CA3024523A1 - Kras g12c inhibitors - Google Patents
Kras g12c inhibitors Download PDFInfo
- Publication number
- CA3024523A1 CA3024523A1 CA3024523A CA3024523A CA3024523A1 CA 3024523 A1 CA3024523 A1 CA 3024523A1 CA 3024523 A CA3024523 A CA 3024523A CA 3024523 A CA3024523 A CA 3024523A CA 3024523 A1 CA3024523 A1 CA 3024523A1
- Authority
- CA
- Canada
- Prior art keywords
- compound
- mmol
- optionally substituted
- alkyl
- 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.)
- Pending
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
- A61K31/5375—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
- 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
- A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines 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
- A61K31/55—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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D487/10—Spiro-condensed 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
- C07D491/08—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)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662338116P | 2016-05-18 | 2016-05-18 | |
| US62/338,116 | 2016-05-18 | ||
| US201762444614P | 2017-01-10 | 2017-01-10 | |
| US62/444,614 | 2017-01-10 | ||
| PCT/US2017/033099 WO2017201161A1 (en) | 2016-05-18 | 2017-05-17 | Kras g12c inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA3024523A1 true CA3024523A1 (en) | 2017-11-23 |
Family
ID=60326411
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3024523A Pending CA3024523A1 (en) | 2016-05-18 | 2017-05-17 | Kras g12c inhibitors |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US11267812B2 (enExample) |
| EP (1) | EP3458445B1 (enExample) |
| JP (1) | JP7039489B2 (enExample) |
| KR (1) | KR102444509B1 (enExample) |
| CN (1) | CN109843856B (enExample) |
| AU (1) | AU2017266911B2 (enExample) |
| CA (1) | CA3024523A1 (enExample) |
| ES (1) | ES2863873T3 (enExample) |
| IL (1) | IL262867B (enExample) |
| MX (1) | MX382339B (enExample) |
| SG (1) | SG11201810171SA (enExample) |
| WO (1) | WO2017201161A1 (enExample) |
Families Citing this family (220)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102444509B1 (ko) | 2016-05-18 | 2022-09-19 | 미라티 테라퓨틱스, 인크. | Kras g12c 억제제 |
| CN110366550A (zh) | 2016-12-22 | 2019-10-22 | 美国安进公司 | 作为用于治疗肺癌、胰腺癌或结直肠癌的KRAS G12C抑制剂的苯并异噻唑、异噻唑并[3,4-b]吡啶、喹唑啉、酞嗪、吡啶并[2,3-d]哒嗪和吡啶并[2,3-d]嘧啶衍生物 |
| AU2018273356B2 (en) | 2017-05-22 | 2021-09-16 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| AU2018329920B2 (en) | 2017-09-08 | 2022-12-01 | Amgen Inc. | Inhibitors of KRAS G12C and methods of using the same |
| US10647715B2 (en) | 2017-11-15 | 2020-05-12 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| LT3710439T (lt) * | 2017-11-15 | 2023-05-10 | Mirati Therapeutics, Inc. | Kras g12c inhibitoriai |
| US10597405B2 (en) | 2017-12-08 | 2020-03-24 | Astrazeneca Ab | Chemical compounds |
| EP3842433B1 (en) | 2018-01-19 | 2023-11-01 | Medshine Discovery Inc. | Pyridone-pyrimidine derivative acting as krasg12c mutein inhibitor |
| 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 |
| WO2019195609A2 (en) | 2018-04-04 | 2019-10-10 | Arvinas Operations, Inc. | Modulators of proteolysis and associated methods of use |
| EP3788053B1 (en) | 2018-05-04 | 2024-07-10 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| 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 |
| MA52564A (fr) | 2018-05-10 | 2021-03-17 | Amgen Inc | Inhibiteurs de kras g12c pour le traitement du cancer |
| US11096939B2 (en) | 2018-06-01 | 2021-08-24 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| MX2020012204A (es) | 2018-06-11 | 2021-03-31 | Amgen Inc | Inhibidores de kras g12c para tratar el cáncer. |
| US11285156B2 (en) | 2018-06-12 | 2022-03-29 | Amgen Inc. | Substituted piperazines as KRAS G12C inhibitors |
| AU2019320945C1 (en) | 2018-08-16 | 2021-09-30 | F. Hoffmann-La Roche Ag | Fused ring compounds |
| ES2961253T3 (es) * | 2018-08-31 | 2024-03-11 | Mirati Therapeutics Inc | Inhibidores de KRas G12C |
| 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 |
| 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 |
| CR20210175A (es) | 2018-09-18 | 2021-06-01 | Nikang Therapeutics Inc | Derivados de anillo tricíclico condensado como inhibidores de la fosfatasa de homología a src 2 (shp2) |
| CN114042070A (zh) | 2018-09-30 | 2022-02-15 | 凯瑞康宁生物工程（武汉）有限公司 | 作为神经元组胺受体-3拮抗剂的化合物及其用途 |
| 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 |
| JP7516029B2 (ja) | 2018-11-16 | 2024-07-16 | アムジエン・インコーポレーテツド | Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法 |
| AU2019384118B2 (en) | 2018-11-19 | 2025-06-12 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法 |
| 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 |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| JP7502337B2 (ja) * | 2019-05-20 | 2024-06-18 | カリフォルニア インスティチュート オブ テクノロジー | Ｋｒａｓ ｇ１２ｃインヒビター及びその使用 |
| WO2020236947A1 (en) | 2019-05-21 | 2020-11-26 | Amgen Inc. | Solid state forms |
| AU2020277398B2 (en) | 2019-05-21 | 2026-01-29 | Amgen Inc. | Solid state forms |
| WO2020234103A1 (en) | 2019-05-21 | 2020-11-26 | Bayer Aktiengesellschaft | Identification and use of kras inhibitors |
| 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 |
| WO2021000885A1 (zh) * | 2019-07-01 | 2021-01-07 | 江苏恒瑞医药股份有限公司 | 喹唑啉酮类衍生物、其制备方法及其在医药上的应用 |
| 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 |
| 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 |
| CN112390796B (zh) * | 2019-08-19 | 2023-06-27 | 贝达药业股份有限公司 | Kras g12c抑制剂及其在医药上的应用 |
| CN112430234B (zh) * | 2019-08-26 | 2023-04-28 | 信达生物制药(苏州)有限公司 | 一种新型kras g12c蛋白抑制剂及其制备方法和用途 |
| MX2022002465A (es) | 2019-08-29 | 2022-05-19 | Mirati Therapeutics Inc | Inhibidores de kras g12d. |
| 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 |
| CN112538084B (zh) * | 2019-09-23 | 2023-06-20 | 信达生物制药(苏州)有限公司 | 新颖的kras g12c蛋白抑制剂及其制备方法和用途 |
| WO2021061749A1 (en) | 2019-09-24 | 2021-04-01 | Mirati Therapeutics, Inc. | Combination therapies |
| 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 |
| AU2020377925A1 (en) | 2019-11-04 | 2022-05-05 | Revolution Medicines, Inc. | Ras inhibitors |
| IL322454A (en) | 2019-11-04 | 2025-09-01 | Revolution Medicines Inc | ras inhibitors |
| TW202132316A (zh) | 2019-11-04 | 2021-09-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| 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 |
| CN114630832A (zh) * | 2019-11-15 | 2022-06-14 | 四川海思科制药有限公司 | 一种嘧啶并环衍生物及其在医药上的应用 |
| 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 |
| EP4065231A1 (en) * | 2019-11-27 | 2022-10-05 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| EP4067343A4 (en) | 2019-11-29 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | NEW PHENOLIC COMPOUND OR SALT THEREOF |
| WO2021106231A1 (en) * | 2019-11-29 | 2021-06-03 | Taiho Pharmaceutical Co., Ltd. | A compound having inhibitory activity against kras g12d mutation |
| WO2021109737A1 (zh) * | 2019-12-02 | 2021-06-10 | 上海璎黎药业有限公司 | 一种含氧杂环化合物、其制备方法及应用 |
| CN112979664B (zh) * | 2019-12-02 | 2024-03-01 | 上海璎黎药业有限公司 | 一种含氧杂环化合物、其制备方法及应用 |
| PH12022551513A1 (en) | 2019-12-20 | 2023-04-24 | Mirati Therapeutics Inc | Sos1 inhibitors |
| WO2021120890A1 (en) | 2019-12-20 | 2021-06-24 | Novartis Ag | Pyrazolyl derivatives useful as anti-cancer agents |
| CN113045565A (zh) * | 2019-12-27 | 2021-06-29 | 微境生物医药科技(上海)有限公司 | 新型K-Ras G12C抑制剂 |
| CN112094269B (zh) * | 2020-01-01 | 2021-12-07 | 上海凌达生物医药有限公司 | 一类饱和六元环并杂环类化合物、制备方法和用途 |
| GB202001344D0 (en) | 2020-01-31 | 2020-03-18 | Redx Pharma Plc | Ras Inhibitors |
| CN115135650A (zh) * | 2020-02-20 | 2022-09-30 | 贝达医药公司 | 作为kras抑制剂的吡啶并嘧啶衍生物 |
| AU2021233058B2 (en) * | 2020-03-12 | 2024-05-16 | D3 Bio(Wuxi) Co., Ltd | Pyrimidoheterocyclic compounds and application thereof |
| TWI811656B (zh) * | 2020-04-22 | 2023-08-11 | 大陸商德昇濟醫藥（無錫）有限公司 | 嘧啶并雜環類化合物及其應用 |
| WO2021219072A1 (zh) * | 2020-04-30 | 2021-11-04 | 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 |
| US11739102B2 (en) | 2020-05-13 | 2023-08-29 | Incyte Corporation | Fused pyrimidine compounds as KRAS inhibitors |
| CN113666923A (zh) * | 2020-05-15 | 2021-11-19 | 苏州泽璟生物制药股份有限公司 | 烷氧基烷基取代杂环基类抑制剂及其制备方法和应用 |
| CN113683616B (zh) * | 2020-05-18 | 2025-12-30 | 广州百霆医药科技有限公司 | Kras g12c突变蛋白抑制剂 |
| 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 |
| CN111646910A (zh) * | 2020-06-15 | 2020-09-11 | 中国药科大学 | 一种盐酸达泊西汀消旋体的制备方法 |
| IL299131A (en) | 2020-06-18 | 2023-02-01 | Revolution Medicines Inc | Methods for delaying, preventing and treating acquired resistance to RAS inhibitors |
| CN115942936A (zh) | 2020-06-24 | 2023-04-07 | 勃林格殷格翰国际有限公司 | 包含sos1抑制剂和kras g12c抑制剂的抗癌组合疗法 |
| CN113912608B (zh) * | 2020-07-10 | 2023-07-14 | 江苏恒瑞医药股份有限公司 | 嘧啶并嘧啶酮类衍生物、其制备方法及其在医药上的应用 |
| CN113980014B (zh) * | 2020-07-27 | 2023-05-12 | 江苏恒瑞医药股份有限公司 | 氢化吡啶并嘧啶类衍生物、其制备方法及其在医药上的应用 |
| US20250195521A1 (en) | 2020-09-03 | 2025-06-19 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| WO2022052895A1 (zh) | 2020-09-11 | 2022-03-17 | 南京明德新药研发有限公司 | 氮杂环丁烷取代化合物的晶型 |
| EP4210833A4 (en) | 2020-09-11 | 2024-09-11 | Mirati Therapeutics, Inc. | CRYSTALLINE FORMS OF A KRAS G12C INHIBITOR |
| CA3194067A1 (en) | 2020-09-15 | 2022-03-24 | Revolution Medicines, Inc. | Ras inhibitors |
| US20230357277A1 (en) * | 2020-09-22 | 2023-11-09 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| JP2023544450A (ja) | 2020-09-23 | 2023-10-23 | エラスカ・インコーポレイテッド | 三環式ピリドン及びピリミドン |
| WO2022068921A1 (zh) * | 2020-09-30 | 2022-04-07 | 上海医药集团股份有限公司 | 一种喹唑啉类化合物及其应用 |
| MX2023004373A (es) * | 2020-10-14 | 2023-07-07 | Ranok Therapeutics Hangzhou Co Ltd | Metodos y composiciones para la degradacion dirigida de proteinas. |
| US20240059703A1 (en) | 2020-10-20 | 2024-02-22 | Amgen Inc. | Heterocyclic spiro compounds and methods of use |
| WO2022087375A1 (en) * | 2020-10-22 | 2022-04-28 | Spectrum Pharmaceuticals, Inc. | Novel heterocyclic compounds |
| WO2022087371A1 (en) * | 2020-10-22 | 2022-04-28 | Spectrum Pharmaceuticals, Inc. | Novel bicyclic compounds |
| WO2022105855A1 (en) * | 2020-11-20 | 2022-05-27 | Jacobio Pharmaceuticals Co., Ltd. | Kras g12d inhibitors |
| EP4247807A4 (en) * | 2020-11-23 | 2024-10-16 | Merck Sharp & Dohme LLC | 6,7-DIHYDRO-PYRANO[2,3-D PYRIMIDINE AS INHIBITORS OF THE KRAS G12C MUTANT |
| KR102503336B1 (ko) | 2020-11-23 | 2023-02-23 | 동의대학교 산학협력단 | 음성지원이 가능한 반려동물의 배변 처리 패드 |
| CN116829151A (zh) * | 2020-12-15 | 2023-09-29 | 米拉蒂治疗股份有限公司 | 氮杂喹唑啉泛KRas抑制剂 |
| JP2023553492A (ja) | 2020-12-15 | 2023-12-21 | ミラティ セラピューティクス， インコーポレイテッド | アザキナゾリン汎ＫＲａｓ阻害剤 |
| 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 |
| US20240100172A1 (en) | 2020-12-21 | 2024-03-28 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| WO2022140472A1 (en) | 2020-12-22 | 2022-06-30 | Nikang Therapeutics, Inc. | Compounds for degrading cyclin-dependent kinase 2 via ubiquitin proteosome pathway |
| US20240092803A1 (en) * | 2021-01-08 | 2024-03-21 | Beigene Switzerland Gmbh | Bridged compounds as kras g12d inhibitor and degrader and the use thereof |
| MX2023009037A (es) * | 2021-02-01 | 2023-08-10 | Medshine Discovery Inc | Compuesto de pirimidopirano. |
| CN116600808B (zh) * | 2021-02-09 | 2024-10-22 | 苏州阿尔脉生物科技有限公司 | 一类作为kras突变体g12c抑制剂的四氢萘啶类衍生物、其制备方法及其应用 |
| WO2022171143A1 (zh) * | 2021-02-09 | 2022-08-18 | 南京明德新药研发有限公司 | 5,6,7,8-四氢吡啶[3,4-d]嘧啶化合物 |
| JP2024509280A (ja) * | 2021-03-10 | 2024-02-29 | ベータ・ファーマ・インコーポレイテッド | Ｋｒａｓ阻害物質としてのピリドピリミジン誘導体 |
| WO2022194192A1 (zh) * | 2021-03-18 | 2022-09-22 | 四川科伦博泰生物医药股份有限公司 | 一类杂芳环化合物、其制备方法及用途 |
| WO2022204112A1 (en) | 2021-03-22 | 2022-09-29 | Incyte Corporation | Imidazole and triazole kras inhibitors |
| CN115124524A (zh) * | 2021-03-26 | 2022-09-30 | 浙江海正药业股份有限公司 | 三环类衍生物及其制备方法和用途 |
| WO2022216648A1 (en) | 2021-04-08 | 2022-10-13 | Mirati Therapeutics, Inc. | Combination therapies using prmt5 inhibitors for the treatment of cancer |
| WO2022217042A1 (en) * | 2021-04-09 | 2022-10-13 | Ikena Oncology, Inc. | Naphthyl-substituted quinoline-4(1h)-ones and related compounds and their use in treating medical conditions |
| JP2024514127A (ja) | 2021-04-09 | 2024-03-28 | 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 | 抗がん剤療法 |
| EP4322954A4 (en) * | 2021-04-16 | 2025-01-29 | Merck Sharp & Dohme LLC | SMALL MOLECULAR INHIBITORS OF THE KRAS G12D MUTANT |
| EP4322945A4 (en) * | 2021-04-16 | 2025-07-16 | Mirati Therapeutics Inc | KRAS G12C INHIBITORS |
| CN117203208A (zh) * | 2021-04-23 | 2023-12-08 | 清华大学 | 靶向活化与失活态kras g12d的抑制剂 |
| CN117203207A (zh) * | 2021-04-30 | 2023-12-08 | 江苏恒瑞医药股份有限公司 | 桥环类化合物、其制备方法及其在医药上的应用 |
| TW202309052A (zh) | 2021-05-05 | 2023-03-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| KR20240017811A (ko) | 2021-05-05 | 2024-02-08 | 레볼루션 메디슨즈, 인크. | 암의 치료를 위한 ras 억제제 |
| US12280055B2 (en) | 2021-05-27 | 2025-04-22 | Mirati Therapeutics, Inc. | Combination therapies |
| EP4347041A1 (en) * | 2021-05-28 | 2024-04-10 | Taiho Pharmaceutical Co., Ltd. | Small molecule inhibitors of kras mutated proteins |
| WO2022261210A1 (en) * | 2021-06-08 | 2022-12-15 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| WO2022266206A1 (en) | 2021-06-16 | 2022-12-22 | Erasca, Inc. | Kras inhibitor conjugates |
| WO2022271823A1 (en) * | 2021-06-23 | 2022-12-29 | Newave Pharmaceutical Inc. | Mutant kras modulators and uses thereof |
| TW202317100A (zh) | 2021-06-23 | 2023-05-01 | 瑞士商諾華公司 | 包含ｋｒａｓ ｇ１２ｃ抑制劑的藥物組合及其用於治療癌症之用途 |
| EP4359081A1 (en) | 2021-06-23 | 2024-05-01 | Novartis AG | Pyrazolyl derivatives as inhibitors of the kras mutant protein |
| CN117460737A (zh) * | 2021-07-05 | 2024-01-26 | 四川科伦博泰生物医药股份有限公司 | 杂芳环化合物、其制备方法及用途 |
| MX2024000357A (es) | 2021-07-07 | 2024-02-12 | Incyte Corp | Compuestos triciclicos como inhibidores de homologo de oncogen viral de sarcoma de rata kirsten (kras). |
| WO2023287896A1 (en) | 2021-07-14 | 2023-01-19 | Incyte Corporation | Tricyclic compounds as inhibitors of kras |
| TW202317589A (zh) | 2021-07-14 | 2023-05-01 | 美商尼坎醫療公司 | 作為ｋｒａｓ抑制劑的伸烷基衍生物 |
| WO2023284537A1 (en) * | 2021-07-16 | 2023-01-19 | Shanghai Zion Pharma Co. Limited | Kras g12d inhibitors and uses thereof |
| WO2023283933A1 (en) * | 2021-07-16 | 2023-01-19 | Silexon Biotech Co., Ltd. | Compounds useful as kras g12d inhibitors |
| KR20240041917A (ko) | 2021-07-27 | 2024-04-01 | 도레이 카부시키가이샤 | 암의 치료 및/또는 예방을 위한 의약품 |
| US12441742B2 (en) | 2021-08-31 | 2025-10-14 | Incyte Corporation | Naphthyridine compounds as inhibitors of KRAS |
| KR20240055778A (ko) | 2021-09-01 | 2024-04-29 | 노파르티스 아게 | Tead 억제제를 포함하는 제약 조합물 및 암의 치료를 위한 이의 용도 |
| EP4389751A1 (en) * | 2021-09-03 | 2024-06-26 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| WO2023040989A1 (en) * | 2021-09-16 | 2023-03-23 | Suzhou Zanrong Pharma Limited | Kras g12c inhibitors and uses thereof |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| MX2024004846A (es) | 2021-10-22 | 2024-05-03 | Jiangsu Hengrui Pharmaceuticals Co Ltd | Compuesto tetraciclico que contiene nitrogeno, metodo de preparacion del mismo y uso medico del mismo. |
| IL312381A (en) * | 2021-11-05 | 2024-06-01 | Frontier Medicines Corp | KRAS G12C inhibitors |
| WO2023099624A1 (en) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| CN117940436A (zh) * | 2021-12-02 | 2024-04-26 | 上海和誉生物医药科技有限公司 | 一种7-(萘-1-基)吡啶并[4,3-d]嘧啶衍生物及其制备和应用 |
| WO2023098425A1 (zh) * | 2021-12-02 | 2023-06-08 | 上海和誉生物医药科技有限公司 | 一种kras抑制剂及其制备和在药学上的应用 |
| CN119212994A (zh) | 2021-12-17 | 2024-12-27 | 建新公司 | 作为shp2抑制剂的吡唑并吡嗪化合物 |
| TW202340202A (zh) | 2021-12-22 | 2023-10-16 | 美國加利福尼亞大學董事會 | Gtp酶抑制劑及其用途 |
| WO2023117681A1 (en) | 2021-12-22 | 2023-06-29 | Boehringer Ingelheim International Gmbh | Heteroaromatic compounds for the treatment of cancer |
| CN116410145A (zh) * | 2021-12-29 | 2023-07-11 | 上海泓博智源医药股份有限公司 | 一种mrtx849中间体的制备方法 |
| WO2023125989A1 (zh) * | 2021-12-31 | 2023-07-06 | 上海医药集团股份有限公司 | 一种喹唑啉类化合物及其应用 |
| WO2023137223A1 (en) * | 2022-01-17 | 2023-07-20 | Newave Pharmaceutical Inc. | Pan-kras inhibitors and uses thereof |
| CN118556063A (zh) * | 2022-01-21 | 2024-08-27 | 上海湃隆生物科技有限公司 | 杂环类化合物、药物组合物及其应用 |
| CA3243798A1 (en) | 2022-02-09 | 2023-08-17 | Quanta Therapeutics, Inc. | Kras Modulators and Their Uses |
| WO2023152255A1 (en) | 2022-02-10 | 2023-08-17 | Bayer Aktiengesellschaft | Fused pyrimidines as kras inhibitors |
| EP4227307A1 (en) | 2022-02-11 | 2023-08-16 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| JP2025510572A (ja) | 2022-03-08 | 2025-04-15 | レボリューション メディシンズ インコーポレイテッド | 免疫不応性肺癌を治療するための方法 |
| CN116891514A (zh) * | 2022-04-06 | 2023-10-17 | 润佳（苏州）医药科技有限公司 | 一种双官能化合物及其用途 |
| CN119053595A (zh) | 2022-03-28 | 2024-11-29 | 尼坎治疗公司 | 作为细胞周期蛋白依赖性激酶2抑制剂的磺酰氨基衍生物 |
| EP4504203A1 (en) | 2022-04-04 | 2025-02-12 | Sanofi | Therapeutic combination of kras g12c inhibitor and tead inhibitor |
| CN116891488B (zh) * | 2022-04-11 | 2025-12-12 | 成都海博为药业有限公司 | 稠环化合物、包含其的药物组合物及应用 |
| WO2023199180A1 (en) | 2022-04-11 | 2023-10-19 | Novartis Ag | Therapeutic uses of a krasg12c inhibitor |
| WO2023220421A1 (en) * | 2022-05-13 | 2023-11-16 | Ranok Therapeutics (Hangzhou) Co. Ltd. | Inhibitors of kras(g12d) |
| WO2023230190A1 (en) | 2022-05-25 | 2023-11-30 | Quanta Therapeutics, Inc. | Pyrimidine based modulators and uses thereof |
| CN117164580A (zh) * | 2022-05-27 | 2023-12-05 | 苏州泽璟生物制药股份有限公司 | 一种kras g12c抑制剂的制备方法及其中间体 |
| CN119790053A (zh) | 2022-06-08 | 2025-04-08 | 霖康疗法公司 | 作为细胞周期蛋白依赖性激酶2抑制剂的磺酰胺衍生物 |
| WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| KR20250024833A (ko) * | 2022-06-14 | 2025-02-19 | 미라티 테라퓨틱스, 인크. | 테트라하이드로피리도피리미딘 PAN-Kras 억제제 |
| JP2025525356A (ja) * | 2022-06-15 | 2025-08-05 | ミラティ セラピューティクス， インコーポレイテッド | アザキナゾリン汎Ｋｒａｓ阻害剤 |
| GB202212641D0 (en) | 2022-08-31 | 2022-10-12 | Jazz Pharmaceuticals Ireland Ltd | Novel compounds |
| JP2025531491A (ja) * | 2022-09-28 | 2025-09-19 | ミラティ セラピューティクス， インコーポレイテッド | 併用療法 |
| WO2024081674A1 (en) | 2022-10-11 | 2024-04-18 | Aadi Bioscience, Inc. | Combination therapies for the treatment of cancer |
| CN120659773A (zh) | 2022-11-09 | 2025-09-16 | 锐新医药公司 | 化合物、复合物以及其制备方法和用途 |
| AU2023375457A1 (en) | 2022-11-11 | 2025-05-01 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway |
| US12448399B2 (en) | 2023-01-26 | 2025-10-21 | Arvinas Operations, Inc. | Cereblon-based KRAS degrading PROTACs and uses related thereto |
| KR20260041941A (ko) | 2023-03-15 | 2026-03-27 | 콴타 테라퓨틱스, 인크. | Kras 조절 인자 및 이의 용도 |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AR132338A1 (es) | 2023-04-07 | 2025-06-18 | Revolution Medicines Inc | Inhibidores de ras |
| CR20250420A (es) | 2023-04-07 | 2025-11-20 | Revolution Medicines Inc | Inhibidores macrocíclicos de ras |
| CN121100123A (zh) | 2023-04-14 | 2025-12-09 | 锐新医药公司 | Ras抑制剂的结晶形式 |
| CN121464140A (zh) | 2023-04-14 | 2026-02-03 | 锐新医药公司 | Ras抑制剂的结晶形式、含有其的组合物及其使用方法 |
| 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 |
| KR20240168510A (ko) * | 2023-05-22 | 2024-12-02 | 주식회사 이노파마스크린 | Kras g12d 및 g12v 돌연변이 표적 화합물 및 그 용도 |
| CN116640104B (zh) * | 2023-05-24 | 2024-04-02 | 杭州科耀医药科技有限公司 | 一种替洛利生的工业合成方法 |
| EP4720678A1 (en) | 2023-05-31 | 2026-04-08 | Boehringer Ingelheim International GmbH | Survivin as a biomarker for predicting the responsiveness of cancer treatment |
| EP4721766A1 (en) | 2023-06-02 | 2026-04-08 | Daiichi Sankyo Company, Limited | Combination of (anti-her3 antibody)-drug conjugate and rasg12c inhibitor |
| CN116675690B (zh) * | 2023-06-02 | 2026-03-27 | 北京康立生医药技术开发有限公司 | 一种肺癌治疗药物的制备方法 |
| WO2025016899A1 (en) | 2023-07-19 | 2025-01-23 | Bayer Aktiengesellschaft | Spirocyclic compounds for the treatment of cancer |
| WO2025026903A1 (en) | 2023-07-31 | 2025-02-06 | Bayer Aktiengesellschaft | Imidazo pyrimidine compounds for the treatment of cancer |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025072462A1 (en) | 2023-09-27 | 2025-04-03 | Nikang Therapeutics, Inc. | Sulfonamide derivatives as cyclin-dependent kinase 2 inhibitors |
| TW202529768A (zh) | 2023-09-29 | 2025-08-01 | 大陸商德昇濟醫藥（無錫）有限公司 | 癌症治療的療法 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| AU2024361909A1 (en) | 2023-10-20 | 2026-03-26 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
| TW202527955A (zh) | 2023-11-27 | 2025-07-16 | 美商尼坎醫療公司 | 用於經由泛素蛋白酶體途徑降解週期蛋白依賴性激酶２和週期蛋白依賴性激酶４的含有２，５－取代的嘧啶衍生物的雙功能化合物 |
| WO2025117981A1 (en) | 2023-12-02 | 2025-06-05 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 via ubiquitin proteasome pathway |
| US20250205238A1 (en) | 2023-12-20 | 2025-06-26 | Boehringer Ingelheim International Gmbh | Anti-cancer combination therapy |
| WO2025145207A1 (en) | 2023-12-29 | 2025-07-03 | Bristol-Myers Squibb Company | Combination therapy of kras inhibitor and treg-depleting agent |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025212828A1 (en) | 2024-04-03 | 2025-10-09 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and cyclin-dependent kinase 4 via ubiquitin proteasome pathway |
| WO2025240536A1 (en) | 2024-05-15 | 2025-11-20 | Nikang Therapeutics, Inc. | Bifunctional compounds containing 2,5-substituted pyrimidine derivatives for degrading cyclin-dependent kinase 2 and/or cyclin-dependent kinase 4 via ubiquitin proteasome pathway |
| 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 |
| WO2026003808A1 (en) | 2024-06-28 | 2026-01-02 | Assia Chemical Industries Ltd. | Solid state form of adagrasib and process for preparation |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015801A1 (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 |
| 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 |
| WO2026064520A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload |
| WO2026064527A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates 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 (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002053558A1 (en) | 2001-01-02 | 2002-07-11 | F.Hoffman-La Roche Ag | Quinazolone derivatives as alpha 1a/b adrenergic receptor antagonists |
| US7105667B2 (en) | 2001-05-01 | 2006-09-12 | Bristol-Myers Squibb Co. | Fused heterocyclic compounds and use thereof |
| WO2002088079A2 (en) | 2001-05-01 | 2002-11-07 | Bristol-Myers Squibb Company | Dual inhibitors of pde 7 and pde 4 |
| NZ590160A (en) * | 2003-11-21 | 2012-07-27 | Array Biopharma Inc | AKT protein kinase inhibitors |
| US20080051387A1 (en) | 2006-06-09 | 2008-02-28 | Yuelian Xu | Tetrahydropyrido[3,4-d]pyrimidines and related analogues |
| WO2008009078A2 (en) | 2006-07-20 | 2008-01-24 | Gilead Sciences, Inc. | 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections |
| EP2518063B1 (en) | 2006-12-21 | 2017-02-01 | Sloan-Kettering Institute For Cancer Research | Pyridazinones and furan-containing compounds |
| WO2008103470A2 (en) | 2007-02-21 | 2008-08-28 | Trustees Of Columbia University In The City Of New York | Oncogenic-ras-signal dependent lethal compounds |
| US20100298289A1 (en) | 2007-10-09 | 2010-11-25 | Ucb Pharma, S.A. | Heterobicyclic compounds as histamine h4-receptor antagonists |
| JP2011516494A (ja) | 2008-04-07 | 2011-05-26 | ギリアード サイエンシーズ， インコーポレイテッド | ステアロイル−ＣｏＡデサチュラーゼの阻害剤として使用するための２Ｈ−ベンゾ［ｂ］［１，４］オキサジン−３（４Ｈ）−オン誘導体 |
| CA2729045A1 (en) | 2008-07-31 | 2010-02-04 | Philippe Bergeron | Pyrimidine compounds, compositions and methods of use |
| WO2010120996A1 (en) * | 2009-04-17 | 2010-10-21 | Wyeth Llc | 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses |
| EP2518064A1 (en) | 2009-12-25 | 2012-10-31 | Mochida Pharmaceutical Co., Ltd. | Novel aryl urea derivative |
| JP2013516422A (ja) | 2009-12-30 | 2013-05-13 | アビラ セラピューティクス， インコーポレイテッド | タンパク質のリガンド−指向性共有的修飾 |
| EP2681215B1 (en) * | 2011-02-28 | 2015-04-22 | Array Biopharma, Inc. | Serine/threonine kinase inhibitors |
| WO2012171015A2 (en) | 2011-06-10 | 2012-12-13 | Translational Genomics Research Institute | Therapeutic combination for cancer treatment |
| EP2836482B1 (en) | 2012-04-10 | 2019-12-25 | The Regents of The University of California | Compositions and methods for treating cancer |
| US9695133B2 (en) | 2012-07-13 | 2017-07-04 | The Trustees Of Columbia University In The City Of New York | Quinazolinone-based oncogenic-RAS-selective lethal compounds and their use |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| CA2904393A1 (en) * | 2013-03-15 | 2014-09-25 | Araxes Pharma Llc | Covalent inhibitors of kras g12c |
| US9745319B2 (en) | 2013-03-15 | 2017-08-29 | Araxes Pharma Llc | Irreversible covalent inhibitors of the GTPase K-Ras G12C |
| JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| EP3055290B1 (en) | 2013-10-10 | 2019-10-02 | Araxes Pharma LLC | Inhibitors of kras g12c |
| JP6279963B2 (ja) | 2014-04-15 | 2018-02-14 | 株式会社神戸製鋼所 | チタンまたはチタン合金からなるスラブの連続鋳造装置 |
| MA40074A (fr) | 2014-05-30 | 2015-12-03 | Univ Columbia | Composés liant ras multivalents |
| WO2016025650A1 (en) | 2014-08-13 | 2016-02-18 | Celgene Avilomics Research, Inc. | Combinations of an erk inhibitor and a cdk4/6 inhibitor and related methods |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| WO2016049568A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Methods and compositions for inhibition of ras |
| WO2016049565A1 (en) | 2014-09-25 | 2016-03-31 | Araxes Pharma Llc | Compositions and methods for inhibition of ras |
| JP2017528498A (ja) | 2014-09-25 | 2017-09-28 | アラクセス ファーマ エルエルシー | Ｋｒａｓ ｇ１２ｃ変異体タンパク質のインヒビター |
| US10017540B2 (en) | 2015-03-11 | 2018-07-10 | California Institute Of Technology | Cyclic peptide binder against oncogenic K-Ras |
| ES2898765T3 (es) | 2015-04-10 | 2022-03-08 | Araxes Pharma Llc | Compuestos de quinazolina sustituidos y métodos de uso de los mismos |
| US10428064B2 (en) | 2015-04-15 | 2019-10-01 | Araxes Pharma Llc | Fused-tricyclic inhibitors of KRAS and methods of use thereof |
| US10421764B2 (en) | 2015-04-24 | 2019-09-24 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Mutant KRas inhibitors |
| AU2016258192B2 (en) | 2015-05-06 | 2021-07-29 | Leidos Biomedical Research, Inc. | K-Ras modulators |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| CN108513588A (zh) | 2015-09-24 | 2018-09-07 | Ionis制药公司 | Kras表达的调节剂 |
| WO2017058805A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356359B1 (en) | 2015-09-28 | 2021-10-20 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356347A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356349A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058902A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356351A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058728A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017070256A2 (en) | 2015-10-19 | 2017-04-27 | Araxes Pharma Llc | Method for screening inhibitors of ras |
| EP3365686A4 (en) | 2015-10-22 | 2019-03-27 | The Scripps Research Institute | REACTIVE CYSTEINSONS AND USES THEREOF |
| WO2017080980A1 (en) | 2015-11-09 | 2017-05-18 | Astrazeneca Ab | Dihydropyrrolopyrazinone derivatives useful in the treatment of cancer |
| WO2017079864A1 (en) | 2015-11-12 | 2017-05-18 | Hangzhou Yier Biotech Co., Ltd. | Treatment of cancers related to chronically active ras |
| KR20180081596A (ko) | 2015-11-16 | 2018-07-16 | 아락세스 파마 엘엘씨 | 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법 |
| US9988357B2 (en) | 2015-12-09 | 2018-06-05 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| KR102444509B1 (ko) | 2016-05-18 | 2022-09-19 | 미라티 테라퓨틱스, 인크. | Kras g12c 억제제 |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| WO2018064510A1 (en) | 2016-09-29 | 2018-04-05 | 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 |
| WO2018069871A2 (en) | 2016-10-13 | 2018-04-19 | Sorrento Therapeutics, Inc. | Anti-kras binding proteins |
| US12150934B2 (en) | 2016-11-30 | 2024-11-26 | Bantam Pharmaceutical, Llc | Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases |
| CA3081983A1 (en) | 2016-11-30 | 2018-06-07 | Bantam Pharmaceutical, Llc | Substituted pyrazole compounds and methods of using them for treatment of hyperproliferative diseases |
| KR20190095355A (ko) | 2016-12-15 | 2019-08-14 | 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 | 암의 치료를 위한 조성물 및 방법 |
| EP3558979B1 (en) | 2016-12-22 | 2021-02-17 | Boehringer Ingelheim International GmbH | Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors |
| CN110366550A (zh) | 2016-12-22 | 2019-10-22 | 美国安进公司 | 作为用于治疗肺癌、胰腺癌或结直肠癌的KRAS G12C抑制剂的苯并异噻唑、异噻唑并[3,4-b]吡啶、喹唑啉、酞嗪、吡啶并[2,3-d]哒嗪和吡啶并[2,3-d]嘧啶衍生物 |
| US10344026B2 (en) | 2017-01-18 | 2019-07-09 | Nantbio, Inc. | Compositions and methods of targeting mutant K-ras |
| EP3573954A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| WO2018140599A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
| US11136308B2 (en) | 2017-01-26 | 2021-10-05 | Araxes Pharma Llc | Substituted quinazoline and quinazolinone compounds and methods of use thereof |
| JP7327802B2 (ja) | 2017-01-26 | 2023-08-16 | アラクセス ファーマ エルエルシー | 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法 |
| WO2018140513A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer |
| EP3573966A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused n-heterocyclic compounds and methods of use thereof |
| JOP20190186A1 (ar) | 2017-02-02 | 2019-08-01 | Astellas Pharma Inc | مركب كينازولين |
| EP3612526A2 (en) | 2017-04-20 | 2020-02-26 | The Regents of the University of California | K-ras modulators |
| AU2018329920B2 (en) | 2017-09-08 | 2022-12-01 | Amgen Inc. | Inhibitors of KRAS G12C and methods of using the same |
| LT3710439T (lt) * | 2017-11-15 | 2023-05-10 | Mirati Therapeutics, Inc. | Kras g12c inhibitoriai |
| US10597405B2 (en) | 2017-12-08 | 2020-03-24 | Astrazeneca Ab | Chemical compounds |
| 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 |
-
2017
- 2017-05-17 KR KR1020187036747A patent/KR102444509B1/ko active Active
- 2017-05-17 EP EP17800088.1A patent/EP3458445B1/en active Active
- 2017-05-17 SG SG11201810171SA patent/SG11201810171SA/en unknown
- 2017-05-17 ES ES17800088T patent/ES2863873T3/es active Active
- 2017-05-17 WO PCT/US2017/033099 patent/WO2017201161A1/en not_active Ceased
- 2017-05-17 CN CN201780044670.5A patent/CN109843856B/zh active Active
- 2017-05-17 MX MX2018013983A patent/MX382339B/es unknown
- 2017-05-17 JP JP2018560589A patent/JP7039489B2/ja active Active
- 2017-05-17 AU AU2017266911A patent/AU2017266911B2/en active Active
- 2017-05-17 US US16/099,398 patent/US11267812B2/en active Active
- 2017-05-17 CA CA3024523A patent/CA3024523A1/en active Pending
- 2017-11-15 US US15/814,279 patent/US10125134B2/en active Active
-
2018
- 2018-10-29 US US16/173,726 patent/US10633381B2/en active Active
- 2018-11-07 IL IL262867A patent/IL262867B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2017201161A1 (en) | 2017-11-23 |
| US20210269432A1 (en) | 2021-09-02 |
| EP3458445A4 (en) | 2019-11-13 |
| AU2017266911A1 (en) | 2018-12-06 |
| MX2018013983A (es) | 2019-08-16 |
| JP7039489B2 (ja) | 2022-03-22 |
| MX382339B (es) | 2025-03-13 |
| CN109843856B (zh) | 2023-05-02 |
| US10125134B2 (en) | 2018-11-13 |
| EP3458445A1 (en) | 2019-03-27 |
| KR102444509B1 (ko) | 2022-09-19 |
| SG11201810171SA (en) | 2018-12-28 |
| US11267812B2 (en) | 2022-03-08 |
| IL262867A (en) | 2019-03-31 |
| EP3458445B1 (en) | 2021-02-17 |
| JP2019516718A (ja) | 2019-06-20 |
| IL262867B (en) | 2022-01-01 |
| US10633381B2 (en) | 2020-04-28 |
| KR20190039475A (ko) | 2019-04-12 |
| US20190062330A1 (en) | 2019-02-28 |
| CN109843856A (zh) | 2019-06-04 |
| AU2017266911B2 (en) | 2021-09-02 |
| US20180072723A1 (en) | 2018-03-15 |
| ES2863873T3 (es) | 2021-10-11 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US11267812B2 (en) | KRAS G12C inhibitors | |
| US10689377B2 (en) | KRas G12C inhibitors | |
| EP4216951B1 (en) | Kras g12d inhibitors | |
| EP3844151B1 (en) | Kras g12c inhibitors | |
| WO2021141628A1 (en) | Kras g12c inhibitors | |
| US20200308170A1 (en) | Kras g12c inhibitors | |
| HK40004211B (en) | Kras g12c inhibitors | |
| HK40004211A (en) | Kras g12c inhibitors |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20220516 |
|
| P11 | Amendment of application requested |
Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - RESPONSE TO EXAMINER'S REQUISITION Effective date: 20240716 |
|
| B12 | Application deemed to be withdrawn, abandoned or lapsed |
Free format text: ST27 STATUS EVENT CODE: N-2-6-B10-B12-B303 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: DEEMED ABANDONED - FAILURE TO RESPOND TO AN EXAMINER'S REQUISITION Effective date: 20240916 |
|
| W00 | Other event occurred |
Free format text: ST27 STATUS EVENT CODE: N-6-6-W10-W00-W200 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: REQUEST OR RESPONSE SUBMITTED ONLINE Effective date: 20240925 |
|
| W00 | Other event occurred |
Free format text: ST27 STATUS EVENT CODE: N-6-6-W10-W00-W111 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CORRESPONDENT DETERMINED COMPLIANT Effective date: 20240926 |
|
| P11 | Amendment of application requested |
Free format text: ST27 STATUS EVENT CODE: N-6-6-P10-P11-P102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT DETERMINED COMPLIANT Effective date: 20241220 |
|
| P13 | Application amended |
Free format text: ST27 STATUS EVENT CODE: N-6-6-P10-P13-X000 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: APPLICATION AMENDED Effective date: 20241220 |
|
| P11 | Amendment of application requested |
Free format text: ST27 STATUS EVENT CODE: A-2-2-P10-P11-P100 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: AMENDMENT RECEIVED - RESPONSE TO EXAMINER'S REQUISITION Effective date: 20250213 |
|
| MFA | Maintenance fee for application paid |
Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 8TH ANNIV.) - STANDARD Year of fee payment: 8 |
|
| U00 | Fee paid |
Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED Effective date: 20250402 |
|
| U11 | Full renewal or maintenance fee paid |
Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL Effective date: 20250402 |
|
| R00 | Party data change recorded |
Free format text: ST27 STATUS EVENT CODE: A-2-2-R10-R00-R113 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: CHANGE OF ADDRESS OR METHOD OF CORRESPONDENCE REQUEST RECEIVED Effective date: 20251218 |
|
| MFA | Maintenance fee for application paid |
Free format text: FEE DESCRIPTION TEXT: MF (APPLICATION, 9TH ANNIV.) - STANDARD Year of fee payment: 9 |
|
| U00 | Fee paid |
Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED Effective date: 20260401 |
|
| U11 | Full renewal or maintenance fee paid |
Free format text: ST27 STATUS EVENT CODE: A-2-2-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL Effective date: 20260401 |