JP2025539080A - 大環状ｋｒａｓ阻害剤及び使用方法 - Google Patents

大環状ｋｒａｓ阻害剤及び使用方法

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Publication number
JP2025539080A
JP2025539080A JP2025527103A JP2025527103A JP2025539080A JP 2025539080 A JP2025539080 A JP 2025539080A JP 2025527103 A JP2025527103 A JP 2025527103A JP 2025527103 A JP2025527103 A JP 2025527103A JP 2025539080 A JP2025539080 A JP 2025539080A
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JP
Japan
Prior art keywords
compound
cancer
salt
alkylene
compounds
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
Application number
JP2025527103A
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English (en)
Japanese (ja)
Inventor
バウワー，アドリアーノ
アメガジエ，アルバート
スマリゴ，アンドリュー
ウィグマン，ベンジャミン
ランマン，ブライアン・アラン
モール，クリストファー
エメティエール，ファビアン
ステルワーゲン，ジョン・チャールズ
メディナ，ホセ・エム
リー，カーシュエ
ペタス，リピング・エイチ
ヤマノ，マイケル・マサハル
チェン，ニン
ナバラトネ，プリマリ・バスンデラ
リウ，チンイエン
テルセニオ，クエンティン
ラヒモフ，レーネ
ブルツ，ライアン・ポール
ブッカー，ション
ジャオ，ウェイ
リー，シャオフェン
リー，ユンシャオ
ウー，ジーチェン
ジークムント，アーロン・シー
ジャクソン，ジェフリー
Original Assignee
アムジエン・インコーポレーテツド
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.)
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Application filed by アムジエン・インコーポレーテツド filed Critical アムジエン・インコーポレーテツド
Publication of JP2025539080A publication Critical patent/JP2025539080A/ja
Pending legal-status Critical Current

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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
    • A61K31/535—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
    • A61K31/5386—1,4-Oxazines, e.g. morpholine 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
    • A61K31/55—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

  • 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)
  • 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)
JP2025527103A 2022-11-14 2023-11-14 大環状ｋｒａｓ阻害剤及び使用方法 Pending JP2025539080A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US202263383674P 2022-11-14 2022-11-14
US63/383,674 2022-11-14
US202363497978P 2023-04-24 2023-04-24
US63/497,978 2023-04-24
US202363582751P 2023-09-14 2023-09-14
US63/582,751 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
JP2025539080A true JP2025539080A (ja) 2025-12-03

Family

ID=91085388

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2025527103A Pending JP2025539080A (ja) 2022-11-14 2023-11-14 大環状ｋｒａｓ阻害剤及び使用方法
JP2023193597A Active JP7743484B2 (ja) 2022-11-14 2023-11-14 大環状ｋｒａｓ阻害剤及び使用方法
JP2025149982A Pending JP2025179208A (ja) 2022-11-14 2025-09-10 大環状ｋｒａｓ阻害剤及び使用方法

Family Applications After (2)

Application Number Title Priority Date Filing Date
JP2023193597A Active JP7743484B2 (ja) 2022-11-14 2023-11-14 大環状ｋｒａｓ阻害剤及び使用方法
JP2025149982A Pending JP2025179208A (ja) 2022-11-14 2025-09-10 大環状ｋｒａｓ阻害剤及び使用方法

Country Status (13)

Country Link
US (3) US20240294551A1 (enExample)
EP (1) EP4598921A1 (enExample)
JP (3) JP2025539080A (enExample)
KR (1) KR20250095749A (enExample)
CN (1) CN120500482A (enExample)
AU (1) AU2023382606A1 (enExample)
CL (1) CL2025001425A1 (enExample)
CO (1) CO2025006813A2 (enExample)
IL (1) IL320388A (enExample)
MX (1) MX2025005539A (enExample)
PE (1) PE20252237A1 (enExample)
TW (1) TW202430532A (enExample)
WO (1) WO2024107686A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2024220916A1 (en) 2023-02-14 2025-05-29 F. Hoffmann-La Roche Ag Tricyclic compounds for the treatment of cancer
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
US20250154171A1 (en) 2023-10-12 2025-05-15 Revolution Medicines, Inc. 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
WO2025194057A1 (en) * 2024-03-14 2025-09-18 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
WO2025230878A1 (en) * 2024-04-29 2025-11-06 Amgen Inc. Macrocyclic compounds as modulators of kras and uses thereof
WO2025230860A1 (en) * 2024-04-29 2025-11-06 Amgen Inc. Solid forms of macrocyclic compounds and uses thereof
WO2025230862A1 (en) * 2024-04-29 2025-11-06 Amgen Inc. Macrocyclic amino compounds as modulators of kras and uses therof
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
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
WO2025255438A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021041671A1 (en) * 2019-08-29 2021-03-04 Mirati Therapeutics, Inc. Kras g12d inhibitors
WO2021147967A1 (zh) 2020-01-21 2021-07-29 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
MX2023007084A (es) 2020-12-15 2023-08-30 Mirati Therapeutics Inc Inhibidores de pan-kras de azaquinazolina.
WO2022133038A1 (en) 2020-12-16 2022-06-23 Mirati Therapeutics, Inc. Tetrahydropyridopyrimidine pan-kras inhibitors
WO2022177917A2 (en) 2021-02-16 2022-08-25 Theras, Inc. Compositions and methods for inhibition of ras
AU2022235948A1 (en) 2021-03-17 2023-11-02 Genfleet Therapeutics (Shanghai) Inc. Pyrimidine-fused cyclic compound, preparation method therefor and use thereof
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

Also Published As

Publication number Publication date
TW202430532A (zh) 2024-08-01
US20250236631A1 (en) 2025-07-24
JP2024071370A (ja) 2024-05-24
EP4598921A1 (en) 2025-08-13
US20250304599A1 (en) 2025-10-02
MX2025005539A (es) 2025-06-02
CN120500482A (zh) 2025-08-15
WO2024107686A1 (en) 2024-05-23
CL2025001425A1 (es) 2025-08-29
JP7743484B2 (ja) 2025-09-24
KR20250095749A (ko) 2025-06-26
US20240294551A1 (en) 2024-09-05
IL320388A (en) 2025-06-01
PE20252237A1 (es) 2025-09-15
CO2025006813A2 (es) 2025-06-06
JP2025179208A (ja) 2025-12-09
AU2023382606A1 (en) 2025-05-08

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