AU2020403443B2 - New methylquinazolinone derivatives - Google Patents

New methylquinazolinone derivatives Download PDF

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Publication number
AU2020403443B2
AU2020403443B2 AU2020403443A AU2020403443A AU2020403443B2 AU 2020403443 B2 AU2020403443 B2 AU 2020403443B2 AU 2020403443 A AU2020403443 A AU 2020403443A AU 2020403443 A AU2020403443 A AU 2020403443A AU 2020403443 B2 AU2020403443 B2 AU 2020403443B2
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AU
Australia
Prior art keywords
compound
formula
cancer
treatment
braf
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AU2020403443A
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English (en)
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AU2020403443A1 (en
Inventor
Cosimo Dolente
David Stephen HEWINGS
Daniel Hunziker
Daniela Krummenacher
Piergiorgio Francesco Tommaso PETTAZZONI
Juergen Wichmann
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • C07D207/48—Sulfur atoms

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Harvester Elements (AREA)
  • Combines (AREA)
AU2020403443A 2019-12-10 2020-12-08 New methylquinazolinone derivatives Active AU2020403443B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP19214941.7 2019-12-10
EP19214941 2019-12-10
PCT/EP2020/084976 WO2021116055A1 (en) 2019-12-10 2020-12-08 New methylquinazolinone derivatives

Publications (2)

Publication Number Publication Date
AU2020403443A1 AU2020403443A1 (en) 2022-05-12
AU2020403443B2 true AU2020403443B2 (en) 2023-02-23

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AU2020403443A Active AU2020403443B2 (en) 2019-12-10 2020-12-08 New methylquinazolinone derivatives

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US (2) US12116349B2 (enExample)
EP (2) EP4483882A3 (enExample)
JP (2) JP7108146B2 (enExample)
KR (1) KR102836833B1 (enExample)
CN (2) CN114787156B (enExample)
AR (1) AR122351A1 (enExample)
AU (1) AU2020403443B2 (enExample)
CL (1) CL2022001529A1 (enExample)
CO (1) CO2022008968A2 (enExample)
CR (1) CR20220251A (enExample)
DK (1) DK4073065T3 (enExample)
ES (1) ES3023264T3 (enExample)
FI (1) FI4073065T3 (enExample)
HR (1) HRP20250418T1 (enExample)
HU (1) HUE071148T2 (enExample)
IL (2) IL316473A (enExample)
LT (1) LT4073065T (enExample)
MA (1) MA58087B1 (enExample)
MX (1) MX2022006783A (enExample)
PE (1) PE20221778A1 (enExample)
PH (1) PH12022551119A1 (enExample)
PL (1) PL4073065T3 (enExample)
PT (1) PT4073065T (enExample)
RS (1) RS66721B1 (enExample)
SI (1) SI4073065T1 (enExample)
TW (2) TWI877268B (enExample)
UA (1) UA128299C2 (enExample)
WO (1) WO2021116055A1 (enExample)
ZA (2) ZA202204675B (enExample)

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CA3158541A1 (en) * 2019-12-10 2021-06-17 Cosimo Dolente New braf inhibitors as paradox breakers
SI4073065T1 (sl) 2019-12-10 2025-06-30 F. Hoffmann-La Roche Ag Novi derivati metilkinazolinona
MX2022015703A (es) 2020-06-09 2023-01-24 Array Biopharma Inc Compuestos para el tratamiento de enfermedades y trastornos asociados a braf.
AU2022290851A1 (en) 2021-06-08 2023-11-23 C4 Therapeutics, Inc. Therapeutics for the degradation of mutant braf
IL308015A (en) * 2021-06-09 2023-12-01 Hoffmann La Roche Combination of a particular braf inhibitor (paradox breaker) and a pd-1 axis binding antagonist for use in the treatment of cancer
CN117642166A (zh) * 2021-06-09 2024-03-01 中外制药株式会社 用于癌症治疗的组合疗法
JP2024522603A (ja) * 2021-06-09 2024-06-21 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト (3r)-n-[2-シアノ-4-フルオロ-3-(3-メチル-4-オキソ-キナゾリン-6-イル)オキシ-フェニル]-3-フルオロ-ピロリジン-1-スルホンアミドの新規固形物
EP4378478A4 (en) 2021-07-27 2025-11-12 Toray Industries MEDICINE FOR THE TREATMENT AND/OR PREVENTION OF CANCER
IL312171A (en) 2021-11-04 2024-06-01 Hoffmann La Roche Innovative use of the quinazolinone compound for cancer treatment
TW202409040A (zh) 2022-07-19 2024-03-01 大陸商西藏海思科製藥有限公司 作為激酶抑制劑的喹唑啉酮衍生物的製備及其用途
JP2025537786A (ja) 2022-11-18 2025-11-20 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト 進行性固形がんまたは転移の治療のためのbraf阻害剤としてのキナゾリノン化合物
EP4634171A1 (en) * 2022-12-15 2025-10-22 F. Hoffmann-La Roche AG Process for the preparation of a quinazolinone derivative
JP2025541200A (ja) * 2022-12-15 2025-12-18 エフ・ホフマン-ラ・ロシュ・アクチェンゲゼルシャフト がん処置のための併用療法
IL324898A (en) 2023-07-04 2026-01-01 Hoffmann La Roche New solid forms of (3r)-n-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinozolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide
WO2025108405A1 (zh) 2023-11-22 2025-05-30 西藏海思科制药有限公司 作为激酶抑制剂的喹唑啉酮衍生物的制备及其用途
WO2025153057A1 (zh) 2024-01-17 2025-07-24 海思科医药集团股份有限公司 一种含braf抑制剂的药物组合物及其在医药上的应用
WO2026037755A1 (en) 2024-08-13 2026-02-19 F. Hoffmann-La Roche Ag New methylquinazolinone derivatives
WO2026046946A1 (en) 2024-08-28 2026-03-05 F. Hoffmann-La Roche Ag New solid forms of (3r)-n-[2-cyano-4-fluoro-3-(3-methyl-4-oxo-quinazolin-6-yl)oxy-phenyl]-3-fluoro-pyrrolidine-1-sulfonamide

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Publication number Publication date
CN114787156B (zh) 2024-07-26
EP4073065B1 (en) 2025-02-19
BR112022011123A2 (pt) 2022-08-23
LT4073065T (lt) 2025-04-25
MA58087B1 (fr) 2025-04-30
CN118791472A (zh) 2024-10-18
PH12022551119A1 (en) 2023-08-23
TW202136245A (zh) 2021-10-01
JP7108146B2 (ja) 2022-07-27
ZA202204675B (en) 2022-12-21
HRP20250418T1 (hr) 2025-06-06
AU2020403443A1 (en) 2022-05-12
SI4073065T1 (sl) 2025-06-30
US20240174621A1 (en) 2024-05-30
KR102836833B1 (ko) 2025-07-22
KR20220110554A (ko) 2022-08-08
PE20221778A1 (es) 2022-11-16
EP4483882A3 (en) 2025-03-05
ES3023264T3 (en) 2025-05-30
IL316473A (en) 2024-12-01
PT4073065T (pt) 2025-04-15
HUE071148T2 (hu) 2025-08-28
IL292161A (en) 2022-06-01
RS66721B1 (sr) 2025-05-30
MX2022006783A (es) 2022-07-11
CL2022001529A1 (es) 2023-02-10
PL4073065T3 (pl) 2025-05-19
US20220298119A1 (en) 2022-09-22
IL292161B2 (en) 2025-04-01
EP4483882A2 (en) 2025-01-01
FI4073065T3 (fi) 2025-04-16
AR122351A1 (es) 2022-09-07
TWI877268B (zh) 2025-03-21
WO2021116055A1 (en) 2021-06-17
CA3162883A1 (en) 2021-06-17
NZ787393A (en) 2025-07-25
ZA202206923B (en) 2024-10-30
CR20220251A (es) 2022-07-11
US12116349B2 (en) 2024-10-15
CN114787156A (zh) 2022-07-22
IL292161B1 (en) 2024-12-01
DK4073065T3 (da) 2025-04-22
TW202504895A (zh) 2025-02-01
EP4073065A1 (en) 2022-10-19
TWI908405B (zh) 2025-12-11
JP7802514B2 (ja) 2026-01-20
JP2022531609A (ja) 2022-07-07
UA128299C2 (uk) 2024-05-29
CO2022008968A2 (es) 2022-07-19
JP2022124458A (ja) 2022-08-25

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