JP2022507514A - Ｅｒｋインヒビター及びその使用 - Google Patents

Ｅｒｋインヒビター及びその使用 Download PDF

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Publication number
JP2022507514A
JP2022507514A JP2021526509A JP2021526509A JP2022507514A JP 2022507514 A JP2022507514 A JP 2022507514A JP 2021526509 A JP2021526509 A JP 2021526509A JP 2021526509 A JP2021526509 A JP 2021526509A JP 2022507514 A JP2022507514 A JP 2022507514A
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JP
Japan
Prior art keywords
optionally substituted
alkyl
compound
independently
heterocyclyl
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
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JP2021526509A
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English (en)
Japanese (ja)
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JP2022507514A5 (enExample
Inventor
リーブス，コリー，エム．
オーボイル，ブレンダン，エム．
ヒルフ，ジャスティン，エー．
コンクリン，ディラン
マクダーモット，マルティナ，エス．
オーブライアン，ニール，エー．
パラッツォロ，マイケル，ジェイ．
スレイモン，デニス
ウィッテンバーガー，スティーブン，ジェイ．
ローソン，オリバー，シー．
バートバーガー，マイケル，ディー．
ストルツ，ブライアン，エム．
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.)
University of California San Diego UCSD
Original Assignee
University of California San Diego UCSD
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 University of California San Diego UCSD filed Critical University of California San Diego UCSD
Publication of JP2022507514A publication Critical patent/JP2022507514A/ja
Publication of JP2022507514A5 publication Critical patent/JP2022507514A5/ja
Pending legal-status Critical Current

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    • 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
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further 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
    • A61K31/535—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
    • 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
    • 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
    • C07D471/02—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 system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C12N9/1205—Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Biomedical Technology (AREA)
  • General Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2021526509A 2018-11-16 2019-11-15 Ｅｒｋインヒビター及びその使用 Pending JP2022507514A (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201862768565P 2018-11-16 2018-11-16
US62/768,565 2018-11-16
US201962908965P 2019-10-01 2019-10-01
US62/908,965 2019-10-01
PCT/US2019/061750 WO2020102686A1 (en) 2018-11-16 2019-11-15 Erk inhibitors and uses thereof

Publications (2)

Publication Number Publication Date
JP2022507514A true JP2022507514A (ja) 2022-01-18
JP2022507514A5 JP2022507514A5 (enExample) 2022-12-09

Family

ID=70730924

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2021526509A Pending JP2022507514A (ja) 2018-11-16 2019-11-15 Ｅｒｋインヒビター及びその使用

Country Status (12)

Country Link
US (1) US12428416B2 (enExample)
EP (1) EP3880677A4 (enExample)
JP (1) JP2022507514A (enExample)
KR (1) KR20210130701A (enExample)
CN (1) CN113423707A (enExample)
AU (1) AU2019381808A1 (enExample)
BR (1) BR112021009430A2 (enExample)
CA (1) CA3119988A1 (enExample)
IL (1) IL283106A (enExample)
MX (1) MX2021005171A (enExample)
SG (1) SG11202104404XA (enExample)
WO (1) WO2020102686A1 (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4212531A1 (en) * 2022-01-14 2023-07-19 AGV Discovery Azaindole derivatives and their use as erk kinase inhibitors
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
US20250049810A1 (en) 2023-08-07 2025-02-13 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
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
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
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
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
JP2007531740A (ja) * 2004-04-02 2007-11-08 バーテックス　ファーマシューティカルズ　インコーポレイテッド Ｒｏｃｋの阻害剤として有用なアザインドールおよび他のプロテインキナーゼ
WO2016026078A1 (en) * 2014-08-19 2016-02-25 Changzhou Jiekai Pharmatech Co., Ltd. Heterocyclic compounds as erk inhibitors
WO2017085230A1 (en) * 2015-11-18 2017-05-26 Agv Discovery Azaindole derivatives and their use as erk kinase inhibitors

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA200700751B (en) 2004-06-30 2008-08-27 Vertex Pharma Azalndoles useful as inhibitors of protein kinases
UA95244C2 (ru) * 2005-06-22 2011-07-25 Плексикон, Инк. Соединения и способ модулирования активности киназ, и показания для их применения
DE102008031517A1 (de) * 2008-07-03 2010-01-07 Merck Patent Gmbh Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate
ES2402087T3 (es) * 2008-07-23 2013-04-26 Vertex Pharmaceuticals Incorporated Inhibidores de la pirazolopiridina quinasa
DE102009043260A1 (de) 2009-09-28 2011-04-28 Merck Patent Gmbh Pyridinyl-imidazolonderivate
DE102009060174A1 (de) * 2009-12-23 2011-06-30 Merck Patent GmbH, 64293 Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate
WO2012094313A1 (en) 2011-01-04 2012-07-12 Kinentia Biosciences Llc Pyrazole derivatives as erk inhibitors
US9096598B2 (en) 2011-10-03 2015-08-04 Merck Sharp & Dohme Corp. Azaindoles as Janus kinase inhibitors
MX2015004615A (es) * 2012-10-16 2015-07-17 Hoffmann La Roche Inhibidores de serina/treonina cinasa.
WO2014109414A1 (ja) 2013-01-11 2014-07-17 富士フイルム株式会社 含窒素複素環化合物またはその塩
SG11201602572YA (en) * 2013-10-03 2016-04-28 Kura Oncology Inc Inhibitors of erk and methods of use
EP3247353A4 (en) * 2015-01-23 2018-07-04 Confluence Life Sciences, Inc. Heterocyclic itk inhibitors for treating inflammation and cancer
CN107973783B (zh) * 2016-10-21 2024-09-06 正大天晴药业集团股份有限公司 作为erk抑制剂的苯胺嘧啶衍生物
CN108948002A (zh) 2017-05-19 2018-12-07 厦门大学 五元并六元氮杂芳环类化合物、其制备方法、药用组合物及其应用

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007531740A (ja) * 2004-04-02 2007-11-08 バーテックス　ファーマシューティカルズ　インコーポレイテッド Ｒｏｃｋの阻害剤として有用なアザインドールおよび他のプロテインキナーゼ
WO2016026078A1 (en) * 2014-08-19 2016-02-25 Changzhou Jiekai Pharmatech Co., Ltd. Heterocyclic compounds as erk inhibitors
WO2017085230A1 (en) * 2015-11-18 2017-05-26 Agv Discovery Azaindole derivatives and their use as erk kinase inhibitors

Also Published As

Publication number Publication date
SG11202104404XA (en) 2021-05-28
BR112021009430A2 (pt) 2021-08-17
KR20210130701A (ko) 2021-11-01
WO2020102686A1 (en) 2020-05-22
US20220002294A1 (en) 2022-01-06
MX2021005171A (es) 2021-10-01
AU2019381808A1 (en) 2021-05-27
EP3880677A1 (en) 2021-09-22
EP3880677A4 (en) 2022-06-22
CA3119988A1 (en) 2020-05-22
IL283106A (en) 2021-06-30
CN113423707A (zh) 2021-09-21
US12428416B2 (en) 2025-09-30

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