JP2025510656A - 複素環式化合物、その組成物、及びそれらを用いた治療方法 - Google Patents
複素環式化合物、その組成物、及びそれらを用いた治療方法 Download PDFInfo
- Publication number
- JP2025510656A JP2025510656A JP2024555128A JP2024555128A JP2025510656A JP 2025510656 A JP2025510656 A JP 2025510656A JP 2024555128 A JP2024555128 A JP 2024555128A JP 2024555128 A JP2024555128 A JP 2024555128A JP 2025510656 A JP2025510656 A JP 2025510656A
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- compound
- fluoro
- pyrrolidin
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
- A61K31/537—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 spiro-condensed or 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- 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)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2022082722 | 2022-03-24 | ||
| CNPCT/CN2022/082722 | 2022-03-24 | ||
| PCT/CN2023/083294 WO2023179703A1 (en) | 2022-03-24 | 2023-03-23 | Heterocyclic compounds, compositions thereof, and methods of treatment therewith |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2025510656A true JP2025510656A (ja) | 2025-04-15 |
| JPWO2023179703A5 JPWO2023179703A5 (https=) | 2026-04-08 |
| JP2025510656A5 JP2025510656A5 (https=) | 2026-04-08 |
Family
ID=88100085
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024555128A Pending JP2025510656A (ja) | 2022-03-24 | 2023-03-23 | 複素環式化合物、その組成物、及びそれらを用いた治療方法 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20250101028A1 (https=) |
| EP (1) | EP4499639A1 (https=) |
| JP (1) | JP2025510656A (https=) |
| CN (1) | CN118900838A (https=) |
| WO (1) | WO2023179703A1 (https=) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4373822A2 (en) | 2021-07-23 | 2024-05-29 | Theras Inc. | Compositions and methods for inhibition of ras |
| JP2024543879A (ja) * | 2021-11-24 | 2024-11-26 | メルク・シャープ・アンド・ドーム・エルエルシー | Ｋｒａｓ変異型タンパク質の小分子阻害剤 |
| JP2025525938A (ja) * | 2022-08-05 | 2025-08-07 | セラス， インコーポレイテッド | Ｋｒａｓの阻害のための組成物及び方法 |
| WO2024112654A1 (en) | 2022-11-21 | 2024-05-30 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| EP4687905A1 (en) | 2023-03-30 | 2026-02-11 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| 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 |
| AU2024323424A1 (en) | 2023-08-17 | 2026-03-05 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| AU2024337913A1 (en) | 2023-09-08 | 2026-03-26 | Gilead Sciences, Inc. | Pyrimidine-containing polycyclic derivatives as kras g12d modulating compounds |
| TW202528315A (zh) | 2023-09-21 | 2025-07-16 | 美商樹線生物科學公司 | 螺環二氫哌喃并吡啶ＫＲａｓ抑制劑 |
| US20250114339A1 (en) | 2023-10-09 | 2025-04-10 | Incyte Corporation | Combination therapy comprising a kras g12d inhibitor and an egfr inhibitor |
| AU2024357850A1 (en) | 2023-10-09 | 2026-04-23 | Incyte Corporation | Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025090811A1 (en) * | 2023-10-25 | 2025-05-01 | Kumquat Biosciences Inc. | Methods of modulating cell proliferation |
| 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 |
| 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 |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| 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 |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026035945A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload |
| WO2026035947A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates 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 (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP4192585A4 (en) * | 2020-08-04 | 2024-08-21 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| WO2022132200A1 (en) * | 2020-12-15 | 2022-06-23 | Mirati Therapeutics, Inc. | Azaquinazoline pan-kras inhibitors |
| AU2022224511A1 (en) * | 2021-02-16 | 2023-08-10 | Lawrence Livermore National Security, Llc | Compositions and methods for inhibition of ras |
| WO2022214102A1 (zh) * | 2021-04-09 | 2022-10-13 | 杭州英创医药科技有限公司 | 作为kras g12d抑制剂的杂环化合物 |
| 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 |
| WO2022247760A1 (zh) * | 2021-05-22 | 2022-12-01 | 上海科州药物研发有限公司 | 作为kras抑制剂的杂环化合物，及其制备和治疗用途 |
| WO2022248885A2 (en) * | 2021-05-28 | 2022-12-01 | Redx Pharma Plc. | Compounds |
| EP4373822A2 (en) * | 2021-07-23 | 2024-05-29 | Theras Inc. | Compositions and methods for inhibition of ras |
| WO2023020521A1 (en) * | 2021-08-18 | 2023-02-23 | Jacobio Pharmaceuticals Co., Ltd. | Pyridine fused pyrimidine derivatives and use thereof |
| CN117858878A (zh) * | 2021-08-18 | 2024-04-09 | 北京加科思新药研发有限公司 | N-环丙基吡啶并[4,3-d]嘧啶-4-胺衍生物及其用途 |
| WO2023056951A1 (zh) * | 2021-10-08 | 2023-04-13 | 杭州德睿智药科技有限公司 | 芳基取代并杂环化合物 |
| WO2023061294A1 (zh) * | 2021-10-13 | 2023-04-20 | 再鼎医药(上海)有限公司 | 含氮杂环类衍生物调节剂、其制备方法及应用 |
| WO2023072188A1 (zh) * | 2021-10-29 | 2023-05-04 | 贝达药业股份有限公司 | Kras g12d抑制剂及其在医药上的应用 |
| TW202334138A (zh) * | 2021-11-05 | 2023-09-01 | 美商新領域醫藥公司 | 癌症治療方法 |
-
2023
- 2023-03-23 CN CN202380028687.7A patent/CN118900838A/zh active Pending
- 2023-03-23 JP JP2024555128A patent/JP2025510656A/ja active Pending
- 2023-03-23 EP EP23773949.5A patent/EP4499639A1/en active Pending
- 2023-03-23 WO PCT/CN2023/083294 patent/WO2023179703A1/en not_active Ceased
-
2024
- 2024-09-19 US US18/889,657 patent/US20250101028A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP4499639A1 (en) | 2025-02-05 |
| US20250101028A1 (en) | 2025-03-27 |
| CN118900838A (zh) | 2024-11-05 |
| WO2023179703A1 (en) | 2023-09-28 |
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| RD04 | Notification of resignation of power of attorney |
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| RD02 | Notification of acceptance of power of attorney |
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| A521 | Request for written amendment filed |
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| A621 | Written request for application examination |
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