AU2019341273B2 - Quinazoline derivatives as antitumor agents - Google Patents

Quinazoline derivatives as antitumor agents Download PDF

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Publication number
AU2019341273B2
AU2019341273B2 AU2019341273A AU2019341273A AU2019341273B2 AU 2019341273 B2 AU2019341273 B2 AU 2019341273B2 AU 2019341273 A AU2019341273 A AU 2019341273A AU 2019341273 A AU2019341273 A AU 2019341273A AU 2019341273 B2 AU2019341273 B2 AU 2019341273B2
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Prior art keywords
triazolo
pyrimidin
yloxy
methylphenyl
amine
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AU2019341273A
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AU2019341273A1 (en
Inventor
Ziqiang CHENG
Ding Zhou
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Priority to AU2024204847A priority Critical patent/AU2024204847A1/en
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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)
AU2019341273A 2018-09-18 2019-09-17 Quinazoline derivatives as antitumor agents Active AU2019341273B2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2024204847A AU2024204847A1 (en) 2018-09-18 2024-07-15 Quinazoline Derivatives as Antitumor Agents

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

Related Child Applications (1)

Application Number Title Priority Date Filing Date
AU2024204847A Division AU2024204847A1 (en) 2018-09-18 2024-07-15 Quinazoline Derivatives as Antitumor Agents

Publications (2)

Publication Number Publication Date
AU2019341273A1 AU2019341273A1 (en) 2020-11-19
AU2019341273B2 true AU2019341273B2 (en) 2024-09-26

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AU2019341273A Active AU2019341273B2 (en) 2018-09-18 2019-09-17 Quinazoline derivatives as antitumor agents
AU2024204847A Pending AU2024204847A1 (en) 2018-09-18 2024-07-15 Quinazoline Derivatives as Antitumor Agents

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AU2024204847A Pending AU2024204847A1 (en) 2018-09-18 2024-07-15 Quinazoline Derivatives as Antitumor Agents

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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=)

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EP4523755A2 (en) 2025-03-19
US20230293533A1 (en) 2023-09-21
ES2971927T3 (es) 2024-06-10
SI4360713T1 (sl) 2025-02-28
JP7546550B2 (ja) 2024-09-06
HUE065578T2 (hu) 2024-06-28
EP3853220B1 (en) 2024-01-03
RS65413B1 (sr) 2024-05-31
PT4360713T (pt) 2025-01-07
KR20250171398A (ko) 2025-12-08
EP3853220A1 (en) 2021-07-28
HRP20240293T1 (hr) 2024-05-24
EP4360713B1 (en) 2024-10-30
JP2024164018A (ja) 2024-11-26
EP4523755A3 (en) 2025-06-11
EP4360713A2 (en) 2024-05-01
EP4360713A3 (en) 2024-05-22
DK3853220T3 (da) 2024-03-04
CN112654612A (zh) 2021-04-13
PT3853220T (pt) 2024-02-22
AU2024204847A1 (en) 2024-08-01
FI4360713T3 (fi) 2024-12-27
KR102889933B1 (ko) 2025-11-24
WO2020057511A1 (en) 2020-03-26
AU2019341273A1 (en) 2020-11-19
JP2022501338A (ja) 2022-01-06
KR20210061329A (ko) 2021-05-27
PL3853220T3 (pl) 2024-09-02
JP2026009898A (ja) 2026-01-21
SMT202400524T1 (it) 2025-01-14
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US20210386742A1 (en) 2021-12-16
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