JP7546550B2 - 抗腫瘍剤としてのキナゾリン誘導体 - Google Patents

抗腫瘍剤としてのキナゾリン誘導体 Download PDF

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JP7546550B2
JP7546550B2 JP2021514381A JP2021514381A JP7546550B2 JP 7546550 B2 JP7546550 B2 JP 7546550B2 JP 2021514381 A JP2021514381 A JP 2021514381A JP 2021514381 A JP2021514381 A JP 2021514381A JP 7546550 B2 JP7546550 B2 JP 7546550B2
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triazolo
pyrimidin
yloxy
methylphenyl
amine
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JP2022501338A5 (https=
JP2022501338A (ja
JPWO2020057511A5 (https=
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ディン、ゾウ
チーチャン、チェン
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エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト
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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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • 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
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10—Spiro-condensed systems
    • 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)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Microbiology (AREA)
  • Mycology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2021514381A 2018-09-18 2019-09-17 抗腫瘍剤としてのキナゾリン誘導体 Active JP7546550B2 (ja)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2024120830A JP2024164018A (ja) 2018-09-18 2024-07-26 抗腫瘍剤としてのキナゾリン誘導体
JP2025150799A JP2026009898A (ja) 2018-09-18 2025-09-11 抗腫瘍剤としてのキナゾリン誘導体

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CNPCT/CN2018/106098 2018-09-18
CN2018106098 2018-09-18
CNPCT/CN2019/091078 2019-06-13
CN2019091078 2019-06-13
PCT/CN2019/106233 WO2020057511A1 (en) 2018-09-18 2019-09-17 Quinazoline derivatives as antitumor agents

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JP2022501338A JP2022501338A (ja) 2022-01-06
JP2022501338A5 JP2022501338A5 (https=) 2022-09-28
JPWO2020057511A5 JPWO2020057511A5 (https=) 2022-09-28
JP7546550B2 true JP7546550B2 (ja) 2024-09-06

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JP2021514381A Active JP7546550B2 (ja) 2018-09-18 2019-09-17 抗腫瘍剤としてのキナゾリン誘導体
JP2024120830A Withdrawn JP2024164018A (ja) 2018-09-18 2024-07-26 抗腫瘍剤としてのキナゾリン誘導体
JP2025150799A Pending JP2026009898A (ja) 2018-09-18 2025-09-11 抗腫瘍剤としてのキナゾリン誘導体

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JP2025150799A Pending JP2026009898A (ja) 2018-09-18 2025-09-11 抗腫瘍剤としてのキナゾリン誘導体

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US (2) US11723908B2 (https=)
EP (3) EP3853220B1 (https=)
JP (3) JP7546550B2 (https=)
KR (2) KR20250171398A (https=)
CN (2) CN118255772A (https=)
AU (2) AU2019341273B2 (https=)
CA (1) CA3099776A1 (https=)
DK (2) DK4360713T3 (https=)
ES (2) ES2971927T3 (https=)
FI (2) FI4360713T3 (https=)
HR (2) HRP20241743T1 (https=)
HU (2) HUE069764T2 (https=)
LT (2) LT3853220T (https=)
PL (2) PL3853220T3 (https=)
PT (2) PT3853220T (https=)
RS (2) RS65413B1 (https=)
SI (2) SI3853220T1 (https=)
SM (1) SMT202400524T1 (https=)
WO (1) WO2020057511A1 (https=)

Cited By (1)

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JP2024164018A (ja) * 2018-09-18 2024-11-26 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト 抗腫瘍剤としてのキナゾリン誘導体

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CN111377850B (zh) * 2018-12-31 2022-10-18 艾琪康医药科技（上海）有限公司 一种手性n-取代-3,3-二氟-4-羟基哌啶衍生物及其制备方法
CN113527215B (zh) * 2020-04-17 2023-12-05 北京赛特明强医药科技有限公司 一种喹唑啉类化合物、制备方法及其应用
WO2021209039A1 (zh) * 2020-04-17 2021-10-21 北京赛特明强医药科技有限公司 一种喹唑啉类化合物、制备方法及其应用
TW202214641A (zh) 2020-06-30 2022-04-16 美商艾瑞生藥股份有限公司 Ｈｅｒ２突變抑制劑
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US20240299387A1 (en) * 2021-06-22 2024-09-12 Blueprint Medicines Corporation Heterocyclic egfr inhibitors for use in the treatment of cancer
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CN121135654A (zh) * 2021-09-30 2025-12-16 北京赛特明强医药科技有限公司 一种喹唑啉类化合物、组合物及其应用
CN115894455B (zh) * 2021-09-30 2024-04-19 北京赛特明强医药科技有限公司 一种喹唑啉类化合物、组合物及其应用
JP2024539212A (ja) * 2021-10-20 2024-10-28 エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト キナゾリン誘導体の結晶形態、調製、組成物およびその使用
CN116478129B (zh) * 2022-01-21 2025-01-07 深圳默元生物科技有限公司 喹啉化合物及其用途
KR20250009417A (ko) * 2022-03-14 2025-01-17 후야바이오 인터내셔널, 엘엘씨 혈액-뇌 장벽 교차 mll1-wdr5 단백질-단백질 상호작용 저해제 화합물 및 이의 용도
JP2025509995A (ja) 2022-03-28 2025-04-11 江蘇恒瑞医薬股▲ふん▼有限公司 含窒素複素環系化合物、その調製方法及びその医薬的使用
CN115650977A (zh) * 2022-10-09 2023-01-31 广东润兴生物科技有限公司 一种妥卡替尼的合成方法
TW202446386A (zh) * 2023-04-14 2024-12-01 大陸商迪哲（江蘇）醫藥股份有限公司 喹唑啉ＥｒｂＢ抑制劑的藥物形式
WO2024249642A1 (en) * 2023-06-02 2024-12-05 Acerand Therapeutics (Hong Kong) Limited Egfr inhibitors
WO2025067396A1 (zh) * 2023-09-27 2025-04-03 江苏恒瑞医药股份有限公司 一种喹唑啉衍生物的可药用盐、其结晶形式及用途
WO2025195333A1 (en) 2024-03-19 2025-09-25 F. Hoffmann-La Roche Ag Pharmaceutical formulation of erbb2 inhibitors

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