JP7823181B2 - 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 - Google Patents

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

Info

Publication number
JP7823181B2
JP7823181B2 JP2024519229A JP2024519229A JP7823181B2 JP 7823181 B2 JP7823181 B2 JP 7823181B2 JP 2024519229 A JP2024519229 A JP 2024519229A JP 2024519229 A JP2024519229 A JP 2024519229A JP 7823181 B2 JP7823181 B2 JP 7823181B2
Authority
JP
Japan
Prior art keywords
group
phenyl
trifluoromethyl
ethyl
methylpropyl
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.)
Active
Application number
JP2024519229A
Other languages
English (en)
Japanese (ja)
Other versions
JPWO2023214576A1 (https=
JPWO2023214576A5 (https=
Inventor
発夫 河田
宏治 鷹野
智也 小竹
未来 陰
哲 橋本
実 田宮
佑真 若宮
竜児 林
雄也 森田
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Chugai Pharmaceutical Co Ltd
Original Assignee
Chugai Pharmaceutical Co Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Chugai Pharmaceutical Co Ltd filed Critical Chugai Pharmaceutical Co Ltd
Publication of JPWO2023214576A1 publication Critical patent/JPWO2023214576A1/ja
Publication of JPWO2023214576A5 publication Critical patent/JPWO2023214576A5/ja
Application granted granted Critical
Publication of JP7823181B2 publication Critical patent/JP7823181B2/ja
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • 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
    • 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
    • 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)
JP2024519229A 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 Active JP7823181B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2022076449 2022-05-06
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 (3)

Publication Number Publication Date
JPWO2023214576A1 JPWO2023214576A1 (https=) 2023-11-09
JPWO2023214576A5 JPWO2023214576A5 (https=) 2026-01-15
JP7823181B2 true JP7823181B2 (ja) 2026-03-03

Family

ID=88646541

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2024519229A Active JP7823181B2 (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

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)

* Cited by examiner, † Cited by third party
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

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021090855A1 (ja) 2019-11-07 2021-05-14 中外製薬株式会社 Ｋｒａｓ阻害作用を有する環状ペプチド化合物
WO2022234852A1 (ja) 2021-05-07 2022-11-10 中外製薬株式会社 環状ペプチド化合物の医薬用途
WO2022234853A1 (ja) 2021-05-07 2022-11-10 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

Family Cites Families (35)

* Cited by examiner, † Cited by third party
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
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
AU2022270498A1 (en) 2021-05-07 2023-10-05 Chugai Seiyaku Kabushiki Kaisha Preparation containing cyclic peptide compound and method for producing same
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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021090855A1 (ja) 2019-11-07 2021-05-14 中外製薬株式会社 Ｋｒａｓ阻害作用を有する環状ペプチド化合物
WO2022234852A1 (ja) 2021-05-07 2022-11-10 中外製薬株式会社 環状ペプチド化合物の医薬用途
WO2022234853A1 (ja) 2021-05-07 2022-11-10 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

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
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
IL316253A (en) 2025-01-01
EP4512818A1 (en) 2025-02-26

Similar Documents

Publication Publication Date Title
JP7823181B2 (ja) 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
EP4309741A1 (en) Cyclic compound having inhibitory effect selective for kras but not for hras and nras
EP4603105A1 (en) Pharmaceutical composition containing cyclic compound having selective kras inhibitory effect against hras and nras
EP4592308A1 (en) Cyclic compound having selective kras inhibitory effect on hras and nras
JP7179241B1 (ja) 環状ペプチド化合物の医薬用途
US12371454B2 (en) Cyclic peptide compound having Kras inhibitory action
WO2022234639A1 (ja) 変異型ｒａｓ（ｇ１２ｄ）に対する選択的結合性を示す結合分子
KR20240082196A (ko) Hras 및 nras에 대해서 선택적인 kras 저해 작용을 갖는 환상 화합물을 포함하는 의약 조성물
WO1997010261A1 (fr) Derives peptidiques
HK40096863A (zh) 相对於hras和nras具有选择性kras抑制作用的环状化合物
HK40124102A (zh) 包含具有相对於hras和nras的选择性kras抑制作用的环状化合物的药物组合物
EA052654B1 (ru) Циклическое соединение, имеющее селективное ингибирующее действие в отношении kras по сравнению с hras и nras
HK40096352A (zh) 环状肽化合物的药物用途
CN101100483B (zh) 胞壁酰二肽的类似物

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20260106

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20260106

A871 Explanation of circumstances concerning accelerated examination

Free format text: JAPANESE INTERMEDIATE CODE: A871

Effective date: 20260106

RD02 Notification of acceptance of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7422

Effective date: 20260106

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20260120

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20260218

R150 Certificate of patent or registration of utility model

Ref document number: 7823181

Country of ref document: JP

Free format text: JAPANESE INTERMEDIATE CODE: R150