CN113423707A - Erk抑制剂及其用途 - Google Patents

Erk抑制剂及其用途 Download PDF

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Publication number
CN113423707A
CN113423707A CN201980085273.1A CN201980085273A CN113423707A CN 113423707 A CN113423707 A CN 113423707A CN 201980085273 A CN201980085273 A CN 201980085273A CN 113423707 A CN113423707 A CN 113423707A
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CN
China
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optionally substituted
compound
alkyl
heterocyclyl
aryl
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Pending
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CN201980085273.1A
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English (en)
Chinese (zh)
Inventor
C·M·里夫斯
B·M·奥博伊尔
J·A·希尔夫
D·康克林
M·S·麦克德莫特
N·A·奥布莱恩
M·J·帕拉佐罗
D·斯拉蒙
S·J·维滕贝格
O·C·洛森
M·D·巴特伯格
B·M·斯托尔茨
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.)
California Institute of Technology
University of California San Diego UCSD
1200 Pharma LLC
Original Assignee
California Institute of Technology
University of California San Diego UCSD
1200 Pharma LLC
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Filing date
Publication date
Application filed by California Institute of Technology, University of California San Diego UCSD, 1200 Pharma LLC filed Critical California Institute of Technology
Publication of CN113423707A publication Critical patent/CN113423707A/zh
Pending legal-status Critical Current

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    • 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
    • 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
    • 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
    • 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)
CN201980085273.1A 2018-11-16 2019-11-15 Erk抑制剂及其用途 Pending CN113423707A (zh)

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 (1)

Publication Number Publication Date
CN113423707A true CN113423707A (zh) 2021-09-21

Family

ID=70730924

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201980085273.1A Pending CN113423707A (zh) 2018-11-16 2019-11-15 Erk抑制剂及其用途

Country Status (12)

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

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 (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005103050A2 (en) * 2004-04-02 2005-11-03 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of rock and other protein kinases
CN101228160A (zh) * 2004-06-30 2008-07-23 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吖吲哚
WO2010000364A1 (de) * 2008-07-03 2010-01-07 Merck Patent Gmbh Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate
WO2010011756A1 (en) * 2008-07-23 2010-01-28 Vertex Pharmaceuticals Incorporated Pyrazolopyridine kinase inhibitors
WO2011035855A1 (de) * 2009-09-28 2011-03-31 Merck Patent Gmbh Pyridinyl-imidazolonderivate zur hemmung von pi3-kinasen
WO2011076316A1 (de) * 2009-12-23 2011-06-30 Merck Patent Gmbh Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate
WO2012094313A1 (en) * 2011-01-04 2012-07-12 Kinentia Biosciences Llc Pyrazole derivatives as erk inhibitors
WO2013052355A1 (en) * 2011-10-03 2013-04-11 Merck Sharp & Dohme Corp. Azaindoles as janus kinase inhibitors
WO2014060395A1 (en) * 2012-10-16 2014-04-24 F. Hoffmann-La Roche Ag Serine/threonine kinase inhibitors
WO2015051341A1 (en) * 2013-10-03 2015-04-09 Araxes Pharma Llc Inhibitors of erk and methods of use
WO2016026078A1 (en) * 2014-08-19 2016-02-25 Changzhou Jiekai Pharmatech Co., Ltd. Heterocyclic compounds as erk inhibitors
WO2016118951A2 (en) * 2015-01-23 2016-07-28 Confluence Life Sciences, Inc. Heterocyclic itk inhibitors for treating inflammation and cancer
WO2017085230A1 (en) * 2015-11-18 2017-05-26 Agv Discovery Azaindole derivatives and their use as erk kinase inhibitors
CN107973783A (zh) * 2016-10-21 2018-05-01 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

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA95244C2 (ru) * 2005-06-22 2011-07-25 Плексикон, Инк. Соединения и способ модулирования активности киназ, и показания для их применения
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
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 (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005103050A2 (en) * 2004-04-02 2005-11-03 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of rock and other protein kinases
CN101228160A (zh) * 2004-06-30 2008-07-23 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的吖吲哚
WO2010000364A1 (de) * 2008-07-03 2010-01-07 Merck Patent Gmbh Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate
WO2010011756A1 (en) * 2008-07-23 2010-01-28 Vertex Pharmaceuticals Incorporated Pyrazolopyridine kinase inhibitors
WO2011035855A1 (de) * 2009-09-28 2011-03-31 Merck Patent Gmbh Pyridinyl-imidazolonderivate zur hemmung von pi3-kinasen
WO2011076316A1 (de) * 2009-12-23 2011-06-30 Merck Patent Gmbh Pyrrolopyridinyl-pyrimidin-2-yl-amin-derivate
WO2012094313A1 (en) * 2011-01-04 2012-07-12 Kinentia Biosciences Llc Pyrazole derivatives as erk inhibitors
WO2013052355A1 (en) * 2011-10-03 2013-04-11 Merck Sharp & Dohme Corp. Azaindoles as janus kinase inhibitors
WO2014060395A1 (en) * 2012-10-16 2014-04-24 F. Hoffmann-La Roche Ag Serine/threonine kinase inhibitors
WO2015051341A1 (en) * 2013-10-03 2015-04-09 Araxes Pharma Llc Inhibitors of erk and methods of use
WO2016026078A1 (en) * 2014-08-19 2016-02-25 Changzhou Jiekai Pharmatech Co., Ltd. Heterocyclic compounds as erk inhibitors
WO2016118951A2 (en) * 2015-01-23 2016-07-28 Confluence Life Sciences, Inc. Heterocyclic itk inhibitors for treating inflammation and cancer
WO2017085230A1 (en) * 2015-11-18 2017-05-26 Agv Discovery Azaindole derivatives and their use as erk kinase inhibitors
CN107973783A (zh) * 2016-10-21 2018-05-01 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

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
JP2022507514A (ja) 2022-01-18
US12428416B2 (en) 2025-09-30

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Application publication date: 20210921