CN120500482A - 大环kras抑制剂及使用方法 - Google Patents
大环kras抑制剂及使用方法Info
- Publication number
- CN120500482A CN120500482A CN202380088000.9A CN202380088000A CN120500482A CN 120500482 A CN120500482 A CN 120500482A CN 202380088000 A CN202380088000 A CN 202380088000A CN 120500482 A CN120500482 A CN 120500482A
- Authority
- CN
- China
- Prior art keywords
- compound
- salt
- cancer
- alkylene
- alkyl
- 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
-
- 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
- A61K31/495—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
- A61K31/529—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring 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
- A61K31/535—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
- A61K31/535—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
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring 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
-
- 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
-
- 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
- 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
- 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
- C07D513/22—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
-
- 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)
- Health & Medical 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)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202263383674P | 2022-11-14 | 2022-11-14 | |
| US63/383674 | 2022-11-14 | ||
| US202363497978P | 2023-04-24 | 2023-04-24 | |
| US63/497978 | 2023-04-24 | ||
| US202363582751P | 2023-09-14 | 2023-09-14 | |
| US63/582751 | 2023-09-14 | ||
| PCT/US2023/079582 WO2024107686A1 (en) | 2022-11-14 | 2023-11-14 | Macrocyclic kras inhibitors and methods of use |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN120500482A true CN120500482A (zh) | 2025-08-15 |
Family
ID=91085388
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202380088000.9A Pending CN120500482A (zh) | 2022-11-14 | 2023-11-14 | 大环kras抑制剂及使用方法 |
Country Status (15)
| Country | Link |
|---|---|
| US (3) | US12570672B2 (https=) |
| EP (1) | EP4598921A1 (https=) |
| JP (3) | JP7743484B2 (https=) |
| KR (2) | KR102919887B1 (https=) |
| CN (1) | CN120500482A (https=) |
| AU (1) | AU2023382606A1 (https=) |
| CL (1) | CL2025001425A1 (https=) |
| CO (1) | CO2025006813A2 (https=) |
| IL (1) | IL320388A (https=) |
| JO (1) | JOP20250111A1 (https=) |
| MX (1) | MX2025005539A (https=) |
| PE (1) | PE20252237A1 (https=) |
| TW (1) | TW202430532A (https=) |
| UY (1) | UY40522A (https=) |
| WO (1) | WO2024107686A1 (https=) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN120813588A (zh) | 2023-02-14 | 2025-10-17 | 豪夫迈·罗氏有限公司 | 用于治疗癌症的三环化合物 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| WO2025123007A1 (en) * | 2023-12-08 | 2025-06-12 | Kestrel Therapeutics Inc. | Ras inhibitors and methods of use thereof |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025194054A1 (en) * | 2024-03-14 | 2025-09-18 | Amgen Inc. | Spirocyclic compounds as modulators of kras and uses thereof |
| TW202602882A (zh) * | 2024-03-14 | 2026-01-16 | 美商安進公司 | 作為ｋｒａｓ調節劑的大環化合物及其用途 |
| WO2025230862A1 (en) * | 2024-04-29 | 2025-11-06 | Amgen Inc. | Macrocyclic amino compounds as modulators of kras and uses therof |
| WO2025230860A1 (en) * | 2024-04-29 | 2025-11-06 | Amgen Inc. | Solid forms of macrocyclic compounds and uses thereof |
| WO2025230878A1 (en) * | 2024-04-29 | 2025-11-06 | Amgen Inc. | Macrocyclic compounds as modulators of kras and uses thereof |
| WO2025240465A1 (en) * | 2024-05-14 | 2025-11-20 | Amgen Inc. | Processes for preparing macrocyclic compounds |
| WO2025240582A1 (en) * | 2024-05-14 | 2025-11-20 | Amgen Inc. | Macrocyclic compounds as modulators of kras and uses thereof |
| 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 |
| 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 |
| 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 |
| WO2026055477A1 (en) * | 2024-09-06 | 2026-03-12 | Amgen Inc. | Macrocyclic compounds as modulators of kras and uses thereof |
| WO2026064527A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload |
| WO2026064520A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and 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 (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4302834A3 (en) | 2016-07-12 | 2024-07-17 | Revolution Medicines, Inc. | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors |
| JP7240319B2 (ja) | 2017-01-23 | 2023-03-15 | レヴォリューション・メディスンズ，インコーポレイテッド | アロステリックｓｈｐ２阻害剤としての二環式化合物 |
| 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 |
| TW201930292A (zh) | 2017-10-12 | 2019-08-01 | 美商銳新醫藥公司 | 作為變構ｓｈｐ２抑制劑的吡啶、吡嗪和三嗪化合物 |
| JP2022513967A (ja) | 2018-12-20 | 2022-02-09 | アムジエン・インコーポレーテツド | Ｋｉｆ１８ａ阻害剤として有用なヘテロアリールアミド |
| JP7686559B2 (ja) | 2018-12-20 | 2025-06-02 | アムジエン・インコーポレーテツド | Ｋｉｆ１８ａ阻害剤 |
| AU2019401495B2 (en) | 2018-12-20 | 2025-06-26 | Amgen Inc. | Heteroaryl amides useful as KIF18A inhibitors |
| MA54543A (fr) | 2018-12-20 | 2022-03-30 | Amgen Inc | Inhibiteurs de kif18a |
| MX2022002465A (es) * | 2019-08-29 | 2022-05-19 | Mirati Therapeutics Inc | Inhibidores de kras g12d. |
| CN115003668A (zh) * | 2020-01-21 | 2022-09-02 | 南京明德新药研发有限公司 | 作为kras抑制剂的大环类化合物 |
| 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 |
| BR112023016299A2 (pt) * | 2021-02-16 | 2023-11-28 | L Livermore Nat Security Llc | Composições e métodos para inibir kras |
| CA3211725A1 (en) * | 2021-03-17 | 2022-09-22 | Tao Jiang | Pyrimidine-fused cyclic compound, preparation method therefor and use thereof |
| US20250255868A1 (en) * | 2021-04-09 | 2025-08-14 | Hangzhou Innogate Pharma Co., Ltd. | Heterocyclic compound acting as kras g12d inhibitor |
| CN115304623A (zh) * | 2021-04-30 | 2022-11-08 | 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 |
| WO2022246092A1 (en) | 2021-05-21 | 2022-11-24 | Blossomhill Therapeutics, Inc. | Macrocyclic compounds for treating disease |
| WO2023040989A1 (en) | 2021-09-16 | 2023-03-23 | Suzhou Zanrong Pharma Limited | Kras g12c inhibitors and uses thereof |
| EP4573095A1 (en) | 2022-08-17 | 2025-06-25 | Treeline Biosciences, Inc. | Pyridopyrimidine kras inhibitors |
-
2023
- 2023-11-14 AU AU2023382606A patent/AU2023382606A1/en active Pending
- 2023-11-14 EP EP23892383.3A patent/EP4598921A1/en active Pending
- 2023-11-14 UY UY0001040522A patent/UY40522A/es unknown
- 2023-11-14 IL IL320388A patent/IL320388A/en unknown
- 2023-11-14 PE PE2025001022A patent/PE20252237A1/es unknown
- 2023-11-14 TW TW112143850A patent/TW202430532A/zh unknown
- 2023-11-14 KR KR1020257019826A patent/KR102919887B1/ko active Active
- 2023-11-14 KR KR1020267002540A patent/KR20260017504A/ko active Pending
- 2023-11-14 JP JP2023193597A patent/JP7743484B2/ja active Active
- 2023-11-14 WO PCT/US2023/079582 patent/WO2024107686A1/en not_active Ceased
- 2023-11-14 JP JP2025527103A patent/JP2025539080A/ja active Pending
- 2023-11-14 CN CN202380088000.9A patent/CN120500482A/zh active Pending
-
2024
- 2024-03-25 US US18/614,911 patent/US12570672B2/en active Active
- 2024-10-30 US US18/931,588 patent/US20250304599A1/en active Pending
-
2025
- 2025-04-11 US US19/176,333 patent/US20250236631A1/en active Pending
- 2025-05-12 MX MX2025005539A patent/MX2025005539A/es unknown
- 2025-05-13 JO JOJO/P/2025/0111A patent/JOP20250111A1/ar unknown
- 2025-05-14 CL CL2025001425A patent/CL2025001425A1/es unknown
- 2025-05-23 CO CONC2025/0006813A patent/CO2025006813A2/es unknown
- 2025-09-10 JP JP2025149982A patent/JP2025179208A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| PE20252237A1 (es) | 2025-09-15 |
| US12570672B2 (en) | 2026-03-10 |
| CL2025001425A1 (es) | 2025-08-29 |
| US20250304599A1 (en) | 2025-10-02 |
| JOP20250111A1 (ar) | 2025-05-13 |
| TW202430532A (zh) | 2024-08-01 |
| UY40522A (es) | 2024-05-15 |
| JP2025539080A (ja) | 2025-12-03 |
| US20240294551A1 (en) | 2024-09-05 |
| JP2025179208A (ja) | 2025-12-09 |
| JP7743484B2 (ja) | 2025-09-24 |
| MX2025005539A (es) | 2025-06-02 |
| CO2025006813A2 (es) | 2025-06-06 |
| JP2024071370A (ja) | 2024-05-24 |
| KR20250095749A (ko) | 2025-06-26 |
| IL320388A (en) | 2025-06-01 |
| WO2024107686A1 (en) | 2024-05-23 |
| EP4598921A1 (en) | 2025-08-13 |
| KR102919887B1 (ko) | 2026-01-29 |
| KR20260017504A (ko) | 2026-02-05 |
| AU2023382606A1 (en) | 2025-05-08 |
| US20250236631A1 (en) | 2025-07-24 |
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