CN116249534B - 嘧啶化合物的结晶 - Google Patents

嘧啶化合物的结晶 Download PDF

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Publication number
CN116249534B
CN116249534B CN202180061122.XA CN202180061122A CN116249534B CN 116249534 B CN116249534 B CN 116249534B CN 202180061122 A CN202180061122 A CN 202180061122A CN 116249534 B CN116249534 B CN 116249534B
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compound
crystals
crystal
fumaric acid
equivalent
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CN116249534A (zh
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中村浩之
山中博义
浅井隆宏
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Taiho Pharmaceutical Co Ltd
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Taiho Pharmaceutical Co Ltd
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    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/15—Fumaric acid
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/70596—Molecules with a "CD"-designation not provided for elsewhere
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • C07K14/705—Receptors; Cell surface antigens; Cell surface determinants
    • C07K14/71—Receptors; Cell surface antigens; Cell surface determinants for growth factors; for growth regulators
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • C07K14/82—Translation products from oncogenes
    • 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)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
    • C12Y207/10—Protein-tyrosine kinases (2.7.10)
    • C12Y207/10001—Receptor protein-tyrosine kinase (2.7.10.1)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Genetics & Genomics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Zoology (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Wood Science & Technology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Toxicology (AREA)
  • Cell Biology (AREA)
  • General Engineering & Computer Science (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Biomedical Technology (AREA)
  • Biotechnology (AREA)
  • Microbiology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Liquid Crystal Substances (AREA)
CN202180061122.XA 2020-07-15 2021-07-14 嘧啶化合物的结晶 Active CN116249534B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2020-121520 2020-07-15
JP2020121520 2020-07-15
PCT/JP2021/026460 WO2022014638A1 (ja) 2020-07-15 2021-07-14 ピリミジン化合物の結晶

Publications (2)

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CN116249534A CN116249534A (zh) 2023-06-09
CN116249534B true CN116249534B (zh) 2025-03-25

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US (1) US12492208B2 (https=)
EP (1) EP4183788A4 (https=)
JP (1) JP7391226B2 (https=)
KR (1) KR102914926B1 (https=)
CN (1) CN116249534B (https=)
AU (1) AU2021307245B2 (https=)
BR (1) BR112023000765A2 (https=)
MX (1) MX2023000692A (https=)
MY (1) MY207540A (https=)
PH (1) PH12023550116A1 (https=)
TW (1) TWI905228B (https=)
WO (1) WO2022014638A1 (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP4351737A4 (en) * 2021-05-24 2025-05-14 Taiho Pharmaceutical Co., Ltd. Treatment methods for subjects with cancer having an aberration in egfr and/or her2

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113271950A (zh) * 2019-01-11 2021-08-17 大鹏药品工业株式会社 嘧啶化合物或其盐

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8426428B2 (en) * 2008-12-05 2013-04-23 Principia Biopharma, Inc. EGFR kinase knockdown via electrophilically enhanced inhibitors
TW201336847A (zh) * 2012-02-07 2013-09-16 Taiho Pharmaceutical Co Ltd 喹啉基吡咯并嘧啶化合物或其鹽
KR101852738B1 (ko) * 2015-01-30 2018-04-27 다이호야쿠힌고교 가부시키가이샤 축합 피리미딘 화합물의 신규한 염 및 그 결정
JP6537601B2 (ja) * 2015-05-12 2019-07-03 大鵬薬品工業株式会社 アザ二環式化合物の結晶
BR112018004175B8 (pt) * 2015-09-01 2023-10-31 Taiho Pharmaceutical Co Ltd Composto pirazolo[3,4-d]pirimidina, composição farmacêutica e usos terapêuticos do dito composto
KR102674711B1 (ko) * 2017-02-28 2024-06-12 다이호야쿠힌고교 가부시키가이샤 피라졸로[3,4-d]피리미딘 화합물을 사용한 항종양 효과 증강제
WO2020004546A1 (ja) 2018-06-28 2020-01-02 日本電気株式会社 遠隔制御装置、遠隔制御方法及びプログラム
MA53509A (fr) 2018-08-29 2021-07-07 Taiho Pharmaceutical Co Ltd Agent thérapeutique contenant un composé pyrazolo[3,4-d]pyrimidine comme ingrédient actif
JP7164455B2 (ja) 2019-01-31 2022-11-01 理想科学工業株式会社 容器
EP4183395A4 (en) 2020-07-15 2024-07-24 Taiho Pharmaceutical Co., Ltd. PYRIMIDINE COMPOUND-CONTAINING COMBINATION FOR USE IN TUMOR TREATMENT
MX2023000693A (es) 2020-07-15 2023-02-13 Taiho Pharmaceutical Co Ltd Inhibidor de egfr.

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113271950A (zh) * 2019-01-11 2021-08-17 大鹏药品工业株式会社 嘧啶化合物或其盐

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Publication number Publication date
TWI905228B (zh) 2025-11-21
JP7391226B2 (ja) 2023-12-04
JPWO2022014638A1 (https=) 2022-01-20
US20230331730A1 (en) 2023-10-19
KR20230034341A (ko) 2023-03-09
MX2023000692A (es) 2023-02-13
CA3189457A1 (en) 2022-01-20
US12492208B2 (en) 2025-12-09
PH12023550116A1 (en) 2024-06-24
WO2022014638A1 (ja) 2022-01-20
BR112023000765A2 (pt) 2023-02-07
CN116249534A (zh) 2023-06-09
EP4183788A1 (en) 2023-05-24
MY207540A (en) 2025-03-04
TW202216717A (zh) 2022-05-01
EP4183788A4 (en) 2024-07-17
KR102914926B1 (ko) 2026-01-19
AU2021307245B2 (en) 2024-02-29
AU2021307245A1 (en) 2023-03-02

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