TWI899184B - 治療或抑制急性骨髓性白血病復發之化合物 - Google Patents

治療或抑制急性骨髓性白血病復發之化合物

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Publication number
TWI899184B
TWI899184B TW110109254A TW110109254A TWI899184B TW I899184 B TWI899184 B TW I899184B TW 110109254 A TW110109254 A TW 110109254A TW 110109254 A TW110109254 A TW 110109254A TW I899184 B TWI899184 B TW I899184B
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TW
Taiwan
Prior art keywords
mmol
pyrrolo
pyrimidin
amino
phenoxyphenyl
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TW110109254A
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English (en)
Chinese (zh)
Other versions
TW202200583A (zh
Inventor
涵誠 吳
志雄 葉
丁克家
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國立研究開發法人理化學研究所
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Publication of TW202200583A publication Critical patent/TW202200583A/zh
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Publication of TWI899184B publication Critical patent/TWI899184B/zh

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    • 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines 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
    • A61K31/63Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • 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
    • C07D487/04Ortho-condensed systems
    • 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
    • C07D487/10Spiro-condensed 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
TW110109254A 2020-03-16 2021-03-16 治療或抑制急性骨髓性白血病復發之化合物 TWI899184B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
WOPCT/CN2020/079464 2020-03-16
PCT/CN2020/079464 WO2021184154A1 (en) 2020-03-16 2020-03-16 Compounds for treating or inhibiting recurrence of acute myeloid leukemia

Publications (2)

Publication Number Publication Date
TW202200583A TW202200583A (zh) 2022-01-01
TWI899184B true TWI899184B (zh) 2025-10-01

Family

ID=77767943

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TW110109254A TWI899184B (zh) 2020-03-16 2021-03-16 治療或抑制急性骨髓性白血病復發之化合物

Country Status (15)

Country Link
US (1) US11963960B2 (enExample)
EP (1) EP4121430A4 (enExample)
JP (1) JP7744358B2 (enExample)
KR (1) KR20220154164A (enExample)
CN (1) CN115298180B (enExample)
AR (1) AR121570A1 (enExample)
AU (2) AU2020436612A1 (enExample)
BR (1) BR112022018345A2 (enExample)
CA (1) CA3168988A1 (enExample)
IL (1) IL296296A (enExample)
MX (1) MX2022011407A (enExample)
PE (1) PE20230461A1 (enExample)
PH (1) PH12022552169A1 (enExample)
TW (1) TWI899184B (enExample)
WO (2) WO2021184154A1 (enExample)

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* Cited by examiner, † Cited by third party
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AU2020436612A1 (en) 2020-03-16 2022-09-01 Flash Therapeutics, Llc Compounds for treating or inhibiting recurrence of acute myeloid leukemia
RS65962B1 (sr) 2020-05-08 2024-10-31 Halia Therapeutics Inc Inhibitori nek7 kinaze
EP4161933A1 (en) * 2020-06-08 2023-04-12 Halia Therapeutics, Inc. Inhibitors of nek7 kinase
CN114075190A (zh) * 2020-08-20 2022-02-22 北京诺诚健华医药科技有限公司 杂环类btk抑制剂
CN113861179A (zh) * 2021-10-22 2021-12-31 上海应用技术大学 一种新型flt3激酶抑制剂及其合成与应用
WO2025124429A1 (zh) * 2023-12-11 2025-06-19 北京康辰药业股份有限公司 芳香胺化合物及其药物组合物、应用
CN121039131A (zh) * 2024-01-11 2025-11-28 佩勒梅德有限公司 新型吡咯并三嗪衍生物及其用途
KR20250157634A (ko) 2024-04-29 2025-11-05 대한민국(질병관리청 국립보건연구원장) Bax 활성제를 유효성분으로 포함하는 항-hiv-1 조성물

Citations (7)

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WO1998041525A1 (en) * 1997-03-19 1998-09-24 Basf Aktiengesellschaft Pyrrolo[2,3d]pyrimidines and their use as tyrosine kinase inhibitors
WO2002080926A1 (en) * 2001-03-22 2002-10-17 Abbott Gmbh & Co. Kg Pyrazolopyrimidines as therapeutic agents
US20030153752A1 (en) * 1998-09-18 2003-08-14 Hirst Gavin C. Pyrrolopyrimidines as therapeutic agents
WO2008121742A2 (en) * 2007-03-28 2008-10-09 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
WO2014017659A1 (ja) * 2012-07-27 2014-01-30 独立行政法人理化学研究所 急性骨髄性白血病の治療又は再発抑制剤
CN105481862A (zh) * 2015-01-21 2016-04-13 中国科学院合肥物质科学研究院 Flt3激酶的新型抑制剂及其用途
WO2018052120A1 (en) * 2016-09-15 2018-03-22 Riken A hck inhibitor and a bcl-2 inhibitor for treating acute myeloid leukemia

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ID29028A (id) * 1998-09-18 2001-07-26 Basf Ag Pirolopirimidina sebagai penghambat protein kinase
JP2003509428A (ja) * 1999-09-17 2003-03-11 アボツト・ゲー・エム・ベー・ハー・ウント・コンパニー・カーゲー 治療薬としてのピラゾロピリミジン
MXPA03008560A (es) * 2001-03-22 2004-06-30 Abbot Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos.
JP2007520559A (ja) * 2004-02-03 2007-07-26 アボット・ラボラトリーズ 治療薬としてのアミノベンゾオキサゾール類
WO2007064931A2 (en) * 2005-12-02 2007-06-07 Bayer Healthcare Llc Substituted 4-amino-pyrrolotriazine derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
ES2545907T3 (es) * 2005-12-29 2015-09-16 Abbvie Inc. Inhibidores de proteína quinasa
ES2396613T3 (es) * 2008-05-19 2013-02-22 OSI Pharmaceuticals, LLC Imidazopirazinas e imidazotriazinas sustituidas
USRE48175E1 (en) * 2012-10-19 2020-08-25 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
CN105017256A (zh) * 2014-04-29 2015-11-04 浙江导明医药科技有限公司 多氟化合物作为布鲁顿酪氨酸激酶抑制剂
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WO1998041525A1 (en) * 1997-03-19 1998-09-24 Basf Aktiengesellschaft Pyrrolo[2,3d]pyrimidines and their use as tyrosine kinase inhibitors
US20030153752A1 (en) * 1998-09-18 2003-08-14 Hirst Gavin C. Pyrrolopyrimidines as therapeutic agents
WO2002080926A1 (en) * 2001-03-22 2002-10-17 Abbott Gmbh & Co. Kg Pyrazolopyrimidines as therapeutic agents
WO2008121742A2 (en) * 2007-03-28 2008-10-09 Pharmacyclics, Inc. Inhibitors of bruton's tyrosine kinase
WO2014017659A1 (ja) * 2012-07-27 2014-01-30 独立行政法人理化学研究所 急性骨髄性白血病の治療又は再発抑制剤
CN105481862A (zh) * 2015-01-21 2016-04-13 中国科学院合肥物质科学研究院 Flt3激酶的新型抑制剂及其用途
WO2018052120A1 (en) * 2016-09-15 2018-03-22 Riken A hck inhibitor and a bcl-2 inhibitor for treating acute myeloid leukemia

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期刊 Koda Y, et al. "Identification of pyrrolo [2,3-d]pyrimidines as potent HCK and FLT3-ITD dual inhibitors" Bioorganic & medicinal chemistry letters 27(22): Elsevier 2017; 4994-4998;期刊 Yuki H, et al. "Activity cliff for 7-substituted pyrrolo-pyrimidine inhibitors of HCK explained in terms of predicted basicity of the amine nitrogen" Bioorganic & medicinal chemistry 25(16): Elsevier 2017; 4259-4264 *
期刊 Yuki H, et al. "Activity cliff for 7-substituted pyrrolo-pyrimidine inhibitors of HCK explained in terms of predicted basicity of the amine nitrogen" Bioorganic & medicinal chemistry 25(16): Elsevier 2017; 4259-4264

Also Published As

Publication number Publication date
KR20220154164A (ko) 2022-11-21
EP4121430A1 (en) 2023-01-25
AR121570A1 (es) 2022-06-15
WO2021184154A1 (en) 2021-09-23
JP2023518035A (ja) 2023-04-27
CA3168988A1 (en) 2021-09-23
PE20230461A1 (es) 2023-03-14
IL296296A (en) 2022-11-01
AU2021239828B2 (en) 2025-06-26
AU2021239828A1 (en) 2025-04-03
BR112022018345A2 (pt) 2022-11-08
WO2021188417A1 (en) 2021-09-23
US11963960B2 (en) 2024-04-23
CN115298180B (zh) 2025-06-10
US20210299128A1 (en) 2021-09-30
JP7744358B2 (ja) 2025-09-25
PH12022552169A1 (en) 2024-01-29
AU2020436612A1 (en) 2022-09-01
TW202200583A (zh) 2022-01-01
EP4121430A4 (en) 2024-04-17
CN115298180A (zh) 2022-11-04
MX2022011407A (es) 2022-10-13

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