CA3119988A1 - Erk inhibitors and uses thereof - Google Patents

Erk inhibitors and uses thereof Download PDF

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Publication number
CA3119988A1
CA3119988A1 CA3119988A CA3119988A CA3119988A1 CA 3119988 A1 CA3119988 A1 CA 3119988A1 CA 3119988 A CA3119988 A CA 3119988A CA 3119988 A CA3119988 A CA 3119988A CA 3119988 A1 CA3119988 A1 CA 3119988A1
Authority
CA
Canada
Prior art keywords
optionally substituted
compound
instance
halogen
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
Application number
CA3119988A
Other languages
English (en)
French (fr)
Inventor
Corey M. Reeves
Brendan M. O'boyle
Justin A. HILF
Dylan CONKLIN
Martina S. MCDERMOTT
Neil A. O'Brien
Michael J. Palazzolo
Dennis Slamon
Steven J. Wittenberger
Oliver C. LOSON
Michael D. Bartberger
Brian M. Stoltz
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
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 California Institute of Technology, University of California San Diego UCSD, 1200 Pharma LLC filed Critical California Institute of Technology
Publication of CA3119988A1 publication Critical patent/CA3119988A1/en
Pending legal-status Critical Current

Links

Classifications

    • 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
    • C07D471/04Ortho-condensed 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • CCHEMISTRY; METALLURGY
    • C12BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12NMICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10Transferases (2.)
    • C12N9/12Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
    • C12N9/1205Phosphotransferases with an alcohol group as acceptor (2.7.1), e.g. protein kinases

Landscapes

  • 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)
CA3119988A 2018-11-16 2019-11-15 Erk inhibitors and uses thereof Pending CA3119988A1 (en)

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
CA3119988A1 true CA3119988A1 (en) 2020-05-22

Family

ID=70730924

Family Applications (1)

Application Number Title Priority Date Filing Date
CA3119988A Pending CA3119988A1 (en) 2018-11-16 2019-11-15 Erk inhibitors and uses thereof

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

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR049333A1 (es) * 2004-04-02 2006-07-19 Vertex Pharma Azaindoles inhibidores de proteinquinasas rock y otras proteinas quinasas. composiciones farmaceuticas.
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
WO2016026078A1 (en) * 2014-08-19 2016-02-25 Changzhou Jiekai Pharmatech Co., Ltd. Heterocyclic compounds as erk inhibitors
EP3247353A4 (en) * 2015-01-23 2018-07-04 Confluence Life Sciences, Inc. Heterocyclic itk inhibitors for treating inflammation and cancer
EP3170822A1 (en) 2015-11-18 2017-05-24 AGV Discovery Azaindole derivatives and their use as erk kinase inhibitors
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

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
IL283106A (en) 2021-06-30
JP2022507514A (ja) 2022-01-18
CN113423707A (zh) 2021-09-21
US12428416B2 (en) 2025-09-30

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