JP2024510606A - Kras g12d阻害剤 - Google Patents

Kras g12d阻害剤 Download PDF

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Publication number
JP2024510606A
JP2024510606A JP2023555666A JP2023555666A JP2024510606A JP 2024510606 A JP2024510606 A JP 2024510606A JP 2023555666 A JP2023555666 A JP 2023555666A JP 2023555666 A JP2023555666 A JP 2023555666A JP 2024510606 A JP2024510606 A JP 2024510606A
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JP
Japan
Prior art keywords
diazabicyclo
chloro
methoxy
fluoro
methyl
Prior art date
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Pending
Application number
JP2023555666A
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English (en)
Japanese (ja)
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JP2024510606A5 (https=
JPWO2022192794A5 (https=
Inventor
エドワード フィンク,ブライアン
ジョセフ チャーニー,ロバート
グ,ケヒョン
ベラパルチ,アッペンダー
デイビッド バッカロ,ウェイン
ルアン,ジェミン
チン,ラン-イン
エス シルデ,プラビン
ラーマン,ハシブル
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.)
Bristol Myers Squibb Co
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Bristol Myers Squibb Co
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Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of JP2024510606A publication Critical patent/JP2024510606A/ja
Publication of JP2024510606A5 publication Critical patent/JP2024510606A5/ja
Publication of JPWO2022192794A5 publication Critical patent/JPWO2022192794A5/ja
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/08Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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 system contains two hetero rings
    • C07D471/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2023555666A 2021-03-12 2022-03-14 Kras g12d阻害剤 Pending JP2024510606A (ja)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US202163160431P 2021-03-12 2021-03-12
US63/160,431 2021-03-12
US202163173021P 2021-04-09 2021-04-09
US63/173,021 2021-04-09
US202163220386P 2021-07-09 2021-07-09
US63/220,386 2021-07-09
US202163236497P 2021-08-24 2021-08-24
US63/236,497 2021-08-24
PCT/US2022/020239 WO2022192794A1 (en) 2021-03-12 2022-03-14 Kras g12d inhibitors

Publications (3)

Publication Number Publication Date
JP2024510606A true JP2024510606A (ja) 2024-03-08
JP2024510606A5 JP2024510606A5 (https=) 2025-03-24
JPWO2022192794A5 JPWO2022192794A5 (https=) 2025-03-24

Family

ID=81213567

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2023555666A Pending JP2024510606A (ja) 2021-03-12 2022-03-14 Kras g12d阻害剤

Country Status (11)

Country Link
US (1) US20240317769A1 (https=)
EP (1) EP4305038B1 (https=)
JP (1) JP2024510606A (https=)
KR (1) KR20230169967A (https=)
AU (1) AU2022232523A1 (https=)
BR (1) BR112023017763A2 (https=)
CA (1) CA3210053A1 (https=)
ES (1) ES3013592T3 (https=)
IL (1) IL305568A (https=)
MX (1) MX2023010430A (https=)
WO (1) WO2022192794A1 (https=)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2024517695A (ja) * 2021-04-29 2024-04-23 アムジエン・インコーポレーテツド 複素環式化合物及び使用方法

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US20230365563A1 (en) * 2020-09-30 2023-11-16 Shanghai Pharmaceuticals Holding Co., Ltd. Quinazoline compound and application thereof
CN115181106B (zh) * 2021-04-07 2024-04-05 药雅科技(上海)有限公司 喹唑啉类krasg12d突变蛋白抑制剂的制备及其应用
WO2023278600A1 (en) * 2021-06-30 2023-01-05 Dana-Farber Cancer Institute, Inc. Small molecule inhibitors of kras g12d mutant
WO2023114733A1 (en) * 2021-12-13 2023-06-22 Quanta Therapeutics, Inc. Kras modulators and uses thereof
MX2024008849A (es) 2022-01-21 2024-07-25 Usynova Pharmaceuticals Ltd Compuestos de benzopirimidina y uso de estos.
CN118556063A (zh) * 2022-01-21 2024-08-27 上海湃隆生物科技有限公司 杂环类化合物、药物组合物及其应用
AU2023218370B2 (en) 2022-02-09 2024-11-28 Quanta Therapeutics, Inc. Kras modulators and uses thereof
CN119136806A (zh) 2022-03-08 2024-12-13 锐新医药公司 用于治疗免疫难治性肺癌的方法
CN118344386A (zh) * 2023-01-13 2024-07-16 苏州泽璟生物制药股份有限公司 取代桥环类抑制剂及其制备方法和应用
IL317601A (en) 2022-05-25 2025-02-01 Quanta Therapeutics Inc Pyrimidine-based modulators and their uses
WO2023240263A1 (en) 2022-06-10 2023-12-14 Revolution Medicines, Inc. Macrocyclic ras inhibitors
TW202416976A (zh) * 2022-09-16 2024-05-01 大陸商南京明德新藥研發有限公司 含六氫螺環[環丙烷—1,2'—吡咯𠯤]的化合物
WO2024061365A1 (zh) * 2022-09-22 2024-03-28 成都奥睿药业有限公司 嘧啶并环类化合物及其制备方法与用途
AU2023349002A1 (en) * 2022-09-30 2025-05-15 Trasveda Ltd. Compounds with anti-kras mutant tumor activity
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JP2025536369A (ja) 2022-10-21 2025-11-05 リーディングタック ファーマシューティカル(シャオシン)カンパニー,リミテッド Kras g12d分解剤及びその製造方法並びに応用
CN117263959A (zh) * 2022-10-24 2023-12-22 药雅科技(上海)有限公司 芳香类kras突变蛋白抑制剂的制备及其应用
WO2024092420A1 (zh) * 2022-10-31 2024-05-10 上海皓元医药股份有限公司 一种((2R,7aS)-2-氟六氢-1H-吡咯嗪-7a-基)甲醇的制备方法
CN121419983A (zh) 2023-01-26 2026-01-27 阿尔维纳斯运营股份有限公司 基于小脑蛋白的kras降解protac及其相关用途
WO2024186680A1 (en) * 2023-03-03 2024-09-12 Frontier Medicines Corporation Methods for preparing pyrrolizidine compounds
WO2024192424A1 (en) 2023-03-15 2024-09-19 Quanta Therapeutics, Inc. Kras modulators and uses thereof
EP4687905A1 (en) 2023-03-30 2026-02-11 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
KR20260005904A (ko) 2023-04-07 2026-01-12 레볼루션 메디슨즈, 인크. 매크로사이클릭 ras 억제제
CN121263418A (zh) 2023-04-07 2026-01-02 锐新医药公司 大环ras抑制剂
WO2024215862A2 (en) * 2023-04-12 2024-10-17 Board Of Regents, The University Of Texas System Heterocyclic compounds as nras inhibitors
KR20250172857A (ko) 2023-04-14 2025-12-09 레볼루션 메디슨즈, 인크. Ras 억제제의 결정형
AU2024252105A1 (en) 2023-04-14 2025-10-16 Revolution Medicines, Inc. Crystalline forms of ras inhibitors, compositions containing the same, and methods of use thereof
CN121419984A (zh) * 2023-04-26 2026-01-27 珃诺生物医药科技(杭州)有限公司 Kras(g12d)的二氮杂双环辛烷抑制剂及用途
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WO2024230707A1 (zh) * 2023-05-07 2024-11-14 上海医药集团股份有限公司 一种喹唑啉类化合物及其应用
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
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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
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KR102738924B1 (ko) * 2023-12-26 2024-12-06 주식회사 베노바이오 Kras g12d 변이가 존재하는 암 치료를 위한 신규한 화합물 및 이를 이용한 암의 예방 또는 치료용 조성물
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JP2023512113A (ja) * 2019-11-29 2023-03-23 大鵬薬品工業株式会社 Kras g12d変異に対して阻害活性を有する化合物
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JP2020521742A (ja) * 2017-05-25 2020-07-27 アラクセス ファーマ エルエルシー Krasの共有結合性阻害剤
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Publication number Priority date Publication date Assignee Title
JP2024517695A (ja) * 2021-04-29 2024-04-23 アムジエン・インコーポレーテツド 複素環式化合物及び使用方法

Also Published As

Publication number Publication date
BR112023017763A2 (pt) 2023-10-03
IL305568A (en) 2023-10-01
KR20230169967A (ko) 2023-12-18
MX2023010430A (es) 2023-09-12
US20240317769A1 (en) 2024-09-26
EP4305038A1 (en) 2024-01-17
ES3013592T3 (en) 2025-04-14
WO2022192794A1 (en) 2022-09-15
EP4305038B1 (en) 2025-01-29
CA3210053A1 (en) 2022-09-15
AU2022232523A1 (en) 2023-11-16

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