JP2024510606A - Kras g12d阻害剤 - Google Patents

Kras g12d阻害剤 Download PDF

Info

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
Authority
JP
Japan
Prior art keywords
diazabicyclo
chloro
methoxy
fluoro
methyl
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
JP2023555666A
Other languages
English (en)
Japanese (ja)
Other versions
JP2024510606A5 (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
Original Assignee
Bristol Myers Squibb Co
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 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
Pending legal-status Critical Current

Links

Classifications

    • 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

Landscapes

  • 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)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (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 (2)

Publication Number Publication Date
JP2024510606A true JP2024510606A (ja) 2024-03-08
JP2024510606A5 JP2024510606A5 (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=)

Cited By (1)

* 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

Families Citing this family (49)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019195609A2 (en) 2018-04-04 2019-10-10 Arvinas Operations, Inc. Modulators of proteolysis and associated methods of use
WO2022068921A1 (zh) * 2020-09-30 2022-04-07 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
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
EP4363412A4 (en) * 2021-06-30 2025-05-14 Dana-Farber Cancer Institute, Inc. Small-molecule inhibitors of the KRAS G12D mutant
WO2023114733A1 (en) * 2021-12-13 2023-06-22 Quanta Therapeutics, Inc. Kras modulators and uses thereof
EP4371991A4 (en) * 2022-01-21 2025-02-26 Usynova Pharmaceuticals Ltd. Benzopyrimidine compounds and use thereof
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
CA3243798A1 (en) 2022-02-09 2023-08-17 Quanta Therapeutics, Inc. Kras Modulators and Their Uses
JP2025510572A (ja) 2022-03-08 2025-04-15 レボリューション メディシンズ インコーポレイテッド 免疫不応性肺癌を治療するための方法
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
WO2023230190A1 (en) 2022-05-25 2023-11-30 Quanta Therapeutics, Inc. Pyrimidine based modulators and uses thereof
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
JP2025534419A (ja) * 2022-09-30 2025-10-15 トラスヴェダ リミテッド Kras変異腫瘍に対する抗腫瘍活性を有する化合物
EP4631942A1 (en) 2022-10-21 2025-10-15 Leadingtac Pharmaceutical (Shaoxing) Co., Ltd. Pan-kras degrading agent, and preparation method therefor and use thereof
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
US12448399B2 (en) 2023-01-26 2025-10-21 Arvinas Operations, Inc. Cereblon-based KRAS degrading PROTACs and uses related thereto
WO2024186680A1 (en) * 2023-03-03 2024-09-12 Frontier Medicines Corporation Methods for preparing pyrrolizidine compounds
CN117903192A (zh) * 2023-03-12 2024-04-19 上海相辉医药科技有限公司 一种3-甲氧基异喹啉化合物中间体的制备方法
KR20260041941A (ko) 2023-03-15 2026-03-27 콴타 테라퓨틱스, 인크. Kras 조절 인자 및 이의 용도
AU2024241633A1 (en) 2023-03-30 2025-11-06 Revolution Medicines, Inc. Compositions for inducing ras gtp hydrolysis and uses thereof
CR20250420A (es) 2023-04-07 2025-11-20 Revolution Medicines Inc Inhibidores macrocíclicos de ras
AR132338A1 (es) 2023-04-07 2025-06-18 Revolution Medicines Inc Inhibidores de ras
WO2024215862A2 (en) * 2023-04-12 2024-10-17 Board Of Regents, The University Of Texas System Heterocyclic compounds as nras inhibitors
CN121100123A (zh) 2023-04-14 2025-12-09 锐新医药公司 Ras抑制剂的结晶形式
CN121464140A (zh) 2023-04-14 2026-02-03 锐新医药公司 Ras抑制剂的结晶形式、含有其的组合物及其使用方法
WO2024227091A1 (en) * 2023-04-26 2024-10-31 Ranok Therapeutics (Hangzhou) Co. Ltd. Diazabicyclooctane inhibitors of kras (g12d) and uses
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ras相關疾病或病症之組合療法
CN121100120A (zh) * 2023-05-07 2025-12-09 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
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
US20250109147A1 (en) 2023-09-08 2025-04-03 Gilead Sciences, Inc. Kras g12d modulating compounds
US20250114346A1 (en) 2023-10-09 2025-04-10 Incyte Corporation Combination therapy using a kras g12d inhibitor and pd-1 inhibitor or pd-l1 inhibitor
US20250114339A1 (en) 2023-10-09 2025-04-10 Incyte Corporation Combination therapy comprising a kras g12d inhibitor and an egfr inhibitor
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
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
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
TW202547461A (zh) 2024-05-17 2025-12-16 美商銳新醫藥公司 Ras抑制劑
WO2025255438A1 (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
WO2026015796A1 (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
WO2026015790A1 (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 (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017172979A1 (en) * 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
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
WO2021031952A1 (zh) * 2019-08-16 2021-02-25 劲方医药科技(上海)有限公司 氧代六元环并嘧啶类化合物,其制法与医药上的用途
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
JP2023531269A (ja) * 2020-06-30 2023-07-21 インベンティスバイオ カンパニー リミテッド キナゾリン化合物、その製造方法および用途
JP2024505594A (ja) * 2021-02-09 2024-02-06 メッドシャイン ディスカバリー インコーポレイテッド ピリミジン芳香環化合物
JP2024508755A (ja) * 2021-02-16 2024-02-28 セラス, インコーポレイテッド Krasを阻害するための組成物及び方法

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4475196A (en) 1981-03-06 1984-10-02 Zor Clair G Instrument for locating faults in aircraft passenger reading light and attendant call control system
US4447233A (en) 1981-04-10 1984-05-08 Parker-Hannifin Corporation Medication infusion pump
US4439196A (en) 1982-03-18 1984-03-27 Merck & Co., Inc. Osmotic drug delivery system
US4447224A (en) 1982-09-20 1984-05-08 Infusaid Corporation Variable flow implantable infusion apparatus
US4487603A (en) 1982-11-26 1984-12-11 Cordis Corporation Implantable microinfusion pump system
US4486194A (en) 1983-06-08 1984-12-04 James Ferrara Therapeutic device for administering medicaments through the skin
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
WO2022061251A1 (en) * 2020-09-18 2022-03-24 Plexxikon Inc. Compounds and methods for kras modulation and indications therefor

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017172979A1 (en) * 2016-03-30 2017-10-05 Araxes Pharma Llc Substituted quinazoline compounds and methods of use
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
WO2021031952A1 (zh) * 2019-08-16 2021-02-25 劲方医药科技(上海)有限公司 氧代六元环并嘧啶类化合物,其制法与医药上的用途
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
JP2023531269A (ja) * 2020-06-30 2023-07-21 インベンティスバイオ カンパニー リミテッド キナゾリン化合物、その製造方法および用途
JP2024505594A (ja) * 2021-02-09 2024-02-06 メッドシャイン ディスカバリー インコーポレイテッド ピリミジン芳香環化合物
JP2024508755A (ja) * 2021-02-16 2024-02-28 セラス, インコーポレイテッド Krasを阻害するための組成物及び方法

Cited By (1)

* 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

Also Published As

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

Similar Documents

Publication Publication Date Title
JP2024510606A (ja) Kras g12d阻害剤
JP7735594B2 (ja) アザ四環式オキサゼピン化合物及びその使用
EP4305037B1 (en) Kras inhibitors
KR102934231B1 (ko) 항암제로 유용한 융합 삼환식 화합물
WO2022216762A1 (en) Oxazepine compounds and uses thereof in the treatment of cancer
KR20250048078A (ko) Kras 억제제
CN105555780B (zh) Syk抑制剂
WO2025006967A1 (en) Kras inhibitors
TW202016109A (zh) 作為hpk1抑制劑的吡咯並[2,3-b]吡啶或吡咯並[2,3-b]吡嗪及其用途
JP2025519584A (ja) Kras阻害剤としてのピリド[4,3-d]ピリミジン誘導体
CN117242074A (zh) Kras g12d抑制剂
CN117177976A (zh) Kras抑制剂
EA050518B1 (ru) Ингибиторы kras g12d

Legal Events

Date Code Title Description
RD04 Notification of resignation of power of attorney

Free format text: JAPANESE INTERMEDIATE CODE: A7424

Effective date: 20241115

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250313

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20250313

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20251216

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20251218

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20260313

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20260327