IL316253A - A cyclic compound with selective KRAS inhibitory effect on HRAS and NRAS - Google Patents
A cyclic compound with selective KRAS inhibitory effect on HRAS and NRASInfo
- Publication number
- IL316253A IL316253A IL316253A IL31625324A IL316253A IL 316253 A IL316253 A IL 316253A IL 316253 A IL316253 A IL 316253A IL 31625324 A IL31625324 A IL 31625324A IL 316253 A IL316253 A IL 316253A
- Authority
- IL
- Israel
- Prior art keywords
- trifluoromethyl
- phenyl
- ethyl
- methylpropyl
- spiro
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K9/00—Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequence; Derivatives thereof
- C07K9/006—Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequence; Derivatives thereof the peptide sequence being part of a ring structure
-
- 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
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/04—Linear peptides containing only normal peptide links
- C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/50—Cyclic peptides containing at least one abnormal peptide link
- C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/50—Cyclic peptides containing at least one abnormal peptide link
- C07K7/54—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring
- C07K7/56—Cyclic peptides containing at least one abnormal peptide link with at least one abnormal peptide link in the ring the cyclisation not occurring through 2,4-diamino-butanoic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/64—Cyclic peptides containing only normal peptide links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Gastroenterology & Hepatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Hydrogenated Pyridines (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022076449 | 2022-05-06 | ||
| PCT/JP2023/017112 WO2023214576A1 (ja) | 2022-05-06 | 2023-05-02 | Ｈｒａｓおよびｎｒａｓに対して選択的なｋｒａｓ阻害作用を有する環状化合物 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| IL316253A true IL316253A (en) | 2025-01-01 |
Family
ID=88646541
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL316253A IL316253A (en) | 2022-05-06 | 2023-05-02 | A cyclic compound with selective KRAS inhibitory effect on HRAS and NRAS |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US12410212B2 (https=) |
| EP (1) | EP4512818A1 (https=) |
| JP (1) | JP7823181B2 (https=) |
| KR (1) | KR20250008758A (https=) |
| CN (1) | CN119731195A (https=) |
| AR (1) | AR129238A1 (https=) |
| AU (1) | AU2023264918A1 (https=) |
| CA (1) | CA3256645A1 (https=) |
| CL (1) | CL2024003354A1 (https=) |
| CO (1) | CO2024016293A2 (https=) |
| IL (1) | IL316253A (https=) |
| MX (1) | MX2024013352A (https=) |
| PE (1) | PE20251872A1 (https=) |
| TW (1) | TW202406927A (https=) |
| WO (1) | WO2023214576A1 (https=) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI787670B (zh) | 2011-12-28 | 2022-12-21 | 日商中外製藥股份有限公司 | 具有環狀部之胜肽化合物及其醫藥組成物 |
| US12391971B2 (en) | 2017-01-31 | 2025-08-19 | Chugai Seiyaku Kabushiki Kaisha | Method for synthesizing peptides in cell-free translation system |
| WO2018225851A1 (ja) | 2017-06-09 | 2018-12-13 | 中外製薬株式会社 | Ｎ－置換アミノ酸を含むペプチドの合成方法 |
| EP3878836B1 (en) | 2018-11-07 | 2025-07-23 | Chugai Seiyaku Kabushiki Kaisha | O-substituted serine derivative production method |
| US12404299B2 (en) | 2019-11-07 | 2025-09-02 | Chugai Seiyaku Kabushiki Kaisha | Method for producing peptide compound comprising highly sterically hindered amino acid |
| PE20221323A1 (es) | 2019-11-07 | 2022-09-09 | Chugai Pharmaceutical Co Ltd | Compuesto de peptidos ciclicos que tiene accion inhibidora de kras |
| TW202309065A (zh) | 2021-05-07 | 2023-03-01 | 日商中外製藥股份有限公司 | 包含n-取代胺基酸殘基之環狀化合物的製造方法 |
| WO2024101386A1 (ja) * | 2022-11-09 | 2024-05-16 | 中外製薬株式会社 | Ｈｒａｓおよびｎｒａｓに対して選択的なｋｒａｓ阻害作用を有する環状化合物 |
| TW202434275A (zh) * | 2022-11-09 | 2024-09-01 | 日商中外製藥股份有限公司 | 含有相對於ｈｒａｓ與ｎｒａｓ具有選擇性ｋｒａｓ抑制作用之環狀化合物的醫藥組成物 |
| KR20250160895A (ko) | 2023-03-20 | 2025-11-14 | 추가이 세이야쿠 가부시키가이샤 | 고리형 펩타이드의 공결정을 제조하는 방법 |
| 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 |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025162428A1 (en) * | 2024-01-29 | 2025-08-07 | Syneron Technology Co. Ltd. | Cyclic peptide compounds and compositions as ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202547852A (zh) * | 2024-03-13 | 2025-12-16 | 日商中外製藥股份有限公司 | 具有環狀結構的胜肽化合物的製造方法 |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras 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 |
| WO2026004834A1 (ja) * | 2024-06-25 | 2026-01-02 | 中外製薬株式会社 | 固体分散体、及びそれを含む組成物 |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015790A1 (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 |
| 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 |
| 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 |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6239979B2 (ja) | 2011-03-04 | 2017-11-29 | ニューヨーク・ユニバーシティ | Ｒａｓの調節因子としての水素結合代替大環状分子 |
| EP2721048A1 (en) | 2011-06-16 | 2014-04-23 | Lonza Ltd | A process for extraction of peptides and its application in liquid phase peptide synthesis |
| TWI787670B (zh) | 2011-12-28 | 2022-12-21 | 日商中外製藥股份有限公司 | 具有環狀部之胜肽化合物及其醫藥組成物 |
| MX383691B (es) | 2015-03-06 | 2025-03-14 | Beyondspring Pharmaceuticals Inc | Método de tratamiento de cáncer asociado con una mutación de ras. |
| DK3269809T3 (da) | 2015-03-13 | 2022-09-12 | Chugai Pharmaceutical Co Ltd | MODIFICERET AMINOACYL-tRNA-SYNTETASE OG ANVENDELSE DERAF |
| JP2018513853A (ja) | 2015-04-10 | 2018-05-31 | アラクセス ファーマ エルエルシー | 置換キナゾリン化合物およびその使用方法 |
| WO2017150732A1 (ja) | 2016-03-03 | 2017-09-08 | 中外製薬株式会社 | チオール基をアミノ基近傍に有するアミノ酸をｎ末端に持つ非環状ペプチド－核酸複合体、そのライブラリー、およびそれから誘導される環状ペプチド－核酸複合体ライブラリーの製造方法 |
| US10954287B2 (en) | 2016-04-15 | 2021-03-23 | Ra Pharmaceuticals, Inc. | Ras binding peptides and methods of use |
| EP4039250A1 (en) | 2016-12-28 | 2022-08-10 | Chugai Seiyaku Kabushiki Kaisha | Self-emulsifying drug formulation for improving membrane permeability of compound |
| US12391971B2 (en) | 2017-01-31 | 2025-08-19 | Chugai Seiyaku Kabushiki Kaisha | Method for synthesizing peptides in cell-free translation system |
| EA201992781A1 (ru) | 2017-05-22 | 2020-04-01 | Эмджен Инк. | Ингибиторы g12c kras и способы их применения |
| JP7232758B2 (ja) | 2017-06-09 | 2023-03-06 | 中外製薬株式会社 | 膜透過性の高い環状ペプチド化合物、及びこれを含むライブラリ |
| WO2018225851A1 (ja) | 2017-06-09 | 2018-12-13 | 中外製薬株式会社 | Ｎ－置換アミノ酸を含むペプチドの合成方法 |
| HRP20230377T1 (hr) | 2017-11-15 | 2023-06-23 | Mirati Therapeutics, Inc. | Inhibitori mutacije kras g12c |
| EP3725796A4 (en) | 2017-12-15 | 2021-09-15 | Chugai Seiyaku Kabushiki Kaisha | METHOD FOR MANUFACTURING PEPTIDE AND METHOD FOR PROCESSING BASES |
| GB201805088D0 (en) | 2018-03-28 | 2018-05-09 | Univ Warwick | Macrocyclization of peptidomimetics |
| EP3878836B1 (en) | 2018-11-07 | 2025-07-23 | Chugai Seiyaku Kabushiki Kaisha | O-substituted serine derivative production method |
| JP7568510B2 (ja) | 2018-11-30 | 2024-10-16 | 中外製薬株式会社 | ペプチド化合物、またはアミド化合物の脱保護法および固相反応における脱樹脂方法、並びにペプチド化合物の製造方法 |
| WO2020122182A1 (ja) | 2018-12-12 | 2020-06-18 | 中外製薬株式会社 | 分子内水素結合可能な官能基を有するアミノ酸とそれらのアミノ酸を含むペプチド化合物、およびそれらの製造方法 |
| WO2020138336A1 (ja) | 2018-12-26 | 2020-07-02 | 中外製薬株式会社 | コドン拡張のための変異ｔＲＮＡ |
| KR20210139366A (ko) | 2019-03-15 | 2021-11-22 | 추가이 세이야쿠 가부시키가이샤 | 방향족 아미노산 유도체의 제조 방법 |
| PE20221323A1 (es) | 2019-11-07 | 2022-09-09 | Chugai Pharmaceutical Co Ltd | Compuesto de peptidos ciclicos que tiene accion inhibidora de kras |
| US12404299B2 (en) | 2019-11-07 | 2025-09-02 | Chugai Seiyaku Kabushiki Kaisha | Method for producing peptide compound comprising highly sterically hindered amino acid |
| JP7744244B2 (ja) | 2019-12-26 | 2025-09-25 | 中外製薬株式会社 | 翻訳用組成物及びペプチドの製造方法 |
| JP7709920B2 (ja) | 2019-12-27 | 2025-07-17 | 中外製薬株式会社 | ペプチド化合物の合成法 |
| EP4144747A4 (en) | 2020-06-03 | 2024-05-29 | Chugai Seiyaku Kabushiki Kaisha | EFFICIENT PEPTIDE CONDENSATION PROCESS FOR DIFFICULT SEQUENCES |
| TW202208623A (zh) | 2020-06-25 | 2022-03-01 | 日商中外製藥股份有限公司 | 具有經改變之遺傳密碼表的轉譯系統 |
| US20230391818A1 (en) | 2020-11-05 | 2023-12-07 | Chugai Seiyaku Kabushiki Kaisha | Peptide synthesis method for suppressing defect caused by diketopiperazine formation |
| JPWO2022138891A1 (https=) | 2020-12-25 | 2022-06-30 | ||
| US20240067674A1 (en) | 2020-12-28 | 2024-02-29 | Chugai Seiyaku Kabushiki Kaisha | Method for loading amino acid on resin for solid-phase synthesis |
| KR102666765B1 (ko) | 2021-05-07 | 2024-05-16 | 추가이 세이야쿠 가부시키가이샤 | 환상 펩타이드 화합물의 의약 용도 |
| AU2022270498A1 (en) | 2021-05-07 | 2023-10-05 | Chugai Seiyaku Kabushiki Kaisha | Preparation containing cyclic peptide compound and method for producing same |
| AR125796A1 (es) | 2021-05-07 | 2023-08-16 | Chugai Pharmaceutical Co Ltd | Compuesto cíclico que tiene una acción inhibitoria selectiva en kras sobre hras y nras |
| WO2022234639A1 (ja) | 2021-05-07 | 2022-11-10 | 中外製薬株式会社 | 変異型ｒａｓ（ｇ１２ｄ）に対する選択的結合性を示す結合分子 |
| TW202309065A (zh) | 2021-05-07 | 2023-03-01 | 日商中外製藥股份有限公司 | 包含n-取代胺基酸殘基之環狀化合物的製造方法 |
| MX2024008002A (es) | 2021-12-28 | 2024-07-12 | Chugai Pharmaceutical Co Ltd | Metodo para producir n-alquilaminoacido y peptido que incluye n-alquilaminoacido. |
| MX2024008358A (es) | 2022-01-21 | 2024-07-19 | Chugai Pharmaceutical Co Ltd | Medicina para tratar o prevenir el cancer. |
| US20250353875A1 (en) | 2022-05-02 | 2025-11-20 | Chugai Seiyaku Kabushiki Kaisha | Peptide synthesis method for suppressing defect caused by diketopiperazine formation |
-
2023
- 2023-05-02 CA CA3256645A patent/CA3256645A1/en active Pending
- 2023-05-02 PE PE2024002242A patent/PE20251872A1/es unknown
- 2023-05-02 AU AU2023264918A patent/AU2023264918A1/en active Pending
- 2023-05-02 TW TW112116268A patent/TW202406927A/zh unknown
- 2023-05-02 JP JP2024519229A patent/JP7823181B2/ja active Active
- 2023-05-02 KR KR1020247039424A patent/KR20250008758A/ko active Pending
- 2023-05-02 CN CN202380038438.6A patent/CN119731195A/zh active Pending
- 2023-05-02 WO PCT/JP2023/017112 patent/WO2023214576A1/ja not_active Ceased
- 2023-05-02 EP EP23799505.5A patent/EP4512818A1/en active Pending
- 2023-05-02 IL IL316253A patent/IL316253A/en unknown
- 2023-05-05 AR ARP230101103A patent/AR129238A1/es unknown
-
2024
- 2024-09-10 US US18/829,566 patent/US12410212B2/en active Active
- 2024-10-29 MX MX2024013352A patent/MX2024013352A/es unknown
- 2024-11-04 CL CL2024003354A patent/CL2024003354A1/es unknown
- 2024-11-28 CO CONC2024/0016293A patent/CO2024016293A2/es unknown
-
2025
- 2025-02-18 US US19/055,932 patent/US20250230193A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| KR20250008758A (ko) | 2025-01-15 |
| US20250230193A1 (en) | 2025-07-17 |
| WO2023214576A1 (ja) | 2023-11-09 |
| US12410212B2 (en) | 2025-09-09 |
| AU2023264918A1 (en) | 2025-01-09 |
| PE20251872A1 (es) | 2025-07-22 |
| TW202406927A (zh) | 2024-02-16 |
| CL2024003354A1 (es) | 2025-03-21 |
| JPWO2023214576A1 (https=) | 2023-11-09 |
| JP7823181B2 (ja) | 2026-03-03 |
| CA3256645A1 (en) | 2025-04-23 |
| CN119731195A (zh) | 2025-03-28 |
| CO2024016293A2 (es) | 2025-02-24 |
| US20250051394A1 (en) | 2025-02-13 |
| AR129238A1 (es) | 2024-07-31 |
| MX2024013352A (es) | 2024-12-06 |
| EP4512818A1 (en) | 2025-02-26 |
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