CN117769554A - Kras突变蛋白的小分子抑制剂 - Google Patents
Kras突变蛋白的小分子抑制剂 Download PDFInfo
- Publication number
- CN117769554A CN117769554A CN202280052819.5A CN202280052819A CN117769554A CN 117769554 A CN117769554 A CN 117769554A CN 202280052819 A CN202280052819 A CN 202280052819A CN 117769554 A CN117769554 A CN 117769554A
- Authority
- CN
- China
- Prior art keywords
- pharmaceutically acceptable
- compound
- acceptable salt
- int
- mixture
- 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
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—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
- A61K31/54—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
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Peptides Or Proteins (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163194852P | 2021-05-28 | 2021-05-28 | |
| US63/194,852 | 2021-05-28 | ||
| PCT/JP2022/023210 WO2022250170A1 (en) | 2021-05-28 | 2022-05-27 | Small molecule inhibitors of kras mutated proteins |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN117769554A true CN117769554A (zh) | 2024-03-26 |
Family
ID=82403667
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202280052819.5A Pending CN117769554A (zh) | 2021-05-28 | 2022-05-27 | Kras突变蛋白的小分子抑制剂 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20240317759A1 (enExample) |
| EP (1) | EP4347041A1 (enExample) |
| JP (1) | JP2024521979A (enExample) |
| CN (1) | CN117769554A (enExample) |
| WO (1) | WO2022250170A1 (enExample) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI831855B (zh) | 2018-10-26 | 2024-02-11 | 日商大鵬藥品工業股份有限公司 | 新穎吲唑化合物或其鹽 |
| CA3158793A1 (en) | 2019-10-28 | 2021-05-06 | Merck Sharp & Dohme Corp. | Small molecule inhibitors of kras g12c mutant |
| WO2021106230A1 (ja) | 2019-11-29 | 2021-06-03 | 大鵬薬品工業株式会社 | 新規なフェノール化合物又はその塩 |
| EP4262803A4 (en) * | 2020-12-16 | 2025-03-12 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| JP2025541682A (ja) | 2022-11-21 | 2025-12-23 | ツリーライン バイオサイエンシズ インコーポレイテッド | スピロ環式ジヒドロピランピリミジンＫＲａｓ阻害剤 |
| TW202504599A (zh) | 2023-06-30 | 2025-02-01 | 美商必治妥美雅史谷比公司 | Kras抑制劑 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| TW202515570A (zh) | 2023-08-17 | 2025-04-16 | 美商樹線生物科學公司 | 螺環二氫哌喃并嘧啶ｋｒａｓ抑制劑 |
| AU2024337913A1 (en) | 2023-09-08 | 2026-03-26 | Gilead Sciences, Inc. | Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds |
| AU2024344161A1 (en) | 2023-09-21 | 2026-03-26 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyridine kras inhibitors |
| IL327306A (en) | 2023-10-12 | 2026-05-01 | Revolution Medicines Inc | Macrocyclic 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 |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| 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 |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| 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 |
| 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 |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
Citations (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109843856A (zh) * | 2016-05-18 | 2019-06-04 | 米拉蒂治疗股份有限公司 | Kras g12c抑制剂 |
| CN111989321A (zh) * | 2017-11-15 | 2020-11-24 | 米拉蒂治疗股份有限公司 | Kras g12c抑制剂 |
| WO2020238791A1 (zh) * | 2019-05-24 | 2020-12-03 | 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 |
| 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 |
| WO2021041671A1 (en) * | 2019-08-29 | 2021-03-04 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| CN112442029A (zh) * | 2019-09-04 | 2021-03-05 | 四川海思科制药有限公司 | 一种四氢吡啶并[3,4-d]嘧啶衍生物及其在医药上的应用 |
| WO2021058018A1 (en) * | 2019-09-29 | 2021-04-01 | Beigene, Ltd. | Inhibitors of kras g12c |
| CN113004269A (zh) * | 2019-12-19 | 2021-06-22 | 首药控股(北京)有限公司 | Kras-G12C抑制剂杂环化合物 |
| 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 |
| CN113135924A (zh) * | 2020-01-19 | 2021-07-20 | 广东东阳光药业有限公司 | 嘧啶衍生物及其在药物中的应用 |
| WO2022066646A1 (en) * | 2020-09-22 | 2022-03-31 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| CN115003677A (zh) * | 2019-11-29 | 2022-09-02 | 大鹏药品工业株式会社 | 对kras g12d突变具有抑制活性的化合物 |
| CN116194456A (zh) * | 2020-04-30 | 2023-05-30 | 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 |
| CN116801883A (zh) * | 2021-03-18 | 2023-09-22 | 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 |
| CN117120058A (zh) * | 2021-02-09 | 2023-11-24 | 金橘生物科技公司 | 杂环化合物及其用途 |
| 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 |
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-
2022
- 2022-05-27 WO PCT/JP2022/023210 patent/WO2022250170A1/en not_active Ceased
- 2022-05-27 US US18/564,866 patent/US20240317759A1/en active Pending
- 2022-05-27 EP EP22738053.2A patent/EP4347041A1/en active Pending
- 2022-05-27 CN CN202280052819.5A patent/CN117769554A/zh active Pending
- 2022-05-27 JP JP2024517826A patent/JP2024521979A/ja active Pending
Patent Citations (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109843856A (zh) * | 2016-05-18 | 2019-06-04 | 米拉蒂治疗股份有限公司 | Kras g12c抑制剂 |
| CN111989321A (zh) * | 2017-11-15 | 2020-11-24 | 米拉蒂治疗股份有限公司 | Kras g12c抑制剂 |
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| WO2022250170A1 (en) | 2022-12-01 |
| WO2022250170A9 (en) | 2023-01-05 |
| JP2024521979A (ja) | 2024-06-04 |
| EP4347041A1 (en) | 2024-04-10 |
| US20240317759A1 (en) | 2024-09-26 |
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