KR20210130701A - Erk 저해제 및 이의 용도 - Google Patents

Erk 저해제 및 이의 용도 Download PDF

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Publication number
KR20210130701A
KR20210130701A KR1020217018334A KR20217018334A KR20210130701A KR 20210130701 A KR20210130701 A KR 20210130701A KR 1020217018334 A KR1020217018334 A KR 1020217018334A KR 20217018334 A KR20217018334 A KR 20217018334A KR 20210130701 A KR20210130701 A KR 20210130701A
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KR
South Korea
Prior art keywords
optionally substituted
compound
alkyl
halogen
pyridinyl
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.)
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KR1020217018334A
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English (en)
Korean (ko)
Inventor
코리 엠. 리브스
브렌던 엠. 오보일
저스틴 에이. 힐프
딜런 콘클린
마티나 에스. 맥더모트
닐 에이. 오브라이언
마이클 제이. 팔라졸로
데니스 슬라먼
스티븐 제이. 위튼버거
올리버 씨. 러썬
마이클 디. 바트버거
브라이언 엠. 스톨츠
Original Assignee
캘리포니아 인스티튜트 오브 테크놀로지
더 리전트 오브 더 유니버시티 오브 캘리포니아
1200 파마 엘엘씨
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Application filed by 캘리포니아 인스티튜트 오브 테크놀로지, 더 리전트 오브 더 유니버시티 오브 캘리포니아, 1200 파마 엘엘씨 filed Critical 캘리포니아 인스티튜트 오브 테크놀로지
Publication of KR20210130701A publication Critical patent/KR20210130701A/ko
Withdrawn legal-status Critical Current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)
KR1020217018334A 2018-11-16 2019-11-15 Erk 저해제 및 이의 용도 Withdrawn KR20210130701A (ko)

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
KR20210130701A true KR20210130701A (ko) 2021-11-01

Family

ID=70730924

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020217018334A Withdrawn KR20210130701A (ko) 2018-11-16 2019-11-15 Erk 저해제 및 이의 용도

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

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Publication number Publication date
SG11202104404XA (en) 2021-05-28
BR112021009430A2 (pt) 2021-08-17
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
CN113423707A (zh) 2021-09-21
US12428416B2 (en) 2025-09-30

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