * | 2019-08-07 | 2021-02-09 | 北京加科思新药研发有限公司 | Kras突变蛋白抑制剂 |
| CN112390788A (zh) * | 2019-08-13 | 2021-02-23 | 苏州闻天医药科技有限公司 | 一种用于抑制krasg12c突变蛋白的化合物及其制备方法和用途 |
| CN112390797A (zh) * | 2019-08-15 | 2021-02-23 | 微境生物医药科技(上海)有限公司 | 新型螺环类K-Ras G12C抑制剂 |
| WO2021043322A1 (zh) * | 2019-09-06 | 2021-03-11 | 正大天晴药业集团南京顺欣制药有限公司 | 氮杂环庚烷并嘧啶类衍生物及其医药用途 |
| US20220402916A1 (en) | 2019-09-18 | 2022-12-22 | Merck Sharp & Dohme Corp. | Small molecule inhibitors of kras g12c mutant |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| WO2021061749A1 (en) | 2019-09-24 | 2021-04-01 | Mirati Therapeutics, Inc. | Combination therapies |
| TW202115062A (zh) * | 2019-09-25 | 2021-04-16 | 大陸商北京加科思新藥研發有限公司 | Kras突變蛋白抑制劑 |
| EP4041399A1 (en) | 2019-10-02 | 2022-08-17 | Tolremo Therapeutics AG | Heterocyclic derivatives, pharmaceutical compositions and their use in the treatment or amelioration of cancer |
| CN114555586B (zh) * | 2019-10-10 | 2023-06-23 | 信达生物制药(苏州)有限公司 | Krasg12c蛋白抑制剂及其制备方法和用途 |
| CN112694475B (zh) | 2019-10-23 | 2025-09-23 | 苏州泽璟生物制药股份有限公司 | 环烷基类和杂环烷基类抑制剂及其制备方法和应用 |
| UA129778C2 (uk) | 2019-10-28 | 2025-07-30 | Мерк Шарп Енд Доум Елелсі | Низькомолекулярні інгібітори g12c-мутантного kras |
| JP7601869B2 (ja) * | 2019-10-30 | 2024-12-17 | ▲勁▼方医▲薬▼科技(上海)有限公司 | 置換された複素環-環系化合物、その調製方法及び医薬への応用 |
| CN113286794B (zh) * | 2019-11-04 | 2024-03-12 | 北京加科思新药研发有限公司 | Kras突变蛋白抑制剂 |
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| CN112778301A (zh) * | 2019-11-07 | 2021-05-11 | 苏州泽璟生物制药股份有限公司 | 四氢吡啶并嘧啶类抑制剂及其制备方法和应用 |
| CN112824410A (zh) * | 2019-11-21 | 2021-05-21 | 苏州泽璟生物制药股份有限公司 | 氮杂七元环类抑制剂及其制备方法和应用 |
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| JP7808058B2 (ja) | 2020-06-02 | 2026-01-28 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | がんを治療するための縮合環化2-アミノ-3-シアノチオフェン及び誘導体 |
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| AU2021372796A1 (en) * | 2020-10-30 | 2023-06-01 | Novartis Ag | New crystalline forms of a kras g12c inhibitor compound |
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