CN115485277B - 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶 - Google Patents

作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶 Download PDF

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Publication number
CN115485277B
CN115485277B CN202180030549.3A CN202180030549A CN115485277B CN 115485277 B CN115485277 B CN 115485277B CN 202180030549 A CN202180030549 A CN 202180030549A CN 115485277 B CN115485277 B CN 115485277B
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compound
cancer
her2
present
pharmaceutically acceptable
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Chinese (zh)
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CN115485277A (zh
Inventor
B·威尔丁
D·博思
H·恩格尔哈特
J·福斯
R·纽穆勒
M·彼得罗茨基
D·沙恩
M·特鲁
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Boehringer Ingelheim International GmbH
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Boehringer Ingelheim International GmbH
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Priority to CN202410494942.3A priority Critical patent/CN118388493A/zh
Priority to CN202410508210.5A priority patent/CN118388494A/zh
Priority to CN202410475949.0A priority patent/CN118307544A/zh
Priority to CN202410479058.2A priority patent/CN118619956A/zh
Priority to CN202410490516.2A priority patent/CN118388491A/zh
Priority to CN202410490491.6A priority patent/CN118388490A/zh
Priority to CN202410475947.1A priority patent/CN118307543A/zh
Priority to CN202410481750.9A priority patent/CN118388488A/zh
Priority to CN202410508211.XA priority patent/CN118388495A/zh
Application filed by Boehringer Ingelheim International GmbH filed Critical Boehringer Ingelheim International GmbH
Priority to CN202410494941.9A priority patent/CN118388492A/zh
Priority to CN202410481753.2A priority patent/CN118388489A/zh
Priority to CN202410479057.8A priority patent/CN118388487A/zh
Publication of CN115485277A publication Critical patent/CN115485277A/zh
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Publication of CN115485277B publication Critical patent/CN115485277B/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Inorganic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN202180030549.3A 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶 Active CN115485277B (zh)

Priority Applications (12)

Application Number Priority Date Filing Date Title
CN202410475949.0A CN118307544A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410479058.2A CN118619956A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410490516.2A CN118388491A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410490491.6A CN118388490A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410475947.1A CN118307543A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410481750.9A CN118388488A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410494942.3A CN118388493A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410494941.9A CN118388492A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410508210.5A CN118388494A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410481753.2A CN118388489A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410479057.8A CN118388487A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410508211.XA CN118388495A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP20171221 2020-04-24
EP20171221.3 2020-04-24
PCT/EP2021/059015 WO2021213800A1 (en) 2020-04-24 2021-04-07 [1,3]DIAZINO[5,4-d]PYRIMIDINES AS HER2 INHIBITORS

Related Child Applications (12)

Application Number Title Priority Date Filing Date
CN202410490491.6A Division CN118388490A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410481753.2A Division CN118388489A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410475949.0A Division CN118307544A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410508210.5A Division CN118388494A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410479058.2A Division CN118619956A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410494942.3A Division CN118388493A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410508211.XA Division CN118388495A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410494941.9A Division CN118388492A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410479057.8A Division CN118388487A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410490516.2A Division CN118388491A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410475947.1A Division CN118307543A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410481750.9A Division CN118388488A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶

Publications (2)

Publication Number Publication Date
CN115485277A CN115485277A (zh) 2022-12-16
CN115485277B true CN115485277B (zh) 2024-05-14

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Family Applications (13)

Application Number Title Priority Date Filing Date
CN202410494942.3A Pending CN118388493A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410490516.2A Pending CN118388491A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410481750.9A Pending CN118388488A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410475947.1A Pending CN118307543A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410481753.2A Pending CN118388489A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410508210.5A Pending CN118388494A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410479057.8A Pending CN118388487A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410475949.0A Pending CN118307544A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410490491.6A Pending CN118388490A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410479058.2A Pending CN118619956A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410508211.XA Pending CN118388495A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202180030549.3A Active CN115485277B (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410494941.9A Pending CN118388492A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶

Family Applications Before (11)

Application Number Title Priority Date Filing Date
CN202410494942.3A Pending CN118388493A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410490516.2A Pending CN118388491A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410481750.9A Pending CN118388488A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410475947.1A Pending CN118307543A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410481753.2A Pending CN118388489A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410508210.5A Pending CN118388494A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410479057.8A Pending CN118388487A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410475949.0A Pending CN118307544A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410490491.6A Pending CN118388490A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410479058.2A Pending CN118619956A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶
CN202410508211.XA Pending CN118388495A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶

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CN202410494941.9A Pending CN118388492A (zh) 2020-04-24 2021-04-07 作为HER2抑制剂的[1,3]二嗪基[5,4-d]嘧啶

Country Status (32)

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US (3) US11608343B2 (enExample)
EP (2) EP4566611A3 (enExample)
JP (2) JP7260723B2 (enExample)
KR (2) KR20250016507A (enExample)
CN (13) CN118388493A (enExample)
AR (1) AR121779A1 (enExample)
AU (1) AU2021260721A1 (enExample)
BR (1) BR112022021514A2 (enExample)
CA (1) CA3173602A1 (enExample)
CL (1) CL2022002579A1 (enExample)
CO (1) CO2022015054A2 (enExample)
CR (1) CR20220537A (enExample)
DK (1) DK4139309T5 (enExample)
DO (1) DOP2022000189A (enExample)
EC (1) ECSP22072777A (enExample)
ES (1) ES3013860T3 (enExample)
FI (1) FI4139309T3 (enExample)
HR (1) HRP20250426T1 (enExample)
HU (1) HUE070805T2 (enExample)
IL (2) IL297490B2 (enExample)
LT (1) LT4139309T (enExample)
MA (1) MA59373B1 (enExample)
MX (1) MX2022013223A (enExample)
PE (1) PE20230827A1 (enExample)
PH (1) PH12022552745A1 (enExample)
PL (1) PL4139309T3 (enExample)
PT (1) PT4139309T (enExample)
RS (1) RS66557B1 (enExample)
SI (1) SI4139309T1 (enExample)
SM (1) SMT202500164T1 (enExample)
TW (1) TW202206432A (enExample)
WO (1) WO2021213800A1 (enExample)

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